Pharmacy Training Book

Prepared by:
Yaqeen Shqerat

Pharmacy 116-NNU

Last update: May-2021

Contents:
Topic 1: Antimicrobial Agents
Antibacterial agents
Antifungal agents
Antiviral agents
Drugs against some parasites

Topic 2: Cardiovascular System

Anti-hypertensive
Drugs for Heart Failure
Anti-arrhythmic drugs
Anticoagulants and Antiplatelet Agents
Antianginal drugs
Antihyperlipidemic drugs

Topic 3: Gastrointestinal System

Acid-lowering drugs
Laxatives
Antidiarrheal Agents
Antispasmodic Drugs
Antiemetic Drugs
Other GI problems
Topic 4: Respiratory System
Drugs for Asthma
Drugs for COPD
Drugs for Allergic Rhinitis
Drugs for cough
Drugs for Common Cold

Topic 5: Central Nervous System

Anxiolytics
Drugs for Bipolar disorder
Antiepileptic drugs
Antipsychotic drugs
Drugs for Parkinson disease
Drugs for Alzheimer disease
CNS stimulants
Anesthetics

Topic 6: Diabetes

Topic 7: Body Hormones

Sex hormones
Growth hormone
Thyroid hormones
Topic 8: Drugs for bone disorders
Drugs for osteoporosis
Disease-Modifying Antirheumatic Drugs (DMARDs)
Drugs for Gout

Topic 9: Corticosteroids

Topic 10: Non-steroidal Anti-inflammatory drugs

Topic 11: Opioid Analgesics

Topic 12: Headache and Migraine

Topic 13: Drugs are not included in previous systems

Topic 14: Some important eye drops and ointments

Topic 15: Some controlled drugs available in the pharmacy

Others extra information

 Topic 1: Antimicrobial Agents

Antibacterial agents
1) B-lactam cell wall inhibitor
-penicillin

→ Natural penicillin (G,V)

→ synthetic penicillin:

1.Antistaphylococcal
(penicillinase resistant):
(Oxacillin/Dicloxacillin/Methicillin /Nafcillin)

2-Extended spectrum:
(Ampicillin / Amoxicillin)

3-Antipseudomonal: (Piperacillin / Ticarcillin/ Cabernicillin)

-Cephalosporin -→(I will be mentioned them later)

- Carbapenem ---→ Imipenem/Meropenem/Ertapenem/Doripenem)

- Monobactam--→ (Azetronam)

2)Non-Beta-lactam cell wall inhibitor:

Others---→ (Vancomycin/ Daptomycin/Telavancin)

Penicillins:
-Bactericidal for rapidly growing gram +ve bacteria → due to disruption of the cell wall

Inhibit cross-linking between peptidoglycan

Penicillin G : for IM injection found in the hospital

→First choice for SYPHILIS(a contagious veneral disease that progressively affects many
tissues)

Phenoxymethyl penicillin(penicillin V): an oral form of penicillin G with poor

bioavailability, has a narrow spectrum of activity

Note: both of them are susceptible for B-lactamase (penicillinase)

Scientific Name Trade Name Company Dosage Form Notes

and strength
Penicillin V Bepen VK Birzeit Tab: 250, 500 ‫ال تصرف بدون‬
-mg ‫وصفة طبية الن‬
-Powder for ‫كثير من‬
Susp: ‫المرضى لديهم‬
250mg/5ml ‫حساسية من‬
‫البنسلين‬
-susp:
stable for
10 days
‫قبل التحضير‬
‫يحفظ في درجة‬
‫حرارة الغرفة‬
‫وبعد التحضير‬
‫في الثالجة لمدة‬
10 ‫اقصاها‬
‫أيام‬
Pen-rafa VK Rafa Caplet:500mg
Pen-rafa VK Rafa Powder for
forte syrup:
250mg/5ml
 Benzetacil 1,2000,000 U Dissolved in
(IM) water for
injection
(Agua para
injyectables)
)‫(قبل االكل‬.‫ يمكن اعطاؤه على معدة فارغة‬,‫ ال يتأثر بالطعام‬,‫ مقاوم لحموضة المعدة‬Penicillin VK

Penicillin: Category B (pregnancy)

Synthetic penicillin:
1)Antistaphylococcal penicillins: Penicillinase-resistant penicillins (do not
break down by B-lactamase):
-Oxacillin / Dicloxacillin /Methicillin /Nafcillin/Cloxacillin
Cloxacillin Cloxacillin Cap:500mg Crescent
‫ الن هذه البكتيريا موجودة‬cellulitis ‫ وغالبا تعطى اللتهابات الجلد‬Methicillin ‫تستخدم مع البكتيريا التي تستجيب لل‬-
‫على الجلد‬
-Used for staphylococcus but its use is declining due to (MRSA) methicillin-resistant S.
aureus

2)Extended-spectrum(penicillin-like antibiotic):
Ampicillin/ Amoxicillin

Amoxicillin Amoxitid Birzeit Cap:250,500,750mg

Susp:250mg/5ml
400mg/5ml
Moxepharm Jerusalem Cap:250,500,750mg
Susp:125mg/5ml
250mg/5ml
400mg/5ml

Amoxicare Pharmacare Cap:250,500mg Susp for 7

Tab:1000mg days
Susp:125mg/5ml
250mg/5ml
400mg/5ml
Moxypen Teva Cap:250mg
 Moxypen Teva Cap:500mg Susp for 14
forte Susp: 250mg days
Moxyvit Vitamed Cap:250mg
Susp:125mg/5ml
Moxyvit Vitamed Cap:500mg Susp stable
forte Susp: 250mg/5ml for 14 days
‫ لكن اذا الشخص معدته بتتعب يوخده بعد‬،‫ في العادة يوصف قبل االكل مباشرة افضل لالمتصاص‬:Amoxicillin
)‫االكل‬

‫ مرات اليوم‬3 500mg ‫ و‬250mg ‫عيار‬

‫ مرتين باليوم‬750mg ‫عيار‬

Note: all amoxicillin store in the refrigerator

‫ وتضاف‬,‫ يكون عن طريق إضافة مياه معدنية أو مياه مغلية و مبردة‬suspension ‫ حل ال‬: ‫ قاعدة عامة‬
.‫ كمية الماء التي يجب إضافتها موجودة على كل علبة دواء‬,‫الكمية على دفعتين‬

‫وقبل اضافة الماء نقوم بتحريك الحبيبات‬

Amoxicillin+ Ogmin Birzeit Caplet: 875+125 cla. Susp stores in

clavulanic acid Acid refrigerator and
‫مرتين باليوم‬ stable for 7 days

Tablet:
500+125 cla. Acid
‫ مرات باليوم‬3

Susp:
125mg
250mg
400mg
600mg

Moclav Sandoz Tab:500mg Susp stores in

Susp: refrigerator and
250,400 stable for 7 days
Clamoxin Jerusalem Tab:500, 875 Susp stores in
Susp: refrigerator and
250,400,600 stable for 7 days
Amoxiclave Teva Tab: 875
 Augmentin GSK Tab: Susp: strawberry
250,500,875 cream flavored
Susp: Stable for 7 days
125,250,400
Augmentin ES GSK Susp: 600mg/5ml ‫جرعته عالية مناسب‬
(extra strength) otitis media ‫لل‬
‫مرتين باليوم‬
Stores in the
refrigerator
Stable for 10
days.
‫ال يعطى لالطفال‬
6 ‫تحت عمر‬
‫سنوات(تعتبر جرعة‬
)‫مرتفعة‬

‫ وكذلك النه يتعب المعدة‬,‫< اوجمين وبدائله االفضل بعد االكل لتقليل فرصة حدوث إسهال كعرض جانبي‬-

‫ مرات باليوم‬3 500mg ‫عيار‬

‫ مرتين باليوم‬875mg ‫عيار‬

Amoxicillin dose for children: 30mg /kg/day (divided by twice or 3 times day)

Note: clavulanic acid is photosensitive, we noticed that it stored in sachets.

- Amoxicillin has better oral absorption than Ampicillin

- used for gram +ve and –ve

Ampicillin Megnacillin forte Birzeit Cap: 500mg

+flucloxacillin ampicillin+250
lucloxacillin
Susp: (granules)
250ampicillin+125
flucloxacillin
Store:1 week
Megacare Pharmacare Cap:250+250
 Megacare forte Pharmacare Cap:500
ampicillin+250
flucloxacillin
Susp:250
ampicillin+125
flucloxacillin
Stable: 1 week
General dosing guideline of ampicillin: 250-500mg q 6 hr (before meal)

Dose of ampicillin for children: 50-100mg/kg/day divided q6hr

Penibrin Ampicillin Teva Vial(IV,IM)

Orbenil Cloxacillin Teva Vial (IV,IM)
Zosyn Pipracillin+ Pfizer IV vial
tazobactam
Tazocin Pipracillin+ Pfizer IV vial
tazobactam

Indications for penicillins with doses:

‫ جرعات ومدة‬3 ‫ وتقسم على جرعتين او‬30-40mg/kg/day ‫ هي‬Amoxicillin ‫ الجرعة من ال‬:‫بشكل عام‬
‫ يوم‬14 ‫الى‬7 ‫العالج تتراوح من‬

100mg/kg/days ‫ ممكن نزيد عنها بحالة التهاب االذن الوسطى وتصل الى‬90mg/kg/day :‫الجرعة القصوى‬

More details:

-They are widely used in the treatment of respiratory infections

-Amoxicillin is employed prophylactically by dentists for patients with abnormal heart

valves who are to undergo extensive oral surgery.(Amoxicillin is the drug of choice in
this case)

Dose of amoxicillin or amoxicillin with clavulanic acid:

Adult: 500mg three times daily

Pediatric: 40-50 mg/kg/day divided in three doses

These doses are for these cases:

 )‫ ايام‬10 ‫ (لمدة‬pharyngitis ‫التهاب الحلق‬ -1
bacterial sinusitis ‫التهاب الجيوب‬ -2
‫ يوم) فترة العالج اسبوعين الن االلتهاب وصل الكلى‬14 ‫ (لمدة‬acute pyelonephritis ‫التهاب الكلى‬ -3
‫ أيام‬3 ‫ لمدة‬Uncomplicated lower UTI -4
)‫ أيام‬10 ‫ الى‬7 ‫ (لمدة‬Complicated lower UTI -5
.Can be used for inflammation before teeth procedure -6
But for →‫ التهاب األذن‬Acute Otitis Media:

Amoxicillin

→80–90 mg/kg/day divided twice daily

‫نالحظ أنها ضعف الجرعة العادية المستخدمة اللتهاب الحلق‬

(streptococcus: ‫(البكتيريا المسببة لاللتهاب الحلق هي‬

Notes:

*Resistance to Amoxicillin and Ampicillin antibiotics is now a major clinical •

problem because of inactivation by plasmid mediated penicillinases.

*β-lactamase inhibitors protect from enzymatic hydrolysis and extends the •

antimicrobial spectrum.

- B- lactamase has no antimicrobial properties

Ex: claculanic acid / Sulbactam / Tazobactam

Examples for combinations:

- Clavulanic acid + amoxicillin

-clavulanic acid + Ticarcillin

- Sulbactam + ampicillin

-Tazobactam + Piperacillin

Piperacillin, Ticarcillin and cabernicillin are anti-pseudomonas agents: has good activity
against Pseudomonas spp. And Enterobacter spp.

Side effects of Penicillins:

1. Hypersensitivity reaction (5-10%) of patients: (most common side effect)

Cross-allergic reactions occur among B-lactam antibiotic.

From simple rash to anaphylaxis.

Can be observed within 2 minutes or up to 3 days.

2. Diarrhea (the most common S.E): due to disruption of the normal balance of the
intestinal microorganisms.

Superinfection: (Pseudomembranous colitis) may occur

3- Amoxicillin and ampicillin are broad spectrum antibiotic so it can decrease the effect
of oral contraceptives (normal flora enhance ethinyl estradiol to reach to the blood) →
so we should use narrow spectrum antibiotic, or increase the dose of oral contraceptive.

More side effects:

4. Nephritis: mainly with Methicillin

5. Hematologic toxicities: with Piperacillin, Ticarcillin and Nafcillin

CBC should be performed.

6- Neurotoxicity: they can provoke seizures if injected intrathecally or if very high blood
level is reached.

Route of Administration:
Only IV or IM :( penicillin G )

(Piperacillin alone or with Tazobactam)

(Ticarcillin alone or with clavulanic acid)

(Ampicillin with sulbactam )

Cloxacillin

Only orally: Penicillin V

 (Amoxicillin alone or with clavulanic acid)

Other penicillins are effective by oral, IV, IM route

IM depot form : (Procaine penicillin G and benzanthine penicillin G) → they are slowly
absorbed and into the circulation and persist at low level for a long time.

Absorptions of penicillin:
→Most of the penicillin are incompletely absorbed after oral administration, and they
.reach the intestine in sufficient amounts to affect the composition of the intestinal flora

→Amoxicillin is almost completely absorbed.

→Absorption of all the penicillinase-resistant penicillin (Anti-staph) is decreased by food

in the stomach, because gastric emptying time is lengthened, and the drugs are
destroyed in the acidic environment.

→Therefore, they must be administered 30 to 60 minutes before meals or 2 to 3 hours

postprandial.

→Other penicillins are less affected by food

‫( يفضل‬Amoxicillin +clavulanic acid) ‫ما عدا‬, ‫ قبل األكل‬penicillins ‫ تؤخذ ال‬: ‫ممكن اتباع هذه القاعدة‬
.‫بعد األكل لمنع ا لعرض الجانبي وهو اإلسهال أو إذا كان المريض يعاني من مشاكل في المعدة يصرف له بعد األكل‬

Route of excretion:
Main route: By the kidney

The dosage regimens must be adjusted with people who have impaired renal functions.

Exceptions: Nafcillin, dicloxacillin and oxacillin→ not eliminated by the kidney.

Write your notes here:

………………………………………………………………………………………………………………………………
……………………………………………………………………………………………………………………………
 Cephalosporins
First generation:
Cephalexin / Cefadroxil / Cefazolin

Second generation:
Cefotixim / Cefatetan / Cefuroxime

Third generation:
Cefdinir / Cefxime / Cefoperazon / Cefotaxim / Ceftizaxime / Ceftriaxone

Fourth generation:
Cefepime
 →MOA of cephalosporins: inhibit cell wall synthesis by inhibit cross-linking
between peptidoglycan.

→Widely distributed in the body:

- all 1st generation do not penetrate to CSF

- all 2nd generation do not penetrate CSF except : Cefuroxime

- all 3rd generation penetrate CSF→for meningitis

except : Cefoperazone does not penetrate CSF.

→Probenceid (drug for gout) slows the secretion of cephalosporins so those patients
need less dose of cephalosporins

→As the generation increased the spectrum increased due to increased resistance
for penicillinase.

→All of them inactive against enterococci, MRSA, clostiridum difficil and L

monocytogenes.
Cephalexin(1st) Cefalex Birzeit Cap:250, 500mg
Susp:125mg/5ml
250mg/5m
Jeflex Jerusalem Cap:250,500,750 ‫قبل او بعد االكل‬
Susp:125mg/5ml ‫بس االفضل بعد االكل النو‬
250mg/5m .‫في ناس بتتعب معدتهم منه‬
4 ‫ تعطى‬500mg : ‫الجرعة‬
6 ‫مرات باليوم (كل‬
)‫ساعات‬
Susp: for 7 days after
reconstitution
Store in the
refrigerator

Cefacare Pharmacare Cap:500mg

Ceforal Teva Cap:250, 500mg
Susp:125mg/5ml
250mg/5m
Cefovit Vitamed Cap:250mg
Susp: 125mg
 Cefovit forte Vitamed
Cap:500mg
Susp:250mg
Dose of cephalexin for adult: the usual dose is 250mg q 6hr or 500mg q 12hr, but 500mg
often taken 4 times daily as the therapeutic level are maintained to 6-8 hours.

Dose of cephalexin for children: 25-50 mg/kg/day q 6-8 hr for 10 days

For otitis media: 75-100mg/kg/day divided q 6hr for 10 days

Cefadroxil(1st) Cefadrox Birzeit Tab:500mg ‫ مرتين‬500mg :‫الجرعة‬

Susp: 125mg/5ml ‫ ساعة) قبل‬12 ‫باليوم(كل‬
250mg/5ml )‫االكل (قبل الفطور والعشا‬
Biodroxil Sandoz Cap: 500mg ‫مرتين‬500mg :‫الجرعة‬
Susp:125mg ‫ ساعة) قبل‬12 ‫باليوم (كل‬
250mg/5ml ‫االكل‬

Cefazin Cefazolin(1st) Birzeit Vial:1000mg/vial

st
Indications for 1 generation cephalosporin:

→UTI

→prophylaxis in various surgical procedures (the first choice is cefazolin)

‫ بعد العملية‬infection ‫وقاية في العمليات خوفا من حدوث‬

→cover gram +ve more than gram –ve

Second Generation:
Zinnat Cefuroxim(2nd) GSK Tab:250,500 Susp stores in
Susp:125mg/ml refrigerator
250mg/5ml For 10 days
(granules)
Zinex Cefuroxim(2nd) Birzeit Tab:250,500
Zinaxim Cefuroxim(2nd) Jerusalem Tab:250,500
Susp:125
(powder)
zinacef Cefuroxim(2nd) GSK Vial:750mg

Dose of cefuroxim for more than 12yr: 250-500 mg q12hr for 10 days (not excess 1000mg daily)

For 3months- 12yr: for pharyngitis/tonsilitis the dose is: 20mg/kg/day----- For otitis media: 30mg/kg/day
For children less than 3 months the safety of cefuroxim is not established.

)‫(مرتين باليوم يؤخذ بعد األكل أو األفضل مع األكل الن امتصاصه يزيد بوجود الطعام‬

Indications for use 2nd generation cephalosporins:

→Has greater activity against gram –ve more than +ve and that is included: H.influenza,
Enterobacter aerogens, Nisseria, Proteus, E.coli, Klebsiella (HENPEcK)

→Decreased activity against gram +ve (Staphylococcus epidermis not covered)

→UTI

‫الزم يبعد المريض عن االكل الحار واللي فيه بهارات‬,‫ مرتين باليوم صبح ومسا بعد االكل‬500mg ‫عيار‬
‫والكوال والشيبس واي شي ممكن يزيد الوضع سوء‬,‫كتيرة‬

→respiratory tract infection

→Bone and soft tissue infection

→Prophylactically in surgical procedures, however the 3rd generation now used more
than 2nd for this purpose.

Third generation:
Dose of cefpodoxime: 100 dose of
Cefpo Cefpodoxime(3rd) Birzeit Tab:100,200
Metoxim Cefpodoxime(3rd) Sandoz Tab:200mg
Susp: 100mg
cefpodoxime: 100 or 200 twice daily.

Rizacef OD Cefixime(3rd) Pharmacare Cap:400mg

Cefix Cefixime(3rd) Jerusalem Susp:100mg/5ml Used within 14
days
‫يحتوي حبيبات‬
‫صغيرة من االفضل‬
‫تحريك العلبة جيدا‬
‫قبل اضافة الماء‬
‫واضافته على‬
‫دفعتين والخلط جيدا‬
Doraceph Cefixime(3rd) Birzeit Tab:400mg
Dose of cefixime for adult: 400mg once daily after meal

Dose of cefixime for children: 8mg/kg/day in single dose of divided q 12hr

Adcef Cefdinir(3rd) Pharmacare Cap:300mg -Susp is Strawberry

Susp:125mg/5ml flavored
250mg/5m -Not stores in
refrigerator
-Used for 10 days
Cefimed Cefdinir(3rd) Birzeit Cap: 300mg
Susp: 125mg/5ml
250mg/5ml
Dose of cefdinir for children: 14mg/kg/day divided in 2 doses

Tixon Ceftriaxone(3rd) Jerusalem Vial:1000mg

To prepare:
IM with
lidocain
IV with water
or normal
saline
Cefixon Ceftriaxone(3rd) Birzeit Vial:1000mg
IM,IV with
Ceftriaxone Ceftriaxone(3rd) Teva Vial
Rocephin Ceftriaxone(3rd) Roche Vial: 500,
1000mg
Pan-ceftriaxone Ceftriaxone(3rd) Panpharma Vial:1000mg
Dose of ceftriaxone for children:50-100mg/kg/day

Note: ceftriaxone should not be mixed or simultaneously infused with calcium-

containing solutions such as Harmann's or Ringer's because of risk of
precipitation.

Clafoxim Cefotaxime(3rd) Birzeit Vial:1000mg

Claforan Cefotaxime(3rd) Sanofi Vial:1000mg

Dose for children of cefotaxim:50-180mg/kg/day

Jephazim Ceftazidime(3rd) Jerusalem Vial:1000mg
IV,IM
Profort Ceftazidime(3rd) Birzeit Vial:1000mg
Ceftazidime Ceftazidime(3rd) Abic
Fortum Ceftazidime(3rd) GSK

Cefizox Ceftizoxime GSK Vial for injection

Indications:
Cefrtriaxone→ for sexually transmitted infections caused by gonorrhea

→in empiric therapy for community-acquired meningitis

Niasseria ‫ هي ال‬meningitis ‫من أكثر أنواع البكتيريا المسببة ل‬

(Ceftriaxone and cefotaxime are the agents of choice for meningitis)

→ceftriaxone is contraindicated in neonates because it displaces bilirubin from albumin

binding sites, resulting in a higher free bilirubin serum concentration with subsequent
accumulation of bilirubin in the tissues. (kernicterus)

In this case cefotaxime is used.

Ceftazidime→ has activity against P.aeruginosa

Others→Lyme disease(Borrelia)

→serious hospital-acquired infections, alone or in combination with an

aminoglycoside

Fourth generation:
Cefepime
→must be administered parenterally(in hospital)

→ has a wide antibacterial spectrum

→It is active against streptococci and staphylococci (but only those that are
methicillin susceptible).
→Cefepime is also effective against aerobic gram-negative organisms, such
as Enterobacter species, E coli, K. pneumoniae, P. mirabilis, and P.
aeruginosa.
‫ يترك‬, resistance ‫ما نبدأ باستخدام الجيل الرابع من السيفالوسبورين من اولها عشان ما يصير‬
‫للحاالت الخطيرة‬

Fetroja : Cefiderocol → is a first in class siderophore cephalosporin with

broad coverage against many drug-resistant gram-negative bacteria.
Highly stable against B-lactamase
Is approved in 2019 for the treatment of complicated UTI including
pyelonephritis when no other options are available (used with pt. 18 years
old or more)

Uses of cephalosporins with doses:

Examples

Pharyngitis ‫التهاب الحلق‬

Cephalexin
Adult: 250-500 mg four times daily
Pediatric: 25–50 mg/kg/day divided in four doses (for 10 days)

Acute Otitis Media ‫التهاب االذن‬

Cefdinir, Cefuroxime: Non-severe
Ceftriaxone (1-3 days): Severe

Bacterial sinusitis ‫التهاب الجيوب‬

Cefuroxime
Adult: 250-500 mg twice daily
Pediatric: 15 mg/kg/day divided in two doses
Cefaclor
Adult: 250-500 mg three times daily
Pediatric: 20 mg/kg/day divided in three doses

cefdinir
Adult: 600 mg daily or divided in two doses.
Pediatric: 14 mg/kg/day in one dose divided in two doses

UTI

→There are no major advantages of these agents over other agents in the
treatment of UTIs

→They are more expensive

→They may be useful in cases of resistance to amoxicillin and trimethoprim–

sulfamethoxazole

Side effects of cephalosporin:

→Hypersensetivity reactions(2-5%)

→5-10% of penicillin-sensitive persons are also hypersensitive to cephalosporins

The rate of highest allergic cross sensitivity is between penicillin and first generation
cephalosporins.

‫اذا كان المريض لديه حساسية من البنسلين من االفضل عدم اعطاءه السيفالوسبورين واذا اضطرننا لالستخدامه‬
.‫يجب يعمل فحص حساسية للتأكد‬

→Steven Johnson Syndrome, toxic epidermal necrosis (rare)

→Alcohol intolerance(disulfiram-like) is seen with ceftriaxone.

→May cause bleeding disorders that can be prevented by Vit K administration.

→Nephrotoxic when administered with diuretics.

→Note: cephalosporins (except ceftriaxone) are eliminated by the kidney, so, dose
adjustment should be considered in patients with renal insufficiency.

→May cause superinfection with gram +ve organisms or fungi

→cephalosporins are the number one cause of hospital-acquired clostridium difficile

colitis, a potentially life-threatening infection.

→Pain at intramuscular injection sites

‫الزم نطمن المريض انو طبيعي االلم‬

→Phlebitis (inflammation of the vein)after intravenous administration

Administration:
→ Many of the cephalosporins must be administered IV or IM because of their poor oral
.absorption.

→Medications taken orally are

Cefadroxil – 1st Cefdinir – 3rd

Cephalexin – 1st Cefixime – 3rd

Cefuroxime axetil – 2nd Ceftibuten – 3rd

-------------------------

Elimination:
.→Elimination occurs through tubular secretion and/or glomerular filtration

→Doses must be adjusted in cases of severe renal failure.

Exception:

Ceftriaxone which is excreted through the bile into the feces→It is

frequently employed in patients with renal insufficiency:

But in patient with hepatic failure, ceftriaxone should not be used→ cefotaxime can be
used instead, as it secreted by kidney
Distribution
Adequate therapeutic levels in the CSF, regardless of inflammation, are achieved only
with select a few cephalosporins.

→For example, ceftriaxone or cefotaxime is effective in the treatment of -

neonatal and childhood meningitis caused by H. influenza.

→Cefazolin is effective for most surgical procedures, including orthopedic surgery

because of its ability to penetrate bone.

Cefazolin finds application as a single prophylaxis dose prior to surgery.

Additional intraoperative cefazolin doses may be required if the surgical procedure lasts
longer than 3 hours.

Carbapenem:
Include: Imipenem-Clistatn/Meropenem/Ertapenem/Doripenem

Meropenem Meropenem Teva 500mg IV

J-penem Meropenem Jerusalem Vial (0.5g,1g)
IV use only
For hospital
use
Meronem Meropenem Astrazeneca
Meropenem Meropenem Birzeit
Mero-Avenir Meropenem BioAvenir 500mg, 1g

→For hospital use (as IV infusion over15-30min or IV bolus over 5min)

→Relatively resistant to Beta-lactamase (penicillinase and cephalosporinase), so they

are useful for infections caused by penicilllinase-producing : S-aureus, E.coli, Klebsiella
spp, Enterobacter spp, H.influenzae

→They are powerful against Pseudomonas infections.

→Demonstrate no cross-resistance with other antibiotics

→Imipenem is marketed in the combination product Imipenem/Clistatin

→Clistatin is an inhibitor of renal dehydropeptidase which inactivates Imipenem.

→Most common adverse effects: Nausea/ Vomiting/ Diarrhea/ Skin rash/ and at higher
doses seizures(particularly for imipenem).

Monobactam:
(Aztreonam)

→Administered parenterally →For hospital use

→lack of thiazolidine ring, highly resistant to Beta-lactamses

→Has a good activity against only gram negative organisms→useful for E.coli/
P.aeruginosa/ Enterobacter spp.

→Lacks activity against anaerobes and gram +ve

→Has no cross-reactivity with penicillins or cephalosporins for hypersensitivity

reactions.

Teicoplanin(glycopeptide): inhibit cell wall synthesis.

Targocid Teicoplanin Sanofi Vial:200mg

 Other inhibitors of bacterial cell wall biosynthesis:

Vancomycin Daptomycin Telavancin

MOA Prevent elongation of
peptidoglycan and cross
linking due to inhibition of
transglycosylase→
destroy cell wall
Uses Parenterally:(slow IV
infusion)
-active against gram +ve and
–ve, resistant to some
strains
-MRSA and MRSE
-in patient allergy to
penicillin and cephalosporin
Orally:
Antibiotic-associated
enterocolitis (C. difficil)
Depolarize the cell
membrane →loss of
membrane potential and
rapid cell death.
- similar to vancomycin
+ vancomycin-resistant
enterococci(VRE)
+complicated skin infection
+endocarditis
NOTE:
Never use in pneumonia ,
because lung surfactant
inactivate it
-derivative of vancimycin
-similar of vancomycin and
daptomycin in MOA
(destroy cell wall and cell
mem.
- in complicated skin infection
caused by resistant gram +ve
bacteria
-not active against VRE.

SE -Rapid administration cause( - -nausea/vomiting/metallic

Red man syndrome)→ headache/nausea/consipati taste/insomnia/headach
Fever/chills/flushing/ on/nsomnia
phlebitis/ anaphylactoid rxn -foamy urin
-Myalgia
-ototoxicity and Note: other myopathic drug -prolongation QT interval
nephrotoxicity →rare and at should be avoided ex: Statin
high doses -interference with
coagulation tests(PT/PTT/INR)
Vancomycin merk--- for
mylan
IV
vial(500mg,1g)
vancovenir--- 500mg,1g
vial
vanco-teva---vial
 Inhibitors of Bacterial Protein Synthesis
 30s ribosome inhibitors→ Tetracyclin

→Glycylcyclines

→Aminoglycoside

 50s ribosome inhibitors→Macrolides

→Lincosamide

 Tetracyclines:
Include: Tetracycline / demeclocycline /doxycycline /minocycline/
oxytetracyclin

→MOA: bind with 30 subunit of ribosome→prevent tRNA from binding to mRNA-

ribosome complex→ inhibit protein synthesis.

→coverage:

Gram +ve / -ve / organisms other than bacteria

→Broad spectrum→ bacteriostatic

‫بتعيق عملية تصنيع البروتينات‬
→Resistance to one tetracycline confers resistance to some, but not all tetra
‫ بتصير نسبيا‬cross resistance ‫يعني ال‬
Tetracare Tetracycline Pharmacare Ointment 3%

Doxypharm Doxycycline Jerusalem Tab:100mg

Doxal Doxycycline Beit Jala Tab:100mg
Doxylin Doxycycline Dexcel Tab:100mg
‫ حبة لحبتين يوميا‬:‫الجرعة‬
 Pregnancy: category D

Uses of doxycycline in the treatment of acne vulgaris:

→Is the first choice between oral antibiotic (in case of sensitivity of tetracycline or
patient under 8 years old, the alternative is Macrolides like erythromycin or
azithromycin)

→indicate for use in moderate to severe inflammatory acne

→should used in combination with topical retiniods (adapaline or tretinoin) and

Benzoyl peroxide

→The patient should use sunblock and stay away from the sun because the drug
can cause photosensitivity reaction.

→Dose: doxycycline (initial dose is 100 or 200 mg daily, followed by 50mg daily
as a maintenance dose after improvement )

Minocycline 100mg/day or 50mg twice daily)

Minocycline Minocycline Rafa Cap:

50mg (30cap)
100mg (10cap)
Minocin Minocycline Pfizer Tab: 100 mg

Oxycin Oxytetracyclin Birzeit Eye Ointment

Jordacycline Oxytetracyclin Beit Jala Eye Ointment

Indications of tetracycline:
→useful for the treatment of inflammatory acne vulgaris

→Rocky Mountain spotted fever: Rickettsial infections(tetracycline is the 1 st choice)

→used in combination regimens for Heliobacter pylori infections

Tetracycline:100mg four times daily)is one of the drug in Bismuth-based four-drug

regimens (Bismuth+Tetracycline+PPI)
→Cholera

→Lyme disease(single, 200mg of doxycycline, given within 72 hours after a tick bite,
can prevent development of the disease)

→Infections caused by Chlamydia spp(sexually transmitted disease)(doxycyclin and

azithromycin used for it )

, →Mycoplasma pneumonia(respiratory tract infection)( tetracycline is the drug of

choice).

→minocycline only reach CSF at therapeutic dose

→Demeclocydine is an ADH antagonists: used in the treatment of syndrome of

inappropriate ADH secretion (SIADH)

Side effects of tetracyclines:

1. gastric discomfort

2.Hepatotoxicity:Rare and at high doses

Particularly with pregnant women and patient with preexisting hepatic dysfunction and
renal impairment.

3.Deposition in the bone and primary dentition during the calcification process in
growing children.(bind strongly to calcium ions)

This may cause→discoloration and hypoplasia of teeth

→temporary stunting of growth

Tetracycline should not used in patient less than 8 years old.

4.Phototoxicity: sever sunburns may occur in exposed to sun or UV

→ patients should be advised to wear adequate sun protection.

5.Vestibular dysfunction: with minocycline and doxycycline.

Dizziness, vertigo, and tinnitus particularly minocycline, which concentrates in the

endolymph of the ear and affects fubction.
6.Pseudotumor cerebri:

→Benign, intracranial hypertension→headache/blurred vision→rare

→although discontinuation of drug reverses this condition, it is not clear whether

permanent sequelae.

7.superinfection : (due to broad spectrum coverage), by:

→ Resistant staphylococci and clostridia as a result of altered GI ecology, this condition

can be life-threatening.

→Vaginal candida

Tetracyclins is contraindicated in:

→pregnancy:
Category D
Animal studies have revealed evidence of embryotoxicity and teratogenicity, including toxic
effects on skeletal formation

There are no controlled data in human pregnancy, however, congenital defects and maternal
hepatotoxicity have been reported.

When used during tooth development (second half of pregnancy) tetracycline may cause
permanent yellow-gray-brown discoloration of the teeth and enamel hypoplasia.

The use of tetracycline during pregnancy is generally not recommended, especially during the
last half of pregnancy.

If there is a need for using tetracycline in pregnant women with no other choices, it can be
used until the week 15 of pregnancy, because the formation of bone and teeth in the fetus
has been delayed after that

→in this case, the choice is Doxycycline, because it is the least one that could make a
chelation for the Ca+

→ breast-feeding:
Tetracycline is excreted into human milk in small amounts.
Theoretical risks of dental staining and inhibition of bone growth exist, although are unlikely.

In one study, tetracycline level were undetectable in nursing infants.

Tetracycline is considered compatible with breast-feeding by the American Academy of

Pediatrics.

However, the manufacturer recommends that because of the risk of serious potential adverse
reactions in nursing infants, a decision should be made whether to continue breast-feeding or
discontinue of the drug, taking into account the importance of the drug to the mother.

→Patients less than 8 years old.

Notes:
-orally →adequate absorption

-can also be administered parenterally

-absorption is impaired by stomach contents, especially milk and entacids/ca/iron.

→doxycycline is the least agent affected by food or dairy products

(however, better to be taken 30 min before meal).

-primary route of elimination: kidney

→doxycycline does not accumulate and hence is the safest tetracycline to administer in
patient with impaired renal function.

Counseling about tetracycline:

‫الزم نحكي للمريض يبعد عن الشمس قدر االمكان ويستخدم واقي شمس‬

‫يوخد الدوا قبل االكل بساعة او بعد بساعتين‬

‫ويبعد منتجات الحليب ساعتين قبل الدوا وساعتين بعد‬

doxycycline ‫يشرب كاسة مي كبيرة مع الحبة ويشرب مي كتير باليوم لتقليل حدوث تهيج بالمريء بسبب ال‬
‫والن عائلة التتراسايكلين تسبب العطش‬
  Glycyclines:
Tigecycline→derivative of minocycline

Tigecycline Tygacil Vial:50mg Pfizer

→the same MOA

→uses: complicated skin and soft tissue infection/ complicated intra-abdominal

infections

→overcome the resistance to tetracycline

→SE: well-tolerated

The main SE: nausea/vomiting

→inhibit the clearance of warfarin → anticoagulation should be monitored

Aminoglycoside:

Gentamycin /neomycin/tobramycin/streptomycin/spectinomycin/ amikacin

Gentacin Gentamycin Jerusalem Cream 0.1%

Ointment
Gentatrim Gentamycin Trima Cream
Garamine Gentamycin Biet Jala Cream 0.1%
Zetamycin Gentamycin Birzeit Ampoules:20 IV
,40 IM ,80 mg IV and IM
Gentacol Gentamycin Birzeit Eye and ear drops
3mg/1ml
Lacromycin Gentamycin Dr.Fisher Eye drops

Aflumycin Gentamycin 0.16% Perrigo Cream For local skin inflammation

+prednisolone 0.5% associated with bacterial
infection
Dose: 4 times daily
Valecort-G Gentamycin 0.1% Birzeit Cream
Betamethasone 0.1% Ointment
Betacare-G Gentamycin 0.1% Pharmacare Cream /Note: Betacare contain only
Betamethasone 0.1% betamethasone
Diprogenta Gentamycin 1 mg MSD Cream
Betamethasone 0.5mg Ointment

Betacorten-G Gentamycin 0.1% Trima Cream

Betamethasone 0.1% Ointment

Triderm Gentamycin 1mg MSD Cream

Clotrimazole 10mg
Betamethasone 0.643mg

Decomb Gramicidin(antibiotic) Birzeit Cream

Neomycin(antibiotic) ‫ مرات باليوم‬3 ‫مرتين ل‬
Nystatin(antifungal)
Triamcinolone acetonide(corticosteroids)

Dermacombin Gramicidin(antibiotic) Taro Cream

Neomycin(antibiotic) Ointment
Nystatin(antifungal)
Triamcinolone acetonide(corticosteroids)

Medhist Neomycin Birzeit Cream Treatment of

Clotrimazole dermatitis involving
Dexamethasone acetate bacterial and fungal
infection
Dose: twice daily
Tevacutan // Tave Cream //
Polycutan // Perrigo Cream //

Neomycin Neomycin Rekah Tab: 500mg

 Neodex Neomycin+ Beit Jala Eye drops
Dexamethasone
Dexamycin Neomycin+ Teva Eye drops
Dexamethasone

Maxitrol Neomycin+ Novartis Eye drops and

Polymyxin + eye ointment
dexamethasone
Otodex Neomycin+ Bir zeit Ear drops
Polymyxin +
Dexamethasone
Neocort Neomycin+ Beit Jala Ear drops
Polymyxin +
Dexamethasone
Dexotic Neomycin Teva Ear drops
Polymyxin
Dexamethasone

Dexefrin Neomycin Dr.Fischer Ophthalmic Should be

Dexamethason drops stored in
Phenylephrin refrigerator
5cc

Otomycin Neomycin Taro Ear drops

Phenylephrin Should store at
room temp

Neo-medrol Neomycin Pfizer Acne-lotion

Methylprednisolone
Aliminium chlorohydroxide complex

Tobrex Tobramycin 0.3% Alcon Ointment

Solution

Amecane Amikacin Jerusalem Ampoules

 IV , IM

MOA→ inhibit protein synthesis by interact with 30s ribosomal subunit

→Passively diffuse through outer membrane of gram negative aerobic bacteria

→Bacteriocidal depend on concentration

Do not act against gram positive ( does not have outer membrane) and anaerobic
bacteria

For gram positive: used with B- lactam antbiotic ( to destroy the cell wall and
) allow for aminoglycoside to enter

→Streptomycin only for: plague/ sever cases of brucellosis/ adjunct for

mycobacterial infections

→Gentamicin and topramycin for gram -ve

→Amikacin: gram -ve infection resistant to gentamicin and topramycin

→Neomycin: topically— for soft tissue infection( often in combination bacitracin

)and polymyxin

Orally:1-destroy GI bacteria →prevent ammonia

production→ prevent hepatic encephalopathy

2-And to prepare the bowel prior to surgery

Does not given Iv- toxic (cause sever nephrotoxicity)

Aminoglycoside is highly polar→ poor absorption→ used IV(except neomycin)

or topically.

Once daily dosing is better than divided small doses—- less toxicity

SE of Aminoglycoside:
-Narrow therapeutic index
 -Ototoxicity : especially with other ototoxic drug such as (cisplatin/ loop diuretics /
furosemide/bumetanide/ethacrynic acid)
-Nephrotoxicity — renal function should be monitored (urea and creatinin level
-At high dose—neuromuscular blockade with respiratory paralysis ( patients with
myasthenia gravis are at risk)
In this case the antidote is calcium gluconate and neostigmine
-Hypersensitive reaction: rare

elimination: by kidney
Requires dose modification in case of renal failure

Pregnancy: category D
‫خطير على الكلى والسمع للبيبي‬
Aminoglycosides are not recommended for parenteral use in pregnancy
Oral or local application of aminoglycoside is indicated→minimal systemic absorption
(water-soluble).

 Macrolides:
Erythromycin→Natural

Clarythromycin/Azithromycin→Semi-synthetic

Bacteriosratic ( can be bacteriocidal at high conc. )

MOA: inhibit protein synthesis by binding irreversibly to 50s subunit of

ribosome →bacteriostatic

Do not cover anaerobic bacteria

Administered orally( adequate absorption)
Food interferes with the absorption of erythromycin and azithromycin

Erythromycin Erythrotab Birzeit Tab:250mg

Erythrolet Birzeit Susp: 125, 200
Erythro-teva Teva Tab:250,500
Erythrocare Pharmacare Susp:200mg/5ml Should be store at
400mg/5ml refrigerator
‫الزم بالثالجة بعد الحل‬
Acnetrim Trima Sol: 2% For acne
 Erythromycin Genmedix Eye ointment
ophthalmic
Ointment
Akne-mycin Hermal Emulsion 4% For acne

Erythromycin Akne-mycin plus Hermal Solution 4%, 2% For acne

Tritinoin
Erythromycin3% Benzomycin Mediline Gel For acne
Benzoyl peroxide5%
Erythromycin

‫ مرات باليوم على معدة فاضية بعد االكل بساعتين‬3 ‫ يؤخذ‬250mg ‫عيار‬

‫السسبنشن يجب وضعه بالثالجة بعد الحل‬

Esters ( stearate, estolate,ethylsuccinate) provide improved acid stability (because
erythromycin base is destroyed by gastric acid)

Note: clarythromycin and azithromycin is stable to stomach acid)

Erythromycin is category B safe for pregnant

With caution in lactation

Coverage→similar to penicillin G→Alternative for penicillin in case of hypersensitivity to

B-lactam antibiotic

Indications:

-Acute respiratory exacerbation in chronic bronchitis 500mg orally every 6 hours

-Pharyngitis: 40mg/kg/day divided into 2 to 4 times daily (maximum: 1g/day)

-For inflammatory acne (topically) at conc. 1% to 4% ( if combined with zinc this enhance
the penetration of erythromycin)

- oral erythromycin has efficacy similar to tetracycline but it includes higher rates of
bacterial resistance.

Laricid Clarithromycin Birzeit Tab:250,500mg Do not refrigerate after

Susp:125mg/5ml reconstitution
250mg/5ml
Klacid Clarithromycin Abbot Tab:250,500 Klacid Xl
Klacid Xl :tab 500mg ‫مرة واحدة يوميا‬
 Klacid granules:susp Susp: stable for 14 days
125,250 granules ‫السبب في صناعته على شكل‬
‫ان الدواء يترك طعم مرار في الفم‬
Klarimax Clarithromycin Beit Jala Caplet:500mg Do not refrigerate after
Susp:125, 250 reconstitution
Susp: stable for 10 days
Klaricare Clarithromycin Pharmacare Tab:250,500 Do not refrigerate after
Klaricare Xl 500 reconstitution
(extended release) Susp: stable for 7 days
Susp:125,250
Clarithro Clarithromycin Sama Susp:125,250 Do not refrigerate after
Dry granules reconstitution

→Clarithromycin suspension: should not store at refrigerator after reconstitution

Dose of clarithromycin for children: 15 mg/kg/day

→‫يوصف مرتين باليوم بعد االكل‬500mg ‫عيار‬

→Clarythomycin→More potent against gram positive(staph and strep) than

erythromycin.

→Can be given with food ( more acid stability than erythromycin)

→Clarythromycin 500mg twice daily for invasive(dysentery-like)diarrhea)

→clarythromycin 250-500 mg twice daily for acute respiratory exacerbation in

chronic bronchitis

→otitis media: clarythromycin 15mg/kg/day divided twice daily

→Clarythromycin: for eradication of H. pylori (500mg twice daily is one of the

drugs in PPI-based three-drug regimens)

Azimex Azithromycin Birzeit Cap:250mg (tripak=3 cap)

500mg(6 cap)
Susp:200mg/5ml
Azytra Azithromycin Beit Jala Cap:250mg
Susp:200mg/5ml
Azicare Azithromycin Pharmacare Cap:250, 500(tripack)
Susp:200mg/5ml
 Azenil Azithromycin Pfizer Cap:250mg
Susp: 200mg/5ml
Zitrocin Azithromycin Jerusalem Cap:250, 500mg
Susp: 200mg/5ml
Aziro Azithromycin Sama Cap: 250mg
Caplet: 250 , 500mg
Susp: 200mg/5ml
Zithromax Azithromycin Pfizer Cap:250mg
Vial:500mg for IV
Azithromycin Azithromycin Sandoz Tab: 250, 500

Azithromycin
‫ن‬
‫ مرة واحدة باليوم‬، )‫بساعتي(يجب ان يؤخذ عىل معدة فارغة‬ ‫يوصف قبل االكل بساعة او بعد‬

Half-life more than 40 hours→ taken once daily

Dose of azithromycin for children: 10mg/kg/day

→Slightly less effective against gram positive bacteria

→Worked more than erythromycin and clarithromycin against Haemophilus influenzae(
gram negative)→used to treat pneumonia
→Worked great against atypical mycobacteria.
→Invasive (dysentery-like) diarrhea -- Shigella
500 mg orally × 1 day, then 250 mg orally daily × 4 days

→Invasive (dysentery-like) diarrhea – Salmonella

1,000 mg orally × 1 day, followed by 500 mg orally once daily × 6 days

→Acute Respiratory Exacerbations in Chronic Bronchitis

250-500 mg Once daily.

→Bacterial Pneumonia
500 mg orally × 1 day, then 250 mg orally daily × 4 days

→Otitis Media
10 mg/kg/day for 3 days OR
10 mg/kg/day 1, then 5 mg/kg /day for days 2–5
In general: the duration for therapy is 3 to 5 days

MyRox Roxithromycin Beit Jala tab:150,

caplet: 300mg
On empty
stomach
Ruled roxithromycin Sanofi Tab:150, 300

Rovamycin Spiramycin Sanofi Tab: 1.5 MIU

Uses of Macrolides:
→chlamydia infections

Safe alternative to tetracycline in pregnant women with STDs( among macrolides:

azithromycin is preferred therapy for urethritis caused by Chlamydia trachomatis)

Note: tetracycline is the drug of choice for chlamydial infection

→against staph and strept

Safe alternative for patients sensitive to beta-lactam ( the most effective

macrolides is clarythromycin)

→GI infection:

-Campylobacter gastroenteritis

-Helicobacter pylori infection

(clarithromycin has higher activity in these cases than erythromycin)

→AIDs related infection

Atypical mycobacterial infection /toxoplasmosis encephalitis/ cryptosporidium

diarrhea

→Diphtheria and pertussis-

→Leginonnaires disease

→Mycoplasma infection

Toxicity:
1.Epigastric distress with large doses of erythromycin( the most common
side effect)

2.Cholestatic Jaundice with estolate ester of erythromycin (rare)

3.Ototoxicity

Note:

All macrolide (except Azithromycin) inhibits CYP3A4, thereby potentiate the

effects of:

Carbamazepine / corticosteroids / cyclosporine/ digoxin / ergot alkaloids /

theophylline / triazolam / valproate / warfarin/lovastatin/simvastatin

Clarithromycin increase the level of pimozide(antipsychotic) and that lead

to QT interval prolongation, arrythmia, sudden death.

significant renal dysfunction as risk of bleeding may be increased

Apixaban:(Eliquis) 2.5 , 5mg for Pfizer

Erythromycin: (Erythrotab) for Birzeit

‫ لمنع‬Azithromycin ‫ االفضل‬Macrolides ‫اذا كان المريض يأخذ اكثر من دواء ونريد اعطاءه من‬
CYP3A4 ‫ عبر‬Metabolism ‫حدوث تداخل مع دواء اخر اذا كان ال‬

Erythromycin is safe and effective in pregnancy (cat:c)

But erythromycin estolate should nor be used during pregnancy.

Newer marcolides are second choice macrolides (azithromycin)

 Spiramycin is the drug of choice for the treatment of toxoplasmosis during the
first trimester.

Clarithromycin: cardiovascular malformation reported in rates, no evidence in

human (cat: c) →may be required in treating peptic ulcer

Ketolides
→Telithromycin only ketolides in the market

→semisynthetic derivative of erythromycin

→Coverage: similar to Azithromycin

→Ketolides are effective against macrolide-resistance bacteria

‫ نستخدم‬resistance ‫ لكن البكتيريا عاملة‬macrolide ‫في حال كان المريض بحاجة الى استخدام‬
ketolides

Others:

Fidaxomicin / Chloramphenicol / clindamycin/ linezolid

Streptogramins (dalfopristin/quinupuristin)

 Chloramphenicol:

Ramacetine Chloramphenicol 5% Birzeit Eye Ointment

Ramacetine HC Chloramphenicol1% Birzeit Eye Ointment
Hydrocorticone 0.5%
Synthomycin Chloramphenicol 5% Rekah Eye Ointment
Lomixin Chloramphanicol 0.5% Beit Jala Eye drops
Dermasept Chloramphenicol 3% Birzait Ointment
Dexacol Chloramphenicol 2mg Birzeit Eye drops
Dexamethasone 0.25%
Threolone Chloramphenicol 3% ABIC Ointment
Prednisolone 0.5%
Chlorosone Chloramphenicol 2mg BirZiet Eye drops
Dexamathasone 0.25%
Polymyxin 2500IU
Polymicin Chloramphenicol 0.2% Jerusalem Eye and ear
Polymyxin 2500 IU drops
All eye drops that contain chloramphenicol should store at refrigerator.

→Broad spectrum of coverage

→Bacteriostatic

→reversibly bind to ribosome

→orally→rapid absorption

→parenterally

→Readily penetrated CNS, with or without inflammation, so it can be used for

meningitis but not as first line due to its toxicity

→elimination by the kidney

Uses: as a seconde choice in these cases:

-Typhoid fever (salmonella enteric)

- Bacterial meningitis

-Anaerobic infection

-Rickettsial disease note: the first line is tetracycline

Side effects:

1.Hypersensetivity reaction

2. Hematological toxicity: cause anemia and aplastic anemia

3. nausea/vomiting/nasty taste/diarrhea→ following oral dose

4. Gray baby syndrome → can also occur in adults who overdose on

chloramphenicol

→ Death occurs in 40% of patients

Drug interaction: (cytochrom inhibitors)

Prolongs half-lives of drugs that use cytochrome P450 isozyme pathway for
metabolism such as warfarine, and anti-retroviral protease inhibitors.

→Chloramphenicol is contraindicated in pregnancy

It is relatively toxic (agranulocytosis and aplastic anemia in mother and fetus)

Gray-baby syndrome →inadequate metabolism

----------------------------------

 Clindamycin

Clindacin Clindamycin Birzeit Cap:150mg

Clindex Clindamycin Pharmacare Gel
vaginal cream
topical solution
Denacine Clindamycin Beit Jala Cap:150, 300mg
Emulgel
Topical solution
Dalacin C Clindamycin Pfizer Cap:150, 300mg
Vaginal ovules 100mg
Dalacin T Clindamycin Pfizer Topical solution
Zindaclin Clindamycin Taro Gel 1%
Duac Clindamycin Stiefel Gel
Benzoyl peroxide Store at refrigerator before
opening, but after opening store it
below 25 c
Using within months after first
opening.
‫يجب ان ال يالمس الدواء الشعر والمالبس‬
BP ‫الحتواءه على ال‬
Dalagis Clindamycin Agis Lotion
Amycin T Clindamycin Jerusalem Lotion

→particulary effective against anaerobes except in brain because it does not pass
through BBB
Also effective against staohylococcal infections.

Spectrum and MOA: like macrolide

→parenterally/ topically / orally (food does not interfere with absorption)

→Penetration into bone is good and occurs even in the absence of •

inflammation.

-→ SE:

Diarrhea(common)

Skin rash (uncommon to common )

Others are not common

→Pregnancy:

Clindamycin is only indicated when penicillin, cephalosporin, erythromycin

or other macrolides are nor effective.

No controlled date on the first trimester, but in the 2nd and 3rd trimester it
can be used.

Streptogramins are a group of cyclic peptide antibiotics that inhibit, like

macrolides and lincosamide, the synthesis of bacteria protein. They are
derivatives of the naturally occurring pristinamycin, the later developed
derivatives quinupristin and dalfopristin are used in a fixed combination.

Quinupristin- Dalfopristin→ is a combination of two antibiotics used to treat

infections by staphylococci and by vancomycin-resistant Entercoccus faecium.

Write your notes:

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 Fluoroquinolones:
First generation: Nalidixic acid

Second generation: ciprofloxacin / Norfolixacin / Ofloxacin

Third generation: Levofloxacin → has increased activity against gram +ve

Fourth generation: Moxifloxacin, gatifloxacin, gemifloxacin → active against anaerobic

and gram +ve

This classification is according to its coverage.

MOA: inhibit DNA gyrase(topoisomerase 2) and topoisomerase 4.

Bacteriocidal

U-gram Nalidixic acid Jerusalem Tab: 250, 500

Susp: 250
For UTI

Ceproxx Ciprofloxacin Birzeit Tab:250mg

Caplet:500,750
Floxin Ciprofloxacin Jerusalem Tab:500mg
Floxin HC Ciprofloxacin 0.2 Jerusalem Otic suspension
Hydrocortisone 1 ‫ترج جيدا قبل االستخدام‬
Used for acute otitis externa
7 ‫ ساعة لمدة‬12 ‫ نقاط باألذن المصابة كل‬3
‫أيام‬
‫ صالحة ألسبوعين بعد‬, ‫ال توضع بالثالجة‬
‫الفتح‬
Ciprocare Ciprofloxacin Pharmacare Tab: 250,500,750
Ciprocare XR:1000mg
‫مرة باليوم‬
Ciprodex Ciprofloxacin Dexcel Tab: 500mg
Ciprofloxacin Ciprofloxacin Accord Tab: 500mg
Ciloxan Ciprofloxacin Novartis Eye drops 0.3%
Ciprofloxacin with or without food, be sure to consume plenty of fluids
while taking ciprofloxacin,
Shouldn't be taken along with dairy products or calcium fortified juices, it should
be taken at least 2 hours before or after consuming these products.

)‫ يؤخد مرتين باليوم (لعمر صغير‬250 mg ‫عيار‬

‫ مرات باليوم‬3 ‫ مرتين ل‬500mg ‫عيار‬

‫ مرة لمرتين باليوم‬750 mg ‫عيار‬

Dose of ciprofloxacin for children: 20-40 mg/kg/day

Indications of ciprofloxacin:

Particularly useful in treating infections caused by many Enterobacteriaceas (such

as :E. Coli / salmonella / shigella) and other gram negative bacilli

For example:

-Effective for UTI more than trimethprim-sulfamethoxazole

-Traveler's diarrhea (Norfloxacin and ciprofloxacin used)

- it is the most potent of the fluoroquinolone for Pseudomonas aeroginosa

- alternative for aminoglycoside due to its toxicity

- typhoid fever

-shigllosis

-ciprofloxacin useful for Bacillus anthracis ( the alternative is doxycycline)

Ofloxacin teva Ofloxacin Teva Tab: 200mg

Taricin Ofloxacin Biet Jala Tab: 200mg
Taricin drops Ofloxacin Biet jala Eye and ear drops
Oflodex Ofloxacin Dexcel Caplet: 200mg
Ultracin Ofloxacin Birzeit Eye drops
Cap: 200mg
Oflox Ofloxacin 0.3% Allercan Eye drops solution
Tarivid Ofloxacin sanofi Tab:200mg
Taricin once daily

General rule: eye drops are stable for 30 days after open
 Voloxal Levofloxacin Birzeit Tab: 500, 750
0.5%
Voloxal-eye Levofloxacin Birzeit Eye drops
drops (twice daily)
Cornexal Levofloxacin Birzeit Eye drops (twice
1.5% daily)
Levox Levofloxacin Jerusalem Tab:500, 750
Tavanic Levofloxacin Sanofi Tab: 500
Levoflox Levofloxacin Sama Tab:
250,500,750
Vivaxin Levofloxacin Biet Jala Tab: 250, 500,
0.5% 750
Vivaxin –eye Levofloxacin Biet Jala Eye drops
drops (twice daily)
Levact Levofloxacin Pharmacare Tab: 500 mg
Livotreat Levofloxacin Beit Jala Eye drops
1.5%

Levofloxacin is very useful for upper respiratory tract infection such as

bronchitis and sinusitis, also for lower respiratory tract infection .

Levofloxacin for UTI : 250mg once daily for 10 days

Higher doses if for respiratory infections.

Megaxin Moxifloxacin Bayer Tab: 400mg

Moxiflox Moxifloxacin Pharmacare Tab: 400mg
Basilox Moxifloxacin Birzeit Tab: 400mg
Eye drops
Vigamox Moxifloxacin Novartis Eye drops 0.5%
Moxifloxacin cannot be used for UTI because its elimination is not through
the kidney, instead is metabolized by the liver so it does not used with
hepatic failure.

Moxifloxacin work better than older generation against S. pneumonia, but

all of them work well against atypical orgaisms causing community-
acquired pneumonia( Mycoplasma and Chlamydia pneumonia)
Moxifloxacin has activity against many anaerobes

Factive gemifloxacin Jerusalem Tab:320 mg

Available as 5
days or 7 days
therapy

Zymaxid Gatifloxacin Allercan Ophthalmic solution

0.5%(2.5ml)
Zymar Gatifloxacin 0.3% Allercan Ophthalmic solution
(5ml)
Note: fluoroquiolone is no longer recommended for N. gonorrheae due to
resistance.

Note: using of fluoroquinolone for treatment to E.coli can induce shiga-like

toxin expression, this toxin is responsible for hemolytic uremic syndrome )

Note: fluoroquinolones are ideal for osteomylitis, joint infection and soft
tissue infection such as diabetic foot and venous ulcers

Note: levofloxacin and moxifloxacin are referred as (respiratory

fluoroquinolones, because they have excellent activity against
S.pneumoniae which is a common cause of community-acquired
pneumonia CAP

Note: fluoroquinolone is the second choice as alternatives for patients with

severe B-lactam allergy ( erythromycin Is the first)

Note: ciprofloxacin and ofloxacin are excreted in breast milk so they are
contraindicated in lactation
Side effects of fluoroquinolone:
1. nausea, vomiting, diarrhea

2. phototoxicity: sunscreen should be used and avoid excess exposure to

sunlight

If it is occurring, the discontinuation of the drug is advisable.

3. Articular cartilage erosion (arthropathy):

So, it should be avoided in pregnancy, lactation and in children under 18

years old.

FDA pregnancy category C

Note: quinolones should only be used in case of complicated infections

resistant to the antibiotic of choice in pregnancy

→ciprofloxacin and norfloxacin are the choice, because of their relatively

large documented experience.

4. prolong QT interval: should not be used with arrhythmias

5. ciprofloxacin can increase the level of theophylline by inhibiting its

metabolism

6. fluoroquilones are cytochrome inhibitor so they may raise the level of

warfarin, caffeine and cyclosporine

Fluoroquinolones are contraindicated with:

Pregnancy

Lactation

Children under 18 years old

Arrhythmia
 Patient counseling:
→Oral fluoroquinolones tablets may be taken with or without food

→take exactly as directed and for the time period indicated to reduce the
risk of resistance

→ Take the drug at least two hours before or two hours after
magnisum/aliuminium containing antacid or preparation containing iron or
zinc

→avoid administration of drug with dairy product

→ensure you keep hydrate to prevent crystal formation in the urine

→protect yourself from sunlight and avoid excess exposure of sun, when
sunblock when outdoor

‫بنحكي للمريض يبعد عن الشمس ويستخدم واقي شمس لما يطلع من البيت‬

‫يبعد عن منتجات الحليب ومضادات الحموضة والمنتجات اللي فيها حديد وزنك اقل اشي ساعتين قبل وبعد‬
‫الدوا‬

‫يشرب الدوا مع كمية مي كبيرة ويكتر مي خالل اليوم‬

Lormyx Rifaximin Tab: 200mg MOA:

Inhibit RNA synthesis by binding to the beta-subunit
of bacterial deoxyribonucleic acid(DNA)dependent
ribonucleic acid (RNA) polymerase.
This binding blocks translocation, which stops
transcription.

Indications:
Traveller’s diarrhea
Reduction of hepatic encephalopathy recurrence
Irritable bowel syndrome with diarrhea
Folate antagonists:
Inhibitors of folate synthesis:→ Silver sulfadiazine

→Sulfasalazine

→Sulfisoxazole

Inhibitors of folate reduction→ Pyrimethamine

→Trimethoprim

Combination of inhibitors of folate synthesis and reduction→Cotrimazole

(Trimethoprime + sulfamethoxazole)

Sulprim Sulphamethoxazole Jerusalem Tab: 400 +80 mg

+ trimethoprim
Sulprim forte // Jerusalem Tab: 800+ 160 mg
Resprim // Teva Susp: 200+40 mg
For Pediatric
Sulfaprim // Beit Jala Tab: 400+80mg
Susp: 200+ 40mg
Diseptyl // Rekah Susp: 200+ 40mg
Diseptyl forte // Rekah Caplet: 800+160mg

Septrin // Gsk Ampoule

Septrin DS // Gsk Tab: 400 +80 mg
Bactrim // Roche Tab:400+80
Dose: based on trimethoprim:

For adult: total 360mg/ day ( 4 tablets of sulprim or 2 tablets of sulprim

forte

For pediatric: 8 mg/kg divided into 2 times.

Can be taken with or without food→take with food if it causes as stomach

upset.
 Silverol Silver ABIC Cream 1% - to prevent burn wound
infections
sulfadiazine ‫مستحضر مضاد للجراثيم يستعمل كعالج‬-
‫موضعي للحروق والتقرحات المتلوثة‬
‫ال يستعمل لالشخاص الذين يعانون من‬-
‫ وال الحوامل وال‬sulfur ‫حساسية من ال‬
‫المرضعات وال الرضع خالل االشهر‬
‫االولى من حياتهم‬
‫ يوم بعد فتح العلبة للمرة‬30 ‫يستعمل لغاية‬-
‫االولى‬
Silvezin Silver Beit Jala cream
sulfadiazine

Salazopyrin Sulfasalazine pfizer Tab:500mg ‫يستخدم لعالج التهاب القولون‬

‫التقرحي ومرض كرون‬
Salazopyrin Sulfasalazine pfizer Tab: 500 mg En:enteric coated
EN To treat rhumatoide
arthariritis and
pyoderma
gangrenosum

Sulfonamides:

-Bacteriostatic in general, Bacteriocidal in urine

-Broad spectrum ( both G+ and G-)

-Competitive inhibitors of dihydropteroate synthase.

-Eliminated mostly by kidney into the urine, partially uncharged, partially

metabolized.

Indication :
Cotrimazole ( sulfamethoxazole + trimethoprim):

Widely used to treat:

- UTI (very effective)

-is the drug of choice for Nocardiosis ( severe pulmonary infection in

immunocompromised hosts)

-Gastrointestinal infection

-Respiratory tract infection

- Pneumocystis infections.( fungal aportiunstitic infection)( the most effective

therapy)

----

Sulfasalazine→ poor oral absorption→ to treat ulcerative colitis and irritable

bowel syndrome

Sulfactemide→ to treat ophthalmic infections

Silver sulfadiazine or Mafenide → to prevent burn wound infections

Sulfadiazine plus pyrimethamine → for toxoplasmosis

Sulfadoxine→ long acting sulfonamides, comined with pyrimethamine to prevent

and treat malaria

Toxicity and contraindications :

1. Crystalluria

sulfamethoxazole and sulfadiazine can crystallize in acid urine or in dehydrated patients causing
urinary obstructions → prevented by alkalizing with sodium bicarbonate or increasing hydration
( common to uncommon)

2. Hematopoietic system (rare to extremely rare)

Acute hemolytic anemia ( in patient with G6PG deficiency

Agranulocytosis

Aplastic anemia
3. hypersensitivity reaction( skin rash, necrosis of liver(rare) )

4.Nausea /vomiting / anorexia (common)

5. Kernicterus (newborns)→ sulfa drugs displace bilirubin from binding sites on

serum albumin. (sulfonamides are not given to pregnant, especially near to
delivery or lactating women).

6. sulfonamide potentiate effect of:

Oral anticoagulants

Sulfonylurea hypoglycemia

Hydntoin anticonvulsants ex: phenytoin

7. Cotrimazole

→ dermatologic reaction(common and severe in the elderly)

→ GI: nausea/ vomiting /glossitis /stomatitis

→phototoxicity due to sulfamethoxazole

→Hematologic disorders

→fever/rash/diarrhea/pancytopenia frequently in patients infected with HIV

and has P.jiroveci pneumonia

→prolonged prothrombin time in patient receving both trimethoprim and

warfarin (reported)

→plasma phenytoin may be increased due to inhibition its metabolism

→methotrexate levels may rise due to displasment from albumin-binding sites by

sulfamethoxazole

Note: trimethoprim or cotrimazole can be used in UTI if penicillin and

cephalosporin is ineffective.
 Is this case we try to avoid using them in the first trimester, and when there
is a need→ folic acid (0.5mg/day) is recommended

Should not be used near to delivery (Kernicterus)

Cat: B, but D near term

Urinary tract antiseptic:

The most common cause of UTI is E. Coli

Urinary tract antiseptic are:

Methenamine/ Nitrofurantoin/ Nalidixic acid

These drugs are concentrated in the urine

Metheamine →decomposes at acidic PH producing formaldehyde which is

toxic to most bacteria and do not develop resistance to it.

→should not be used in patient with indwelling catheters

→effective for lower UTI not upper

→also produce ammonium in bladder that metabolized to urea by the

liver so it is contraindicated in hepatic dysfunction

→SE: GI distress / albuminuria, hematuria and rash at higher doses

Macrofuran Nitrofurantoin Birzeit Cap: 100mg

4 times daily
-For UTI
-Taken with food or milk to
improve absorption and
tolerance
-Should not be used in
patient with G6PD
deficiency
Nitrofurantoin sensitive bacteria reduce the drug to a highly active
.intermediate that inhibits various enzymes and damages bacterial DNA

→Antibiotic activity is greater in acidic urine

→It is useful against E. coli

→Gram-positive cocci are susceptible

→Bacteria that are susceptible rarely become resistant during therapy

→Hemolytic anemia is encountered in patients with G6PD def

.→This medicine can turn urine a dark yellow or brown colour

→Contraindications: Anuria, oliguria, significant impairment of renal function

→Nitrofurantoin can be given during pregnancy to treat UTI when the antibiotics
of choice have been ineffective.

Also, it can be used as prophylaxis of UTI and to treat asymptomatic bacteriuria in

pregnancy

Cat:B

It can be used until week 38, because there is a risk of hemolytic anemia,
especially if the baby has G6PD-defficency.

Urinary tract analgesic:

Utised Phenazopyridine Birzeit Tab: ‫هو فقط مسكن لاللم لذلك عند اخذه مع‬
100mg ‫المضاد الحيوي يعطى لمدة يومين فقط‬

‫ يغير لون البول الى االحمر ويجب‬:‫مالحظة‬

.‫اخبار المريض بهذه المعلومة‬
G6PG deficiency ‫ال يعطى لمريض‬
Sedurol Phenazopyridine Rekah Tab:
100mg
 Also for UTI:

Cefuroxime like Zinat 500mg twice daily → the most safest one even for
pregnant women

Ciprofloxacin like floxin twice daily→ not used during pregnancy

Trimethoprime + sulfamethoxazole like sulprim

→should not be used in patient with sulfur allergy.

Note: if the patient has fungal infection also

→Fluconazole like dican : once weekly- can be given for 3 weeks

→or Itranox : two tablets in the morning and two tablets in the evening for
one day

Other antibiotics:

Monurol Fosfomycin Rafa Sachets: powder -bacteriostatic at low dose

for oral solution -bacteriocidal at high dose
3g in each sachet -Not intended for infant or children under 12
years
-Not intended for patient less than 50 kg
-used as single dose: 1-2 times weekly
-for UTI:
Primarily for bladder infection
Occasionally for prostate infection
Not recommended for kidney infection, and
it does not used if the patient has renal
impairment
-the bladder should be empty when it used,
also the stomach should be empty(2 hours
before or after meal)
-preferably before bedtime after emptying
the bladder
- improvement should be expected within 2
to 3 days, if not tell the doctor.
 Bactroban Mupirocin GSK Ointment 2%
Mupirocin teva Mupirocin Teva Ointment 2%
Mupiricin: it is topical antibiotic that work by blocking the ability of bacteria of
producing protein, it is used for superficial infections such as impetigo (caused by
streptococcus) or folliculitis.

Fucidin Fucidic acid Leo Cream

Ointment 2%
Fusylin cream Fucidic acid Jerusalem Cream 2%
Ointment 2%
Sidi cream Fucidic acid Sama
Zydex Fucidic acid Beit jala Cream2%
Ointment 2%
Eye gel 1%
Fucithalmic Fucidic acid Amdipharm Viscous eye
drops
(sustained
release)
Staphiderm Fucidic acid Taro Cream
Applied 3 to 4 times daily on the skin

Fucidic H Fucidic acid+ LEO Cream

hydrocortisone
acetate
Fusylin-H Fucidic acid+ Jerusalem Cream
hydrocortisone
acetate
Zydex HC Fucidic acid+ Beit Jala Cream
hydrocortisone
acetate

Fusicort Fusidic acid+ Leo Cream

betamethasone
Zydex-B Fusidic acid+ Beit Jala Cream
betamethasone
Sidi-Zone Fusidic acid+ Sama Cream
betamethasone
 Fusylin Sodium fusidate Jerusalem Ointment 2%
ointment
Zydex ointment Sodium fusidate Beit Jala Ointment

Metronidazole:

Metrozole Metronidazole Birzeit Tab:250,500

Entogyl Metronidazole Jerusalem Tab:250,500
Flagyl Metronidazole Sanofi Tab:250

Antibacterial and anti-amoebic agent

It has broad spectrum cidal activity against protozoa, includind Giardia Iamblia

Is selectively toxic to anaerobic microorganisms

MOA: it enters the cell by diffusion then its nitro group is reduced by redox
proteins (nitroreductase) to highly reactive nitro radical which exerts cytotoxicity
by damaging DNA and other critical biomolecules.

Administerd orally→completely absorbed→ widely distributed-→metabolized in

liver→excreted in urine

Side effects: (GI SE)→anorexia/ nausea/ metallic taste/ abdominal cramps/

dryness of mouth/ loose stool is occasional

Headache

Contraindication:

-neurological disorder→because at the long use it cause peripheral neuropathy

-blood dyscrasias (abnormality in blood)

- first trimester of pregnancy( but it can be used in the second and third
trimester)

-chronic alcoholism

Interactions:

Disulfiram like intolerance→patient should avoid drinking

→when metronidazole is given with alcohol→abdominal distress, nausea,

vomiting, flushing, headache, tachycardia, hyperventilation

Metronidazole is enzyme inducer(like phenobarbitone, rifampicin)

Cimetidine reduce metabolism

It decreases renal metabolism of lithium

Clinical uses of metronidazole:

1.Amoebiasis 2. Giardiasis

3.Trichomonas vaginitis 4. Anerobic bacterial infection

5. pseudomembranous enterocolitis

Uroclean Hexamine+ Beit Jala Powder For UTI

sodium benzoate

Anti-infectives for lactating women:

1st choice: penicillin

2nd choice: cephalosporins (second generation are preferable)

3rd choice: B-lactam and clavulanic acid

Others:

Macrolide: erythromycin, Roxithromycin

Tetracycline: are excreted into milk (Doxycycline is compatible with breast feeding)

Quinolones: should not be used during breastfeeding

Aminoglycoside: are preferred not to be used (is has poor absorption but possible
adverse effects on GI flora and risk of bloody diarrhea.

Clindamycin: should not be used routinely (no enough data)

Chloramphenicol: is contraindicated, especially in the first month

Metronidazole: better vaginally (if used orally, should be in the evening after the last
breastfeed)

Management of common infections with antimicrobials guidance clinical

practice guidelines 2019 by the National Institute for Health and Care
Excellence :

Acute Sore Throat:

For low-risk patients, use acetaminophen (first choice) or ibuprofen for

pain.

The decision for antibiotics is based on the fever pain or centor score

Preferred antibiotics: penicillin VK ( first choice) or clarithromycin (if

penicillin allergy) or erythromycin ( in pregnant women)

Sinusitis:

Use acetaminophen or ibuprofen for pain

Do not use antibiotic in patient with symptoms for 10 days or less

Consider high-dose nasal corticosteroid in patient older than 12 years

High-risk patients should receive immediate antibiotic therapy

The preferred antibiotic is penicillin VK.

In patient with a penicillin allergy, use clarithromycin (if 12 years old or

more), erythromycin ( if pregnant)

Amoxicillin/clavulanate is the second choice or forst choice in high-risk

patients.

Lower Urinary Tract Infection

In nonpregnant women→ preferred antibiotic is nitrofurantoin

Second choices include amoxicillin or cephalexin

Other choices: TMP-SMX, fosfomycin

For pregnant women→ the choices are amoxicillin(or with clavulanic acid),
ampicillin, cephalosporin

Note: trimethoprim or cotrimazole can be used in UTI if penicillin and

cephalosporin is ineffective.

Is this case we try to avoid using them in the first trimester, and when there
is a need→ folic acid (0.5mg/day) is recommended

Should not be used near to delivery (Kernicterus)

Note: Nitrofurantoin can be given during pregnancy to treat UTI when the
antibiotics of choice have been ineffective.

Also, it can be used as prophylaxis of UTI and to treat asymptomatic bacteriuria in

pregnancy

In men→ preferred antibiotic include trimethoprim or nitrofurantoin

In children older than 3 months→ first choices include trimethoprim or

nitrofurantoin (if eGFR≥45ml/min)

→second line agents: nitrofurantoin if not used

as first choice, amoxicillin or cephalexin
The duration of antibiotic therapy for UTI in patients with acute cystitis episodes
should be as short as is reasonable (typically no longer than 7 days)

UTI symptoms that persist after antimicrobial therapy should prompt repeat urine
culture to guide further treatment.

Acute Prostatitis

First line: ciprofloxacin, ofloxacin or trimethoprim

Second choice: levofloxacin or clotrimazole

Toxicity of antibiotic:
-Harmful effects have resulted from allergic reaction or intravenous
overdose.

-serious toxicity from a single acute ingestion is rare.

-Clinical presentation after acute oral overdose, most agents cause only
nausea, vomiting and diarrhea or abdominal pain.

- IV presentation may contain preservatives such as benzyl alcohol or large

amounts of potassium or sodium

- drug interaction may increase toxic effects.

Specific drugs and antidote:

1-Trimethoprim ( dihydropholate reductase inhibitors): inhibit the

reduction of dihydrofolic acid (DHF) to tetrahydrofolic acid (THF)

Trimethoprim can cause thrombocytopenia(low level of platelets) by

lowering folic acid metabolite levels, this may also cause megaloblastic
anemia.

Poisoning: administer leucovorin (folinic acid) folic acid is not effective.

2- Dapsone overdose: Dapsone metabolites oxidize the ferrous iron
hemoglobin complex to the ferric state (methemoglobinemia)

Administer methylene blue for symptomatic methemoglobinemia.

3- Treat isoniazid (INH) overdose with pyridoxine (vitamin B6)

Peripheral neuropathy and CNS effects ( a seizure disorder) are associated

with the use of isoniazid and are due to pyridoxine depletion.

Probiotics

‫ تزيد من عدد‬،‫هي مستخلصات بكتيرية حيوية موجودة على شكل مستحضرات دوائية مختلفة‬
.‫البكتيريا النافعة بالجسم‬

Lactobacillus Hexibios Sachets:

granules
Acidophilus Cap ‫يوضع بالثالجة بعد‬
‫فتح العلبة‬
Probiotique Cap Jamieson

Antibiotics that do not refrigerate:

Azithromycin

Clarithromycin

Cefdinir

Cefixime

Cefadroxil

Note: Erythromycin should be stored at refrigerator

 TO ANYONE WHO IS READING THIS …
MAY CLARITY REPLACE CONFUSION …
MAY PEACE AND CALMNESS FILL YOUR LIFE…
YOU HAVE TO KEEP ON… ♥
 Antifungal agents
Fungal infections are called mycosis → can be superficial or penetrate the skin and
cause subcutaneous or systemic infections
The risk of fungal infections increases with immunosuppression cases such as in organ
transplantation, cancer chemotherapy or HIV.
Main component of fungal cell wall: ergosterol

Drugs for systemic fungal infection:

Amphotericin B
→it is the drug of choice for severe and life-threatening mycoses (it is very toxic)
→Slow IV infusion because of infusion toxicity, it can also cause nephrotoxicity
Note: Liposomes amphotericin B (with artificial lipids) overcome these problems
→large volume of distribution (but does not reach CSF)
→Category B in pregnancy (dose not cross the placenta)→it is the choice in serious
mycoses.
→SE:
Fever and chills: 1 to 3 hours after IV administration
Renal impairment
Hypotension and hypokalemia
Thrombophlebitis: adding heparin to the infusion can reduce this problem
Flucytosine
→orally
→disrupts nucleic acid and protein synthesis
→give synergistic effects with amphotericin B
➔ Has hematologic SE (decrease WBCs) and GI SE (N/V/D)
Azole antifungals:
MOA: inhibit fungal cell growth by inhibit C-14 alpha demethylase enzyme responsible
for ergosterol synthesis. (Fungistatic)
All of them are CYP450 3A4 inhibitors
1. Triazole: given systemically for systemic and topical infection
Fluconazole / Itraconazole / Voriconazole / Posaconazole
Fluconazole Cap: 150mg Teva
Fluconazole Trican Cap: 50,100, 150, Pfizer
200mg
Diflucan Powder for Pfizer
suspension:
50mg/5ml
Triflucan IV infusion Pfizer
Flucanol Cap: 100, 150, Rafa
200mg
Dican Cap: 150mg Pharmacare
Monozole Cap: 150mg Jepharm
Flucan Cap: 150mg Birzeit

Fluconazole –> is used for prophylaxis against invasive fungal infections in

recipients of bone marrow transplants, and it is effective for most forms of
candidiasis.
Fluconazole is the choice for treating fungal infections systemically in pregnant
women.

Itraconazole Sporanox Cap: 100mg Janssen

Oral solution
Itranols Cap: 100mg Rafa
Itranox Cap:100mg Birzeit
Neomixin Eye ointment Beit Jala

Itraconazole → it is used for the treatment of onychomycoses (fungal infections

of nails)
It is not very effective for candidiasis.
Should be used on an empty stomach, 1 hr before or 2 hr after meal.
 Voriconazole Vortimal Vial: 200mg/vial Anfarm Hellas
Vfend Tab: 50 Pfizer

Tab:200mg R-Pharm

Powder for oral Fareva

susp: 40mg/ml
Vial: 200mg/vial

2. Imidazole: for topical infection (tinea ‫)النهابات فطرية بالجلد‬

Miconazole / Ketoconazole / Bifonazole / Clotrimazole / Isonazole

Miconazole Daktazole Cream 2% Jepharm

Oral gel 2%

Gyno-daktazole Vaginal ovule4%

Vaginal cream 4%
Fungitrin Cream Birzeit
Oral gel

Gyno-Fungitrin Ovules/soft caps

Daktarin Cream Janssen

Oral gel
Pitrion Cream Rafa
Fungazole Cream Pharmacare
Miconazole Mico-Cort Cream Jepharm
Hydrocortisone Daktacort Cream Janssen
(stored in
refrigerator)

Ketoconazole Orazole Tab: 200mg Birzeit

Shampoo
Ketoral Tab: 200mg Pharmacare
Shampoo
Nizoral Tab: 200mg Janssen
 Shampoo
Cream
Ketozole Shampoo Perrigo
Dandrex Shampoo Beit Jala
Abket Cream Sama
Ketoconazole: it requires acid for its absorption (after meal, 2 hr after PPI and
antacid), it is not used now for systemic fungal infection because of the risk of
severe liver injury, adrenal insufficiency and adverse drug interaction.

Bifonazole Agispor Gel Perrigo

Shampoo
Solution
Cream
Bifonazole Cream Rekah
Bifocare Cream Pharmacare
Powder
Solution
Bifonazole +urea Keratospor Ointment Perrigo
‫تساعد اليوريا على نمو‬
‫األضافر كما ان لها تأثير‬
‫مقشر‬
Bifonazole Comagis Cream Agis
Fluocinonide
It is used for relief
of inflammatory
conditions
accompanied by
fungal infection.
Bifonazole: broad spectrum antifungal.

Clotrimazole Canesten Cream Bayer

Mycoten Cream Beit Jala
Vaginal cream
Vaginal tab
Agisten cream Cream Perrigo
Agisten baby Solution for ear
Agisten Alovera use
Agisten solution Vaginal tab
Trimazole Cream Sama
Clothree Tab: 200mg Teva
 Oralten Tab:10mg Perrigo
Clotrimazole Hydroagisten Cream Perrigo
Hydrocortisone Mycoten HC Cream Beit Jala
Clotrimazole Tevacutan Cream Teva
Dexamethasone Polucutan Cream Perrigo
Neomycin Medihist Cream Birzeit
Clotrimazole Triderm Cream MSD
Betamethasone
Gentamycin
Note: Clotrimazole and Miconazole are the drug of choice for topical treating
fungal infections in pregnant women.
Clotrimazole is the most effective OTC antifungal product.
.‫في عالج الفطريات موضعيا يفضل استخدام كريم وليس مرهم الن المرهم يعزز الرطوبة‬

Isonazole Isogen Cream Perrigo

Other antifungals:
Terbinafine
Terbinafine Terbinafine TEVA Caplet: 250mg Teva
Tinasil Tab: 125mg, 250mg Beit Jala
Solution
Cream
Lamirase Tab: 250mg Birzeit
Cream
Spray
Lamisil Cream GSK
Spray
DermGel
Lamifast Cream Pharmacare
Spray

It Is the drug of choice for treating fungal infections on nails. (it is more effective than
itraconazole, miconazole or griseofulvin)
Duration of therapy: 3 months but it still shorter that with griseofulvin.
Topical terbinafine is used for tinea pedis ‫فطريات القدم‬, tinea corporis (ringworms) ‫فطريات‬
‫ )في الرقبة او الظهر او البطن وتظهر على شكل دوائر لونها احمر ومركزها فارغ‬, tinea cruris ‫فطريات في‬
‫المنطقة التناسلية‬,
‫فطريات القدم ممكن يتم وضع بودرة عليها لحتى تمتص الرطوبة‬
‫فطريات الجلد اذا كانت المنطقة صغيرة ممكن نكتفي بالعالج الخارجي اما اذا كانت المنطقة كبيرة يفضل اخذ ادوية‬
‫فموية‬
Duration of therapy with terbinafine is usually 1 week.

Terbinafine is CYP450 2D6 inhibitor.

Note: For the tinea cruris → the drug of choice is clotrimazole.
Note: for treating tinea capitis ‫(فطريات في فروة الرأس‬topical antifungals are ineffective),
oral antifungal is required (griseofulvin, terbinafine, itraconazole)

Butenafine
Its structurally related to Terbinafine
Butenafine Mentax Cream Agis

Griseofulvin
Griseofulvin Sporofulvin Tab:125mg Beit Jala
Susp :125mg/5ml
MOA: inhibit fungal mitosis
For onychomycoses→ it has been replaced by terbinafine
For fungal infection of the scalp and hair →it is still used
Duration of therapy: long →ex: 3-6months for nail fungal infection
Its absorption enhanced by high-fat meals
It is CYP450 inducer
It is contraindicated in pregnancy.
Nystatin
Nystatin Candistan Oral drops Birzeit
Nystatin ready mix Oral drops Taro
Nystatin Nystazole Vaginal ovule Birzeit
Metronidazole
Nystatin Dermacombin Cream Taro
Neomycin Ointment
Gramicidin Decomb Cream Birzeit
Triamcinolone Ointment
Resemble of amphotericin B
It is used for the treatment of cutaneous and oral candida infections (swish and swallow
or swish and spit) ‫مضمضمة ثم بلع او مضمضة ثم بصق‬
It is not absorbed by GIT
It is not used parenterally because it is nephrotoxic.
→Nystatin can be used throughout pregnancy without restriction.
It is the drug of choice for the treatment of superficial candida infections in mouth,
intestine and vagina.

Tolnaftate
Tolnaftate Phytoderm Ointment Teva
Benzoic acid compositum
Salicylic acid

Disrupt the growth of fungi

It is used topically for tinea pedis, cruris, corporis.

Ciclopirox
Ciclopirox Cicloderm Cream Trima
Topical Solution
Ciclopirox Cicloderm-C Cream Trima
Gentamicin
Is a synthetic antifungal, it is most useful against tinea versicolor (fungus interfere with
the normal pigmentation of the skin, resulting in small, discolored patches).

In pregnancy:
Amphotericin B is the choice in serious mycoses in early pregnancy.
Clotrimazole and Miconazole are the drug of choice for topical treating fungal infections
in pregnant women.
Fluconazole is the choice for treating fungal infections systemically in pregnant women.
Nystatin can be used throughout pregnancy without restriction, It is the drug of choice
for the treatment of superficial candida infections in mouth, intestine and vagina.
Griseofulvin is contraindicated in pregnancy.
Terbinafine should not be used during pregnancy (because there is no enough data and
nail infection is not an urgent condition).

In lactation:
Topical therapy is preferred
If systemic therapy is needed: Fluconazole is the preferable agent. (because it used as
single dose).
If possible, should be taken at night after the last breastfeed.

Notes:
Tinea corporis and cruris require once to twice daily treatment for 2 weeks
Tinea pedis require treatment for 4 weeks
Treatment should be continued for at least one week after symptoms have resolved.
---------------------------------------------------------------------------------------------------------------------
Antiviral drugs
Drugs for herpes:
Acyclovir / Ganciclovir / Foscarnet
Acyclovir Virax Susp Birzeit
Virax cold sores Cream
Virax HC Cream
Supraviran Tab: 200, 800mg Pharmacare
Susp:200mg/5ml
Cream /cold sores cream
Zovirax Tab:200,400,800mg GSK
Ophthalmic ointment
Cream /Genital cream
Amp
Acyclo-V Tab: 200,400mg CTS
Acyclovenir IV infusion: 250mg Avenir
Acyclovir is active against herpes viruses ex: herpes simplex and varicella zoster, but
does not eradicate them, they may be reactivated in case of immunodeficiency and
stress.
MOA: inhibit nucleic acid synthesis.
It is effective orally, topically or parenterally
High oral doses are effective in treating severe shingles by VZV ‫حزام ناري‬

Valcyclovir is a prodrug of acyclovir (orally), it has higher bioavailability than it.

Valcyclovir Valtrex Tab: 500mg GSK

Acyclovir and pregnancy:

Topical use is safe.
Oral treatment is used for genital herpes to prevent vertical transmission of the virus to
the fetus.
IV administration is indicated for life-threatening conditions such as varicella pneumonia
or disseminated herpes simplex infection. (it should not be routinely administered in
case of uncomplicated herpes zoster).
--------
Ganciclovir is used only for severe cases in which acyclovir is not effective such as severe
cytomegalovirus infections.
(it is resistant to acyclovir because this virus dose not have kinas for activation of
acyclovir)
Valganciclovir: prodrug of ganciclovir
Valganciclovir Valcyte Tab: 450mg Roche
Valganciclovir Tab:450mg Teva
TEVA
--------------
Drugs for HIV:
→Zidovudine/Stavudine/ Didanosine / Zalcitabine / Lamivudine
inhibit reverse transcriptase of HIV (orally)
→Lamivudine: MOA: compete with cytosine triphosphate for incorporation into the
developing viral DNA. This result in chain termination.
Lamivudine Lamivudine Tab:150mg Teva
Zeffix Tab:100mg GSK
Epivir Tab:150mg GSK
Amuved Tab:100mg Birzeit

→Saquinavir / Ritnavir
Protease inhibitor
-------
Drugs for influenza
Amantadine / Zanamivir
 Amantadine PK-Merz Tab: 100mg Megapharm
It has a narrow spectrum and influenza vaccine is usually preferable.
-------------------------------------------------------------------------------------------------------------------

Anthelmintic drugs
Mebendazole
Mebendazole Vermox Tab: 100mg Janssen
Susp: 100mg/5ml
Vermazole Tab: 100mg Jerusalem
Susp: 100mg/5ml (Jepharm)
Vermacare Tab: 100mg Pharmacare
Susp: 100mg/5ml

MOA: Blocks glucose uptake in the parasites and depletion of glycogen store
It has minimal oral absorption, it excreted in urine as inactive metabolite ( ‫مكان عمله‬
‫)بالجهاز الهضمي ما في داعي يصير امتصاص‬
SE: no adverse effects with short term therapy, mild GIT disturbances (nausea/diarrhea
and abdominal pain)
Dosage regimen:
Adults: 100mg q 12hr for 3 days, then repeated after 10-14days
Children: 5ml q 12hr for 3 days, then repeated after 10-14days
Mebendazole in pregnancy:
It is better to delay the treatment after first trimester but if it is required before that it
can be used.
--------
Albendazole Eskazole Tab: 400mg GSK
It must not be given in the first trimester of pregnancy.
Metronidazole
Metronidazole Flagyl Tab: 250mg Sanofi 6
Susp:125mg/5ml
Metrozole Caplet: 250,500mg Birzeit
Susp 125mg/5ml
Rectal supp:100mg
Entogyl Tab: 250, 500mg Jerusalem
Susp: 125mg/5ml
Nedomet Tab: 250, 500mg Beit Jala
Susp: 125mg/5ml
Gel
Metrotab Tab: 250,500mg Sama
Rozex Gel Rafa
Metronidazole Vial Fresenius
Zidoval Vaginal gel with Rafa
applicator
Dosage:
Adults: 500-750mg q 8hr for 5-10 days.
Infants and Children: 30mg/kg/day divided q 6hr (not to exceed 4g/day).

Completely absorbed from intestine and widely distributed in the body.

Highly active amebicide, also work against anaerobic bacteria.

SE: metallic taste / nausea / anorexia / abdominal cramps/ loose stool is occasional.
Prolonged use causes peripheral neuropathy.
It is a cytochrome inducer
 Tinidazole Tinogyn Tab: 500mg Jerusalem
Fasigyn Tab: 500mg Pfizer

In pregnancy:
Metronidazole reaches to the fetus after systemic administration even by vaginal route.
It is recommended to treat bacterial vaginosis in pregnancies using metronidazole
because it may cause preterm delivery. (in this case oral therapy is more effective than
intravaginal therapy).
It is also can be used orally for trichomoniasis

Vaginal treatment not very effective as orally, also it exposes fetus to drug for longer
duration (oral therapy is safer)
IV therapy is used only in life-threatening anaerobic infections.
Conclusion: Metronidazole can be used for pregnant women if strongly indicated but
with caution in the first trimester.
Using of tinidazole is contraindicated during the first trimester of pregnancy.
In lactation:
Low-dose therapy, up to 500mg three times daily for a 7 to 10 days course are
considered to be compatible with breastfeeding.
Tinidazole → a nursing mother may chose to pump and discard her milk during
treatment and for 72 hours after last dose.
Note: metronidazole is contraindicated with Mebendazole: Stevens Johnson Syndrome
or toxic epidermal necrosis.
 Wishing the best to anyone struggling nowadays
May you find the relief you desire and the resolution you need
Keep going… ♥
 Topic 2: Cardiovascular System
Hypertension
It is happened because of elevation of vascular tone (unknown cause)
It is a risk factor for: kidney disease, MI, HF, stroke, blindness.
Systolic mmHg Diastolic mm Hg
Normal <120 And <80
Per-hypertensive 120-139 Or 80-90
Stage 1 140-159 Or 90-99
Stage 2 ≥160 Or ≥100
Hypertensive ≥180 Or ≥120
emergency

In the treatment of HTN, blood pressure goal is: systolic <140, diastolic <90
If elderly patient → the goal is less than 150/90
Stage 1 HTN is normally treated with monotherapy: (all of them are first line
agents):
ACE- inhibitor → ‫اذا العالج بدأ بدوا من عيلة تانية وقررنا نضيف كمان دوا بنضيف من هاي العيلة‬
Angiotensin receptor blocker
Calcium channel blocker
Thiazide diuretic
Stage 2 HTN is treated with two drugs with different mechanisms
Other drugs can be used:
B-blocker (not alone)
Alpha 1 blocker
Alpha 2 agonist
Adrenergic antagonist
Direct renin inhibitor
Arterial vasodilator

Angiotensin-converting enzyme inhibitors (ACE-I)

Captopril, Enalapril, Ramipril, Lisinopril
MOA: inhibit the converting of angiotensin 1 to 2 which is a vasoconstrictor and
stimulate aldosterone secretion.
Captopril Aceril Tab: 12.5, 25, 50mg Dexcel
Cardiopril Tab: 25mg Birzeit
Captopril Tab:25,50mg Teva

Enalapril maleate Vasotec (brand) Tab: 2.5,5,10,20mg Merck

Enalapril Tab:5, 10, 20mg
Anapril Tab:5, 10, 20mg Jerusalem
Angiocare Tab: 20mg Pharmacare
Enaladex Tab: 5,10,20 mg Dexel

Ramipril Tritace Tab:2.5, 5mg Sanofi aventis

Tritace comp: with Tab: 2.5, 5 mg

hydrochlorothiazide
Ramipril Teva Tab: 5mg Teva
Ramitens Tab: 1.25, 2.5 , 5, Rafa
10mg

Lisinopril Tensopril Tab:5, 10, 20mg MSD

SE:
1.Dry cough: due to increased level of bradykinin
2.Angioedema: due to increased level of bradykinin
3.Hyperkalemia: risk is increased with potassium-sparing diuretic, and potassium supplements
4.hypotension: ‫العالج وزيادة الجرعة يكون تدريجيا‬
 5. increase serum creatinine
ACE-I contraindicated in pregnancy because of increased risk of fetal renal damage and
inhibiting urine production.

‫ممكن ينوصفو لمريض ما عنده ضغط ؟ بكون لحماية الكلى خاصة لو مريض سكري‬

Angiotensin receptor blocker

Losartan, Valsartan, Candesartan, Olmesartan, Azilsartan.

Lozar Tab:50mg Birzeit

Ocsaar Tab:50mg MSD
Losartan potassium
Ocsaar plus:
(Brand: Cozaar for MSD) With Tab:50 + 12.5mg
hydrochlorothiazide
losarta Tab:50mg CTS
Losardex Tab:50 , 100mg Dexcel

Losardex plus:
With Tab:50 +12.5mg
hydrochlorothiazide
Lotan Tab:50mg Unipharm

Lotan plus: Tab:50+12.5 mg

With HCT

Amicor plus: Tab: 5/80 Birzeit

With Amlodipine 5/160
10/160

Atusar: 25/160
Valsartan With HCT
Valforj : Tab: 5/160 Bietjala
With Amlodipine 10/160
Valzan Tab: 80 Pharmacare
160

Valzan -HCT Tab:80/12.5

 160/12.5

Valzadepine: Tab:5/80
With Amlodipine 5/160
10/160
Valzadepine-HCT Tab:
160/5/12.5
160/10/12.5
160/10/25

ARBOZIDE Tab: Jerusalem

80/12.5
With HCT 160/12.5
160/25
320/25
Atifade Tab:80, 160 Sama

Amoval: Tab:
With Amlodipine 160/5
160/10
Diovan Tab: 80, 160mg Novartis

Co-Diovan: Tab:
With 80/12.5
hydrochlorothiazide 160/12.5
160/25
Exforge: Tab: Novartis
With Amlodipine 80/5
160/5
160/10
Valcard Tab:80, 160 Efroze

Co-valcard: Tab:
With 80/12.5
hydrochlorothiazide 160/12.5
160/25
 Candesartan Atacand Tab: 8, 16 mg Astrazeneca
as cilexetil
Atacand Plus: Tab:
With 16/12.5
hydrochlorothiazide

ARBs are more effective with CCB or thiazide diuretic.

These are no benefits of giving ACE-I and ARBs, and the risk of SE increased.
ARBs have the same SE as ACE-I, except the risk of dry cough and angioedema is significantly
lower
➔ ARBs can be used as alternative to ACE-I in this case
Aliskiren: is a renin inhibitor that block the converting of angiotensinogen to angiotensin 1.
→can cause dry cough, angioedema and diarrhea

Calcium Channel Blocker

1-Dihydropyridines (DHP): work only on the blood vessels
Ex: Nifedipine, Amlodipine, Felodipine, Nimodipine / Lercanidipine
2-Nondihydropyridine (NDHP): Work on the blood vessels and heart

Ex: Diltiazem, Verapamil.

Nifedipine Nifdilong Tab:30, 60mg CTS
(Brand:Adalat) Angilat Tab:10, 20mg Birzeit
Nifedipine XL Tab:30mg, 60 mg Teva
Osmo-Adalat Tab:20,30,60mg Bayer
Pressolat Tab:10mg Agis
Antrolin Rectal cream:
Nifedipin+Lidocain
For hemorrhoid

Amlodipine Amicor Tab:5,10mg Birzeit

Amicor Plus: 5/160

With valsartan 10/160
 Norvasc Tab: 5, 10mg Pfizer
Vascopin Tab:5mg Jerusalem
Secure Cap:5,10mg Beit Jala
Zalmodipine Tab:5,10mg Sama
Amlodipine Tab:10mg Teva
Amlostat : Tab:10/10 Beit Jala
Amlodipine+Atorvastatin
Valsartan ‫باإلضافة لألدوية اللي انذكرو بجدول‬
Nimodipine Brainal Tab:30mg Prevent contraction of
arteries in the brain, so
For Aristo prevent oxygen
deprivation in the brain
Modina Tab:30mg Tetrafarm

Lercanidipine Vasodip Tab: 10mg Dexcel

Diltiazem Adizem Cap:120, 180, Rafa

240mg
Diltiazem Tab:60mg Teva

Verapamil Verapress SR Tab:240mg Dexcel

These drugs block calcium channels so prevent the contraction of smooth muscles and
reduce its tone→ CCB dilate mainly arterioles but not the vein.

DHP→high doses should be avoided because of increased risk of MI due to excessive

vasodilation and reflex cardiac stimulation.
NDHP→have negative ionotropic and dromotropic effects
Compelling indication to start with CCB in treating HTN are: coronary artery disease and
DM.

CCB can be used as initial therapy or add on therapy

They are useful in the treatment of HTN with coexisting asthma, DM or peripheral
vascular disease.
Indications:
HTN (DHP, NDHP)
Angina (NDHP)
Atrial fibrillation (NDHP only)
Subarachnoid hemorrhage (Nimodipine only) (the MOA is unknown)

SE of CCB:
First degree AV block and constipation →verapamil
Hypotension, headache, fatigue, dizziness, reflex tachycardia→more with DHP
Peripheral edema, gingival hyperplasia

Contraindication: HF, AV block

Diuretics
MOA in treating HTN: decrease blood volume →decrease peripheral resistance.
If only HTN→ Thiazide diuretics is the choice
Thiazide diuretic: (block Na/Cl transporter in renal distal tubule)
Chlorothiazide, hydrochlorothiazide,
Thiazide-like diuretic:
Indapamide, Metolazone

Hydrochlorothiazide Disothiazide Tab: 25mg Dexcel

Kaluril: Tab:50 +5mg Teva
With
Amiloride
Moduril: Tab:50+5mg Jerusalem
With
Amiloride
 Metolazone Zaroxolyn Tab: 5mg Teofarma
Indapamide Pamid Tab: 2.5mg CTS

Thiazide is not effective in patient with diminished renal functions

If HTN with edema or chronic kidney disease→ loop diuretic is the choice
Loop diuretics: (block Na/K/Cl transporter in renal loop of Henle).
Furosemide, Bumetanide, Torsemide, Ethacrinic acid
Furosemide Fusid Tab: 40mg Teva
Amp:20mg/2ml
Furosemide Amp:20mg/2ml
Urix Tab: 40mg Birzeit
Diasix Tab: 40mg BeitJala
Furovenir Amp: 250mg /25ml BioAvenir

Note: k+-sparing diuretic (ex: Amiloride) is better used with thiazide or loop to prevent
hypokalemia.
Aldosterone-antagonists (ex: spironolactone) are k+-sparing diuretics, which are additionally
beneficial in reducing cardiac remodeling associated with heart failure.
SE of k+-sparing diuretics:
Hyperkalemia particularly in patient with impaired renal function (the treatment is insulin+
glucose injection)
‫ليه االحسن يستخدم المريض مدر بول مع ادوية الضغط األخرى؟‬
‫النه االنواع التانية من ادوية الضغط تسبب احتباس االمالح والماء في الجسم‬
Both thiazide and loop diuretics cause decrease the level of K and Na in the body
Thiazide cause increase the level of Ca, but loop cause decrease Ca (so furosemide injection is
used in treating hypercalcemia)
Thiazide cause hyperglycemia, but loop has less effect on glucose level.
Magnesium and potassium level in the body effect on the heart and low level of them may
cause arrythmia, especially in patient who take digoxin, or have ischemic heart disease.
Loop diuretics, thiazide diuretics, carbonic anhydrase inhibitors→ contain sulfa-group
→contraindication in patients with sulfa allergy
Note: ethacrynic acid is the only loop diuretic that does not contain sulfa group
Diuretics that do not contain sulfa→ex: spironolactone, eplerenone

Other diuretics:

Acetazolamide Uramox Tab: 250mg Taro

Uses:
to treat glaucoma
symptoms of altitude sickness (mountain sickness): 250mg every 12 hr

B-blockers
MOA:
-Have negative ionotropic and chronotropic effect→ reduce cardiac output
-inhibit renin release
Can be used as first choice in case of coronary artery disease or after MI
Types:
1-Nonselective
Propranolol, Nadolol, Timolol

Propranolol Prolol Tab:10, 40mg Dexcel

Blocadril Tab:10, 40mg BirZeit
Deralin Tab: 10, 40mg Abic
Inderal (Brand) Tab:10, 40mg Astrazeneca

2-cardioselective
Atenolol, Bisoprolol, Metoprolol, Nebivolol

Atenolol Normin Tab:100mg Birzeit

Corotenol Tab: 50, 100mg Jerusalem
Atenomin Tab:50, 100mg Sama
Normalol Tab: 25, 50, 100mg Dexcel
Normiten Tab:25, 50, 100mg Teva
 Bisoprolol Hypocor Tab: 2.5, 5,10mg Jerusalem
Bisopress Tab:2.5,5,10 mg Sama

Co-Bisopress: Tab:
With HCT 2.5/6.25
5/6.25
5/12.5
10/25
Bisotens Tab: 5, 10mg Pharmacare
Bisoprolol-Inovamed Tab: 2.5, 5mg Inovamed
Concor Tab:2.5, 5, 10mg Merck
CARDILOC Tab:1.25, 2.5, 5, 10mg Unipharm

Metoprolol NEOBLOC Tab: 100mg Unipharm

3- alpha/beta-blockers:
Carvedilol, Labetalol

Carvedilol Aricard Tab: 6.25, 12.5 mg Beit Jala

Carvedilol Tab: 6.25, 12.5mg Teva
Carvedexxon Tab:6.25, 12.5mg Dexcel

Labetalol Trandate Tab:5, 100, 200mg Aspen

Labetalol Amp: 5mg/ml West-Ward

Block alpha→ peripheral vasodilation

Indications:
HTN
HF → carvedilol decrease lipid peroxidation and vascular wall thickening.

Labetalol may be used as

-Alternative to methyldopa for pregnant women
-IV for HTN emergencies.
4- Antagonists with partial agonist activity:
Pindolol, Acebutolol, Carteolol
Indications:
-HTN patients with moderate bradycardia
-Diabetic HTN patients: because carbohydrate metabolism is less affected

Side effects for B-blockers:

1- Propranolol: has CNS effects: vivid dreams and nightmares, dizziness, hallucinations
2- Non-selective: Bronchoconstriction: contraindicated in asthma and COPD due to danger
of death by asphyxiation.
3- Arrhythmia: associated with abrupt discontinuation (B-blockers must be tapered off
gradually over 1 to 2 weeks).
4- Bradycardia
5- Av conduction abnormality
6- Sexual dysfunction: unclear reasons
7- Metabolic disturbances: decrease glycogenolysis and glucagon secretion→fasting
hypoglycemia may occur
They also prevent the appearance of hypoglycemia symptoms such as: tremor,
tachycardia, nervousness
8- Increase LDL and TAG, decrease HDL

Selective Alpha 1-Blockers

Prazosin, Terazosin, Doxazosin

Doxazosin Cadex Tab: 1, 2, 4mg Dexcel

MOA:
Inhibit catecholamine uptake by smooth muscle→vasodilation
They are useful in case of HTN + benign prostatic hyperplasia
SE:
1- Sodium and water retention → they are given with thiazide diuretics
2- First-dose phenomena: orthostatic hypotension, dizziness, palpitation, syncope
→so, they are given at bedtime

Other alpha 1 blocker: Tamsulosin, Alfuzosin → not effective for treatment of HTN
They are used in the treatment of benign prostatic hyperplasia and chronic prostatitis and to
help with the passage of kidney stones.

Tamsulosin Tamsuloin INOVA Tab: 0.4mg Inovamed

Tamsulin Tab: 0.4mg Rafa
Omnic Cap 0.4mg CTS

Omnic Ocas: Tab:0.4mg

Prolonged-release film coated
tablet
It has improved safety/efficacy ratio
compared to conventional omnic
Duodart: Tab: 0.4/0.5mg GSK
With dutasteride
Promnix Cap: 0.4mg Taro

Alfuzosin Xatral XL Tab:10mg Sanofi

Centrally acting adrenergic drugs (alpha 2 agonist):

Clonidine, Methyldopa

Clonidine Clonnirit Tab:0.025mg Rafa

Normopresan Tab:0.15mg Rafa
Clonidine is useful in case of HTN with renal disease.
It is also used for migraine and flushing after menopause
Methyldopa can be used in pregnant women

Methyldopa Aldopa Tab:250mg Jepharm

Vasodilators (the last choice)

Hydralazine, Minoxidil, Nitroprusside, Diazoxide

Hydralazine Hydralazine Tab: 50mg

It works by enhancing nitric oxide release.
→they are not primary anti-HTN drugs
→Hydralazine can be used for gestational HTN
→they are additive drugs not alternatives
 MOA:
Direct dilation of vessels →reflex tachycardia and increasing of contractility
Increase renin release →sodium and water retention
So, concomitant administration of B-blockers and diuretics reduce these side effects and
contribute to HTN treatment. (hydralazine with thiazide) (Minoxidil with loop diuretic
because it is more potent).

SE:
Hydralazine → reversible lupus-like syndrome, tachycardia, arrhythmia, sweating, headache
Minoxidil → Hypertrichosis (growth of body hair) → Off-label use

Minoxidil Hairmax Spray (topical BeitJala

solution): 2%, 5%
Minoxi Spray: 2%, 5% Trima
Hairgain
Regrow Topical solution: 2%, Jerusalem
5%

Nitroprusside→ cyanide toxicity, Methemoglobinemia

Hypertensive emergency:
Can cause organ damage: MI, stroke.
Treatment
CCB: amlodipine
Vasodilators: nitroglycerine, nitroprusside, hydralazine
Adrenergic blockers: phentolamine, esmolol, labetalol
Dopamine agonist: Fenoldopam.

Hypertension in pregnancy:
BP decrease during the first 20 weeks of pregnancy and HR increased
So, if a pregnant has high blood pressure during this period→she may has chronic blood
pressure before pregnancy.
BP rise during delivery then it drops few weeks after that.
Blood volume increase from week 5 until the end of pregnancy.

Types of HTN in pregnancy

1-chronic HTN:
It is diagnosed before or during pregnancy
2-pregnancy-induced hypertension or gestational HTN
Occurs after week 20, return to normal after 12 weeks of delivery
Without proteinuria
50% of them developed to pre-eclampsia
3-pre-aclamsia:
HTN with proteinuria
Should be treated to prevent development to eclampsia
4-eclampsia
HTN with proteinuria + seizures +coma +death of mother and baby
So, delivery should happen quickly
◼ Threshold for HTN in pregnancy: 140/90
◼ Treatment should be initiated only at levels higher than:160/110

→Treatment of HTN:
1st line: methyldopa
2nd line: metoprolol, hydralazine, nifedipine, clonidine
→Treatment of pre-eclampsia:
1st line: hydralazine, nifedipine, labetalol (it is used mainly if there is also high HR or edema)
----
Among B-blocker→labetalol and metoprolol can be used for treatment of HTN
and propranolol for prophylaxis from migraine
Others should be avoided, atenolol is contraindicated.
Hydralazine →for hypertensive emergencies
Among CCB→Nifedipine (for HTN) and verapamil (for arrythmia) can be used.
ACE-I→ contraindicated. Because of:
→at 1st trimester: cardiovascular damage
→at 2nd and 3rd trimester: renal and lung damage and growth retardation.
ARBs→contraindicated (renal damage)
-----
Eclampsia: is the onset of convulsion in pre-eclampsia
If she is after week 30 of pregnancy→the best treatment is delivery
If not→ restrict activity, bed rest, close monitoring
Magnesium sulfate is the drug of choice for treatment of seizures in eclampsia. (improved
uterine circulation and has tocolytic effect)

Prazosin (alpha-blocker)→ ‫مش ممنوع بس من الخيارات األخيرة‬

Thiazide and loop →better to be avoided
Thiazide In mother cause hypovolemia, hypotension. Hypokalemia, inhibit labor
In fetus cause bradycardia, hypotonia, and hyponatremia
Furosemide -->at 1st trimester cause hypospadias (congenital defect in the opening of the
urethra).

Hypertension in lactation:
1st choice: Methyldopa
2nd choice: Metoprolol, Propranolol, Labetalol
Others: (when antihypertensives of choice are not effective)
CCB: Diltiazem, Nifedipine, Verapamil
ACE-I: captopril, enalapril, benazepril
ARBs are contraindicated
 Heart Failure
HF: progressive clinical syndrome, caused by inability of the heart to pump
sufficient blood to meet the body’s metabolic needs.
Main causes: MI, HTN
2 types:
1-Systolic dysfunction: inability of heart to contract
2-Diastolic dysfunction: inability of heart to relax or to fill
‫المريض ممكن يكون مصاب بنوع منهم او التنين مع بعض‬

Usually, the ejection fraction in HF is less than 40%

→there are some precipitating factors that convert compensated HF patient to
decompensated:
1-Myocardial ischemia and MI
2-artiral fibrillation
3-Pulmonary infection
4-nonadherence to diet→ fluid: maximum 2L/day from all sources, low dietary intake of sodium
5-inappropriate medication use: (should be discontinued)
-negative ionotropic drugs: B-blocker / NDHP CCB
-direct cardiotoxic drug: ducirubicin / cocaine / amphetamine
-drugs increase sodium and water retention: corticosteroids /sex hormones /NSAID

→Classes of HF:
Class1: no limitation of physical activity
Class 2: slight limitation
Class3: marked limitation
Class 4: patients are unable to carry on physical activity without discomfort.

→patient who has HF should be vaccinated against influenza(yearly) and pneumococcus (every
5 years)

→Treatment of HF according to stages:

Stage A: at risk/ no structural heart disease /no symptoms
-stop smoking
-control HTN, DM, dyslipidemia
-ACE-I or ARBs are recommended if the patient has multiple risk factor
Stage B: no structural heart disease /no symptoms
-ACE-I or ARBs and B-blocker
If he has previous MI →statin is also added

Stage C: with structural heart disease and has previous or current symptoms: (all following
drugs should be given)
1-ACE-I or ARBs
2-B-blockers
3-loops-diuretic
4-aldosteron antagonist
5-hydralazine, isosorbide dinitrate
And in select patient: digoxin, sacubitril/valsartan

Stage D: advanced HF
Require drugs with specialized interventions such as mechanical circulatory support and cardiac
transplantation.
Notes:
Diuretics →should be start with low dose and increased gradually to avoid hypotension and
fatigue.
In the presence of renal impairment →loop diuretic is more effective than thiazide.
When thiazide is preferred over loop?
In patient with mild fluid retention and elevated BP (because of their persistent
antihypertensive effect)

Dose of ACE-I is gradually increased to the target dose to minimize the risk of hypotension and
renal insufficiency.

→When ARBs are recommended to use?

When the patient is taking ACE-I and B-blocker, and he is still having symptoms but he cannot
take aldosterone antagonist.

→Combined use of ACE-I, ARBs and aldosterone antagonist is not recommended because of
increased risk of renal dysfunction and hyperkalemia.
→Recommended ARBs in HF are: candesartan, losartan, valsartan.
→B-blockers are given:
-for all patient with stable HF
- start with low doses then slow upward to target dose
Target dose of bisoprolol is 10mg
-doses should be doubled every 2 weeks
Recommended B-blockers are: Carvedilol, metoprolol, bisoprolol
Aldosterone antagonist: (Block aldosterone receptors)
Spironolactone, eplerenone

Spironolactone spirone tab: 25, 100 mg Birzeit

aldactone tab: 25mg pfizer

spironolactone Tab: 25, 100mg Teva

Eplerenone inspra (Brand name) Tab: 25,100mg Pfizer

The rule for these drugs in HF is by inhibiting extracellular matrix and collagen deposition. (Not
due to their diuretic effect).

Should be avoided in patient with renal impairment and hyperkalemia.

SE: interact with androgen and progesterone receptor and cause : gynecomastia, impotence,
menstrual irregularities.

Note: eplerenone does not cause these SE because it is selective.

These are some drugs that are added to some patient if he still has symptoms:

1- Nitrates and hydralazine

Isosorbide mononitrate Monocord Tab: 20,30,40mg Dexcel

vasocor Tab: 20, 40 mg Birzeit

Isoned Tab: 20,40 mg Jerusalem

Monolong Tab:20, 60 mg CTS

Mononit Tab: 40mg Sanofi

Isosorbide dinitrate Isoket Amp: 1mg/1ml GSK

Isorem 5 Sublingual tab:5mg

Nitrates → venodilators
Hydralazine→ arterial vasodilators

They are alternative when the patient cannot tolerate ACE-I and ARBs
SE: headache, dizziness.

2-ARB/Neprilysin inhibitor (valsartan/sacubitril):

valsartan/sacubitril Entresto (brand name) Tab: 50,100,200 Novartis

Neprilysin → is an enzyme that breaks down the endogenous natriuretic peptide which is a
vasodilator.

Sacubitril→ is a Neprilysin inhibitor and it is a prodrug that is converted to the active form inside
the body.

4- Ivabradine:
As an alternative to the B-blocker or add on with it to decrease heart rate.

5- Digoxin:

Digoxin Lanoxin Elixir: 0.05mg/ml Perrigo

Amp: 0.5mg/2ml

Digoxin-Kern Pharma Tab: 0.25mg Trima

MOA: regulation of cytosolic calcium concentration. It increases contractility of the heart.
SE: nausea/V/D and cardiac arrythmia.
In the absence of digoxin toxicity or serious side effects, digoxin should be continued in most
patients who need it. (patients with severe HF after initiation of other standard therapy).
It does not improve survival but it improves symptoms.
It has a narrow therapeutic index. (0.5-0.9 ng/ml).

Note: digoxin is a substance of P-glycoprotein, thus P-gp inhibitors like clarithromycin,

Amiodarone and verapamil can elevate digoxin toxicity.

Antidote: Digoxin immune fab.

It is also used to treat atrial fibrillation

-----
In hospital setting, some drugs can be given as IV infusion for short-term treatment:
1-B-adrenergic agonist: dopamine and dobutamine
2-Phosphodiasterase inhibitors: Milrinone (MOA: elevate the level of cAMP.
 Antiarrhythmic Drugs

Arrhythmias can be:

1-Bradyarrythmias (slow heart rhythms)
2-Tachyarrythmias (fast heart rhythms)

Treatment of tachyarrhythmia
Class 1: Na-channel blockers:

Quindine Quindine Tab:200mg Rekah

Flecainide Tambocor (Brand) Tab: 50,100mg Megapharm

Propafenone Profex Tab: 150,300mg Taro

(B-antagonist Rythmex Tab: 300mg Teva
activity)

Class 2: B-adrenoceptor antagonists:

Propranolol, metoprolol, nadolol, esmolol
They are frequently used to prevent recurrent MI which is a risk factor for arrythmia.
They are used to treat tachyarrhythmia.

Class 3: K+_channel blockers:

Amiodarone, sotalol, ibutilide, dofetilide

Amiodarone Amiocard Tab: 150, 200mg CTS

Procor Tab: 200mg Unipharm
Daronex Tab: 200mg Birzeit
They have long half-life: 14-100 days
It requires several hours for effect to start and its effects on abnormal rhythms may not seen
for several days
Its effect may last for weeks or months after the drug is continued.
SE:
Pulmonary fibrosis ‫تليف بالرئة‬
Skin pigmentation
Corneal deposits ‫تصبغات‬
Interfere with the thyroid function ( reduce the production of T4 because they has similar
structures)

Class 4: CCB
Verapamil, diltiazem
They should not be used to treat arrythmia in patient with HF
Also, they should not be used in patient with AV block

Class 5:
1-Adenosine: bind with purinergic receptors

Adenocor Adenosine Vials: 6 mg Sanofi

2-Digoxin: cause slow conduction on AV node →control atrial fibrillation →decrease HR.

Treatment of bradyarrhythmia:
1-Atropine: block the effect of acetylcholine

Atropine sulfate Atropin JPM Amp: 1mg Jerusalem

Atropine sulfate Amp: 1mg Teva

2-Isoproternol: stimulate B-adrenoceptors

It is used to maintain adequate heart rate and cardiac output in patients with AV block
 Anticoagulants and Antiplatelet Agents
Thrombotic disorders:
MI, deep venous thrombosis (DVT), pulmonary embolism (PE), acute ischemic
stroke.
Diagnosis of MI: ECG / rising or/and falling of cardiac biomarker: Troponin
Unstable angina may develop to myocardial infarction when a fully occlusive
coronary thrombus happened.
→Arterial thrombosis: platelet-rich clot → antiplatelet are used
→Venous thrombosis: fibrin-rich clot → anticoagulants are used

Platelet Activation Inhibitors

1-COX-1 inhibitor: Aspirin

2-Blockade of ADP receptors:

Ticlopidine, Clopidogrel, Prasugrel, Ticagrelor

3-Blockade of GP IIb/IIIa:
Abciximab, Eptifibatide, Tirofiban.

4-PDE III inhibitors:

Dipyridamole, Cilostazol
Aspirin
Aspirin Aspirin Tab:100mg Birzeit
Aspirin cardio Tab:100mg Bayer
Cartia Tab:100mg Aspen
Godamed Tab:100mg Godamed
Tevapirin Tab:100mg Teva
Baby Aspirin Tab:100mg Beit Jala
Micropirin Tab:100mg Dexcel

MOA: irreversible inhibition of COX-1 enzyme, thus prevent TXA2 synthesis, thereby preventing
platelets aggregation.
Inhibition of platelets aggregation lasts for the life of the platelets(7-10days)
The recommended dose: 50-325 mg
Complete inactivation of platelet occurs with daily 75mg

SE:
Increase bleeding time, increase risk of hemorrhagic stroke and GI bleeding (especially at high
doses)
Salicylism: a toxic condition produced by the excessive intake of salicylic acid →symptoms
-tinnitus (ringing in the ear ‫)طنين باالذن‬
-nausea, vomiting.
- acidosis at high doses
Treatment: sodium bicarbonate.

Note: other NSAID like ibuprofen interfere with aspirin on the enzyme
Blockade of ADP receptors
Ticlopidine / Clopidogrel / Prasugrel / Ticagrelor
Clopidogrel Plavix (Brand) Tab:75mg Sanofi
Clovix Tab:75mg Birzeit
Clopid Tab:75mg Jerusalem
Pidogrel Tab:75mg Pharmacare
Clopidex Tab:75mg Beit Jala
Platlock Tab:75mg Sama

Ticagrelor Brilinta (Brand) Tab:90mg Astrazenca

Prasugrel Effient Tab: 5,10mg Lilly

Ticlopidine →reserved for patient intolerant to other therapies due to life-threatening

hematologic reactions.
Clopidogrel→prodrug and activated by CYP2C19, it is not suitable for poor metabolizer
patients.
SE:
Increasing bleeding time →Prasugrel, Ticagrelor
Sever hematologic reactions→Ticlopidine
Thrombotic thrombocytopenia purpuria (TTP)→Clopidogrel, Prasugrel, Ticagrelor.

Note: concomitant administration of Aspirin reduces the efficacy of Ticagrelor (Brilinta)

Blockade of GP IIb/IIIa
Abciximab / Eptifibatide / Tirofiban
Eptifibatide Integrilin Injection:0.75mg/ml MSD
2mg/ml
MOA: block GP IIb/IIIa receptors on the platelet, thus prevent the binding of fibrinogen
and von Willebrand factor.
Abciximab→ is a monoclonal antibody which is approved for unstable angina not
responding to conventional therapy (Aspirin and Heparin) when PCI ( ‫ )عملية القسطرة‬is
planned withing 24 hr.
Eptifibatide →is a cyclic peptide.
Tirofiban → is chemical compound.

SE:
Bleeding especially if used with anticoagulants like heparin.

Phosphodiesterase III inhibitors

Dipyridamole / Cilostazol
Dipyridamole Cardoxin Tab: 75mg Rafa
Amp
Dipyridamole Aggrenox Cap: 200/25 Boehringer
+Aspirin Extended release Ingelheim

MOA: elevate cAMP, thus decrease TXA2 synthesis caused vasodilation and inhibit
platelets aggregation.
It inhibits clot formation when given chronically and causes blood vessel dilation when
given at high doses over a short time.
Dipyridamole usually given with Aspirin
Cilostazol increase the level of HDL and decrease triglyceride and it is contraindicated in
HF because it increases the mortality in those patients.
Anticoagulants
Heparin and Low Molecular Weight Heparin → inhibit the action of coagulant
factors
Warfarin →inhibit the synthesis of coagulant factors
--------
Heparin and LMWH
LMWH are:
Enoxaparin / Deltaparin / Tinzaparin
Enoxaparin Clexane Prefil syringe: Sanofi
20, 40, 60, 80,
100mg
SC or IV
Prolongin

Dalteparin Fragmin syrige: 2500, Pfizer

5000, 7500, 10000
IU/0.2mlSC SC or
IV

Protamine sulfate is the antidote for heparin and LMWH. (it required in case of
bleeding)
Administration:
heparin →SC or IV (bolus then slow infusion), but they are not given IM because
of intramuscular hematoma.
LMWH → SC
MOA:
Heparin → bind with antithrombin 3 → irreversibly inactivate Thrombin 2 and factor 10
→ prevent the conversion of fibrinogen to fibrin
LMWH-AT 3 complex inactivate factor 10 only.

Heparin required monitoring by (aPTT) (activated partial thromboplastin time)→ it

should be 1.5-2.5 folds of the normal control.
LMWHs do not required monitoring, thus given foe inpatient and outpatient, but it can
be monitored by the level of factor 10.

SE:
Hypersensitivity reaction / fever / urticaria
Heparin-induced thrombocytopenia (HIT) ‫نقصان في عدد الصفائح الدموية‬
Osteoporosis with prolonged use

Contraindication:
Bleeding disorders (hemophilia)
Recent surgery in the brain, eye, spinal cord
History of thrombocytopenia

Fondaparinux
MOA: like LMWH
SE: bleeding (no antidote)
Contraindication: in sever renal impairment because it is eliminated renally unchanged.
Direct thrombin 2 inhibitors
Argatroban / Bivaluridin / Desirudin / Dabigatran etexilate.
Dabigatran Pradaxa Cap: 75, 110, 150 mg Boehringer
etexilate (Brand) Ingelheim

MSS ‫المستورد‬

MOA: directly inhibit thrombin→ inhibit fibrin generation

Administration: parenterally
Only Dabigatran etexilate can be given orally, and it has long half-life (8-14 hr).

They are the alternative drugs to heparin in patients with history of HIT.
aPTT → for monitoring except for Dabigatran etexilate
SE:
Bleeding (no antidote)
Dabigatran etexilate→GI SE: dyspepsia ‫ سوء هضم‬/ esophagitis / GI bleeding

Inhibitors of factor Xa (10)

Rivaroxaban / Apixaban
Rivaroxaban Xarelto (Brand) Tab: 2.5, 10, 15, 20mg Bayer
Rivoxar Tab: 10,15,20mg Jerusalem

Apixaban Eliquis Tab: 2.5, 5 mg Pfizer

Quest Tab: 2.5, 5mg Pharmacare
MOA: directly inhibit factor Xa thereby inhibit thrombin generation.
Administration: orally
SE: bleeding (no antidote)
No monitoring is required

Coumarin anticoagulants (vit K antagonist) (Warfarin)

 Warfarin Coumadin Tab: 0.5, 1, 2, Taro
(Brand) 2.5,5 mg

Acenocumarol Sintrom Tab: 4mg Novartis

MOA: it prevents the conversion of oxidized Vit K to its reduced form which is required
to convert factors (2,7,9,10) to their active form.
Oral bioavailability: 100%
Extensively binds plasma albumin → low distribution to CSF, urine, breast milk.
Has narrow therapeutic window→ INR for monitoring
Normal range (2-3) and in some patient with prosthetic valves (2.5-3.5)

Note: heparin has immediate effect but the anticoagulation effect of warfarin is not
observed immediately, so patient with MI is given heparin for 3 days then warfarin
(latency period before effect: 36-48 hr)
Antidote: Vit K
Drug interactions:
→CYP-450 inhibitors: Amiodarone, SSRI →increase anticoagulant effect
Miconazole is strong inhibitor of CYP2C9 one of the main enzymes involved in warfarin
metabolism →increase the likelihood of bleeding
Antibiotic that are safe to be used with warfarin: penicillin, 1st and 2nd gene.
Cephalosporins, clindamycin.
→CYP-450 inducers: Phenytoin, Carbamazepine, Barbiturate → decrease anticoagulant
activity
→Aspirin increase its coagulant function by replacing warfarin from plasma protein and
increase the level of free warfarin
→Antibiotics increase warfarin effect by eradicate intestinal normal flora which
decrease Vit K production.
SE:
Bleeding
Teratogenic

Management of warfarin toxicity:

→Minor bleeding:
Drug withdrawal or administrated Vit K
→Severe bleeding:
High dose of parenteral Vit K
Infusion of whole blood, frozen plasma or plasma concentrated of blood factors.

Thrombolytic Drugs
Alteplase / Retaplase / Tenectaplase / Steprokinase / Urokinase
MOA: facilitate the conversion of plasminogen to plasmin which hydrolyze fibrin
Administration: IV
SE: bleeding
Contraindication: pregnancy, intracranial bleeding / healing wounds / head trauma/
Metastatic cancer
------
→Pentoxifylline
Xanthine derivative, it is a hemorheologic agent with primary actions that include
increasing erythrocyte flexibility, reducing blood viscosity and increasing
microcirculatory flow and tissue perfusion.

Pentoxifylline Oxopurin Tab: 400mg Dexcel

(the brand name is
Trental)
Drugs used to treat bleeding
Vit K deficiency is one of the causes of bleeding
→Reasons of deficiency:
Elderly with impaired absorption of fat, Newborns, Dietary deficiency, Antimicrobial
therapy.
→Treatment of vit K deficiency:
Oral or parenteral administration of Phytonadione (Vit K)
It is recommended that all newborns should receive an injection of Phytonadione at
birth.
Desmopressin is a vasopressin receptor agonist and it is used to treat diabetes insipidus,
but it also can increase concentration of von Willebrand factor and factor 8→ so, it is
used to prepare patient with Willebrand deficiency or hemophilia A for elective surgery.

Antiplasmin agents:
Aminocaproic acid / Tranexamic acid / Aprotonin
Tranexamic acid Hexakapron Tab: 20mg Teva
Amp: 500mg/ml

MOA: inhibit plasminogen activation→inhibit fibrinolysis

It is used to treat bleeding.

Anticoagulants and pregnancy:

The risk of VTE, DVT and PE increase during pregnancy because of:
-hypercoagulability: high level of estrogen stimulates clotting factor synthesis
-vascular damage (surgery or trauma)
-stasis
-placenta produce high level of plasminogen activator inhibitors, so level of plasmin
decreases and its ability to breakdown fibrin decrease

Heparins and LMWH (ex: Enoxaparin) do not cross the placenta because of high
molecular weight and its negative charge →safe in pregnancy
LMWH is more preferred than heparin because:
-long half life
-lower incidence of allergy
-lower incidence of heparin-induced of thrombocytopenia
-need less monitoring
→ LMWH is the drug of choice for prophylaxis and treatment of VTE in pregnancy.
Note: a combination of LMWH + low-dose aspirin →is recommended if there is a high
risk of thrombosis

Protamine-HCL and protamine sulfate is the antidote of heparin and LMWH and it can
be used during pregnancy.
Coumarin derivatives ex: warfarin is contraindicated in pregnancy
MOA: oral anticoagulants that prevent vit K from acting as a cofactor in the hepatic
synthesis of the vitamin K-dependent coagulation factors (2,7,9,10)
Cross the placenta→reach the fetus→ coumarin syndrome (DiSala syndrome)
Vit K
Oral 1-2mg of vit k should be given to newborns directly after birth
If the pregnant took vit-k-antagonizing drugs (ex: carbamazepine, phenobarbital,
phenytoin or rifampicin) → parenteral administration of vit K should be given to the
baby directly, also oral 1-2mg of vit K two to three times a week during the first 2 weeks
after birth.

Fibrinolytic agents (ex: streptokinase, urokinase, alteplase) are used only in life-
threatening situations because they are strong and there a risk of bleeding.
 Antianginal Drugs
Coronary artery disease = ischemic heart disease
Symptoms of angina pectoris:
>Typical: sudden, severe chest pain that may radiate to the neck, jaw, back and
arms.
>Atypical: indigestion, nausea, vomiting, diaphoresis.

Types of angina:
→stable: effort-induced (such as physical activity, stress or excitement)
Pathogenesis: atherosclerosis causes a fixed obstruction of coronary artery
Duration: seconds to minutes
→unstable: can be happened even without effort
Symptoms not relieved by rest or nitroglycerin.
Duration: longer than 20 minutes, can quickly progress to MI and death.
→prinzmetal: vasospasm in coronary artery.
Occurs at rest due to coronary artery spasm.
Respond promptly to coronary vasodilators (nitroglycerin and CCB).

Treatment:
Non-pharmacologic:
Smoking cessation, physical activity, weight management
Management of modifiable risk factors: HTN, DM, dyslipidemia.
Pharmacologic:
Classes of anginal drugs:
-B-blockers
-CCB
-Organic nitrate
-Sodium channel blockers

These agents help to balance the cardiac oxygen supply and demand.

B-blockers: are recommended as initial therapy for all patients except vascopastic
angina (they require coronary dilator such as nitrate and CCB)
They decrease O2 demand
B-blockers with intrinsic sympathomimetic activity such as Pindolol should be avoided
for all types of angina.
B-blockers should be avoided in severe bradycardia

Non-selective B-blockers should be avoided for patients with asthma. (atenolol,

metoprolol can be used).
Recommended B-blockers: (Bisoprolol / Metoprolol / Carvedilol)
--

CCB: are arteriolar vasodilators (coronary and peripheral arteries) (decrease O2

demand and increase O2 supply).
They are used with or alternative to B-blocker
Propranolol + Nifedipine → is more effective combination
Note: short acting DHP should be avoided due to reflex tachycardia and increase O2
demand, so they are used as extended-release oral formulation ex: Nifedipine.
NDHP are contraindicated if there is HF.

--
Organic nitrate: Nitroglycerin, Isosorbide mononitrate
MOA: release nitric oxide
Isosorbide mononitrate Monocord Tab: 20,30,40mg Dexcel

vasocor Tab: 20, 40 mg Birzeit

Isoned Tab: 20,40 mg Jerusalem

Monolong Tab:20, 60 mg CTS

Mononit Tab: 40mg Sanofi

Isosorbide dinitrate Isoket Amp: 1mg/1ml GSK

Isorem Sublingual tab: 5mg Remedica

Glyceryl trinitrate Nitrolingual spray Spray: 0.4mg Give protection

(nitroglycerin) for 30 min
Nitroderm TTS Transdermal Novartis
patches
Reduce O2 demand and increase the supply.
Effective in all types of angina.
They are used with CCB or B-blocker (not recommended alone because patient is not
protected at night)
→Tolerance to organic nitrates: because of desensitized to vasodilation.
It can be overcome by (daily-nitrate-free-intervals)
Nitroglycerin patches are worn for 12 hours and removed for 12 hours.

This free interval should be started early in patient with variant angina (prinzmetal).
Onset of action:
➢ Nitroglycerin: 1min
➢ Isosorbide mononitrate: 30min
Sublingual nitroglycerin or buccal spray nitroglycerin is the drug of choice for prompt
relief effort-induced angina. (all patient should have it all the time for attacks)
Nitroglycerin administered sublingually or transdermally (patch or ointment) to avoid
extensive first pass metabolism and to give rapid onset of action.
Transdermal nitrate: are alternative to B-blockers
Isosorbide mononitrate can be used orally→ for chronic treatment of angina.
(isosorbide dinitrate gives 2 mononitrates in the body)
SE: postural hypotension / facial flushing / reflex tachycardia
It is contraindicated with phosphodiesterase type 5 inhibitors (ex: Sildenafil) because
both of them increase cAMP, so there is a risk of over vasodilation→ hypotensive shock
/ reflex tachycardia.

--
Antiplatelet
Aspirin / Clopidogrel
For stable IHD
Aspirin: 75-162 mg daily (because the patient is at high risk to clotting).
Clopidogrel: 75mg as alternative to aspirin in case of allergy or intolerance.
Or both of them in high-risk patient

There is a doubt about the interaction between clopidogrel and omeprazole

(omeprazole is cytochrome P450 inhibitor) → it is better to use other PPI such as
pantoprazole or other class such as famotidine.
-----
Sodium channel blocker (Ranolazine)
It is used if the traditional therapy insufficient or unsuccessful.
Decrease O2 demand
Has also antiarrhythmic activity.
SE: prolong QT interval
It is the last choice before PCI (percutaneous coronary intervention) ‫قسطرة‬
--

ACE-I or ARBs
Not as a treatment but they help in prevent increasing of atherosclerosis.
‫(كمان لحماية القلب لحتى ما يصير‬HF)

→If unstable angina developed to MI because of complete obstruction:

The most serious form of acute coronary disease is ST-elevation MI
Treatment
In hospital:
1-O2 if saturation is low
2-fibrinolytic (thrombolytic) if STEMI without PCI
3-aspirin→first time (non-enteric coated/ high dose 162-325mg) for all patient
4-clopidogrel → 75mg for all patients at least for 1 year, but it stopped before surgery.
5-GP receptor inhibitor →if STEMI with PCI and take heparin
6-Anticoagulant→ for all patients, just in hospital
7-B-blocker→IV if high BP (not with HF or cardiogenic shock)
8-Nitrate→sublingual then IV
9-statin
10-ACE-I

For NSTEMI:
The same as STEMI but with some differences:
1-Never fibrinolytic
2-GP I →if PCI with heparin or enoxaparin
3-Morpgine →for refractory angina

After hospitalization:
1-aspirin → 75-162 mg /day (‫)لحماية القلب‬
2-ACE-I (to protect the heart).
3-Statin →high intensity dose (or moderate if the patient above 75yr) (to decrease
atherosclerosis).
4-clopidogrel for at least 12 months
5-B-blocker→ oral for at least 3 years if ejection fraction is normal or indefinitely if EF is
40% or less → ‫يعطى لحتى يريح القلب‬
6-spironolactone in the first 7 days of MI for all patient with EF less than 40% or with
DM. →to prevent HF.

Aspirin and clopidogrel are given for patient after stenting ‫بعد القسطرة او إضافة الشبكيات‬

Obesity
Obesity: body mass index (30kg/m2 or greater)
Lipase inhibitor: Orlistat
Orlistat Orlislim Cap: 120mg Birzeit Taken orally
with each meal
that contain fat.

It has minimally
systemic
absorption and
is mainly
excreted in
feces.
 Slimcare Cap: 120mg Pharmacare
Orlix Cap: 120mg Beit Jala

MOA: it inhibits gastric and pancreatic lipase, thus decreasing the breakdown of dietary diet,
thus decreasing fat absorption by about 30%
GI adverse effects associated with the drug may also contribute to an overall decreased intake
of food.
GI symptoms: oily spotting, flatulence, fecal urgency and increased defecation.
Orlistat is contraindicated in pregnancy and in patients with chronic malabsorption syndrome
or cholestasis.
It interferes with fat-soluble vitamins and B-carotene. (patient should be advised to take these
supplements with the drug, but not within 2 hours of taking it).
It also may interfere with the absorption of other drugs.
-------------------
Phentermine: sympathomimetic amines: is as appetite suppressant
It is amphetamine derivative (CNS stimulant) so it is a controlled drug →no longer used for
obesity.

Phentermine Razin Cap:15mg CTS

-------------------------------------------------------------------------------------------------------------------------------
 Hyperlipidemia
Primary goal: Reduction of the LDL level.
Lipoproteins Normal Values mg/dl
Total cholesterol Less than 200
LDL Less than 100
HDL 40-50
Triglycerides Less than 150

Lipid-lowering drugs:
1.HMG-CoA reductase inhibitors:
Lovastatin / Simvastatin / Fluvastatin / Atorvastatin / Rosuvastatin /Pravastatin
/Cerivastatin
Simvastatin Simvastatin Teva Tab: 20,40,80mg Teva
Simvaxon Tab: 10,20,40,80mg Dexcel
Simvacor Tab: 10,20,40,80mg Unipharm
Solon Tab: 20, 40mg Sama

Fluvastatin Lescol XL Tab: 80mg Novartis

Atorvastatin Lipitor (brand) Tab: 10,20,40,80mg Pfizer

Lipidex Tab:10,20,40mg Birzeit
Liponil Tab:10,20,40mg Jerusalem
Lolip Tab:20,40,80mg Beit Jala
Trovan Tab:20,40,80mg Pharmacare
Lipovast Tab:10,20,40mg Sama
Atorvastatin + Atozet Tab:10/10mg MSD
Ezetimibe 10/20mg
10/40mg
10/80mg
Atorvastatin + Amlostat Tab: 10/10mg Beit Jala
Amlodipine
 Rosuvastatin Crestor (brand) Tab:10,20mg AstraZeneca
Roxardio Tab:10,20,40mg Sandoz
Rosuvastatin Tab: 40mg Teva
Rosulip Tab: 10,20mg Birzeit
Rovatin Tab:10,20mg Jerusalem
Liprose Tab:10,20,40mg Pharmacare
Novastat Tab:10,20mg Beit Jala
Savtin Tab:10,20mg Sama

Most efficacious and well tolerated.

They inhibit the rate limiting step in cholesterol synthesis, this will result in a compensatory
increase in hepatic uptake of plasma cholesterol which also contribute in lowering the level it in
the plasma.
Lovastatin and Simvastatin→Prodrugs, cross BBB and cause sleep disturbances.
Atorvastatin, Rosuvastatin, Pitavastatin → the most potent in decreasing LDL.
Atorvastatin and Rosuvastatin →long acting
Atorvastatin → antioxidant
Pravastatin and Fluvastatin → complete absorption after oral absorption
They are taken in the evening because most cholesterol is synthesized when dietary intake is at
its lowest.
All are metabolized in the liver and excreted through bile and feces, but there is also some
urinary elimination.
Half-life: 1.5-2 hour
Adverse effects:
Myopathy (muscle tenderness) and rhabdomyolysis. (the risk is the lowest with Fluvastatin)
Sleep disturbances
Hepatotoxicity
Headache
They may increase warfarin levels.
They are contraindicated in pregnancy, breastfeeding, children and teenagers.
There is a major interaction between diltiazem and simvastatin →diltiazem increase the level of
simvastatin →thus, increase risk of rhabdomyolysis (breakdown of skeletal muscle) and may
cause kidney damage and even death.
-------------

2.Bile acid-binding resins: (Bile acid sequestrants)

Cholestyramine / Colestipol / Colesevelam

Colestipol Colestid Granules for oral Pfizer

suspension

They are neither digested nor absorbed in the gut ‫ال يتم هضمها وال امتصاصها باالمعاء وانما ترتبط مع‬
‫العصارة وتمنع امتصاص الدهون بالجسم‬
Usually, they not used as monotherapy, but in combination with Statins.
Cholestyramine can relive pruritus caused by accumulation of bile acids in patients with biliary
obstruction.
It is also used to treat diarrhea because it makes constipation as an adverse effect.
Note: the only medications currently acceptable during pregnancy are bile acid sequestrants,
since they are not systemically absorbed and therefore not felt to pose fetal risk. (used as
monotherapy without statins because they are contraindicated in pregnancy). Use is limited
due to side effects of elevated triglyceride and constipation.
Adverse effects:
GI disturbances such as constipation and nausea, particularly with cholestyramine and
colestipol, also they are impairing the absorption of fat-soluble vitamins (E, D, A, K) at high
doses.
Other drugs should be taken 1-2 hours before or 4-6 hours after the bile acid-binding resins,
such as tetracycline, digoxin, phenobarbital, warfarin, pravastatin, Fluvastatin, aspirin, thiazide
diuretics.
-------------------

3.Cholesterol uptake inhibitor: Ezetimibe

Ezetimibe Hi Tri Tab: 10mg Beit Jala
Atorvastatin + Atozet Tab:10/10mg MSD
Ezetimibe 10/20mg
 10/40mg
10/80mg

MOA: bind with brush border of the small intestine and decrease cholesterol absorption.
Can be used with simvastatin to prevent compensatory mechanisms which is production of
cholesterol.
Patients with moderate to severe hepatic insufficiency should not be treated with Ezetimibe
because it metabolized in the liver (and small intestines)
Half-life: 22 hours
----------------------

5.Niacin (Nicotinic acid)

Nicotinic acid+ Babyzyme Oral drops
Pepsin +
Glycerophosphate
Multivitamin’s products contain Niacin
Rapid effect: within minutes → Decrease in plasma levels of free fatty acid.
Effect after few hours →reduces in VLDL and TG
After days → Reduce level of LDL, Cholesterol, increasing HDL
This is the most effective drug in increasing HDL .

Adverse effects:
-Potentiate gout (decrease uric acid secretion), hyperglycemia (diabetes), and peptic ulcer
-Hepatotoxicity (especially in combination with Statins)
-Vasodilation (flushing, itching).
-------------------------------

6.Fibric acid derivatives:

Fenofibrate / Gemfibrozil / Clofibrate /Bezafibrate/ Ciprofibrate

Bezafibrate Bezafibrate Tab: 400mg Medisson

Norlip Tab: 200mg Unipharm
 Ciprofibrate Lipanor Cap:100mg CTS

Gemfibrozil Lopid Tab:300,600,900mg Pfizer

MOA: interact with the receptor (PPAR alpha) which regulate gene expression of enzyme
involved in fatty acid oxidation.
They lower serum triacylglycerol (by increase expression of lipoprotein lipase which enhances
its clearance) and increase HDL levels (by increase expression of Apo A1 and Apo A2).
Fenofibrate: prodrug →fenofibric acid

Adverse effects:
-Gall stones with Clofibrate
-Nausea / skin rash
-Myopathy (muscle weakness, tenderness and rhabdomyolysis) particularly in combination with
Statins, so they are contraindicated with each other.

Note: Patient who take coumarin anticoagulant (warfarin) ang Fibrates should monitor INR
frequently, because fibrates compete with it for binding site on plasma proteins (increase the
risk of bleeding).
Note: concomitant therapy with a sulfonylurea in diabetic patient and fibrate is associated with
an often-delayed increased rate of severe hypoglycemia.
 “Someday when you are at peace,
You will be so glad you did not give up” ♥
 Topic 3: Gastrointestinal System
Antacids
→Weak bases that neutralize gastric acid and reduce pepsin activity

→ Reduce the pain of peptic ulcer and prompt healing

•Sodium Bicarbonate

•Calcium carbonate

Both of them Should not be used for long-term

Both of them absorbed by GI so cause systemic side effects.

Sodium carbonate Contraindicated in HTN because of the content of Na

Calcium carbonate Contraindicated in renal disease

Calcium carbonate May stimulate gastrin release and cause rebound acid production

Note: sodium bicarbonate is the least preferred antacid for pregnant women because it is
absorbed in the body leading to increase the level of sodium in her body, so increase the risk of
edema and hypertension.

Note: Calcium has SE: rebound acidosis. ‫بترجع الحموضة اصعب من قبل‬

‫الحليب البارد بخفف الحموضة بسبب برودته واحتواءه على الكالسيوم لكن بعدها بترجع الحموضة مرة تانية بسبب الكالسيوم برضو‬
‫ لهيك ال ينصح باستخدامه‬,‫والدهنيات اللي فيه النها بتزيد الحموضة‬

The risk of hypercalcemia in pregnant is when the drug taken with high doses and the pregnant
has kidney abnormalities → lead to milk-alkali syndrome (hypercalcemia and metabolic
alkalosis). → hypercalcemia in fetus →suppress parathyroid hormones → after delivery →
hypocalcemia in fetus → seizures.

•Magnesium hydroxide

•Aluminum hydroxide

Both of them:

Not absorbed by GI so does not cause systemic effects

can be used for long term

Most frequent SE of Magnesium Hydroxide: Diarrhea

 →high doses of magnesium may relax the uterus

Most frequent SE of Aluminum hydroxide: Constipation

→excessive daily amount of aluminum hydroxide throughout the entire pregnancy

may lead to functional disturbances in sensitive organs for the fetus such as kidney and
CNS

To make a balance between these 2 side effects (diarrhea and constipation), a

combination product of magnesium hydroxide and aluminum hydroxide is used.

This combination is the preferred for pregnant

Magnesium trisilicate: at high doses lead to

-nephrolithiasis (kidney stones)

-hypotonia

-respiratory distress

-cardiovascular impairment in the fetus.

-->Drug-drug interaction with antacids.

1.Antacids decrease the absorption of acidic drugs→ by increasing the gastric PH

Ex: antacid decrease the absorption of iron because it required acidic environment, also
calcium and iron effect on the absorption of each other.

2.antacids increase the excretion of acidic drugs→ by its effect on the kidney

3.Chelate other drugs and prevent the absorption→ because of metal content

Ex: Digoxin and tetracycline

Rennie Calcium carbonate 680mg Chewable Bayer

Magnesium carbonate 80mg
tablet For adults (more than 12
yr)
Usual dosage: 1 to 2
tablets initially
Up to 3-4 tablets per day.

M.H.C Birzeit

Gaviscon sodium alginate chewable Reckitt

Sodium bicarbonate tablet ‫ سنة‬١٢ ‫يستخدم فوق عمر‬
Calcium carbonate Suspension
 ‫ أقراص مضغ بعد الوجبة وقبل‬٤-٢
‫النوم‬

Maalox magnesium hydroxide Tab Sanofi

Aluminum hydroxide
‫لعالج حموضة المعدة‬
oral Safe in pregnancy
suspension
Tab: 1 tab between meals
Susp: 5-10 ml between
meals

Maalox plus magnesium hydroxide Tab Pregnancy : cat c

Susp
Aluminum hydroxide

Tab: with Dimethicone

Susp: with simethicone

Baby Nam sodium bicarbonate syrup Beit Jala

Anethol

Peppermint oil

Calcimore Calcium carbonate Chewable Taro

tablet:600mg

Oracol Birzeit

It can be used as antacid

(not to exceed 7g/day)
Or as ca supplement
Recommended(1g/day)

Note: about 40% of

calcium carbonate is
elemental calcium.

It is better to take antiacids with food or soon after eating because this is when you are most
likely to get indigestion or heartburn.
Mucosal protective agents:
Sucralfate: is a water-soluble aluminum salt of a sulfated polysaccharide, attaches to the
surface of an ulcer and thus protects the mucosa from further injury by acid and pepsin.

Sucralfate Ulsanic Tab Teva

Carafate susp Aptalis Pharma

It works fast to provide relief from heartburn, stomach cramps and pains, indigestion, nausea
and acid reflux. It also helps with peptic ulcers and to soothe an inflamed stomach lining.

H2 receptor antagonists (Anti histamine)

1- Ranitidine (All products of Ranitidine were Withdrawn from the market)

2- Famotidine.

3- cimetidine

4-Nizatidine

Scientific Product name Form and strength Company

Name

Ranitidine GI care Tab:150mg Pharmacare

Randin Tab:150mg Jerusalem

Amp:50mg/2ml

Ratidine Tab:150mg Birzeit

Amp:50mg/2ml

Zantac Tab:75,150mg GSK

(brand)
Syrup:150mg/5ml
Amp:50mg/2ml
 Samadine Tab:75,150,300mg Sama

Zaridex Tab:150,300mg Dexcel

Famotidine Famotidine-Teva Tab:20,40mg Teva

(Brand:Pepcid) Gastrix Tab:20,40mg Birzeit

Famodin Tab:20,40mg Jerusalem

Famo Tab:20,40mg CTS

Gastro Tab:10,20,40mg Unipharm

Famotidine + Acidex complete Chewable tab Pharmacare

MgOH + CaCO3

Cimetidine Tagamet (brand) Tab:200mg

——-

Famotidine:

Taken 15 min before meal

→Benign gastric ulcer

Tab: usual dose 20-40mg [ tab once to twice daily]

Maximum dose 80mg (40mg twice daily before meal)

These drugs are rapidly absorbed, and effects are observed within a few minutes to hours.

H2-Blockers: Used in the treatment of ulcers, gastroesophageal reflux disease and common
heartburn.

The selective H2 blockers are less potent in inhibiting acid production than the proton pump
inhibitors (which block the final step in acid secretion)

The effect of H2 blockers is largely on basal and nocturnal acid secretion, which is important in
peptic ulcer healing.

– Very effective for nocturnal acid secretion, which is mainly mediated by histamine.
– They are not as useful for meal-stimulated acid release, since this process also depends on
gastrin and acetylcholine.

when they are used as sole agents for ulcers, recurrence is observed in 90% of patients.

Can be used as prophylaxis is patient with at risk of recurrence ulcer.

Side effects are uncommon, usually minor and include diarrhea, constipation, fatigue,
drowsiness, headache and muscle aches.

Among the four agents, cimetidine is distinctive in its potent inhibition of the P450 system (CYP
1A2, 2C9 and 2D6), which can result in significant drug interactions.

For pregnancy

Cimetidine: has weak anti-androgenic effects in animal studies.

Ranitidine: the best studied agent (not available at pharmacies right now)

Famotidine: is the choice

Note: H2-blocker may be used during labor to prevent gastric acid aspiration.

Proton Pump Inhibitors (PPIs)

1- Omeprazole.

2- Esomeprazole.

3- Lansoprazole.

4- Pantoprazole.

Omeprazole Omepra Cap:20,40mg Rafa

(Brand:Prilosec) Omepradex Caplet:20,40mg Dexcel

Mepral Capsule:20,40mg Birzeit

Pepticum Capsule:20,40mg Pharmacare

Marial Capsule:10,20,40mg Biet Jala

Locid Capsule:20mg Jepharm

Losec Capsule:10,20mg Astrazeneca

Omeprazole:

a ½ hr before meal

→For gastric ulcer ‫لقرحة المعدة‬

40 mg PO qDay for 4 weeks

Comment: If patients are not fully healed after 4 weeks, treatment may continue for
another 4 weeks.

→Usual Adult Dose for Helicobacter pylori Infection ‫لجرثومة المعدة‬

Dual therapy: 40 mg orally once a day, taken concomitantly with clarithromycin

-Duration of therapy: 14 days

Triple therapy: 20 mg orally 2 times a day, taken concomitantly with amoxicillin and
clarithromycin

-Duration of therapy: 10 days

---

→GERD ‫لالرتجاع المريئي‬

20 mg PO qDay for 4 weeks

----

→For Esophagitis ‫التهاب المريء‬

20 mg PO qDay for 4-8 weeks

Maintenance: 20 mg PO qDay for up to 1 year

Esmoprazole Nexium (brand) Tab:20,40mg Astrazeneca

Vials:40mg
Esmoprazole Tab:20mg Teva
Ezomax Capsule:20,40mg Pharmacare
Vimovo Modified-release tab Astrazeneca
(naproxen+esmoprazole)
Solezol Vial: 40mg Anfarm-Hellas
Esomeprazole:

For H.Pylori eradication:

Esomeprazole→ 40mg daily for 10 days

Amoxicillin → 1000mg q12 hr for 10 days

Clarithromycin → 500mg q 12hr for 10 days

For frequent heartburn:

OTC: 20mg daily for 14 days

For GERD:

40mg once daily for 4 weeks

Maximum dose of Esomeprazole is 40mg daily

It is taken half an hour before meal.

Lansoprazole Lanton Capsule:15,30mg Rafa

Lansoprazole-Teva Capsule:15,30mg Teva

Zoton Caplet:15,30mg Pfizer

Samaprazole Capsule:30mg Sama

Lansoprazole:

For duodenal ulcer→ 15mg/day

For gastric ulcer→30mg/day

For NSAID-induced ulcer→ 30mg/day for 8 weeks

For GERD→ 15mg/day

 Dexlansoprazole Dexilant modified-release cap: 30,60 mg Takeda

Pantoprazole Controloc Enteric coated Takeda

tab:20,40mg
(Brand:protonix)
Vial

Pantover Enteric coated Jepharm

tab:40mg

Ulceron Vial:40mg/ml Anfarm-Hellas

Pantovenir Vial:40mg/ml BioAvenir

Pantocid Tab:40mg Sama

For pregnant women: the best choice is omeprazole

First line: antacid and sucralfate
Second line: H2-blocker
Third line: PPI
Note: ketoconazole need acid for its absorption →antiacid, H2-antagonist, PPI should not be
taken for 2 hours after ketoconazole

H-blocker, PPI→have been associated with B-12 deficiency, the risk increased when taken daily
for two years or more.

Prolonged use of PPI may cause osteoporosis because of decrease Ca absorption.

Calcium citrate supplements are absorbed more easily than calcium carbonate. They can be taken on an
empty stomach and more readily absorbed by people who take acid-reducing heartburn medications.
But because calcium citrate is giving only % 20 elemental calcium, you may need more tablets to get
your daily requirement.

Calcium carbonate supplements dissolve better in an acid environment, so they should be taken with a
meal, but calcium citrate supplements can be taken anytime because they do not need acid to dissolve.

Note: most kidney stones are calcium stones usually in the form of calcium oxalate (the preferred
calcium supplement for people at risk of stone formation is calcium citrate).
 Treatment of peptic and duodenal ulcers:

The most common cause of ulcers is H.pylori

‫→اذا السبب مش البكتيريا ممكن نعالجه ب‬PPI

‫اذا رجعت تكررت الحالة بكون السبب البكتيريا و رح نمشي بطريقة معينة في العالج‬

1-Triple therapy: 2 antibiotics + PPI → for 14 days

Clarithromycin + Amoxicillin (metronidazole may be used in penicillin-allergic patients)

Carithrimycin + Peptipac Pharmacare

Amoxicillin + Tripac Birzeit

Omeprazole

Note: clarithromycin is category c in pregnancy because of its effect on the

cardiovascular system of the fetus

Amoxicillin: safe in pregnancy with caution at first trimester

Metronidazole: at first trimester, application of metronidazole should be carefully

considered.

Recommended treatment in pregnancy is:

Amoxicillin + clarithromycin + omeprazole

→in case there is penicillin allergy→ metronidazole can be used instead of amoxicillin

2-Quadruple therapy: is used when triple therapy is failed or may be ineffective because
of local bacterial resistance.

Bismuth subsalicylate + metronidazole+ tetracycline+ PPI

Note: bismuth is contraindicated in pregnancy because of lack of human studies.

Tetracycline after week 15 is contraindicated

So quadruple therapy is contraindicated in pregnancy.

--------------
 Prostaglandins:

Misoprostol(Controlled drug):It is used to treat or prevent NSAID-induced gastric ulcer

It is contraindicated in pregnancy: category X

So, for NSAID-induced ulcer in pregnancy the choice is PPI only

Misoprostol Cytotec (Brand) Tab:200mcg Pfizer

Arthtotec Enteric coated Pfizer

tab:200mcg+50mg
(misoprostol+
200mcg+75mg
Diclofenac sodium)

Treatment of constipation:
Constipation: Hard, dry stool, painful, less than 3 times a week

‫ اذا اقل من أسبوع بنقدر نعالجه او تي سي‬،‫بنسأله كم صرله عنده امساك‬

.‫اذا قوي كتير واعراضه شديدة ممكن يكون السبب مشكلة تانية متل التهاب الزائدة الدودية‬

Causes:
Insufficient fiber and fluid intake
Decreased physical activity
Medications: NSAID, narcotics, anti-cholinergic, Aluminum hydroxide
Hypothyroidism
Obstruction by cancer (in this case, laxatives should not be used)

Laxatives
1- Bulk-forming agents
MOA: increase luminal mass which stimulate peristalsis.
it is the choice in the chronic constipation→ the effect occurs after 2-4 days
ex: psyllium, methylcellulose
should be taken with adequate amount of water

SE: abdominal cramping, flatulence

Laxmed 500mg of soluble Adult: Simulate bowel
fiber Cos-64 3 tab 2 times daily movement

Children:
2 tab 2 times daily
I hr before meal
 Psyllium Konsyl easy mix Rafa
Konsyl orange SR Rafa
Kalsic powder Maccabicare
Detoxner sachets New medicine

2- Osmotic agents: ‫هاد النوع مفضل استخدامه‬

MOA: retain water in the lumen by osmosis, cause a reflex increase in peristalsis
Not suitable for rapid relief of constipation (take 2-3days to give effect)
Ex:
Salt-containing: magnesium salts, sodium phosphate.
→contraindicated in renal failure because of hypermagnesemia
→with caution and for short term in patient with HTN, DM, HF
Salt-free agents: lactulose, glycerin, polyethylene glycol-electrolyte solution

Polyethylene glycole Hydralax (Fave di Fuca) Powder in Coswell-

With sucralose sachets itally

Normalax powder Taro

Meroken Powder Taro

Laxanorm Powder Jerusalem

Peglax Powder Floris

For the treatment of constipation

→need 24 or more to work

→Depending on age (Normalax / Laxanorm / Meroken)

Less than 1 year: 4g once daily

1-4 years: 4g twice daily or 8g once daily

4-8 years: 14g once daily

More than 8 years :17g once daily

The powder is dissolved in a cup of water and taken in the evening

Hydralax:

Children (2-4 yr)→ 1 sachets dissolve in 100 ml water in the morning and evening

Adults → 2 sachets dissolved in 100ml water 2-3 times daily

 They can be given for pregnant women but by a prescription.

Glycerine supp for adults: 2.15 gr

supp supp for children: 1.104g :‫لالطفال‬

)‫ أيام او اكثر‬4 ‫ ايام عند اللزوم (شرط يكون مر على بداية حدوث اإلمساك‬٣ ‫تحميلة كل‬

:‫للكبار‬

‫ تحميلة بنفس اليوم‬٢ ‫تحميلة كل يوم او بصير‬

Laxin Glycerin supp

Child:1.23g/supp Beit jala
Adult:2.6g/supp

Laxipro Contain sorbitol and glycerin ‫ نصف قنينة‬:‫ سنة‬١٢-٣

Enema ‫ قنينة واحدة‬:‫سنة‬١٢ ‫فوق‬
.‫كبار السن يوصى باستشارة طبيب‬

‫يجب ع الشخص االكثار من شرب السوائل للمساعدة في تليين البراز‬

Tree of life

Fleet enema Monobasic sodium phosphate Dexcel

Dibasic sodium phosphate

Microlet Contain: For the relief of constipation

enema Glycerol Continuous use may cause dependency on laxatives
Sod. Citrate
Sod. Laurylsulphacetate

Razalax Glycerol For rectal use

children / adult To treat constipation

The effect start: 3-6 hours after oral administration and 5-15min after rectal administration.

‫ مع بعض عند اللزوم في حال‬laxadin ‫ حبة من ال‬٢ ‫ بنعطيه لحتى يلين حركة االمعاء مع الوقت بس معه بنوصف‬Normalax ‫ال‬
،‫امساك قوي وما في اخراج‬

‫ بهدول الحاالت ممكن نعطي تحاميل‬laxadine ‫ ما بنعطو‬Crohn's ‫للحامل ومريض القولون العصبي وكانسر باالمعاء و مريض‬
hydralax ‫ مع ال‬glycerin

Babyzim Pepsin for the treatment of constipation and flatulence

Nicotinic acid Especially effective for infant
Sodium glycerophosphate 0-1 : 5 drops after each feeding
1-2 : 20 drops after each meal
2-5 : 40 drops after each meal
5-14 : 5 ml 3 times daily
 Lactulose Imlax Solution: 10mg/15ml Beit jala

Lactuver Solution: 10mg/15ml Jerusalem

Leavlac Solution Megapharm

Lactulose + Avilac Syrup Perrigo

Lactose+ Safe for children

Galactose

This class of laxatives used before surgery or diagnostic procedure, also to eliminate parasite
after anthelmintic administration.

They should use with caution in critically ill patients ex: HTN, because they cause intravascular
volume depletion and may lead to exacerbation of hypovolemic shock.

Lactulose may cause dehydration.

Lactulose is also used to reduce the amount of ammonia in the blood of patients with liver
disease. It works by drawing the ammonia from the blood into the colon where it is removed
from the body.

3-stimulant laxatives

Stimulate intestinal secretions

Onset of action:6-12 hr

Require adequate hydration

Ex: Bisacodyl, senna, castor oil, phenolphthalein

Chromic use of them lead to cathartic colon (laxative dependence)

Bisacodyl is a enteric coated tablets, so it should not be crushed or chewed, also should not be
taken within 1 hr of ingesting antacids or milk. (to prevent dissolving of the coat)

Senna may cause discoloration of intestine and urine

 Easylax Phenolphthalein Tab:120mg Meditic
yellow
For more than 12
years

‫نص حبة او حبة ونص قبل‬

‫النوم‬

SE: change the urine

color to purple.

Bisacodyl Laxadin Tab:5mg Teva

Dilax Tab:5mg Birzeit

Atzirut-X Tab: 5mg CTS

Contalax Supp: 10mg Dr-Fischer

4-Lubricant:

Ex: paraffin oil and glycerin oil

MOA: coat fecal contents and inhibit absorption of water from them, and they facilitate the
passage of stool

Should be taken on an empty stomach

Should not be taken at bedtime or recline after administration.

They interfere with fat soluble vitamins

Should not be taken by patient who has lung problems to avoid aspiration of mineral acid

Should not be given to children less than 6 years.

5-Stool softeners (emollient laxatives)

Ex: Docusate

MOA: facilitate the mixing of water and fatty substances to increase luminal mass and stimulate
peristalsis.

It is used with patient who must avoid straining to pass hard stool like patient who has heart
problems.
Not effective in treating ongoing constipation

Should not be used if there is nausea and vomiting, symptoms of appendicitis and
undetermined abdominal pain

May enhance the uptake of other drugs →toxicity.

Note: all classes of laxatives should not used in undiagnosed rectal bleeding and signs of
intestinal bleeding.

Pico-salax Sachets: Ferring ‫لتفريغ األمعاء قبل المنظار‬

pharmaceuticals
Sod. Picosulfate

Magnesium oxide

Citric oxide

Lax-Ray Syrup: Jerusalem ‫لتفريغ األمعاء‬

Sennoside A + B ‫تشرب الكمية كاملة قبل بيوم‬

‫من المنظار‬

--

Treatment of constipation in pregnancy:

Common due to physiological changes

→progesterone decreases both bowel and colon motility

→the absorption of water and electrolyte increased during pregnancy.

→increased size of uterus.

Firstly, an improvement should be attempted with dietary changes and life style modifications,
including:

-increased fluid and fiber intake (founded in fruits and vegetables)

-Training of the defecation reflex (giving enough time for defecation)

-Increased physical activity.

First choice is: stool-bulking agents: safe in pregnancy

They are non-absorbed substances that increase in volume when absorbing water, they
promote intestinal peristalsis

‫همي عبارة عن فايبر مستخلصين على شكل ادوية‬

‫الزم يتاخدو مع كمية كبيرة من الماء لحتى توخدها المادة وتكبر اما لو ما اتاخدت مع كمية ماء كبيرة رح تمتص الماء من األمعاء وتزيد‬
‫المشكلة‬

Ex: wheat bran, psyllium, wheat germ, methylcellulose.

Second line: Osmotic laxative

Ex: Lactulose →poorly absorbed

MOA: increase osmolar tension

There is no dependency on these drugs.

Third line: Saline laxatives

Ex: sodium sulfate, magnesium sulfate and magnesium citrate. ‫الملح اإلنجليزي‬

→poorly absorbed after oral absorption so the effect on uterus contraction is limited

→the preferred one is magnesium sulfate

Fourth line:

Stimulant laxatives →have dependence effect

Ex: Bisacodyl (the choice in the pregnancy) ‫النو األقل امتصاصا من بينهم بهاي المجموعة‬

‫اخر خيار النو بنخاف يزيد من االنقباضات بالرحم كمان‬

‫هاد الدوا ما بصير ينقسم النو ممكن يعمل تهيج من الداخل ويدايق المريض‬

Senna, cascara, aloe, caster oil should be avoided during pregnancy because some of them
have a stimulant effect on uterine contraction

There is other 2 groups which are contraindicated in pregnancy

→Lubricants (minerals)
1.Interfere with fat-soluble laxative ex: Vit K →neonatal hypoprothrombinemia and hemorrhage

→Vit D → affect fetal development

2. can be absorbed → immune reaction

3. aspiration →pneumonia

→Emollient laxatives

Ex: Docusate

May enhance the uptake of some drugs →toxicity

Treatment of diarrhea:
Having at least three loose or liquid bowel movements each day.

Often lasts for few days and can lead to dehydration:

Signs of dehydration:

-Loss of the normal stretchiness of the skin

-Changes in personality

-Tachycardia because of hypovolemia and hypotension

Most common cause of diarrhea:

Viral (Rotaviruses) or bacterial infection→ the most important thing in this case is to prevent
dehydration, this type of diarrhea helps in elimination of the microbes from the GI tract.

Other causes: lactose intolerance, inflammatory bowel disease, magnesium hydroxide,

antibiotics.

Note: Broad spectrum antibiotics cause diarrhea

Narrow spectrum antibiotics treat diarrhea

Aims of treatment: decrease fecal water content by decrease GI motility and increase transit
time to facilitates water reabsorption.
If it is acute: require symptomatic therapy→ fluid replacement and maintenance of electrolyte
balance. ‫ضروري للطفل اقل من عمر سنتين عشان ما يصير عنده جفاف‬

Me-Lyte Electrolyte Dissolve in 250ml water

3-4 sachets/ day

Orset Effervesant tab

Orset D Sachets powder

Aquamix Solution (zinc, Na, K, cl,

dextrose)

Supplyte kids Solution

Catidral Sachets

Dioclear Sachets

Nodiar Sachets

If it is infectious: bloody stools, high fever → antibiotic is necessary.

Drugs:
Opiates and opioid-containing preparations:
Opium tincture, codeine → SE: nausea, vomiting, sedation.

Diphenoxylate: synthetic meperidine analogue

→to be effective is used as a combination with atropine to reduce abuse and motility

→MOA: react with opiate receptors and inhibit intestinal motility but it does not have
analgesic properties. (has peripheral effect)

→it is not suitable for infectious diarrhea

→can be used during pregnancy

Loperamide: (opiate analog)

→it is the choice to treat diarrhea in pregnant women.

→No CNS activity, its effect on the intestine.

Diacare Loperamide 2mg Pharmacare For symptomatic Adult(more than 12yr)

control of acute dose: one cap 3-4 times
(Capsules) and chronic daily.
diarrhea.
Children (4-12yr): under
physician supervision
only.

Don’t give to children

less than 4 years

Diphenoxylate and loperamide are contraindicated in children due to severe side effects

Adsorbents: ‫ما بتوقف حركة االمعاء فقط تمتص السموم‬

Diosmectite: is a natural silicate of aluminum and magnesium used as an intestinal adsorbent
in the treatment of diarrhea.

Dioclear Sachets Adults: 1 sachet 3 times daily.

Children 6-18 year: 1 sachet 2-3 times daily

Children 1-6 year: 1 sachet 1-2 times daily.

Stoptrans Sachets Adults: 3 sachets/day

Children more than 1 year: 1-3 sachets

Children less than 1 year: 1 sachets /day

NoDiar Sachets: Adults: 3 sachets/day

Diosmectite and
prebiotic fibers

Catidral Sachets: During the first 3 days:

Diosmectite and Children(1-12month): up to 2 sachets

some electrolyte
 More than 1 year: up to 4 satchets

Adults: up to 6 satchets

Then continue with half of the dose until the

diarrhea is treated.

Kaolin and pectin and dietary fiber.

MOA: adsorbing toxic compounds from intestinal water (do not effect on the motility)

Megastop plus Furazolidone Tab: Jerusalem Adults:1-2 tab 3-4 times daily

Kaolin 20, 40, 40mg Children:1-2 teaspoonfuls 3-4 times

daily
Pectin Suspension
(antidiarrheal, intestinal antiseptic)
0.02, 0.6, 0.1 g/5ml

Furamix Furazolidone Tab: BeitJala Adults: 2 tabs 3-4 times daily

Kaolin 50, 100, 20 mg Children 5-12year: 1.5- 2

teaspoonful 3-4 times daily. / or 1
Pectin Suspension: tab 4 times

17.5 , 1000 , 50mg /5ml 1-4years: 1-1.5 teaspoonful 4 times

1month-1year: 0.5-1 teaspoonful 4

times daily.

Bismuth subsalicylate:

Binds toxins produced by Vibrio Cholerae and Escherichia Coli

Reduce fluid secretion in the GI tract

→effective for both treatment and prophylaxis of traveler’s diarrhea

→SE: tinnitus, black tongue and black stool

Relief of digestion disorders (diarrhea, nausea, flatulence, stomach pain)

As a preventive treatment of traveler's diarrhea
 Bismuth Bimatrol tablet Beit Jala
sub Suspension
salicylate
Pepto-Bismol Susp
(Brand)

Pink Bismuth Tab (chewable) Perrigo

Susp

kalbeten Tab Meditic

Susp

Bitin X Tab CTS

Susp

Note: The administration of salicylate should be avoided in children with chicken pox or
influenza because of possible risk of Reye’s syndrome

Bismuth is contraindicated in patients with renal impairment.

Early administration of lactobacillus associated with oral rehydration solution significantly

decreases the amount and duration of diarrhea.

Lactobaciilus Jamisson Probiotic Cap Jamisson

Acidophilus plus Cap Cultech

Hexbio Granules in sachets B-Crobes

1 sachet twice daily

for adult

1 sachet once daily

for children

BioFocus PROBI-UT

‫البكتريا النافعة تساعد في إعادة التوازن البكتيري في األمعاء وبذلك تساعد على إيقاف االسهال‬

Referrals to physician if:

1.patient is younger than 3 or older than 60

2.blood or mucus in the stool

3.high fever(greater than 38)

4. dehydration or weight loss

5.vomitting

6.duration of more than 2 weeks.

‫الرضاعة الطبيعية يجب ان تستمر حتى لو الطفل يعاني من االسهال النو مش هي السبب‬

Treatment of nausea and vomiting (antiemetics):

It works by depress the vomiting center which receives inputs from several sources:

1-Chemoreceptor trigger zone (CTZ)

‫ادوية السرطان تحفز هذه المنطقة فهي مسبب كبير للغثيان واالستفراغ‬

2-vestibular nucleus

‫في االذن الداخلية‬

3-peripheral afferents from the pharynx and gastrointestinal tract

‫من عالمات التهاب األمعاء هو الغثيان واالستفراغ‬

4-psychologic input from the central nervous system (CNS)

→Antiemetics are useful in the treatment of vomiting associated with motion sickness and
chemotherapy.

1-cholinergic antagonist
They are used to treat motion sickness and preoperative situations, but they are not useful in the
treating nausea caused by chemotherapy.

Scopolamine (Hyoscine)

→inhibit cholinergic CNS receptors

→crosses the blood brain barrier

→more effective for emesis than nausea

SE: (atropine-like effect)

Sedation/dry mouth / urinary retention / blurred vision / confusion / hallucinations.

It is also used to reduce stomach cramps and pain

Dose: 10-20mg 3-4 times daily.
The effect begins after 20 min and last for up to 8 hr

Others:

Homatropine /Hyoscyamine / Clidinium/ oxybutynin

Note: butyl scopolamine is the spasmolytic of choice in this group of medications during
pregnancy (is poorly absorbed after oral administration).
If the spasm is combined with infectious diarrhea it should not be treated with
anticholinergic, because the motions of intestines should not be stopped.
Note: in case of kidney and biliary colic, the preferred choice is NSAID, but during
pregnancy we should keep in mind that NSAID should not be used after week 28
 Product Another Active Form Strength Company
Scientific Name Ingredient
Name

Tablets 10 mg , 20
Hyoscine Scobutyl ---- mg Jerusalem
butylbromide Ampoules
20mg / ml

Scobutyl – Paracetamol Tablets 10 mg / Jerusalem

Co (250 mg) 250 mg

Hyoscine —- injection 20mg/Amp wellona

butylbromide Pharma
injection
(Brand)

(Homatropine) + 2.5 mg
Homatropine Spasmin Paracetamol Tablets 500 mg Jerusalem
Papaverine HCl 60 mg
Allobarbitone 30 mg

Hyoscyamine Kolic ---- Oral 0.125 mg / Beit Jala

Drops ml

Clidinium Modex Clidinium Tablets 2.5 Birzeit

Chlordiazepoxide mg+5mg

Librax Tablets 2.5 mg *5 Roche

mg

Oxybutynin Novitropan Tab: 5mg CTS Relief of symptoms

associated with
voiding

Oxybutynin is also used to treat overreactive bladder by relaxing the muscles. (antispasmodic)

Papaverine Papaverine Tab: 40, Rekah

80mg
 For stomach spasm Papaverine sterop Amp: Teva
40mg/2ml

Spasmalgin: (controlled) Tab: 80mg Medetic

With paracetamol 150mg

Codeine 10mg

Atropine 0.4mg

Spasmin: Tab:60mg Jerusalem

With homatropine

Paracetamol

Allobarbitone

2-Anti-Histamines (H1-receptor antagonists)

Diphenhydramine / Dimenhydrinate / Meclizine / promethazine

MOA: inhibit cholinergic pathways of the vestibular apparatus

They are used to treat motion sickness and true vertigo ( ‫دوار ناتج عن التهابات في االذن الداخلية يصاحبه‬
‫)غثيان واستفراغ‬

SE: sedation and dry mouth.

Meclizine and promethazine have minimal anticholinergic side effects and are used most often.
Ancozine Tab: Birzeit 25-100mg / day PO in single dose or
divided q 6-12hr
Meclezine 25mg
‫اذا رح نعطي حبة باليوم بتكون قبل النوم‬
Vit B6 50mg

Paravomine Tab: Beit Jala

Meclezine 25mg

Vit B6 50mg

Diclectin Doxylamine Recommended dose:

Vit B6 4 tabs/day:

1 tab in morning, 1 tab in the afternoon, 2

tabs at bedtime

On an empty stomach with a glass of

water.

‫ممكن نبلش بحبتين باليوم قبل النوم اذا ما نفع بنصير نزيد‬
‫ حبات باليوم‬4 ‫لحد‬

Dimenhydrinate Daramine Tab:50mg Beit jala

Travamin Tab:100mg Rekah

Is an antihistamine to treat or prevent nausea, vomiting and dizziness associated with motion
sickness.

)‫لمنع دوخة السفر (تؤخذ الحبة قبل ربع ساعة من بداية الرحلة‬

3-Dopamine antagonist:
Metoclopramide

MOA:

-Main MOA: blocks D2-receptors within the CTZ

-It increases the sensitivity of the GIT to the action of Ach, this enhances GIT motility and
gastric emptying and increases lower esophageal sphincter tone.

- High doses antagonize serotonin receptors in the vomiting center and GIT.

Uses:

-Nausea due to chemotherapy (cisplatin and doxorubicin)

-Opioid-induced vomiting.
SE:

Sedation / Diarrhea / extrapyramidal effects (parkinsonism) / elevated prolactin secretion.

Emestop Metoclopramide Tab: 10mg Birzeit

Amp: 10mg

Syr:5mg/5ml

Pramin Tab:10mg Rafa

Amp:10mg/2ml

Emegrain Metoclopramide 5mg Tab Beit Jala

Paracetamol 500mg

Metoclopramide: dose in case of gastroesophageal reflex

10mg q6hr 30 min before meals and at bedtime.

Note:

Gastroparesis: partial paralysis of the stomach, is a disease in which the stomach cannot empty itself of
food in a normal way because of damaged nerves and muscles

Treatment:

Metoclopramide: to stimulate the stomach muscles.

Diphenhydramine, ondansetron: to treat nausea and vomiting

Domperidone
D2-dopamine antagonist
Works by blocking the messages between digestive system and brain
→it causes muscles at the entrance of the stomach to tight and the muscles of
the exit of the stomach to relax→ decrease feeling of vomiting
→also, it blocks messages between chemoreceptor trigger zone (CTZ) and the
vomiting center.
 Motilium Domperidone Tab: 10mg

For janssen

Metosim Domperidone Tab: 10mg

‫يقلل حركة المعدة ويرخي الصمام بين المعدة واالمعاء فيسرع من عملية تفريغ الطعام ويقلل الشعور بالزوفان‬

10mg up to 3 times daily (maximum: 30mg/day)

Phenothiazines: prochlorperazine

Butyrophenone: droperidol

They are work like metoclopramide → block dopaminergic in the CTZ

They are used to treat nausea due to chemotherapy and radiation therapy, and to control postoperative
nausea.

They are contraindicated in Parkinson’s disease because of their extrapyramidal effects.

4-5-HT3 antagonist (serotonin antagonist)

Ondansetron
Not effective for motion-sickness-induced nausea.

More effective than metoclopramide against nausea induced by chemotherapy.

It is also used in cases of postoperative nausea

Orally or IV

SE: mild constipation

Zofran Ondansetron Tab: 8mg Novartis

Amp: 8mg/4ml

4mg/2ml

Ondatron Ondansetron Amp: 8mg/4ml Kleva

4mg/2ml

Ondansetron Inova Ondansetron Tab: 4, 8mg Inovamed

Onaset Ondansetron Tab: 4, 8mg Beit Jala

Granisetron { Kytril}

Is a serotonin 5-HT3 receptor antagonist used as antiemetic to treat nausea and vomiting following
chemotherapy and radiotherapy.

Setron Granisteron Tab: 1mg Perrigo

Granisteron TEVA Granisetron Amp: 3mg/3ml Teva

Kytril Granisetron Amp: 1mg/1ml Roche

Tab:1mg

Longer acting and more potent than ondansetron and metoclopramide.

Note: dexamethasone and methylprednisolone (orally or IV bolus) have proven effective in the
prevention of nausea after highly emetogenic cancer chemotherapy and late postoperative nausea and
vomiting (not well understood mechanism).
Dexamethasone Decort Amp: 4mg Birzeit
Tab: 0.5, 0.75, 2 mg
Dexamethasone Amp
Novodexon Syrup : 0.5mg/5ml Beit Jala

Methylprednisolone Medrol Tab: 4mg Pfizer

Depo-medrol Susp for injection: Pfizer
40mg/ml
Solu-medrol Vial : 40, 125, 500, Pfizer
1000mg
Prednisolone Prednitab Tab: 5,20mg Birzeit
Susp: 15mg/5ml
Allow Syrup: 15mg/5ml Jerusalem
These drugs are used for many other conditions which are more common in patients.

Note:
Benzodiazepam acts as anxiolytic agents to reduce anticipatory emesis( ‫بكون المريض متوتر وبستفرغ النه عنده‬
‫)فكرة مسبقة عن الدوا انو بعمل استفراغ‬
They are also useful in the treatment of vertigo, and control symptoms of Meniere disease (disorder in
the inner ear that lead to vertigo) in 60-70% of patients

Diazepam Assival Tab:10mg Teva

Amp:10mg/2ml
Serepam Amp Birzeit
Clonazepam Clonex Tab: 0.5, 2mg Teva
Lorazepam Lorivan Tab: 1mg Dexcel
Lorocare Tab: 1, 2.5mg Pharmacare
 Oxazepam Vaben Tab: 10mg

4-NK1 antagonist
Aprepitant: It is substance P receptor antagonist, used in delayed nausea caused by chemotherapy.

Emend Aprepitant Cap: MSD

1 cap: 125mg ‫بالعادة بعطو الكبسولة األولى‬
2 caps: 80mg ‫قبل الكيماوي بساعة والكبسولة‬
‫التانية والتالتة في اليوم التاني‬
‫والتالت بعد الكيماوي‬

--------
Note: ondansetron, meclizine and doxylamine can be used to treat nausea and vomiting because of
using cabergoline (dopamine agonist), but metoclopramide cannot be used because it is a dopamine
antagonist.

-------

Note: Ipecac→ it is an emetic agent that induce reflex vomiting.

--------

Treating nausea and vomiting in pregnancy:

Causes: elevated HCG level, level of estrogen and progesterone, hyperolfaction, depression,
anxiety
during pregnancy → increased the level of progesterone and estrogen→ decrease
gastric emptying → vomiting and nausea
lower esophageal sphincter tone → GERD
life style modification to decrease these problems:
1-Eat small and frequent meals
2-The meals should be high in carbohydrate and protein, low in fats.
3-Avoid spicy food
4-Avoid caffeine, garlic and onion because they participate in lowering the tone of
the sphincter.
5- No smoking
6- Leave at least 3 hours between the last meal and time of sleeping
Avoid tight cloths

:‫بننصح الحامل تعمل بعض األشياء لحتى تقلل من الغثيان والتقيؤ‬

‫تتناول وجبات صغيرة ومتعددة خالل اليوم‬

‫يحتوي الطعام على نسبة عالية من الكربوهيدرات والبروتين بينما نسبة قليلة من الدهون النها تزيد من افراز الحامض بالمعدة‬
 ‫تناول بعض المكسرات والبسكوت الناشف عند االستيقاظ من النوم‬

‫االبتعاد عن السوائل التي تزيد االستفراغ عند الحامل واالبتعاد عن المالبس الضيقة‬

Pharmacologic treatment:

1.pyridoxine (Vit B6)→ alone is not succeddful→should be combined with antihistamine

2.First-generation antihistamine ex: Doxylamine ( 1st line), Meclizine (less sedating),

Dimenhyrinate and Diphenhydramine (avoided at 3rd trimester because it stimulate uterine
contraction)

‫ كتير خالل النهار‬sedation ‫ يكون بالليل وما يعمل‬Peak ‫قبل النوم لحتى‬

3.Metoclopramide (dopamine antagonist)→ it is also effective in the hyperemesis gravidarum)

(category B)

4.Ondansetron (serotonin antagonist) → should be used only if other antiemetics are not
effective, due to the lack of safety studies.

Note: methylprednisolone (corticosteroids)→modify the chemoreceptor trigger zone→it is

used to control nausea and vomiting associated with chemotherapy and hyperemesis
gravidarum.

Other substances are recommended if the previous have been failed.

Betahistine (histamine analogue)

Betahistine Betastin Tab: 16,24mg Pharmacare

Viraserc Tab: 16mg Birzeit

Betahistine Tab: 16mg Teva

Agiserc Tab: 16mg Perrigo

‫يستخدم أيضا لعالج الدوار بسبب مشاكل باالذن الوسطى او أسباب أخرى‬

Cinnarizine (antihistamine)

Cinnarizine Cinazine Tab: 25, 75mg Pharmacare

Stunarone Tab: 25mg Janssen

scopolamine (anticholinergic)

‫االنتقال من نقطة لغيرها بكون بالتدريج وحسب فعالية الدواء في عالج الحالة‬
Treatment of bloating:
Simethicone

.MOA: changes the surface tension of gas bubbles and causes collapse of formed bubbles

For adults

Eucarbon Senna, Rhei, charcoal, carbo F.Trenka 1-2 tab during meals
vegetab, sulfur depurate……
Safe in pregnancy but
without senna

Carboflor Activated vegetable charcoal Cap Floris ‫المستورد‬

Gas Clear CF pharm

Activated Charcol 300mg

Simethicone 50mg

No Gas Dual Sky health

Activated Charcol 300mg

Simethicone 50mg

Carbosylane Trima
Activated Charcol 140mg ‫الكبسولة الزرقاء تعمل في المعدة‬
‫اما الحمراء فتعمل في األمعاء‬
Simethicone 45mg

Gas and bloating Sandoval

Simethicone 50mg

Balonix Med Chewable tab

Simethicone 80mg

Gazim X CTS
Simethicone 125mg

Dosage of simethicone:
For adults: 40-360mg q6hr after meals and at bedtime PRN (not to exceed 500mg/day)

‫ مرات باليوم‬٣ ‫ مرات باليوم بعد االكل وقبل النوم او حبتين معا صباحا ومساء او حبة‬4 ‫ممكن نوصفه حبة‬

For pediatric:

Less than 2 years: 20mg (0.3ml) q6hr → not to exceed 240mg/day

2-12 years: 40mg (0.6ml) q6hr → not to exceed 480mg/day

Comil ‫يخفف من المغص الناتج عن الغازات‬

Simethicone ‫للرضع واالطفال والبالغين‬
Contain probiotic
With probiotic ‫يتم اذابة الكيس الذي يحتوي البكتيريا النافعة في السائل ويحرك جيدا ويحفظ‬
‫ يوم صالح لالستخدام خاللها‬14 ‫بالثالجة مدة‬
Oral drops

Balonix for infant

simethicone 0.5 ml before each feed
40mg/ml ‫ ايام اذا ما راحت الغازات بنضاعف الجرعة واذا ما تحسن فيراجع‬٤-٣ ‫خالل‬
‫الدكتور‬
Oral drops

Anti Gas less than 2yr: 7 drops q6hr

simethicone 3 (20 mg)
mg/drop More than 2 years: 14 drops q6hr
(40 my)
with probiotic

Oral drops

Simped less than 2 yr : 0.2 ml

simethicone More than 2yr : 0.6 ml
40mg/0.6ml
Birzeit
Oral drops

Simicol CTS
Oral drops:
40mg/0.6ml

Kiddies No Sky health

gas Simethicone ‫ يوم صالح فيهم لالستخدام‬14 ‫يضاف الكيس الى العلبة ويوضع بالثالجة مدة‬
Contain probiotic
With probiotic

Oral drops
Simethicone is safe in pregnancy as carminative,

Plant-based substances which contain anise. Caraway, peppermint, also can be used but in
normal doses.

BabyNam Sodium Syrup Beit Jala For reduce the

bicarbonate symptoms of
stomach spasm
Anise oil and cramping

Peppermint oil

Gastop-B Chamomile Oral drops

Anise oil

Peppermint

Dill essential oil

Colpermin Peppermint oil Cap TILLOTTS Relieve spasm

PHARMA and cramps
associated
with irritable
bowel
syndrome

---------------

Note:

Guna-bowel → drops: for the release of bloating and discomfort

Guna-stomach→drops: for gastric ulcers or duodenal ulcers, abdominal discomfort

---------------------------

Inflammatory bowel disease (IBD):

Is an idiopathic disease caused by a dysregulated immune response to host intestinal microflora.

The two major types od IBD are :

1-Ulcerative colitis: is limited to the colonic mucosa

2-Crohn disease (CD): affect any segment of the gastrointestinal tract from the mouth to the
anus. Involves skip regions and is transmural
 These is a genetic predisposition for IBD, and patients with this condition are more prone to the
development of malignancy.

The medical approach is symptomatic care and mucosal healing for mild disease.

Step-up approach:

Step 1: Aminosalicylates (oral, enema, supp): for treating flares and maintaining
remission, more effective in UC than in CD

Ex: sulfasalazine, mesalamine, balsalazide, olsalazine.

Salazopyrin Sulfasalazine Tab: 500mg Pfizer Salazopyrin is used

for ulcerative colitis
(immunosuppressant EN tab: 500mg and crohn disease
and anti-inflammatory
agent) Salazopyrin EN can
reach the joints so it
is also used in
rheumatoid arthritis
because it reduce
swelling and stiffness
in joints.

Asacol Mesalazine Caplet:400, 800mg Tillotts

pharma
Slow release

Rafassal Mesalazine Enteric coated Rafa

Caplet:500 mg, 1g

Enema:4gram

Supp: 500mg, 1g
Aminosalicylic acid
Enema: 1g

Pentasa Mesalazine Granules: 1g Ferring

Slow release tab:

1g

Tab: 500mg

Supp: 1g

Enema: 1g
Step 2: Antibiotics: metronidazole, ciprofloxacin, rifaximin

Step 3: corticosteroids (IV, oral, topical, rectal)

Cortiment Budesonide Prolonged It is used for Ferring

MMX release tablet: treating mild Pharmaceuticals
9mg to moderate
active
ulcerative
colitis in the
large intestine.

Step 4: immunomodulators: azathioprine, mercaptopurine, methotrexate, cyclosporine,

tofacitinib.

Mercaptopurine Puri-Nethol Tab:50mg Aspen For cancer,

autoimmune
disease, crohn’s
and ulcerative
colitis

Step 5: clinical trial agents

Other drugs may be used: H2-blocker, PPI, antidiarrheal, anticholinergic antispasmodic

agents.

In Pregnant women with IBD: increased risk of preterm delivery, low birth weight, be small for
gestational age.

Mesalazine → the drug of choice for treatment of chronic IBD and mild active case

Sulfasalazine→ the second choice, because sulfonamide moiety might potentiate kernicterus
and neonatal neutropenia.

For active cases the choice is corticosteroids (inhaler budesonide, systemic prednisone or
prednisolone)

Avoid using of immunosuppressive agents, 6-mercuptopurine, methotrexate.

Irritable bowel syndrome (‫)القولون العصبي‬
Mebeverine is a drug used to alleviate some of the symptoms of irritable bowel syndrome. It
works by relaxing the muscles in and around the gut. ‫يساعد في تهدئة القولون العصبي ويصرف عادة مع ادوية‬
‫تعالج تراكم الغازات‬

(antispasmodic, relieve of cramps pain)

Mebeverine Modulon Birzeit

135mg
Meberine Beit Jala

Colotal Perrigo

Mebeverine 135mg: 3 times daily, 20 min before meal.

It is a stress-related disease, so using of psychotropic drugs is effective in treating IBS, such as:

Sulpiride Hypothal Cap:50mg Birzeit

Modal Cap:50mg Rafa

Modal forte Cap:200mg Rafa

Rowachol Pinene, camphene, Cap To breakdown stones in the

cineol, menthol, gallbladder (gallstones or
menthone, Borneol cholelithiasis)

(essential oils) 1 to 2 cap three times a day

On an empty stomach, half an

hour before meals.

Rowatinex Essential oils Cap Help to breakdown and remove

kidney and urinary tract stones,
also relieve muscle spasm, thus
reducing pain.

It increases blood flow to the

kidney and reduce
inflammation
Creon 1000 (for Abbot)→capsules contain 150mg of pancreatin which is a pancreatic enzyme
(mix of amylase, lipase, protease) to treat malabsorption syndrome due to certain pancreatic
problems.

Digestive enzymes Creon 1000 Cap: 150mg Abbot

(pancreatin, amylase, Pankreoflat Cap Abbot

lipase, protease)
New-Biozyme Cap Solgar
“Sometimes the bad things that happen in our lives put us directly on
the path to the best things that will ever happen to us”♥
 Topic 4: Respiratory System
📌Common respiratory diseases:
1. Asthma
2. COPD
3. Allergic rhinitis
4. Cough
5. Common cold

Asthma
📌 Asthma:
Dyspnea due to contraction of airway smooth muscle
Mucus hypersecretion
Airway inflammation
Bronchial hyper-responsiveness.
It is an inspiratory disease: the patient finds a difficulty in taking the breath

📌Most common symptoms.

shortness in breath
cough
chest tightness
wheezing
Rapid respiration
‫ مع وجود السعال‬،‫يشعر المريض بضيق في النفس بسبب تضيق ممر الهواء وهذا يؤدي الى تسارع في اخذ النفس‬

Q: What is the trigger of asthma?

• Exercise ‫كثير ناس بتيجيهم النوبة بعد تمارين معينه اوشغل تعب‬
• Allergens ‫كثير اشياء ممكن نالقي مريضنا بتحسس منها مثل فراء الحيوانات او الغبار او عطور‬
• Dust, smoke
• Cold ‫كثير بنالحظ بفترة الشتاء انهم بزيد الوضع عندهم‬
• After laughter ‫بعد الضحك الهستيري‬

Drugs that exacerbate asthma:(used with caution)

-->Aspirin and other NSAID: because they increase leukotrienes
-->Beta-blocker
-->ACE inhibitors, which are used for heart disease and high blood pressure, can cause a
cough which could be mistaken for an asthma symptom.

note: Asthma is not a progressive disease, but if untreated the severity and incidence of asthma
exacerbations will be happened frequently.
———
•All patients need to have a “quick-relief” medication to treat acute asthma symptoms.
• Drug therapy for long-term control of asthma is designed to reverse and prevent airway
inflammation.
———-
‫‪Drugs used for asthma:‬‬

‫‪Main drugs:‬‬
‫‪Short and long Beta-2-agonist‬‬
‫‪Inhaled corticosteroids‬‬

‫‪Other and alternative drugs:‬‬

‫‪Systemic corticosteroids‬‬
‫‪Anticholinergic‬‬
‫‪Leukotriene inhibitor‬‬
‫‪Cromolyn‬‬
‫‪Aminophylline and theophylline‬‬
‫‪----------‬‬
‫‪Therapy for treatment of asthma:‬‬

‫‪1.Intermittent asthma‬‬
‫حدوث النوبة يكون متقطع اي مرة واحدة باألسبوع‬
‫تستخدم ‪ SABA‬وقت حدوث النوبة‬

‫‪2.Persistent asthma‬‬

‫‪Mild Persistent:‬‬
‫حدوث النوبة يكون مرتين باألسبوع او اكثر‬
‫‪ SABA‬وقت حدوث النوبة فقط‬
‫ما هو الفرق في العالج عن الحالة السابقة؟‬
‫‪+ low dose of ICS‬‬

‫‪Moderate persistent:‬‬
‫حدوث النوبة يوميا‪.‬‬
‫‪ SABA‬وقت النوبة‬
‫مع زيادة جرعة ‪( ICS‬زيادة الجرعة هي زيادة عدد ال ‪)puff‬‬
‫او يستخدم المريض الجرعة المنخفضة مع اضافة ال ‪LABA‬‬
‫واذا لم يشعر بتحسن ممكن اضافة ‪ add on medications‬مثل ‪montelukast, theophylline‬‬

‫‪Severe persistent:‬‬
‫حدوث النوبة يوميا وممكن اكثر من مرة باليوم وهذا يعيق الحياة اليومية للمريض بشكل كبير الن االعراض قوية ويصاحبها السعال‬
‫المستمر‪.‬‬
‫‪ SABA >--‬عند حدوث النوبة‬
‫‪LABA +medium or high dose of ICS‬‬
‫ممكن استخدام ‪ oral cs‬بحيث يكون باقل جرعة ممكنة مع ضمان فعاليتها والقصر فترة ممكنة لتجنب اعراضها الجانبية‬
1. B2 - agonist
MOA: direct relaxation of bronchial smooth muscle (by inhalation)
-Have no anti-inflammatory effects

Other effects:
Relax vascular smooth muscle (in vessel)

LABA (long acting bata2 agonist) SABA (short acting beta2 agonist)

Adjunctive therapy for long term control of disease used for quick relief asthma attack
Shouldn’t be used for quick relief of an acute asthma
attack

Onset of duration: slow, greater than 5 minutes The hallmark SABA is the drug
compared to the SABAs, with up to 15 minutes for salbutamol:
salmeterol —>onset of action of under 5
Long duration: at least 12 hr minutes
—>duration of action: between 3 to
6 hours

-Monotherapy of LABA is contraindicated -Monotherapy with SABAs

-Should be used only in combination with an asthma appropriate for:
controller medication 1- intermittent asthma
2-exercise-induced bronchospasm
-inhaled corticosteroids (ICS) is the long-term controllers
of choice in asthma

Inhaled LABA prefers more SR LABA or All pt. with asthma should have
SR theophylline in nocturnal asthma SABA inhaler

Formoterol / Salmeterol Salbutamol (Albuterol) /

Terbutaline / Levalbuterol /
---------- Pirbuterol

Indacaterol / Olodaerol / Vilanterol:

Ultra-LABAs have the greatest duration of effect, up to

24 hours
onset of action around 5 minutes.
Once daily
Short Acting Beta Agonist: SABA
Salbutamol ( Albuterol) / Terbutaline / Levalbuterol / Pirbuterol

Scientific name Trade names Dosage forms Strengths Company

Ventol tab 2 mg Birzeit

Salbutamol sulfate syrup 2mg/5ml

respiratory solution 5mg/ml

tab 2 mg Gsk

syrup 2mg/5ml

Ventolin resp. solution 5mg/ml

metered dose inhaler 100 mcg/dose

Ventocare tab 2 mg Pharmacare

syrup 2mg/5ml

Salbutamol teva metered dose inhaler 100 mcg/dose Teva

Salbutrim metered dose inhaler 100 mcg/dose Trima

Tab→for abnormal uterine contraction in pregnant women not for asthma

Solution for nebulization and inhaler →For bronchospasm:

Terbutaline Terbulin Syrup 1.5mg/5ml vitam

Bricalin powder inhaler 200doses Teva

Respiratory Solution
Long-Acting Beta Agonist: LABA

Formoterol / Salmeterol
Indacaterol / Olodaerol / Vilanterol

Scientific name Trade names Dosage forms Strengths Company

Formoterol Foradil Inhalation powder in caps 12 mcg Novartis

Salmeterol Serevent inhaler Inhalation Suspension 25 mcg/dose

GSK
Serevent diskus Inhalation Powder 50 mcg/dose

Seretide Inhalation powder 50, 100mcg

GSK

Indacaterol Onbrez Breezhaler Inhalation powder in caps 150 mcg Novartis

(Ultra LABA) 300 mcg
Used mainly for COPD

While most commonly used as airway treatment, nebulized albuterol is also useful as a
treatment for hyperkalemia by providing a rapid shift of intracellular potassium.

Terbutaline is a commonly used short-acting beta-2 agonist as a tocolytic in the cessation of

labor contractions.

Typical administration of these agents is inhalation via metered dosing or dry powder inhalation.
Compared to the alternative oral administration, inhalation has an increase in therapeutic value,
as well as a decrease in systemic side effects

The most common side effects of beta-2 agonists involve the cardiac, metabolic, or
musculoskeletal system.

Side effects of B2 agonist:

1.Tachycardia (common, especially within the first weeks of use)

2.Hypokalemia
Decrease serum potassium levels via an inward shift of potassium into the cells due to an effect
on the membrane-bound Na/K-ATPase.

3.Hypomagnesemia

4.Hyperglycemia:
Beta-2 agonists also promote glycogenolysis.

5.Musculoskeletal tremors:
more commonly with the use of oral beta-2 agonists.

6.Headache
7.insomnia

These side effects are minimized with inhaled dosage forms.

————————

At toxic doses, hyperstimulation of beta-2 receptors leads to:

1.Hyperglycemia

2.Hypokalemia

3.Lactic acidosis
Biochemical pathways by which beta 2-agonist lead to increased lactate production as a direct
effect of inhaled salbutamol

4.Cardiac toxicity: arrhythmias, cardiomyopathy, and ischemia.

Arrhythmias are seen more commonly in fenoterol usage versus albuterol, and arrhythmias
have an increase in frequency in patients with underlying heart disease or concomitant
theophylline use.

———————

2- Corticosteroids

Fluticasone propionate Flixotide Inhaler CFC Free GSK

50,
125,
250 mcg
(Susp for inhalation)
Metered doses

Diskus:
250,500 mcg/ dose

Nebules:
0.5 mg/2ml
(For nebulization)
 Budesonide Miflonide Inhaler Novartis
‫ اقل واحد امتصاص في الجسم‬breezhaler 200mcg
‫فتأثيره يعتبر توبكال اكتر‬ 400mcg

Budesonide Susp for inhalation for use with Teva

Sterinebs nebulizing device only

0.5mg /amp

1mg / amp

Budicort suspension for inhalation

Respules

LABA + Corticosteroid:
Scientific name Trade Dosage forms Strengths Company
names

Budesonide+ Symbicort Inhalation powder 80 /4.5mcg AstraZeneca

Formoterol Turbuhaler 160/4.5 mcg
320/9 mcg

Inhaled powder 160/4.5mcg Teva

DuoResp 320/9 mcg
Spiromax

Fluticasone Flutiform Pressurised inhalation 50/5 mcg Rafa

+Formoterol suspension 125/5 mcg
250/10 mcg

Beclometasone+ Foster Pressurised inhalation 100 /6mcg Chiesi

Formoterol NEXThaler solution

Fluticasone+ Seretide Inhalation Powder 100 /50mcg GSK

Salmeterol diskus 250/50 mcg
500/50 mcg

Inhaler Corticosteroids (ICS)

• Inhaler corticosteroids (ICS) is the drug choice for persistent asthma with any degree
(mild / moderate / severe) →decrease morbidity and mortality
 • Direct anti-inflammatory in the airway,
• Indirectly bronchodilator
• Increase the sensitivity of bronchial system for B2 agonist

Note: corticosteroids should be continuously to be effective in controlling inflammation (several

months of regular use)
‫استخدامه بشكل متقطع يقلل من فعاليته في تقليل االلتهاب‬
Using ICS for several months of regular use, reduces the hyperresponsiveness of the airway for
the stimuli such as allergens, irritants, cold air, and exercise.

MOA: inhibiting phospholipase A2, so inhibiting release arachidonic acid that will lead to:
1. Direct anti-inflammatory effect
2. Decrease the inflammatory cascade (eosinophils, macrophages and T lymphocyte)
3. reverse mucosal edema
4. decrease the permeability of capillary
5. inhibit the release of leukotriene

Systemic CS: maybe added to some patients with severe persistent asthma. It should be used
for short courses (for adults treated with 5-7 days course, but children only 3-5 days)

Short courses of SCS are associated with increased risk of adverse events including loss of
bone density, hypertension and gastrointestinal ulcers/bleeds, in addition to serious impacts on
mental health

Note: oral corticosteroids should be stopped gradually but in this case there is no need for that
because it is used for just short course for about 5 days ( it is not enough time for making
suppression of the pituitary axis )

IV methylprednisolone or oral prednisone is required for patients with severe exacerbation of

asthma (bronchodilator is not enough alone because when its effect ended, a relapse of the
case may occur)

Side effects of systemic corticosteroids

1.cataract and increased the pressure in the eyes (glaucoma)
2.Fluid retention, causing swelling in your lower legs (edema)
3.High blood pressure
4.Problems with mood swings, memory and behavior and other psychological effects, such as
confusion or delirium
5.Weight gain, with fat deposits in your abdomen, face and the back of your neck ( due to
increase of the appetite and edema)
6.High blood sugar, with long term use, insulin resistance may occur and then DM
7.Increased risk of infections, especially with common bacterial, viral and fungal microorganisms
8.poor wound healing
9.osteoporosis (due to decrease calcium absorption in the stomach, and inhibit the action of the
osteoblast)
(common) (cortisone has a negative effect on the bone)
10. Muscle weakness and tissue loss (because corticosteroids consume muscle’s proteins
11. Peptic ulcer (due to increase of acid and pepsin)
12. Cushing syndrome
Side effects of inhaled corticosteroids

When using inhaled corticosteroids, some of the drug may deposit in your mouth and throat
instead of making it to your lungs. This can cause:

1.Oropharyngeal candidiasis; Fungal infection in the mouth (oral thrush) we can avoid it by
advice pt. to " swish & spit"
Corticosteroids is immunosuppressant can cause local immunosuppression
2.Hoarseness. ‫( بحة بالصوت‬common)
3. Suppression of the hypothalamic-pituitary axis: shunting of growth in children may occur

ICS with spacer have fewer systemic effects

Spacer: attached with metered-dose inhaler. Allow the drug particles to reach the target airway
tissue.
——-
Inhalation:
MDI: metered dose inhaler
‫تحتوي على جزيئات متطايرة من الدواء التي تكون مضغوطة داخل األنبوبة‬

: ‫يجب إرشاد المريض بالطريقة الصحيحة ألخذه وهي‬

‫قبل اخذ الدواء على المريض عمل زفير الخراج الهواء ثم وضع رأس االنبوبة في الفم والضغط على البخاخ مع اخذ شهيق بشكل بطيء‬
‫وعميق‬

‫عدم اتباع الطريقة الصحيحة يؤدي الى تراكم جزء من الدواء في الفم والحلق وبالتالي يسبب اعراض جانبية‬

DPI: Dry powder inhaler

‫هذا النوع يتم اخذ نفس عميق وسريع النه عبارة عن بودرة تذوب في اللعاب‬

3-Anticholinergic
Acetylcholine binds to muscarinic receptors to play a key role in the pathophysiology of asthma,
leading to bronchoconstriction, increased mucus secretion, inflammation and airway remodelling

MOA: Anticholinergics antagonize the parasympathetic effects of acetylcholine, thus providing

therapeutic benefit via a supplementary mechanism to ICS and LABA effects in asthma
(Bronchodilator and anti-secretory)

Ipratropium Bromide and Salbutamol nebulized combinedly have a better bronchodilation

effect than Salbutamol alone in acute severe asthma.
They are used mainly for COPD not asthma
In asthma, they are used in case of cholinergic-induced asthma.

Short Acting Muscarinic Antagonist: SAMA

Scientific name Trade Dosage forms Strengths Company

names

Ipratropium Aerovent respirator 0.25 mg/ ml Boehringer

bromide solution Ingelheim
‫تبخيرة‬

Ipravent Respiratory 0.25mg/ml Birzeit

solution

Atrovent Metered aerosol 20 mcg/ metered Boehringer

Inhalation dose Ingelheim

Long Acting Muscarinic Antagonist: LAMA

Scientific Trade names Dosage forms Strengths Company

name

Tiotropium Spiriva caps Inhalation Powder 18 mcg Boehringer Ingelheim

bromide in caps

Spiriva Respimat Inhalation solution

in metered dose 2.5 mcg
inhaler

Glycopyrronium Seebri Breezhaler Inhalation Powder 50 Novartis

in caps mcg/dose

Aclidinium Eklira Genuair Inhalation Powder 322 mcg AstraZeneca

bromide

LABA+LAMA

Scientific name Trade names Dosage forms Strengths Company

 Formoterol Duaklir Genuair Inhalation 12/340 AstraZeneca
+Aclidinium Powder mcg

Indacaterol+ Ultibro Breezhaler Inhalation 110/50 Novartis

Glycopyrronium Powder in mcg
Used mainly for capsule
COPD

Olodaterol + Spiolto Respimat Inhalation 2.5/2.5 Boehringer

Tiotropium Solution in mcg Ingelheim
metered dose

In terms of bronchodilation effect, cholinergic antagonist is less effective than B2 agonist

—-
Inhaled ipratropium used in patients who are unable to tolerate adrenergic agonists.
B2 agonist ‫في حال المريض غير قادر على تحمل االعراض الجانبية ل‬
Slow in onset , so it could be used as alternative to LABA not SABA

nearly free of side effects as inhaler( but they have many side effects as systematic drug)

4-Leukotriene antagonist
MOA:
inhibit of 5-lipooxygenase pathway of arachidonic acid metabolism
Decrease the inflammation

Note: 5-lipooxygenase is found in cells of myeloid organs such as: mast cells, basophils,
eosinophils and neutrophils.

2 types:
1-Leukotriene LTB4 (it is a potent chemoattractant for neutrophils and eosinophils)
2-Cysteinyl leukotrienes: LTC4, LTD4, LTE4
Constrict bronchiolar smooth muscle
Increase endothelial permeability(swelling)
Promot mucous secretion

Leukotriene modifiers

1-Zileuton
Selective and specific inhibitor of 5-lipoxygenase
Inhibit the formation of both LTB4 and cysteinyl leukotrienes

2-Zafirlukast and Montelukast

Selective and reversible inhibitor of cysteinyl leukotrienes
These two drugs are the first choice as alternative, then theophylline

Drugs available in the market:

Montelukast LeukoMont Chewable tab BeitJala

4mg
5mg

Tab : 10 mg

Lucast 5mg chewable tab Birzeit

10 mg tab

Singular 4mg oral granules (sachets) GSK

(Brand)
10 mg (tab)

4,5 mg chew tab.

MontiKast Chewable tab Pharmacare

:4mg, 5 mg

10 mg tab

Note: 2 advantages:
Dosing recommendations for children 1 year and older
Available in chewable tablets and granules formulations

All three drugs approved for the prophylaxis of asthma (long term control) (in persistent
asthma)
Not effective for immediate bronchodilation

Adverse reactions to leukotriene antagonists:

Elevation in serum hepatic enzymes

—> requires monitoring and discontinuation when enzymes exceed three to five times the upper
limit of normal
‫يجب عمل فحص للكبد قبل البدء باستخدام هذه األدوية وكذلك خالل استخدامها لمراقبة عمل الكبد‬
Inflammation of blood vessels (Eosinophils vasculitis) (rare)
Dyspepsia ‫سوء هضم‬

Headache
Both Zileuton and Zafirlukast are cytochrome P450 inhibitors. —> can increase warfarin level

———————
5.Cromolyn and Nedocromil
Cronase Cromolyn sodium Nasal spray Vitamed

"mast cell stabilizers "

MOA: Prevent mast cell degranulation that prevent release of histamine
Effective for the treatment of (asthmatic cough) because it suppresses the response to irritants
It has short duration of action and can be used for patients above 2 years

Indications:
Prophylactic anti-inflammatory agent
Used as an alternative for mild persistent asthma.
It is not a bronchodilator so it is not useful for acute asthma attack.

Common side effects include:

1.Bad taste in your mouth (mild bitter taste)
2.Irritation of the pharynx and larynx

Serious side effects are rare with cromolyn sodium:

1.Angioedema (swelling throughout the skin)
2.Throat swelling
3.Shortness of breath
4.Wheezing

Nedocromil Side Effects:

1.nausea and vomiting
2.cough and throat irritation
3.headache, dizziness
4.elevations of liver function tests (SGPT)

6. Methylxanthines
Theophylline / Aminophylline

Inhibit of phosphdiesterase ➡️ increase CAMP ➡️ relax of smooth muscle in

airway.(bronchodilation)

Aminophylline Aminophylline Amp: 25mg/ 1ml Teva Systamic iv

 Diprophylline Diphyline 150mg Birzeit child Suppositories
1-2 supp daily

Theophylline Theotard Caps: 100, 200, 300 mg CTS

Theotrim 100,200,300 mg tab Trima

Theophylline Teva
extended-release tab
300mg

Administration: orally, IV, rectally (rectally especially for children because it is difficult to give
them an orally drug at the attack)

Short half life

It has narrow therapeutic window (like digoxin, warfarin, TCA)

Theophylline is metabolized in the liver by CYP1A2 (like caffeine and propranolol)
—> Has many drug-drug interactions via alteration of hepatic enzyme

Drugs inhibitor for CYP1A2 are: (increase the level of theophylline)

Cimetidine (H2 blocker)

ciprofloxacin
erythromycin
Allopurinol (in a class of medications called xanthine oxidase inhibitors. It works by reducing the
production of uric acid in the body)

Drugs inducers for CYP1A2 are: Barbiturate phenobarbital / Rifampicin

Side Effects:
Fatal cardiac arrhythmia and seizures (so it is the last choice for asthma)

————-

7 Omalizumab
• Recombinant DNA-derived monoclonal antibody.
• Anti-IgE antibody, lead to decrease the binding of igE to igE receptor on the surface of
mast cells and basophils
• approved to treat of allergic asthma not well controlled by oral or inhaled CS.
. ‫ وما تحسن‬oral CS ‫ اذا المريض وصل اعلى جرعة‬last choice ‫• هاد الدواء يعتبر ال‬
total seum IgE ‫• الجرعة بتكون حسب الوزن و‬
 ‫شيقل‬6000 ‫هو من ادوية الصحة وسعره عالي بوصل‬ •
anaphylaxis ‫يجب مراقبة المريض خاصة عند اعطاء اول جرعة خوفا من حدوث ال‬ •
Drugs available in the market

Xolair Omalizumab 150mg/ dose Novartis For moderate to sever persistent asthma
( vial) 150-375 mg SC q 2-4 weeks

other monoclonal antibody approved by FDA for asthma:

Mepolizumab
Reslizumab
Benralizumab

They recognize and block interleukin-5

→ approved for the maintenance treatment for patients with uncontrolled, persistent asthma
with exacerbation phenotype.
Mepolizumab is approved for patients aged 12 years or older and can reduce the exacerbation
by approximately 50%.
Reslizumab for patients older than 18 years or older.
Bevacizumab for patients older than12 years
-------------------------------

• Safety in pregnancy:

The same protocol as non-pregnant but with more monitoring

Poor asthma control and acute exacerbation during pregnancy are riskier than taking asthma
medications.
1. Beta 2-adrenergic agonists:

Beta 2-adrenergic agonists can be safely used during pregnancy.

The short-acting salbutamol (albuterol), metaproterenol and terbutaline are first-

choice drugs in the treatment of pregnant women.
the preferred choice is salbutamol

They are effective in the treatment of premature labor (tocolytic effect), because
they inhibit uterine contractions in the second and third trimesters (systemic
administration not inhaler)

Formoterol is preferred over salmeterol for pregnant because animal studies

indicated some malformations with salmeterol

High dose beta 2 agonist may cause some reversible adverse effects on
newborns such as: tremor, tachycardia, hypoglycemia (because these drugs
rise the level of glucose in the mother), hypokalemia (should not be treated
because potassium is shifted into cells and after the effect of drug ends, the level
of potassium return to the normal)
2. Inhaled corticosteroids:
Inhaled corticosteroids are among the first drugs of choice for the treatment of
asthma in pregnant women, they are safe to use throughout pregnancy at low to
moderate doses, the lowest effective dose should be used.

Budesonide is the most commonly used and safe ICS during pregnancy.

High dose and long-term use of oral corticosteroids in pregnant:

1-intrauterine growth restriction →best avoided
2-cleft palate in mouse→no evidence of teratogenicity in human
3-adrenal suppression in fetus→ adrenal function should be monitored
4.hypertension in pregnant ‫اكتر اشي بخاف منه‬

Prednisone and prednisolone can be used as oral corticosteroids in there

is a need for it. (safe for fetus)

Note: prednisone is inactive form and the fetus liver cannot convert it to active
form
Prednisolone if enter the body of the fetus, it will be converted to prednisone
‫عكس جسم االم‬

Note: to stimulate surfactant in the fetus lung, prednisone and prednisolone

cannot be used. (Dexamethasone and Betamethasone can be used)
3. ipratropium:
Inhaled ipratropium bromide can be used during pregnancy. (safe)
It is water soluble, so its absorption is limited and does not pass to fetus.

4. Theophylline:
Low dose theophylline is an alternative when ICS alone cannot provide adequate
control of asthma.

Steady-state serum concentrations should be closely monitored, and maintained

at 8-12mcg/ml in pregnant asthmatics.

During pregnancy the plasma protein binding of theophylline is reduced, resulting

in an increase in free drug. Moreover, the elimination of theophylline is
decreased by about 25% in third trimester →monitoring

High doses should be avoided, especially near term.

Newborns, especially when preterm, should be monitored for adverse effects:

vomiting/irritability/bradycardia and tachycardia/cyanosis.
‫اعراض تظهر بسبب نقصان كمية الدواء في جسم الطفل بعد ان كان قد تعود عليه وهو في الرحم‬
(theophylline readily cross the placenta, and is metabolized to caffeine in the fetal
liver→CNS stimulation)
5. Cromolyn:
Sodium cromoglycate can be safely used in pregnant women for the prophylactic
treatment. (in asthma and allergic rhinitis)
6. antileukotrienes:

Montelukast, zafirlukast and zileuton.

The use of montelukast and zafirlukast are only recommended for patients who
had a favorable response to them before becoming pregnant. They are an
alternative to ICSs and not preferred as a treatment option in mild persistent
asthma during pregnancy.

Zileuton should be avoided for use in pregnancy because of the lack of relevant
research.

7.Omalizumab:
safe but it should be dosed according to body weight and pretreatment serum
total IgE levels.
it is injected SC once every 2 or 4 weeks
dose: 75 to 600 mg

another two anti-IL-5 monoclonal antibodies, mepolizumab and reslizumab,

there is no adequate studies on their safety during pregnancy. Due to the fact
that monoclonal antibodies can cross the placenta during the third trimester.
-------------------------------------------------------------------------------------------------------------------------------

COPD
Chronic obstructive pulmonary disease is a chronic, irreversible obstruction of airflow.

It includes:

—> emphysema – damage to the air sacs in the lungs

—> chronic bronchitis – long-term inflammation of the airways.

It is an expiratory disease: the patient find difficulty in taking out the breath, and that can be
noticed by the forced expiratory volume. ( FEV1)

FEV1: is the maximum amount of air that the subject can forcibly expel during the first-second
following maximal inhalation.

Smoking is the greatest risk factor, so it happened for adults, in contrast to asthma which can
happened in children also.
stopping smoking – if the patient has COPD and smoke, this is the most important thing to do to
prevent progressive decline in the lung function.

Another risk factor is age.

The main symptoms of COPD are:

increasing breathlessness, particularly when you're active

a persistent chesty cough with phlegm – some people may dismiss this as just a "smoker's
cough"
frequent chest infections
persistent wheezing

Without treatment, the symptoms usually get progressively worse. There may also be periods
when they get suddenly worse, known as a flare-up or exacerbation.

Treatment:
Inhaled Bronchodilator

The main choice is anticholinergic such as Ipratropium.

Combination of anticholinergic and B2-agonist have greater effect than one of them alone.

Ex: albuterol + ipratropium.

Stages of COPD with treatment:

Stage 1 -- Mild -- FEV-1 ≥80%:

Patient may have no symptoms. He might be short of breath when walking fast on level ground
or climbing a slight hill.

Short-acting anticholinergic when necessary such as ipratropium. TID and IOS

OR
Short acting Beta2 agonist when necessary such as salbutamol.
——
Stage 2 -- Moderate -- FEV-1 50-79%:
If the patient is walking on level ground, he might have to stop every few minutes to catch his
breath.

Long-acting anticholinergic such as: tiotropium:

OR
Long-acting B2-agonist such as: salmeterol
BID

——-
Stage 3 -- Severe -- FEV-1 30-49%:
Patient may be too short of breath to leave the house. He might get breathless doing something
as simple as dressing and undressing.

Inhaled corticosteroids+long-acting B2 agonist

OR
Long-acting anticholinergic
——
Stage 4 -- Very Severe -- FEV-1 ≤30%:
Patients might have lung or heart failure. This can make it hard to catch his breath even when
he is resting.
This is called end-stage COPD.

Inhaled corticosteroids+long-acting B2 agonist

And/OR
Long-acting anticholinergic

Roflumilast Daliresp Tab: 500mcg Rafa

It is a phosphodiesterase 4 inhibitor,used in severe COPD, to reduce the number of episodes or
worsening of symptoms.

Note: Guide lines

For asthma: ICS →LABA → LAMA

For COPD: LAMA →LABA →ICS

------------------------------------------------------------------------------
Allergic Rhinitis
Hay fever, is an allergy-related inflammation of the nasal passages, throat and eye membrane
(conjunctiva), caused by sensitivity to airborne pollens and molds.

Symptoms:
Nasal congestion / watery rhinorrhea/ sneezing/ itchy nose and eye

Classification:
1.seasonal: caused by pollen and molds
2.pereninal: symptoms throughout the year without regard changes in the season (molds, pets,
cockroaches)
‫اذا كان المريض يعاني من حساسية طول العام فالمصدر لها هو من داخل البيت‬
3.combination of both
________
How does the response to the allergen occur in the body?
IgE found at the surface of the mast cell from the exposure to the previous allergen.
The new particles interact with them.

Then, the mediators released from the mast cells:

Such as: histamine/ leukotrienes/ chemotactic factor.

That promote:
Bronchial spasm
Mucosal thickening (due to edema and cellular infiltration)

———
Treatment:

The best treatment is to avoid allergen along with pharmacological treatment.

The preferred therapies for allergic rhinitis are:
Antihistamine and/or intranasal corticosteroids.

The most effective medications are intranasal corticosteroids. WHY?

Because they improve sneezing, itching, rhinorrhea, and nasal congestion.

Note: be careful that corticosteroids used for asthma as inhalers but for allergic rhinitis
as intranasal.
For quick removal of symptoms—> antihistamine
For long-term control—> intranasal corticosteroids
For congestion—> decongestant
——————

Antihistamines (H1-receptor blockers)

• They are more effective for prevention of symptoms: sneezing, watery rhinorrhea, itchy
eyes/nose (these symptoms are mediated by histamine)

Ophthalmic and nasal antihistamine delivery devices are available for more targeted tissue
delivery.

• First-generation antihistamines, such as diphenhydramine, chlorpheniramine,

dimetindene, hydroxyzine, promethazine

Oral antihistamine

Benadryl Diphenhydramine Tab: 25mg Johnson

(The brand)

Dexamin Dexchlorpheniramine Tab: 1mg Jerusalem

Syrup: 0.5mg/5ml

Allergon Chlorpheniramine Tab:2mg Beit Jala

Syrup:2mg/5ml
Ahiston Chlorpheniramine Tab: 2mg Teva

Dimestil Dimetindene Oral drops:1mg/1ml Birzeit

Gel:1mg

Fenstil Dimetindene Oral drops: 1mg/1ml Novartis

(Brand) Gel:1mg
 Prothiazine Promethazine Tab:25mg CTS
Syrup:5mg/5ml
Amp: 25mg/2ml
Histanyl Promethazine Amp: 25mg,50mg Birzeit
IM

They are usually not preferred because of side effects:

sedation,
performance impairment,
anticholinergic effects (dry eyes/mouth, difficulty urinating and/or constipation.
(use caution driving, operating machinery, or performing other hazardous activities.)

Note: diphenhydramine is the most sedative among first generation antihistamine, for that is used
for sedation (ex: Hudu)

• The second-generation antihistamines:

Fexofenadine,
Loratadine,
Cetirizine
Ketotifen
Bilastine
Minimal anticholinergic and sedation effect. (can be used during the day)

Better tolerated.

loratadine Allergy tab: 10mg Teva

Syrup: 5mg/5ml

for allergic rhinitis

—>
Tab 10mg once daily
Or 5 mg twice daily
Not to exceed 10mg per day

Lorastine tab: 10mg Bayer

Syrup: 5mg/5ml

Claristine tab: 10mg BirZeit

Loratadine Tab: 10mg Perrigo

 Lorax Tab: 10mg Beit Jala

Loradin Tab: 10mg Pharmacare

Loratadine Clarinase Tab: 5+120mg Bayer

Pseudoephedrine

Desloratadine Aerius Tab: 5mg MSD

Syrup: 0.5 mg/ 1ml

Lorias Tab: 5mg Jerusalem

Syrup: 0.5mg/ml
Delorax Tab: 5mg Beit Jala
Syrup: 0.5mg/1ml

Rinazal Syrup:2.5mg/5ml Birzeit

Fexofenadine Telfast Tab: 120 , 180 mg Sanofi

FexoEz Tab: 120 , 180 mg Pharmacare

Fexodin Tab: 120 , 180 mg Jerusalem

Tab 120 mg for allergic rhinitis symptoms (sneezing, runny nose…) , tab 180 most commonly
for skin reactions (urticaria, rashes, swelling)

cetirzine Zyrtec (brand) Tab: 10mg UCB pharma

Histazine Tab: 10mg Trima

Syrup: 5mg/5ml

Setahist Tab: 10mg BeitJala

Syrup: 5mg/5ml

Zyllergy cap: 10 mg Dexcal

Cetrisam Tab : 5, 10mg Sama

Syrup: 5mg/5ml
 ketotifen Zaditor Alcon
(brand)

ketotifen Ketofen eye drops: 0.25mg/ml Beit Jala

1 drop twice daily

Tab: 1mg
Syrup: 1mg / 5ml

ketotifen Profiten Tab: 1mg Pharma-Clal

Syrup: 1mg/ 5ml

Bilaxten Bilastine Tab: 20mg Rafa ‫يفضل اخذه قبل‬

‫االكل بساعة او بعد‬
‫االكل بساعتين الن‬
‫الطعام يقلل من‬
‫امتصاص الدواء‬

Cinnarizine (antihistamine)

Cinnarizine Cinazine Tab: 25, 75mg Pharmacare

Stunarone Tab: 25mg Janssen

——-

Betahistine (histamine analogue)

Betahistine Betastin Tab: 16,24mg Pharmacare

Viraserc Tab: 16mg Birzeit

Betahistine Tab: 16mg Teva

Agiserc Tab: 16mg Perrigo

‫يستخدم أيضا لعالج الدوار بسبب مشاكل باالذن الوسطى او أسباب أخرى‬

--------------
If the symptoms only in the eyes without other symptoms, ocular antihistamine is recommended
2 available OTC: pheniramine maleate and antazoline phosphate only in combination with
naphazoline (to decrease the congestion in the eyes)
—> should be avoided in glaucoma
 Ocular antihistamine
Collihist Pheniramine (antihistamine) eye drops Birzeit
Naphazoline (decongestant)

Epihist Epinastine eye drops Beit Jala

Relestat Epinastine eye drops Allercan

ketofen Ketotifen eye drops Beit Jala

Oral antihistamine with decongestant

‫االستخدام األكثر لهذه االدوية في حاالت نزالت البرد والسعال‬

Nussidex chlorpheniramine 1mg Tab Teva

Pseudoephedrine 25 mg

Decongex SR chlorpheniramine 8mg cap Birzeit twice

Pseudoephedrine 120mg daily

Decongex Cold chlorpheniramine 1mg Syrup Birzeit

Pseudoephedrine 15mg
Paracetamol 120mg

Gripmin SR chlorpheniramine 8mg Tab Jerusalem

Pseudoephedrine 120mg

Histadex Dexchloropheniramine Syrup: Trima

Pseudoephedrine 1mg/5ml

Pulmadrin Triprolidine 1.25 my/5ml syrup Birzeit

Pseudoephedrine Banana
30mg/5ml flavour

Tussana Mild Chlorpheniramine Syrup BietJala

Ephedrine
Ammonium chloride s

Broncholate Diphenhydramine Syrup Meditic

+pseudoephedrine
Bronch-kid

Broncholate plus:
+paracetamol

Bronch-d:
+ammonium chloride
Broncholate forte:
With codeine

Nasal spray (antihistamine +decongestant)

Rhinofex Dimetindene (antihistamine) Microdoser Birzeit ‫ بخة في‬2-1
nasal spray ‫كل فتحة انف‬
0.25mg ‫ مرات‬3
‫باليوم‬
Phenylephrine(decongestant)
‫للكبار‬
2.5mg ‫واألطفال فوق‬
‫ سنين‬6 ‫عمر‬

‫مزيل‬
‫لالحتقان‬
‫والتحسس‬

Vibrocil Dimetindene 0.25mg Nasal spray Novartis

Phenylephrine 0.25mg

• Combinations of antihistamines with decongestants are effective when congestion is a

feature of rhinitis.

Antihistamines in pregnancy:
First generation: no risk detected (safe) ex: chlorpheniramine and diphenhydramine
Except: cyproheptadine: has toxic to fetal pancreatic cells
Note: cyproheptadine used also to stimulate the appetite (because of anti-serotonin effect)
Note: Diphenhydramine and dimenhydrinate: safe but when used parenterally, in high dose, in
late pregnancy →stimulate uterine contraction leading to fetal hypoxia (‫)نقص االكسجين عن الطفل‬

‫يفضل استخدام الجيل األول على استخدام الجيل الثاني بسبب توفر عدد اكبر من الدراسات عليه تثبت انه امن‬
If the pregnant want a least sedative one →the choice is Meclizine (the least sedative among first
generation)

Second choices are: Loratadine then cetirizine

(fexofenadine ‫)الدراسات عليه اقل‬
Note: if first generation used perinatal (‫ →)حول فترة الوالدة‬restlessness may happened to the baby
(‫ )ال هو صاحي وال هو نايم‬, respiratory depression.

Ketotifen should be avoided during pregnancy→no data on safety

————-
Alpha-adrenergic agonist (decongestant)

MOA: constrict dilated arterioles in the nasal mucosa

Congestion occurs in the late stages of the allergy.
Optimal combination with antihistamine
Decongestant is not used for long-term treatment.
Short acting: phenylephrine, pseudoephedrine

Nasofrin phenylephrine nasal spray : 5mg/1ml Bit Jala

Sinufed Pseudoephedrine Tab:60mg Teva

(Brand) Syrup: 30mg/5ml

Long-acting: oxymetazoline

Nosacare No Oxymetazoline Nasal Spray Pharmacare ‫مزيل سريع وفعال الحتقان االنف‬
drip 0.5 mg/1ml With metered
dose pump ‫ال تستخدم بعد شهر من الفتح‬
‫ بخة في كل فتحة‬٣-٢ : ‫ سنوات‬٦ ‫لعمر فوق‬
‫انف مرتين باليوم‬

Nosacare Oxymetazoline Nasal spray Pharmacare ‫مزيل سريع وفعال الحتقان االنف مع ترطيب‬
EM )‫( لالنف الجاف‬

Nasocare Oxymetazoline Nasal spray Pharmacare ‫مزيل الحتقان االنف الشديد‬

Mentho Menthol

Nosacare Oxymetazoline Nasal spray Pharmacare ٥-٢ ‫مزيل الحتقان االنف عند االطفال من عمر‬
Child 0.025% :‫سنوات‬

‫ بخة في كل فتحة انف مرتين باليوم‬٣-٢

xylometazoline

Nirvin adult xylometazoline 0.1% Nasal Birzeit More than 12yr

spary :‫البخاخ‬
‫ مرات يوميا‬٤ ‫بخة واحدة في كل فتحة انف‬
 Nasal
drops :‫القطرات‬
‫ مرات يوميا‬٤ ‫ قطرات في كل فتحة انف‬٣-٢

Nirvin Xylometazoline Nasal 2-12 years old

children 0.05% spary :‫البخاخ‬
Nasal ‫ يوميا‬٢ ‫بخة واحدة في كل فتحة مرة الى‬
drops
:‫القطرات‬
‫ يوميا‬٢ ‫ قطرة في كل فتحة مرة او‬٢-١

Nirvin xylometazoline 0.05% Nasal for adult

complete Ipratropium Bromide spary ‫لالحتقان وسيالن االنف المصاحب لنزلة البرد‬
0.06%

Otrivin xylometazolin Nasal spray Novartis

Adult: 0.1%
Children: 0.05%

Otrivin menthol Xylometazoline Nasal spray Novaretis

Otrivin Complete Xylometazoline 0.5mg/ml Nasal spray Novartis

Ipratropium ‫لالحتقان وسيالن االنف‬
0.6mg/ml

Linex Xylometazoline Nasal spray: Teva

Adult:0.1%
Children:0.05%

Marimer Hypertonic solution ‫ لالحتقان‬Gilbert

Marimer For sinusitis and rhinitis

Azolin tetrahydrozoline Eye Dr.Fischer vasoconstrictior works by narrowing

drops swollen blood vessels in the eyes

Allervin Antazoline Eye Jerusalem Anti-allergic decongestants

Naphazoline drops

When administered as an aerosol, these drugs have a rapid onset of action and show few
systemic effects.
But oral decongestant can be given to prevent rebound congestion.
Note: if there is no congestion, antihistamine is sufficient, but if there is congestion,
combination of antihistamine and decongestant is recommended.

Note: recommended agents based on the symptoms: if the patient has just watery eyes,
so ophthalmic eye drops are recommended.

Intranasal decongestant Should be used no longer than 3 days due to the risk of rebound nasal
congestion (rhinitis medicamentosa).

→ • For this reason, the α-adrenergic agents have no place in the long-term treatment of allergic
rhinitis.

• Oral α-adrenergic agonist formulations result in a longer duration of action but also increased
systemic effects.
• Regular use of oral α-adrenergic agonists (phenylephrine and pseudoephedrine) alone or in
combination with antihistamines is not recommended
--------

corticosteroids that could be used intranasally for allergic rhinitis are:

Beclomethasone, Budesonide, Fluticasone, Mometasone, and Triamcinolone.

Intranasal corticosteroids available in the market are:

Fluticasone propionate Flutisone Nasal spray 50mcg Pharmacare

Frinase Nasal spray 50mcg Jepharm

Flixonase Aqueous Nasal spray GSK

50 mcg

Metered dose

Allegro Nasal spray Trima

Fluticasone Furoate Avamys Nasal spray GSK

27.5 mcg

Fluticasone + Zalinase plus Nasal spray Pharmacare

Azelastine

Mometasone Nosatrex Nasal spray Birzeit

Furoate 5mcg/actuation

Nasonex Nasal spray MSD

Fluticasone propionate nasal spray is indicated for adults and pediatric patients aged 4 years
and older.

For patients with chronic rhinitis, improvement may not be seen until 1 to 2 weeks after starting
therapy

Local side effects include:

nasal irritation, nose bleeding, sore throat, and,
rarely, candidiasis.

NOTE: you should instruct the patient not to inhale deeply while administering these drugs
because the target tissue is the nose, not the lungs or the throat.
And that’s to avoid systemic absorption and side effects.

You should advise to shake fluticasone propionate nasal spray gently before each use.

Dose for adults:

The recommended starting dosage in adults is 2 sprays (50 mcg of fluticasone propionate each)
in each nostril once daily.
‫بالعادة يوصف بخة باليوم بكل فتحة انف واذا ما استجاب بصير بختين بكل فتحة انف مرة باليوم‬
After the first few days, patients may be able to reduce their dose to 1 spray in each nostril once
daily for maintenance therapy.
Maximum total daily doses should not exceed 2 sprays in each nostril twice daily (total dose,
200 mcg/day). There is no evidence that exceeding the recommended dose is more effective.

The recommended starting dosage in adolescents and children, aged 4 years and older is 1
spray in each nostril once daily (total daily dose, 100 mcg). Patients not adequately responding
to 1 spray in each nostril may use 2 sprays in each nostril once daily (total daily dose, 200 mcg).
Once adequate control is achieved, the dosage should be decreased to 1 spray in each nostril
once daily.

Pregnancy: category C

-----

Intranasal Cromolyn
• Useful in allergic rhinitis, particularly when administered before contact with an allergen.
• Dosing should begin at least 1 to 2 weeks prior to allergen exposure.
•for patients 2 years and older.
•preventive for symptoms (start one week before allergen contact)
‫خد قبل بداية التعرض بأسبوع‬c‫ ي‬،‫للوقاية وليست عالج‬
)‫ كوقاية‬loratadine ‫(يجوز ايضا استخدام‬
•for treatment of all symptoms (except nasal congestion)
•short duration: dose 3-4 times daily (one spray in each nostril)
Note: cromolyn Sodium: preferred initial drug of choice during pregnancy for rhinorrhea and
sneezing.
—
Exclusive to self-treatment of allergic rhinitis (as OTC)
‫في حال وجود التهاب باألذن‬
‫في حال وجود اعراض التهاب الجهاز التنفسي السفلي‬
‫تاريخ مرضي اللتهاب غير تحسسي‬
———
Note: a person with runny nose and fever should be excluded from OTC treatment unless
seen the physician

----

Summary for OTC treatment of allergic rhinitis:

•if patient has sneezing and rhinorrhea, antihistamine is recommended
—> 1st generation recommended at night because of drowsiness
—>2nd generation cause less or no drowsiness

•if the patient has congestion and rhinorrhea, a combination of antihistamine and decongestant
is recommended.
•decongestant is recommended to be taken orally not topically to avoid rebound congestion.
(symptoms of allergic rhinitis may last more than 7 days but topical decongestant should not be
used more than 3 to 4 days)
•In pregnancy, the safest drug for allergic rhinitis is cromolyn sodium.
•antihistamine as OTC given for older than 12 years old.

Cough
It is only a symptom, not a disease
The common cold is the most frequent cause of acute cough
Cough occurs due to:
-irritation of a sensory nerve and inflammation of cough receptor in the upper airway
‫اذا كان المريض يعاني من التهاب في الرئة وسعال فيجب عالج التهاب الرئة اوال‬
Productive cough: cough with sputum
—>should not be suppressed
:‫اسباب السعال المنتج للبلغم‬
‫التدخين ويكون لونه اصفر وهذا وضع طبيعي للمدخنين وعالجه ايقاف التدخين‬
‫رجوع حمض المعدة الى المريء ويجب عالج هذه الحالة النها مسببة للسعال‬
‫عدوى بكتيرية او فيروسية ويكون لون البلغم اخضر او اصفر وفي هذه الحالة يجب توجيه المريض للطبيب ( اذا كان لو البلغم اصفر‬
)‫ولم يكن مدخن يكون االحتمال االكبر عدوى‬
COPD or Chronic bronchitis
‫وفي هذه الحالة يجب توجيه المريض للطبيب‬
---------
Non-pharmacologic treatment for cough:
Fluids: for thinning the secretion and soothing the irritated throat (honey in hot water, or lemon
juice)
‫شرب سوائل دافية ال تحتوي على الكافيين الن الكافيين يسبب جفاف في الحلق‬
‫وننصح المريض بشرب الماء بعد شرب الشاي او القهوة لمنع جفاف الحلق‬
For Dry cough:

Antitussives are used:

Dextromethorphan
Codeine (not OTC)
Diphenhydramine (antihistamine)--> in a dose less than the dose that causes antihistamine
effect
Camphor and menthol
----
Dextromethorphan:
Non-narcotic
Not analgesic
Not addictive
Works centrally in the medulla to increase the cough threshold

Diphenhydramine:
MOA: like dextromethorphan
Is an antitussive and antihistamine, dose for antitussive effect is half of dose as an
antihistamine.
‫يؤخذ ليال ليساعد المريض على النوم‬
-———
Camphor and menthol
The only FDA approved as topical antitussive.
.‫ يمكن تكرار ذلك ثالث مرات يوميا‬،‫يوضع كطبقة سميكة على الحلق والصدر ويتم تغطية المنطقة بغطاء دافئ وجاف‬
‫عند االطفال تستخدم كمية بسيطة‬
)cold sensory receptors( ‫تعمل من خالل تحفيز االعصاب الحسية‬
It can be used as a steam inhalant:
‫ وتوضع في وعاء فيه ماء ساخن ويتم استنشاق البخار‬،‫ مل من الماء‬1000 ‫ مل منه في‬15
‫ سنين‬6 ‫هذه الطريقة ال يفضل استخدامها لألطفال اقل من‬

Mentholatum Balm ‫لتلطيف اعراض البرد والزكام وحمى القش‬

(Ointment) ‫تلطيف آالم العضالت والتيبس‬
‫لطفح القرصات ولدغات ولسعات الحشرات والحكة‬

VapoRub (menthol) (ointment) ‫يحسن التنفس وتخفيف القحة‬

Menthogel (cream) ‫يساعد في تحسين التنفس في حاالت الرشح والبرد‬

‫تخفيف شد العضالت وعند الرضوض ولسع الحشرات‬

Menthol (5-10 mg) effective as antitussive in oral lozenges or compressed tablets (coolness and
local anesthetic effect)
Ex: Strepsils (menthol and eucalyptus)

-——
For reproductive cough:
‫اهم اشي نحكي للمريض يشرب ماء كتير لحتى يحلل البلغم‬
Expectorant: increase the output of thin respiratory tract fluid by helping to liquefy the mucus

Work by irritating the gastric mucosa and stimulating secretions of the respiratory tract.

Guaifenesin: the only OTC drug approved as expectorant.

Category C
‫يجب شرب كمية كبيرة من الماء مع الدوا‬
‫ ايام واذا لم يشعر المريض بتحسن يجب مراجعة الطبيب‬٧ ‫ال يستخدم اكثر من‬

Dose of Guaifenesin:
Adult:
Syrup: 200-400mg Q 4 hrs
Extended-release tablet: 600-1200 my Q 12 hr

Children (6-12 yr): 100-200 mg q 4 hr

Children(2-5yr): 50-100mg q 4 hr

Pectosin Guaifenesin Syrup: BeitJala for adult: 10-20ml every

100mg/5ml 4 hours
sugar free ‫يمكن استخدامه‬
‫لمريض السكري‬

Resyl Guaifenesin Syrup: 100mg/5ml GSK Expectorant and

relieves cough

Mukigo Guaifenesin syrup: Sama ‫في الحاالت المتقدمة من القحة‬

100mg /5ml ‫القوية‬

Tussin DM Dextromethorphan syrup: Perrigo ‫في الحاالت المتقدمة من القحة‬

Guaifenesin 10mg+100mg/5ml ‫القوية‬

Dexamol paracetamol caplet Decxel For cold, cough and

Cold Guaifenesin nasal congestion
Dextromethorphan

Histafed triprolidine pseudoephedrine syrup Trima

expectorant guafenasine tab

Alcinal chlorpheniramine 1mg Syrup Rekah ‫للقحة التحسسية‬

Dextromethorphan 7.88mg
Guaifenesin 105mg

Oxacatin Oxomemazine(antohistamin) Syrup Taro Antitussive and

1.65mg expectorant
Potassium guaicol sulphonate
33.3mg
 Tussibal Triprolidine 1.25 my/5ml syrup Jerusalem ‫للقحة الجافة‬
Pseudoephedrine 30mg/5ml
Dextromethorphan 10mg

Tussibal expectorant Triprolidine 1.25 my/5ml syrup Jerusalem ‫للقحة مع بلغم‬

Pseudoephedrine 30mg/5ml
Guaifenesin 100mg

Prothiazine Promethazine Syrup CTS

expectorant Guaifenesin

Mucolytic agents: breaks down the mucus that present in the lung

acetylcysteine (and its metabolic byproduct cysteine) exerts its mucolytic action through its free
sulfhydryl group, which reduces the disulfide bonds in the mucus matrix and lowers mucus
viscosity.

Bromhexine
The active metabolite for it is Ambroxol

Carbocisteine

For pregnant women: mucolytic is safe

Also, dextromethorphan is safe
——-
Off-Label use:
N-acetyl-cysteine (NAC), a derivative of amino acid L-cysteine, is currently used mainly as an
antioxidant. NAC also contributes to glutathione (GSH) synthesis and may help restore the
depleted pool of GSH often caused by oxidative stress and inflammation.
(Increased pathological ROS generation leads to sperm dysfunction (lipid peroxidation),
decreased semen quality and sperm DNA damage)

NAC oral supplementation may improve sperm parameters and motility and
oxidative/antioxidant status in infertile males.

Bromhexine Biosolvon (Brand) Oral liquid: 8mg/5ml Boehringer Ingelheim

Tablet: 8mg

Solvex
 Mucocare Tab: 8mg Pharmacare

Elixir: 4mg/5ml

Movex Tab: 8mg Vitamed

Ambroxol Mucosolvan Syrup:30mg/5ml Boehringer Ingelheim

(Brand) cap: 75mg

Muzil syrup: 30mg/5ml Beit jala Sugar free

Ambrocare syrup: 15,30mg/5ml Pharmacare sugar free

Carbocisteine Mucodyne (Brand) Sanofi

Mucolit cap: 375mg CTS

syrup: 250mg/4ml

oral drops: 75mg/ml

Muco-treat Syrup:250mg/5ml Tree of life

Mical Tab: 375 Meditec

N-acetylcysteine Rheunac Effervescent Tree of life ‫ قر صان في‬:‫االستخدام‬

(NAC) tablet: 200mg ‫كأس ماء مرة صباحا‬
‫ومرة مساء‬
‫ أقراص‬4 ‫(المجموع‬
)‫يوميا‬

‫او قرص فوار في كأس‬

‫ مرات يوميا‬3 ‫ماء‬

Siran Effervescent Megapharm

tablet: 200mg

Reolin Effervescent Pharmalogic

tablet: 200mg

Restoux Nac Effervescent

tablet: 200mg
 Bio-solve Cap: 600mg

NAC, is better to be taken on an empty stomach because the absorption of amino acids can be
affected by the food and other amino acids
—————

Triprolidine 1.25 my/5ml Pulmadrin syrup Birzeit ‫للقحة الجافة‬

Pseudoephedrine 30mg/5ml Banana
flavor

Histafed Syrup Trima

Triprolidine 1.25 my/5ml Pulmadrin DM syrup Birzeit ‫للقحة الجافة‬

Pseudoephedrine 30mg/5ml sugar ‫لمرضى‬
Dextromethorphan 10mg free ‫السكري‬

Tussibal Honey Syrup Jepharm

Triprolidine 1.25 my/5ml Pulmadrin expectorant Syrup Birzeit ‫للقحة مع بلغم‬
Pseudoephedrine 30mg/5ml
Guaifenesin 100mg Tussibal expectorant Syrup Jepharm

Histafid expectorant Syrup Trima

Codeine (control) Pulmadrin compound Syrup Birzeit

Pseudoephedrine Tussibal CO Syrup Jepharm

Triprolidine

Oxacatin Oxomemazine (antihistamine for Trima

treatment of cough)
Guaiacolsulphonate(expectorant)

Tussophedrine Dextromethorphan Syrup Trima

Ephedrine

Guaicosulfate

safety and efficacy of pseudoephedrine is not established for less than 2years old

Symphocal Oxolamine citrate Syrup Teva

 (cough suppressant)

-------------------------

Herbal cough drugs:

Apipol white marshmallow Apipharma sooth cough and reduce throat irritation
root + honey
For dry cough

1-3 years: 2.5ml 3 times after a meal

3-12years: 5ml 3 times daily after meal

Above 12: 5ml 3-5 times after a meal

Not used for diabetic patient

Prospan Dry Ivy leaves cough syrup

extract chronic inflammatory bronchial conditions
‫مستخلص أوراق اللبالب‬ and productive coughs due to its actions
‫الجافة‬ as an expectorant.

Can be used for diabetic patients

(sugar-free)

2-6: 2.5ml 2 times daily

6-12: 5ml 2 times daily

adult: 5ml 3 times daily

Cofspan Dry ivy leaves Jerusalem

extract

Pikta thyme syrup ‫ مرات باليوم‬٣ ‫ معلقة صغيرة‬:‫للصغار‬

Pikta forte ‫ مرات باليوم‬٣ ‫ معلقة كبيرة‬: ‫للكبار‬

Restoux Adult syrup: Herbal ‫لمعالجة السعال وتهيجات الحلق والفم‬

syrup with zinc

Baby syrup: 3-36

months

Throat spray
Lichensed ‫مستخلصات نباتية‬ ‫مرطب للحلق ويساعد في تخفيف السعال‬
Syrup : Adult / Baby

Thymoli ‫مستخلص الزعتر‬ Floris

syrup

-----------------------------------------------------------
For pregnant women:
For reproductive cough
Hydration
Mentholatum nebulization
If not effective → NAC, Bromhexine and Ambroxol (safe for pregnant)
If not effective → Guaifenesin (category C)

For dry cough

Dextromethorphan and codeine can be safely used
Not high dose , Not for longer period , Not near delivery → because of respiratory depression
---------------------------------------------------------------------------------------------------------------------

Common Cold
Viral infection (rhinoviruses) in the upper respiratory system

Symptoms:
Cough/sore throat/runny nose/sneezing/headache/fever
‫ عدا سيالن االنف احتمال حدوثه اقل في االنفلونزا‬،‫هذه االعراض تشبه اعراض االنفلونزا لكن تكون اكثر حدة فيها‬
-Recovery: in 7-10 days

Treatment of symptoms:
1-Antihistamin: to relief runny nose
Chlorpheniramine, diphenhydramine
They have sedative effect→ ‫لهيك همي اكتر فعالية من الجيل الثاني في العالج‬
They have anticholinergic effect→ ‫ عدم وضوح الرؤية وجفاف الفم‬:‫اعراض جانبية‬

2-Analgesic:
Also have antipyretic effect:
Paracetamol, Aspirin (for 18years or more), Ibuprofen, Naproxen sodium

3-Decongestant:
Ephedrine, pseudoephedrine, phenylephrine

4-cough suppressant:
Dextromethorphan or/and Guaifenesin
‫ مكونات لعدم إخفاء االعراض في حال وجود عدوى بخاصة‬3 ‫في العالج ال يجوز استخدام اكثر من دوا يحتوي على اكثر من‬
‫الحمى‬
Decongex Chlorpheniramine Cap Bireit BID
Pseudoephedrine

Decongex chlorpheniramine 1mg Syrup Birzeit

Cold Pseudoephedrine 15mg
Paracetamol 120mg
Phenylpropanolamine

Fluaminic chlorpheniramine 1mg syrup pharmacare

Pseudoephedrine 15mg
Paracetamol 160mg
Dextromethorphan 7.5mg

Flu chlorpheniramine 2mg Tab Jerusalem

Phenylephrine 10mg
Paracetamol 350mg
Dextromethorphan 5mg
Caffeine 30mg

Flu syrup pyrilamine 120 mg Syrup jerusalem

Phenylephrine 2mg
Paracetamol 120mg

Paraflu chlorpheniramine2.5mg Tab Biet Jala 3-4 tab daily

Phenylephrine 10mg ‫للرشح واحتقان الجيوب‬
Paracetamol 300mg ‫االنفية‬
Ascorbic acid 100mg ‫األنفلونزا‬
Caffeine 30mg ‫والرشح التحسسي والصداع‬

Paraflu chlorpheniramine Maleate syrup Biet Jala for common cold

1mg 6-12yr: 5ml three
Phenylephrine 2mg times daily
2-6yr: 2.5ml three
times daily

Tussana chlorpheniramine 1mg Syrup Beit Jala for children ‫بطعم‬

mild Ephedrine 1.83 mg ‫الكرز‬
Ammonium chloride 50mg

Teva-cold chlorpheniramine 2mg tab Teva

(coldex) Phenylephrine 10mg
Paracetamol 300mg
Caffeine 30mg

Dexamol paracetamol caplet Decxel For cold, cough and

Cold Guaifenesin nasal congestion
Dextromethorphan
 As long as you are breathing…

There is hope…

There is something beautiful waiting to happen for you…♥

 Topic 5: Central Nervous System
Anxiety
Anxiety disorders includes:
1-Generalized anxiety disorder(GAD) ‫الشخص دائما متوتروقلقان بدون وجود سبب معين او محفز‬
2-Panic disorder‫نوبات ذعر لسبب معين‬
3-Phobias ‫يشكل القسم األكبر وبكون الشخص بخاف من شي معين‬
4-Obsessive- compulsive disorder (OCD) ‫الوسواس القهري‬
5-Post-traumatic disorder ‫ارق وخوف بعد حدوث تجربة او حادثة مع الشخص‬

Anxiolytic (sedative drugs)→calming effect

Hypnotic→produce drowsiness and sleeping

Benzodiazepines:
MOA: potentiate GABA effect (inhibitory)
→Short acting: Midazolam/ Triazolam / Oxazepam
Midazolam Midazolam Amp:5mg/1ml
Midolam Amp:5mg/1ml Rafa
5mg/5ml
15mg/3ml
50mg/10ml

Triazolam Halcion (brand) Tab: 0.125,0.25mg Pfizer

Oxazepam Vaben Tab:10mg Rafa

→intermediate acting: Alprazolam / Clonazepam / Lorazepam

 Alprazolam Xanagis Tab: 0.25, 0.5, 1mg Perrigo
Prazolex Tab: 0.25, 0.5, 1mg Birzeit
Xanax XR Tab: 0.5, 1mg Pfizer
Alpralid Tab: 0.25, 0.5, 1mg CTS

Clonazepam Clonex Tab: 0.5, 2 mg Teva

(controlled)
Rivotril Tab:0.5, 2mg Roche
Oral drops

Clobazam Frisium (brand) Cap:10mg Sanofi

Lorazepam Lorivan Tab: Dexcel

(controlled) Lorocare Tab: 1, 2.5mg Pharmacare

→long acting: Chlordiazepoxide / Diazepam / Flurazepam

Chlordiazepoxide Modex Tab Birzeit To treat stomach spasm, cramps
+ Clidinium and anxiety related to gastric
disorders

Diazepam Assival Amp:10mg Teva

Tab:10mg
Serepam Amp:10mg Birzeit
Tab:10mg

Some information about benzodiazepine:

Antidote: Flumazenil (only IV).20
Not cytochrome inducer
Low dependency ‫يعني احتمالية انو الشخص يتعود عليه قليلة‬
‫واحتمالية اإلدمان عليه قليلة اال اذا الشخص عنده قابلية او تجربة مسبقة لالدمان على ادوية مشابهة‬
Anxiolytic effect and with increasing the dose cause hypnotic effect.
Suppress respiration at high dose
Have anticonvulsant effect
Uses: anxiety disorders, sleep disorder, seizures and muscle spasm, before surgical
procedure and others
Withdrawal symptoms occur mostly with short acting BDZ.
SE of benzodiazepine: Ataxia
They may cause anterograde amnesia ( ‫ )فقدان الذاكرة باالشياء اللي صارت بعد اخد الدوا‬and this
action can be used in surgery.

Barbiturates:
MOA: potentiate the effect of GABA
Can induce anesthesia by blocking Na channel
Ex: Thiopental, Phenobarbital
Phenobarbital Phenobarbitone Tab: 15, 100mg Rekah
Phenotab Tab: 15, 100mg Birzeit

Effect depends on the dose:

Calming → sleeping→anesthesia→coma
(so it is more dangerous than benzodiazepine)
Overdosage cause respiratory depression and death
They are cytochrome inducer.
Cause sever tolerance and dependance
Abrupt withdrawal can result in death
----
Other anxiolytic:
Antidepressant (first line agents):
SSRI → ex: Escitalopram
SNRI → ex: Venlafaxine
They need 4 to 6 weeks to give the effect, so during this interval BDZ is given with
antidepressant then the dose can be tapered.

Buspirone (serotonin partial agonist)

Buspirone Sorbon Tab:10mg Unipharm

Anxiolytic effect appears after a week

-----
Other hypnotic:
1.Zolpidem → for maintain sleeping during the night
Zolpidem Zodorm Tab: 10mg Unipharm
Stilnox Tab: 10mg Sanofi
The duration of therapy should not be more than 4 weeks.
2. Zaleplon → for induce sleep
3.Antihistamine: diphenhydramine/ hydroxyzine / doxylamine
Diphenhydramine Hudu Caplet: 50mg Beit jala

Doxylamine Tonight Tab:25mg CTS

Sleep aid Tab:25mg Perrigo

4. Ramelteon: melatonin agonist

5. Plants extract:
Valerian dry extract Relaxin Tab:500mg Trima
Valerian tincture Drops Floris
Passiflora Calmanervin Tab: Medetic
Valerian dry extract 250mg
Vit B1 60mg
Vit B6 10mg
10mg
Depression ‫االكتئاب‬
Cause: decrease the level of norepinephrine and serotonin in the brain
Group 1: Tricyclic antidepressant (TCA)
Imipramine / Clomipramin / Desipramin / Amitriptyline / Nortriptyline
Imipramine Imipramine Tab:25mg Crescent
Tofranil Tab:25mg Novartis

Clomipramine Anafranil Tab:25mg Novartis

(brand)
Anafranil SR Tab: 75mg
Maronil Tab: 25mg Unipharm

Desipramine Deprexan Tab: 25mg Unipharm

Amitriptyline Elatrolet Tab: 10mg Teva

Elatrol Tab: 25mg Teva
Amitriptyline Tab:10,25mg Abotex

Nortriptyline Nortylin Cap: 25mg Rekah

Doxepin Gilex Cap:10,25mg Rekah

Doxipen Teva Tab:10,25mg Teva
MOA: inhibit reuptake of norepinephrine and serotonin
Onset of action require 2 weeks or longer
Uses:
1.depression
2. imipramine and Amitriptyline →for bed wetting in children over 6 years and older
people.
3-Amitriptyline→ migraine and neuropathic pain ‫النمنمة وعدم الشعور باالطراف‬
4.ADHA → ‫النه هاي االدوية بتزيد انتباه الطفل فبقل نشاطه‬
Adverse effect:
1-Block muscarinic receptor (anticholinergic effect)→dry mouth, blurred vision, urinary
retention, constipation
2-Block alpha receptor→ hypotension, reflex tachycardia
3-Block histamine→sedation ‫تعتبر اشي إيجابي اذا المريض يعاني من ارق‬
4-overdose: arrythmia
TCA have low therapeutic index
-------------------------------------------------

Group 2: SSRI
Fluoxetine / Paroxetine / Sertraline / Citalopram / Escitalopram / Fluvoxamine
Fluoxetine Flutine Cap: 20mg Teva
Prozac Cap: 20mg Lilly
Prizam Tab: 20mg Unipharm
Fluoxicare Cap: 20mg Pharmacare
Oxizac Cap: 20mg Birzeit
→it is an activating agent: administer at morning
Paroxetine Seroxat Tab: 20mg GSK
Paxxet Tab:20mg Unipharm
Paroxetine Teva Tab:20mg Teva
Paroxetine →The most anticholinergic SSRI
→Sedating SSRI: administer at night
→Paroxetine is contraindicated in pregnancy (teratogenic).
→should be avoided if the patient is anxious.
Sertraline Lustral Tab: 50, 100mg Pfizer
Solosert Tab: 50, 100mg Hikma
Serenada Tab:50mg Unipharm
Seraline Tab: 50mg Birzeit

Citalopram Cipramil Tab: 20, 40mg Lundbeck

 Sitram Tab: 20mg Beit Jala
Celeram Tab: 10,20mg Sama

Escitalopram Escitalopram Tab: 10mg Teva

Esram Tab: 10,15,20mg Sandoz
Cipralex Tab: 10, 15, 20mg Lundbeck
Purlex Tab: 10, 15, 20mg Hikma
Esto Tab:10mg Unipharm

Fluvoxamine Favoxil Tab:50mg Perrigo

It is indicated for treatment of obsessive-compulsive disorder

MOA: inhibit serotonin reuptake

Onset of action require at least 2 weeks (anxiolytic effect ‫)كمهدئ يحتاج اسبوعين‬, usual
effect as antidepressant require 4-6 weeks and full benefit require up to 12 weeks or
more.
Uses: Depression (the first choice) They are indicated for patient above 18 years
because of 50% of children become more suicide with SSRI
If it is accompanied with insomnia →Paroxetine (sedating agent)
If it is accompanied with excessive somnolence → Fluoxetine, Sertraline (activating
agent)
Adverse effect: less severe than those for MAOI and TCA
Headache, sweating, GI SE ‫ما بتطول اعراض الجهاز الهضمي تقريبا بتوقف بعد اسبوع‬
Sexual dysfunction ‫(تعتبر سبب لحتى المرضى ما يلتزمو ويوقفو العالج‬if it is happened→replace
with bupropion or mirtazapine) (also, sildenafil, vardenafil, tadalafil may improve sexual
function)
Overdose: seizures
Caution: serotonin syndrome if given with other drugs that increase serotonin level.
‫بصير ارتفاع في درجة الحرارة وتشنجات في العضالت‬
SSRI at third trimester affect negatively on pregnant (respiratory distress, tremor,
hypoglycemia, pulmonary hypertension ….
Avoid using citalopram or escitalopram with omeprazole (increase the risk for QT
prolongation)
------------------------------

Group 3: SNRI
Venlafaxine / Duloxetine / Milnacipran
Venlafaxine Efexor XR Cap:75, 150mg Pfizer
Venal Unipharm
Venlafaxine teva Teva
Viepax IR Tab: 75mg Dexcel

Viepax XR Cap: 75, 150mg

XR: extended release.
It is also used for neuropathic pain

Duloxetine Cymbalta Tab: 30,60mg Lilly

Duloxetine Cap: 30,60mg Teva

Milnacipran Lxel Cap:50mg Perrigo

MOA: inhibit serotonin and norepinephrine reuptake

Used when SSRI are ineffective.
Usual effect within 4-6 weeks.
Effective in treating neuropathic pain such as fibromyalgia, also musculoskeletal pain.

SE: N/V/D, anticholinergic effect, Sexual dysfunction ‫وبتكون اصعب من المجموعة اللي قبل وممكن تدفع‬
‫المريض اليقاف الدواء‬
At high doses: increased BP and HR
Note: paroxetine, duloxetine, fluoxetine, sertraline → CYP2D6 Inhibitors
Group 4: MAO inhibitors
Selegiline /Rasagiline
Selegiline Selgin Tab: 5mg CTS
Jumex Tab:5mg Sanofi

Rasagiline Azilact Tab: 1mg Teva

MOA: inhibit the enzyme that is responsible for neurotransmitter degradation
Selective on MAO-B

last line agents because it does not specific for certain monoamine.
Drug-food interaction with food that contain tyramine at high doses when it lost its
selectivity.

Group 5: Atypical antidepressants

Bupropion / Mirtazapine / Trazodone
Bupropion Wellbutrin XR Tab: 150, 300mg GSK
Zyban Tab: 150mg GSK
Prolonged release
MOA: weak dopamine and norepinephrine reuptake inhibitor
It is contraindicated in patient with seizures, anorexia and bulimia.
It decreases the craving to nicotine.
Mirtazapine Remeron Tab: 30mg MSD
Miro Tab: 30mg Unipharm
Mirtazapine Tab:30,45mg Teva
MOA: alpha 2 antagonist→increase neurotransmitter release
It does not interfere with sexual function
Induce sleeping (it is not first line unless there is insomnia).

Trazodone Trazodil Tab: 50mg Unipharm

Maprotiline Melodil Tab: 25,50mg Unipharm

 )‫ ليس من الضروري إيقاف ادوية االكتئاب تدريجيا (حسب حالة المريض‬:‫مالحظة‬

Bipolar disorder ‫اكتئاب ثنائي القطب‬

The mood is converted between severe depression and high mood (mania)
Treatment:
1-Laithium (classic drug): orally, has low therapeutic index
SE: polydipsia, polyphagia, polyuria, GI distress, dermatologic reaction.
At high doses: hypothyroidism (because its structure like thyroid hormones)
Confusion, ataxia ….
Licarbium Lithium carbonate Tab: 300mg Rekah

2-Newer agents:Antiepileptic ‫ ادوية الصرع‬: carbamazepine, lamotrigine, valproic acid

(mood stabilizer)
Carbamazepine Tegretol Tab: 200mg Novartis
CR tab: 200, 400mg
Syrup
Teril Tab: 200mg Taro
CR tab: 200, 400mg
Timonil Tab: 300, 600mg Desitin

Lamotrigine Lamictal Chewable tab: GSK

(brand) 5,25,50,100,200mg
Lamodex Chewable tab: Dexcel
5,25,50,200mg

Sodium Valproate Valporal Cap:200mg Teva

Syrup: 200mg/5ml
Depalept Tab: 200, 500mg CTS
Oral solution:
200mg /5ml
 Chrono:500mg Sanofi
(prolonged release
tab)
Duvalept Tab: 200mg Birzeit
Syrup

Antipsychotic: olanzapine for mania

Olanzapine Olanzapine Tab:5, 10mg Teva

Zyprexa (brand) Tab: 5, 10mg Lilly
Prexolan Tab: 5,10,15,20mg Jepharm
Benzodiazepine: clonazepam for mania
Clonazepam Clonex Tab: 0.5, 2 mg Teva
(controlled)
Rivotril Tab: 0.5, 2mg Roche
Oral drops

Antiepileptic drugs
Convulsion: involuntary muscular contraction and relaxation.
Seizure: abnormal CNS electrical activity ‫شحنات كهربائية زائدة‬
Epilepsy: consist of both convulsion and seizure
Drugs to control seizure:
1-Na-channel blockers:
Phenytoin, Fosphenytoin, Carbamazepine, Valproic acid, Lamotrigine, Topiramate,
Oxcarbazepine.
Phenytoin Epanutin Cap: 100mg Pfizer
Dilantin Susp: 125mg/5ml Pfizer
Fenitoina Amp:250mg/ml Rubio

SE: hirsutism, acne, coarsening of facial features, gingival hyperplasia

Fetal hydantoin syndrome if the woman takes it during pregnancy: growth retardation,
microencephaly, cleft palate
It may cause cancer for the baby when he is grown(neuroblastoma)
Also, coagulation disturbance due to Vit K deficiency.

Carbamazepine Tegretol Tab: 200mg Novartis

CR tab: 200, 400mg
Syrup
Teril Tab: 200mg Taro
CR tab: 200, 400mg
Timonil Tab: 300, 600mg Desitin
It is also used for trigeminal neuralgia ‫الم بسبب إصابة العصب الخامس الذي يغذي الوجه‬, and
bipolar disorder.
Common SE: diplopia ‫يشوف االشي تنين‬, ataxia ‫تأرجح بالمشي‬
Carbamazepine is liver enzyme inducer.
Carbamazepine cause spina bifida and multiple malformation for the baby.
Also, it causes bleeding because of Vit K deficiency ‫عشان هيك بنعطى الطفل الفيتامين اول ما ينولد‬
Sodium Valproate Valporal Cap:200mg Teva
Syrup: 200mg/5ml
Depalept Enteric coated Tab: CTS
200, 500mg
Oral solution:
200mg /ml
Syrup:200mg/5ml
Sanofi
Chrono:500mg
(prolonged release
tab)
Duvalept Tab: 200mg Birzeit
Syrup
Chrono: valproic acid + sodium valproate
Valproic acid is a free acid that converted in the body to valproate ‫عشان هيك الكرونو بعطي‬
‫مفعول لفترة أطول‬
SE: tremor, transient hair loss, polycystic ovary syndrome, menstrual disturbances, Bone
loss, teratogenic (contraindicated in pregnancy).
Valproic acid is an enzyme inhibitor.
Lamotrigine Lamictal Chewable tab: GSK
(brand) 5,25,50,100,200mg
Lamodex Chewable tab: Dexcel
5,25,50,200mg
SE: toxic epidermal necrosis, steven Johnson syndrome.
Using valproic acid with lamotrigine may increase the level of lamotrigine and cause life-
threatening rash.
Topiramate Topamax Tab: 15, Janssen
25,50,100,200mg
Topiramate Tab: 25,50,100,200 Teva
Topitrim Tab: 25mg Trima
Adjunct therapy.
Also used to prevent migraine
Adverse effects: weight loss, somnolence, paresthesia.
Oxcarbazepine Trileptin Tab:300mg Novartis

2-Ca-channel blocker:
Ethosuximide, Pregabalin (controlled drug)
Pregabalin Lyrica Tab:25,50,75,150,300 Pfizer
Pregabalin Tab: 75,150,300mg Teva
Neuromax Cap: 50, 300mg Jepharm
Gabamax Cap: 150mg Beit Jala
Neuralic Tab:50,75,150,300mg Birzeit
Also used to treat neuropathic pain
3-enhanceing inhibitory GABA impulses
Barbiturate drugs and benzodiazepine
Primidone : is a prodrug that is metabolized to p0henobarbital and
phenylethylmalonamide, both have anticonvulsant activity
Primidone Prysoline Tab: 250mg Rekha

Gabapentin: GABA analog but its MOA unknown: used for seizures and neuropathic pain
Gabapentin Gabapentin inova Cap: 300, 400mg Inovamed
Neurontin Cap: 300, 400mg Pfizer
Nerventin Cap: 100, 300, 400mg Beit Jala
‫يؤخد قبل النوم النه بنعس‬
4- Levetiracetam (has multiple mechanism of action which make it unique from
conventional drugs)

Levetiracetam Keppra Tab: 250,500,1000 GSK

(brand) Syrup
Vial
Setanorm Tab: 250,500 Jerusalem
Syrup:100mg/1ml
Levitrim Tab: 250,500,1000 Trima
Levetiracetam Tab: 250,500,100 Teva
TEVA
Epitam Tab:100,250,500,750 Pharmacare
Levebon Vial:100mg G.L.Pharma

5-GABA analog but does not bind to GABA receptor

Vigabatrin Sabrilan Tab: 500mg Perrigo
MOA: inhibiting the breakdown of gamma-aminobutyric acid (the main inhibitory
neurotransmitter in the brain.
6-interfere with glutamate transmission

Notes:
Several antiepileptic drugs such as: phenytoin, carbamazepine, topiramate,
phenobarbital can increase the metabolism of hormonal contraceptive, decreasing their
effect. (the exception is valproic acid because it is not cytochrome inducer)
Intrauterine device can be used or the dosage of contraceptive can be increased during
ovulation.
Many of them are teratogenic
Treatment with carbamazepine, gabapentin, phenytoin, primidone or valproate may
associated with lowering folate level in the body.

Epilepsy and pregnancy:

Epilepsy is associated with minor and major malformation and seizures lead to an
increased risk of miscarriage, preterm labor, intracranial hemorrhage, hypoxia,
bradycardia.
‫األفضل انو مريضة الصرع ما تحمل النو خطره على الطفل كبير‬
Anticonvulsant teratogenicity is because of folic acid deficiency
→As a minimum 0.4mg folic acid per day is now recommended for any women at least
until the eighth week of pregnancy. ‫على األقل لنهاية اول ثالث شهور من الحمل ويفضل تكمل فيه‬
‫طول الحمل‬
A higher dosage of 4-5mg is recommended by most authors.

→ best choice for treating epilepsy during pregnancy is: carbamazepine

→When a woman is treated with valproic acid →efforts should be made to change her
medication. ‫بس اذ ا المريضة ماشية عليه ووضعها مستقر وتغييره ممكن يزيد من سوء الحالة وترجع نوبات‬
‫الصرع فبنخليه بس بنكون عارفين انو الخطر اله اكبر من أي دوا تاني‬
Valproic acid cause spina bifida and multiple malformation
→Low doses of diazepam or clonazepam is permitted even during the fist trimester.
Benzodiazepine cause floppy infant syndrome: ‫ما في قوة بالعضالت عند الطفل‬
Notes:
Monotherapy should be used
Frequent smaller doses or extended-release formulation may be helpful to avoid high
blood peak levels.

‫خالل الرضاعة كمان يفضل استخدام دواء واحد واذا بدها تستخدم اكتر من دوا الزم تتوقف الرضاعة‬
Monotherapy with phenytoin, valproate or carbamazepine is compatible with
breastfeeding.
Valproate (first choice) ‫هو المفضل النو األقل مرورا للحليب‬
--------------------------------------------------------------------------------------------------------

Psychosis ‫االمراض العقلية‬

Schizophrenia
‫ سماع أصوات او رؤية امورغريبة‬،‫تهيئات واوهام‬
‫يتكلم المريض بصوت منخفض وايقاع صوت ثابت وقليل الكالم‬
‫يفقد القدرة على الشعور بالفرح واالستمتاع‬
Some hypothesis:
-excessive dopaminergic neurons ‫زيادة نشاط الدوبامين في مناطق معينة من الدماغ‬
-excess serotonin activity

Antipsychotic / Neuroleptics:
They prevent episodes but not treat or cure the disease.
→Typical antipsychotic:
Phenothiazine group:
Chlorpromazine / Fluphenazine / Prochlorperazine / Haloperidol / Droperidol
/Zuclopenthixol / Thioridazine
Chlorpromazine Chlorazine Tab: 25, 100mg Birzeit
Chlorpromazine Tab: 100mg
→also used to treat intractable hiccups.
 Fluphenazine Fludecate Amp: 25mg/ml Unipharm
‫ممكن استعماله للغثيان والتقيؤ الناتج عن العالج االشعاعي‬
Trifluoperazine Telazine Tab:10mg Birzeit

Haloperidol Haldol Tab: 5, 10 mg Janssen

Amp: 5mg/1ml
Decanos
:100mg/1ml
Drops: 2mg/1ml
Haloper Tab: 5, 10mg CTS
Peridol Tab: 5mg Birzeit

Zuclopenthixol Clopixol Tab:2,10,25mg H.Lundbeck

Amp:200,500/ml

Periciazine Neuleptil Oral solution Sanofi

(drops)

Thioridazine Ridazin Tab: 10, 25, 100mg Taro

MOA: block D2 receptor → cause extrapyramidal SE

They have the same efficacy, but extrapyramidal symptoms are more likely to happened
with haloperidol than with chlorpromazine.

→Atypical antipsychotic (second generation):

Clozapine / Aripiprazole / Olanzapine / Risperidone / Sulpiride / Amisulpride/Quetiapine
/Clotiapine / Ziprasidone

MOA: block both dopamine and serotonin receptors

Lower incidence of extrapyramidal symptoms →first line in schizophrenia
Clozapine Lozapine Tab: 100mg Taro
Leponex Tab: 25,100mg Novartis
→it is effective in refractory patient who does not respond to other drugs.
→serious SE: bone marrow suppression →severe agranulocytosis
Seizures / cardiovascular SE
So, it is not used as first line in all patient
Aripiprazole Ariply Tab: 10,15,30mg Unipharm

Olanzapine Olanzapine Tab:5, 10mg Teva

OTD: 5, 10mg
Zyprexa (brand) Tab: 5, 10mg Lilly
Prexolan Tab: 5,10,15,20mg Jepharm

Risperidone Risperdal Tab: 1, 2, 3, 4mg Janssen

Solution: 1mg/ml
Consta: 25, 37.5, 50
mg
Decidone Tab: 1, 2, 3, 4mg Jerusalem
Risperdex Tab: 1, 2, 3, 4mg Dexcel

Paliperidone Invega Extended-release Janssen

tab:6mg

Sulpiride Hypothal Cap: 50mg Birzeit

Modal Tab: 50mg Rafa
Modal Forte Tab: 200mg

Amisulpride Solian Tab:50,100,200,400 Sanofi

Quetiapine Seroquel (brand) Tab: AstraZeneca

25,100,200,300
XR Tab:
50,200,300,400 mg
 Clotiapine Entumin Tab: 40mg Taro

Ziprasidone Geodon Cap: 20mg Pfizer

Antipsychotics also used to treat agitation and disruptive behavior, secondary to other
disorder.
Risperidone and haloperidol used to treat motor and phonic tics of Tourette disorder
.‫مرض عصبي ينتج عنه أصوات وحركات مفاجئة وال ارادية‬
Sedation is another SE of these drugs due to blocking of H1 receptors
Seizures are common with chlorpromazine and clozapine
Other SE:
Atropine-like effect (dry mouth, blurred vision, constipation, urinary retention).
Metabolic disorder: hyperglycemia, obesity.
Hyperprolactinemia due to dopamine antagonist effect.
→in women it lead to: amenorrhea /galactorrhea /loss of libido
→in men: gynecomastia / infertility and erectile dysfunction

These drugs should be tapered over a period of time ‫مش الزم يتوقف الدواء بشكل مفاجئ‬
Note:
Neuroleptic malignant syndrome may occur due to excessive blocking of dopamine
receptors
Symptoms:
Muscle rigidity / diaphoresis ‫ تعرق‬/ altered BP and HR / hyperthermia ‫ارتفاع الحرارة‬
Treatment:
Stope the drug
Bromocriptine (dopamine agonist)
Dantrolene / diazepam to reduce muscle rigidity
 Dantrolene sodium Dantrium Cap: 25mg NORGINE
It is a skeletal muscle relaxant to treat symptoms of malignant hyperthermia (muscle
rigidity).

Parkinson’s disease (PD):

Neurodegenerative disorder of the dopaminergic neurons.
(dopamine inhibit GABA) (Acetyl-choline stimulate GABA) (GABA is inhibitory
neurotransmitter).
Symptoms: slow movement/ resting tremor/ muscle rigidity / instability in walking
There is no cure, but treatment of symptoms.

Treatment:
1.Dopamine precursor: Levodopa
Dopicar Carbidopa/levodopa Tab Teva
Sinemet Retard Carbidopa/ levodopa Tab MSD

→should be taken on an empty stomach, typically 30 min before a meal (proteins

decrease the passage of L-dopa to CNS).
→Carbidopa: peripheral dopa decarboxylase inhibitor →reduce the peripheral
(anorexia, nausea, vomiting) and arrythmia.
‫هاد الدوا فعاليت ه بتكون اكتر شي خالل اول كم سنة بعد هيك بتصير استجابة المرضى اقل‬
‫والزم الجرعة تخف مع الوقت لحتى نتجنب االعراض الجانبية‬
‫ممكن بسبب العالج تصير حركات ال ارادية بالوجه او اليدين او الرجلين بس مع هيك ما بنوقف الدوا النه لو وقفناه‬
‫ قلق وكوابيس‬،‫ هلوسة‬،‫ ممكن كمان يصير ارق‬،‫ممكن يبطل حركة نهائيا‬
→Vitamin B6 supplementation above 5-10mg per day reduces the effectiveness of
levodopa. However, combining levodopa with carbidopa prevents this adverse effect, so
Vit B6 may safely be taken with them.

2-COMT (Catechol-O-methyltransferase) inhibitors:

Tolcapone, Entacapone
they inhibit other pathway of levodopa metabolism that convert it to 3-O-methyldopa
which compete with levodopa in passage.

Stalevo Levodopa Tab:150+37.5+200mg Novartis

Carbidopa
Entacapone

3-Dopamine receptor agonist:

Older (ergot derivatives): Bromocriptine / Pergolide
Bromocriptine Bromocriptine Tab: 2.5mg Generis
Generis
Parlodel Tab: 2.5mg Novartis

Newer (non-ergot): Ropinirol /Pramipexole

Ropinirole Requip Modutab Tab: 2, 4 mg GSK
Pramipexole Sifrol Tab: 0.25, 1mg Boehringer
Ingelheim

They do not require enzymatic conversion, and have transporter other than those for
levodopa
They have longer duration than levodopa and less side effects, but they are less efficient
than levodopa in treating the symptoms of Parkinson.
They are given when there is no response to levodopa

4-MAO -B-inhibitor: Selegiline / Rasagline

Selegiline Selgin Tab:5mg CTS

Rasagline Azilect Tab: 1mg Teva

Selective for brain
It increases dopamine level and prolonged the effects of L-DOPA.
It is used as adjunct therapy with levodopa not alone

Drug interaction: not recommended with meperidine, TCA, serotonin reuptake

inhibitors (because they increase the level of serotonin and other catecholamine).

5-Muscaring Acetylcholine Antagonist (anti-cholinergic):

Trihexyphenidyl, Benztropine, Diphenhydramine, Biperiden , Procyclidine
They are used as adjunct to dopaminergic therapy and to treat extrapyramidal side
effects.
Trihexyphenidyl Partane Tab: 2,5mg Taro
Also known as Artidyl Tab: 2,5mg Jepharm
Benzhexol Rodenal Tab:5mg Rekah
(controlled)

Biperiden Dekinet Tab: 2mg Rafa

Procyclidine Kemadrin Tab: 5mg Aspen

6-Amantadine (antiviral):
Amantadine Amantadine Tab: 100mg Heritage
Amantadin Tab: 100mg Neuraxpharm
neuraxpharm
PK-Merz Tab: 100mg Megapharm

For mild PD or as adjunct therapy.

→Drugs that used to treat side effects of anti-PD drugs:

Domperidone: peripheral dopamine antagonist to treat nausea and vomiting
 Domperidone Motilium Tab: 10mg Janssen
Metosim Tab: 10mg Sama
‫ سنة‬12 ‫يستعمل لعمر فوق‬
It does not cross BBB, so it works peripherally which is an advantage in Parkinson to
prevent decreasing dopamine in the brain.

Clozapine, Olanzapine: atypical neuroleptic with minimal D2 blocking properties, to

treat hallucination and psychotic symptoms of levodopa.
Clozapine Lozapine Tab:100mg Taro
Leponex Tab: 25,100mg Novartis

Olanzapine Olanzapine Tab:5, 10mg Teva

OTD: 5, 10mg
‫تحت اللسان‬
Zyprexa (brand) Tab: 5, 10mg Lilly
Prexolan Tab: 5,10,15,20mg Jepharm

→drugs that may cause PD symptoms (parkinsonism): (by blocking dopamine receptors)
Antipsychotic: haloperidol, chlorpromazine, Thorazine
Haloperidol Haldol Drops: 2mg, 5mg/ml
Haloper Tab:5, 10mg CTS
Peridol Tab: 5mg Birzeit

Chlorpromazine Chlorazine Tab: 25,100mg Birzeit

Chlorpromazine Tab: 100mg

Antiemetic: prochlorperazine, metoclopramide

Emestop Metoclopramide Tab: 10mg Birzeit
Amp: 10mg
Syr:5mg/5ml
 Pramin Tab:10mg Rafa
Amp:10mg/2ml
Emegrain Metoclopramide Tab Beit Jala
5mg
Paracetamol
500mg

------------------------------------------------------------------------------------------------------------------------------

Alzheimer disease
Is an irreversible progressive brain disorder that slowly destroys memory and thinking
skills
Cholinesterase inhibitors are prescribed for mild to moderate Alzheimer’s
→increase the level of acetylcholine
They are help in reduce some symptoms and control some behavioral symptoms:
Rivastigmine Exelon Cap:1.5, 3, 4.5, Novartis
6mg
Patches: 5,10mg
Donepezile Donepezile Teva Tab: 5,10mg Teva
(acetylcholinesterase Asenta Tab: 5,10mg Perrigo
inhibitor) Aricept Tab: 5,10mg Pfizer
Memorit Tab: 5,10mg Unipharm
Galantamine Reminyl Tab:8,16,24mg Janssen
Prolonged
tab:4,8,12mg
Memantine Ebixa Tab:10,20mg H.Lundbeck
(NMDA receptor
antagonist)
Piracetam Nootropil Tab: 800mg Ubc
(derivative of GABA) It works by
improving
communication
between the nerve
cells and protect the
 brain, so it treat
memory loss)

---------------------------------------------------------------------------------------------------------------------

CNS Stimulants
They are drugs of abuse.
Two groups:
1-Psychomotor Stimulants:
Methylxanthines→ like: theophylline found in tea
Theobromine found in cocoa
Caffeine found in tea, coffee, chocolate.
Use: xanthine such as theophylline →bronchodilator
SE: insomnia, anxiety →convulsion→ cardiac arrythmias (lethal dose of caffeine
10g =100cups)

Nicotine
Used in smoking cessation like transdermal patch and chewing gums
Bupropion(NSRI) to reduce the craving for cigarettes

Cocaine
It inhibits the reuptake of monoamines (norepinephrine/serotonin / dopamine)
It is highly addictive drug
It is used in local anesthetic

Amphetamine
Dextroamphetamines Attent Tab: 10, 20, 30 mg Teva
Inhibit the release of catecholamine
Inhibit MAO enzyme
Prolonger use cause dependence and anorexia

Uses:
To treat attention deficit hyperactivity disorder (ADHD)
Note: there are nonstimulant drugs used to treat ADHD such as atomoxetine
To treat narcolepsy (sleep disorder with daytime sleeping)
Appetite suppression

SE: insomnia, tremor confusion, palpitation, arrythmias , hypertension, nausea,

vomiting.

Methylphenidate Ritalin (brand) Tab:20, 40mg Novartis

Concerta Extended release Janssen
Tab:18, 27,36mg
It is a stimulant medication used to treat attention deficit hyperactivity disorder and
narcolepsy.

2- Hallucinations
Lysergic acid diethylamide (LSD)→cause colorful hallucination
Marijuana →main ingredient: tetrahydrocannabinol (THC)→euphoria, visual
hallucination, appetite stimulant, increased HR, conjunctivitis
Uses of THC: Antiemetic, Appetite stimulant →used in cancer patients
------------------------------------------------------------------------------------------------------------
Anesthetics
Drugs used in anesthesia:
Thiopental (barbiturate)
Opioids such as: fentanyl, morphine, alfentanil, remifentanil→it is used as analgesic and
for epidural and spinal anesthesia
Etomidate →hypnotic not analgesic
Ketamine

Ketamine Ketalar Injection: Short-acting non-

50mg/1ml barbiturates
anesthetics used to
make dissociative
anesthesia ‫تخدير‬
‫بدون فقدان الوعي‬

Propofol →sedative hypnotic →IV anesthetic, it is preferred over thiopental because it

dose not cause nausea and vomiting, also the induction occurs within 40 seconds and is
smooth with rapid recovery.
Propofol Diprofol Vial:1%
Taro
Propofol Amp: 10mg/1ml
20mg/1ml

Benzodiazepines (BZD): Midazolam, Diazepam, Lorazepam →pre-anaesthetic

medications used because of anxiolytic effect, hypnosis, sedation, amnesia
Midazolam is preferred as it has rapid and short duration
Local anesthetics
Lidocaine→locally to relieve itching, burning and pain from skin inflammation, also used
as dental anesthetic and in minor surgery
It is used also to treat serious ventricular arrhythmias (IV preparation).
Strepsils plus Lozenges: Anesthetic Lozenges
Dichlorobenzyl alcohol For the symptomatic relief
Amylmetacresol of throat infections
Lidocaine including severe sore
throat.
Pitrisol solution Benzoic acid Rekah
Salicylic acid
Lidocaine
Antrolin Rectal Cream: For hemorrhoid
Nifedipine
Lidocaine
Lidocaine Amp Used as solvent with some
types of injections to
reduce pain
Esracain Cream: 5% Local anesthesia
Gel: 1% Rafa
Emla Lidocaine Cream
PriLidAn Lidocaine + Prilocaine Cream
Local anesthesia to relieve
pain before procedures in
the skin.

Proctoglyvenol Cream/supp: For hemorrhoid

Lidocaine
Tribenoside Novartis
Hemoral Ointment/ supp: Beit jala
Hydrocortisone
Lidocaine
Zinc oxide
Lignocaine Amp: 1%, 2 % Jepharm
Gingipant Solution: Beit Jala
Tannic acid ‫مادة قابضة‬
Pantothenate
 Lidocaine
Lidomax Spray: For premature ejaculation
Lidocaine Used 10-15 min before
intercourse
Beit Jala
“You are about to overcome something you have been dealing with,
Your mind and heart will be at peace again soon” ♥
 Topic 6: Diabetes
Definition: group of metabolic disorder characterized by hyperglycemia and
abnormalities of fat, lipid and carbohydrate metabolism
Type1: autoimmune destruction of B-cell in pancreas
—> lead to decrease secretion of insulin and amylin

Function of amylin:
Suppression of inappropriate glucagon secretion
Slow gastric emptying
Central satiety

‫لماذا مريض السكري من النوع االول يشعر بالجوع باستمرار؟‬

‫بسبب نقص االملين الذي يعطي شعور بالشبع‬-1
.‫الن خاليا الجسم بحاجة الى السكر لذلك تعطي امر بالشعور بالجوع‬-2
-usually occur during childhood or puberty
-there is a moderate genetic predisposition for type 1
Type 2:
- it is a progressive disease,
-insulin resistance and impaired secretion of insulin, -reduced incretin effect that lead
to decrease effect of GLP-1 and GIP
Note :
GLP1: glucagon like peptide 1
GIP: glucose independent insulinotropic peptide
‫مواد تحفز الجسم على افراز االنسولين حسب كمية السكر الموجودة في الجسم‬
-increase glucagon secretion: due to resistance to insulin and GLP1 which both suppress
glucagon production.
-up regulation of SGLT-2 in kidney—> reabsorption of glucose
-at late stages, the Beta cell mass gradually decline over time, thus require insulin
therapy.
-Commonly occur over age 35
-there is very strong genetic predisposition for type 2
—
Metabolic Syndrome:
Obesity + lipid or HTN or DM

Other causes of DM:

1-gestational DM (GDM)
2-maturity onset diabetes of youth (MODY)
3- endocrine disorders ex: acromegaly and Cushing syndrome
4-pancreatic endocrine dysfunction
5- infection: cause stress on the body and this increase the level of sugar
6- medications:
Glucocorticoids
Thiazide
Niacin

Complication of DM:
-Microvascular: nephropathy, neuropathy, retinopathy
-Macrovascular: coronary artery disease, stroke, peripheral vascular disease

These complications should be monitored regularly

To decrease these risks:
Smoking cessation/ treated of dyslipidemia/ Control BP/ antiplatelet

Presentation:
Type 1: polyurea, polyphagia, polydipsia, weight loss, lethargy, ketoacidosis
Type 2: often asymptomatic, weight gain
Polyurea, nocturia, polydipsia can be present

Diagnosis of DM
Criteria (any one of the following mean that the person has DM)
1- HbA1c: 6.5% or more (normal level is less than 5.7%)
(monitor glucose level every 3-6 months, it gives an indication of the overall control of blood glucose
levels over the previous 2-3 months)

2- Fasting plasma glucose: (FPG)

( ‫ ساعات اقل اشي ما يكون الشخص ماكل اكل فيه سعرات حرارية‬٨ ‫)قبل الفحص ب‬
126 mg/dL or more (normal level is less than 100)

3- oral glucose tolerance test (OGTT)

The person eats 75 g of sugar dissolved in water and the level of sugar after 2 hours is
measured;
200 mg / dL or more (normal level is less than 140)

4- Random plasma glucose conc 200mg/dL or more plus symptoms

Note:
FPG: 100-125 mg/dL —> impaired fasting glucose (IFG)
OGTT: 140- 199 mg/dL—> impaired glucose tolerance ( IGT)

‫ الحوامل بنفحصلهم السكري وبننتبه عليه اذا عندها‬risk ‫عالي متل تاريخ العائلة في سكري او بالحمل السابق صار‬
‫عندها سكري او عندها سمنة او من عرق عندهم فرصة االصابة بالسكري عالية‬

Target level:
HbA1c. <7%
Preprandial 80-130 my/dL
Postprandial. <180 my/dL

The patient should:

Do regular physical activity ( at least 150min/week)
‫مريض السكري عادي يعمل تمارين قوية اال اذا عنده مشاكل بالقلب او بالعين النو بنخاف من ارتفاع ضغط العين‬
‫والنزيف‬
Monitor the complications regularly
Self-monitoring of glucose
Choose the food appropriately
-moderate carbohydrate
-low saturated fat
-all essential vitamins and minerals
Maintain a healthy weight (weight loss for type 2 patient)
‫ يعني ما بصير يوخد الدوا وما يوكل النو رح يصير هبوط بالسكر‬،‫الزم االكل واالنسولين يمشو مع بعض‬

Treatment of hypoglycemia:
(Rule of 15) for conscious patients
15g of simple carbohydrate
‫ ربع كاسة كوال‬/‫ مربى‬/‫ ملعقة عسل‬/‫ حليب‬/ ‫عصير برتقال‬
Then wait 15 min and measure the level of glucose
If it is less than 70 mg/dL, the patient should take another 15g of simple carbohydrates
Dextrose IV for unconscious patients
Glucagon IM for unconscious patents and if IV access cannot be established
Note: Glucagon used in the treatment of overdose of beta blocker
Has positive ionotropic and chronotropic effect of the heart
It acts by stimulation of glucagon receptors not beta 1 receptor.

Note:
sympathetic →suppress insulin secretion
Parasympathetic →stimulate insulin secretion

Insulin
-Produced by recombinant DNA technology
-Not active orally, inactivated by insulinase (insulin transhydrogenase) found in liver and
kidney , also insulin in a protein which is destructed in the stomach.
-Insulin brust within 2 min, lasts for 15 min, then postprandial insulin secretion
-Dose of insulin is reduced in renal insufficiency (because the insulin is secreted by the
kidney)
-Most common conc used: 100 unit/ml more concentrated: U-200 / U-300 / U-
500
Side effect of insulin:
1-hypoglycemia (the most common and serious SE)
Symptoms of hypoglycemia: Headache/anxiety/shaky/confusion/increase
appetite/vertigo/tachycardia/diaphoresis/blurred vision /weakness
Can results in seizures and coma
2-wight gain
3- hypersensitivity reaction: usually includes a local injection site such as swelling or
redness, but rarely life-threatening anaphylaxis can also occur
(prevented by desensitization protocol)
4-lipodystrophy (lipoatrophy and lipohypertrophy) ( minimized by rotation of injection
sites)
‫ مرة بالجهة اليمين ومرة باليسار‬,‫يعني مرة بالبطن ومرة بالكتف‬
5- hypokalemia (excess insulin can cause shift K+ into cell) so used with cautions with
potassium lowering drugs.

Types of insulin:
Rapid acting insulin:
Lispro, Aspart , Glulisine , Human insulin→ analogs → dissociate more rapidly to
monomer
Rapid onset (given 10-15 min before meal)
Do not cause postprandial hypoglycemia

Novorapid Aspart NovoNordsk 100unit/ml

3ml pen SC
May IV for
emergency
Humalog Lispro Lilly 100unit/ml
3ml pen
10ml vial
Apidra Glulisine Sanofi 100unit/ml
3ml pen Sc
Actrapid Human insulin NovoNordisk 100unit/ml
3ml pen
10 ml vial

Short Acting insulin

1- Regular insulin → also called (soluble human insulin)
SC or IV
It is a hexamer→ dimer→ monomer
If SC given 30 min before meal (slow onset)
 Humalin R Regular insulin Lilly 100unit/ml
10ml vial

Intermediate acting insulin:

NPH (Neutral Protamine Hagedorn) (isophane)
Lente (insulin zinc)
Formed by adding of zinc and protamine to the regular insulin→less soluble→delayed
absorption and prolonged duration

Insulutard NPH NovoNordisk 100unit/ml

3ml pen
10ml vial
Suspension for
SC
Humalin N NPH Lilly 100unit/ml

Q: why you cannot give NPH insulin intravenously?

Because if it is given IV it will mimic the action of regular insulin (its effect will be short
not intermediate)

Note: it is not useful in case of emergency such as Diabetic Ketoacidosis/coma

American Diabetes Association guidelines recommend NPH insulin dose:

0.4 to 1 unit/kg/day SC for type 1
0.1 to 0.2 unit/kg/day SC for type 2

Note: inadequate resuspension is thought to contribute to the high day to day variability
in the pharmacodynamic and pharmacokinetic profile of NPH insulin, leading to
hypoglycemia. Patient can adequately resuspend NPH by rotating the vial several times
until its uniformly cloudy.
Side effect of NPH:
1- Labile glucose response
2- Nocturnal hypoglycemia
3- Fasting hyperglycemia: because the duration of action is not enough to exert its
effect till the morning.
Managed by giving NPH at bedtime rather than with the evening meal.

Long-acting insulin:
-Peakless
- cause less nocturnal hypoglycemia
Onset of action within 2 hours
Glargine / Degludec → once daily (duration of action 20-24hr)
Detemir → twice daily (duration of action 14-24hr) (associate with albumin then
dissociate from it)
Ultralente
Lantus Glargine Sanofi 100unit/ml
3ml pen
10ml vial
Sc only
Tregludec Degludec NovoNordisk 100units/ml
Levemir Detemir NovoNordisk 100unit/ml
3ml pen
Sc only

Note: mixing Levemir with rapid acting insulin analogue like insulin aspart, results in an action profile
with a lower and delayed maximum effect compared to separate injections. Therefore, mixing of rapid
acting insulin with Levemir should be avoided.

Note: long-acting insulins should not be mixed in the same syringe wth other insulins due to
crystallization.
Combinations of insulin:
Mixtard NPH + regular NovoNordisk
70% + 30%
60% + 40% Counselling:
50% + 50% Shake well before use.
‫التحريك بكون بوضعها بين االيدين‬
‫وتمريها يمين ويسار مش متل خض العلبة‬
‫لألدوية الشرابات‬

‫المرضى بعرفوه على انه االنسولين‬

‫العكر‬
Humalin 70/30 70% NPH + 30% regular Lilly
NovoMix Aspart (short) + NovoNordisk
Aspart protamine
(intermediate)
30→30 + 70
50→50 + 50
70→ 70 + 30
Humalog Mix Lispro (short) + lispro Lilly
protamine (intermediate)
50→ 50 + 50
25→ 25 lispro+ 75 lispro
protamine

Syringe : 100 unite = 1ml

50 unit = 0.5 ml
‫ وحدة‬50 ‫حسب جرعة المريض بنعطيه أي وحدة من هدول السرنج اذا كانت اقل او اكتر من‬

Insulin Duration Route

Rapid 3-5 hr SC OR IV Control
postprandial
glucose ‫بعد الوجبة‬
Short(regular) 7-10 hr SC OR IV Control
postprandial
glucose
Intermediate 16-20 hr SC Control fasting
glucose ‫بين الوجبات‬
Long 24-30hr SC Control fasting
glucose
→when the IV route in needed, Regular insulin is most commonly used.
‫ ما بنفضل استخدامه بهاي الحالة خوفا من حدوث هبوط في السكر‬Rapid ‫ال‬:
)‫علبة االنسولين مسموح لحد شهر بعد فتحها بالبيت تكون برا التالجة اما اذا رح تضل عنده اكتر من هيك الزم تضل بالتالجة (بالشتوية‬
‫اما بالصيف الزم يخزنها بالتالجة‬

Technosphere Insulin (Afrezza):

Inhaler (dry powder of regular insulin)
Reach peak about 12 to 15 min
SE: cough, upper respiratory tract infection
Contraindicated in patients with asthma and COPD

Pharmacologic therapy for type 1 DM:

2 methods:
1) 2 needles: (standard insulin therapy)
➔ Before morning meal: NPH + regular or rapid
➔ Before evening meal: NPH + regular or rapid

Note: rapid (lispro / aspart/ glulisine )

Disadvantages of this method:

1-hyperglycemia after afternoon meal
2-noctural hypoglycemia (due to peak of NPH at night)
The solution is transfer NPH of evening to bedtime
Morning: NPH + regular or rapid
Evening: regular or rapid
Bedtime: NPH → The peak will be in the morning instead of at night
 2) Basal-Bolus Regimens: (intensive insulin therapy/ 3 injections or more)
1- If glargine used as basal→ 4 needles
1 glargin needle (at bedtime)+ 3 regular or short needles ( prandial)

2- If detemir used as basal → 4-5 needles

1 or 2 detemir + 3 regular or rapid

3- If NPH used → 3 needles

NPH+ Regular
Regular
NPH+ Regular

Note: NPH can be mixed with regular but not with detemir and glargine
Note: Drug of choice for management of diabetes in pregnancy has
always been insulin.

Note: hypoglycemia is more likely to occur with intensive therapy more

than with standard, in contrast to complication which is more likely to
occur with standard.

Intensive therapy is not recommended in:

-long-acting diabetes
-significant microvascular complication
-advanced age
-those with hypoglycemic unawareness.

-------------------------------------------------------------------------------
Oral Antidiabetic Agents:
֍ Insulin Sensitizers: (Bigunides) ( thiazolidindiones)
Bigunides:
Metformin → increase the insulin sensitivity of hepatic and muscle tissues.(insulin
sensitizer)
→inhibit gluconeogenesis (decrease hepatic glucose output)
→enhance peripheral glucose uptake.
→decrease intestinal glucose absorption
Diamet Metformin BitJala Caplet:500,850,1000
Glucomet , XR Metformin BirZeit Caplet: 850mg
XR: 750mg
Metformin teva Metformin Teva Tab: 850mg
Glucomin Metformin Dexcel Caplet:850mg
Glucophage Metformin MERCK Caplet: 850mg
Diabtin Metformin Sama Tab: 850mg
Maximum dose of metformin: 850mg three times daily
→metformin lead to: decrease LDL and triglyceride
Increase of HDL
→it is the drug of choice for type 2 DM due to :
-low cost
-efficacy
-positive pleiotropic effects
- manageable SE
-decrease the weight
-decrease LDL, TG / increase HDL
-do not produce durable response (the patients need another drug after about 5
years)
Note: Metformin is effective in the treatment of polycystic ovary syndrome (it
lowers the insulin resistance seen in this disorder and can result in ovulation and
pregnancy)
SE of metformin:
1-GI Side effects: abdominal discomfort / stomach upset / diarrhea)
Can be prevented by: -slow dose titration
-take it with or immediately after meal
-extended release metformin
2-Lactic Acidosis (the PH should not be less than 7 )
Usually the body maintains the PH of blood close to 7.40)

→Metformin is contraindicated in these cases because increasing the risk of lactic

acidosis:
(HF, shock, septicemia, acute MI , renal insufficiency, sever lung or liver disease)
→if the patient undergoes cardiac catheterization, metformin should be stopped
and then assist the heart and renal functions in order to return it or not.
→should be temporarily discontinued in patients undergoing procedures
requiring IV radiographic contrast
‫النها تنافس الميتفورمين مما يؤدي الى تراكمه وذلك يزيد فرصة حدوث‬
Lactic acidosis
→long-term use of metformin is associated with biomedical B12 deficiency and
anemia. Routine testing of vitamin B12 levels In metformin-treated patients
should be considered.
→metformin dose should be measured according to GFR
If GFR is 30-45 ml/min →metformin is not given
If the GFR is decreased for the patient already taken metformin, the doctor will
assist the case.
→it is metabolized by CYP450 pathway, is excreted in the urine, and has a half-life
of 2-6 hours.

Thiazolidinediones (Glitazones) (TZD): Pioglitazone / Rosiglitazone

MOA: insulin sensitizer (increase the insulin sensitivity in the muscle and fat by
increasing the GLUT 4 glucose transporters)
Also it increase the level of Adiponectin (a cytokine secreted by fat tissue
which increase the insulin sensitivity)
Has beneficial effects on serum lipid: decrease LDL, increase HDL
Actose Pioglitazone Takeda Tab: 15,30,45mg
Competact Pioglitazone Teva 15/850
+Metformin
Avandia Rosiglitazone GSK Tab: 4, 8 mg
Trogiltazone was withdrawn due to drug-induced hepatitis
→TZDs are taken orally once a day, with or without food
→Maximal glucose-lowering effect are not seen for six weeks to 6 months due to
delay onset of action via modification of gene expression.
→used as monotherapy or in combination with metformin or sulfonylureas
→ Dosing for treatment of T2DM:
Pioglitazone: Initial 15 to 30 mg PO with a meal once a day; may increase the dose by 15 mg
with careful monitoring to 45 mg once a day. The maximum dose is 45 mg.
Rosiglitazone: Initial 4 mg PO once a day. If inadequate response after 8 to 12 weeks, may
increase the dose to 8 mg PO once a day or divided 12 hourly (4 mg twice a day).

→ SE:
1.the main SE is water retention leading to edema and congestive HF (diuretic maybe given
with it)
2.wieght gain due to increase the adipose tissue mass and fluid retention
3.fractures : increase the risk of fractures and decrease the bone density
4. pioglitazone increase the risk of bladder cancer
 Rosiglitazone increases the risk of cardiovascular disease
Note: Troglitazone was removed from the market due to hepatotoxicity.
5. increased ovulation and teratogenic effects
Patients with polycystic ovarian syndrome have shown an increased ovulation rate with the use
of TZD and other insulin sensitizers. This effect may result in ovulation in some premenopausal,
anovulatory women, leading to improved rates of spontaneous pregnancy. However, TZDs have
also been shown to have some teratogenic potential by decreasing fetal maturation.
Premenopausal women should use contraception if they are not trying to conceive and should
get switched to another insulin sensitizer, such as metformin, after conception.

Category: C

Contraindications:
1.HF (contraindicated with class 3 and 4) (used with caution with class 1 and 2)
2. Moderate to sever hepatic impairment
3.Bladder cancer
4.pregnancy
5.High risk of fractures

֍ Insulin secretagogues:
Sulfonylureas / miglitinides

Sulfonylureas
MOA: enhance the secretion of insulin, consequently they are effective only when residual
pancreatic B-cells are present.
Three generations:
First : Acetohexamide / chloropropamide / Tolbutamide / Tolazamide
(no longer used)
Second: Glipizide (10-24hr) / Glyburide (Glibenclamide) (14-24 hr)
Third: Glimiperide (more potent / more efficacious/ fewer side effects/longer duration 24hr)
How do sulfonylureas enhance insulin secretion?
They act by binding to the specific receptor on B-cell, blocking the inflow of potassium K+
through ATP-dependent channel, the flow of K+ within the B-cell goes to zero, the cell
membrane becomes depolarized, thus removing the electric screen which prevents the
diffusion of calcium into the cytosol. The increased flow of calcium into B-cell causes the
concentration of the filaments of actomyosin responsible for the exocytosis of insulin, which is
therefore promptly secreted in large amounts.

Glucocare Glyburide Pharmacare Tab:5mg

Gluben Glyburide Dexcel Tab:5mg
Declamide Glyburide Beit Jala Tab: 5mg

Gluco-Rite Glipizide Perrigo Tab:5mg

Amaryl (the Brand) Glimepride Sanofi Tab: 1,2,3,4

Amarex Glimepride Beit Jala Tab:1,2,3,4
Amiran Glimepride Birzeit Tab: 1,2,3,4
Glimaryl Glimepride Pharmacare Tab: 1,2,3,4
Bride Glimperide Sama Tab: 1,2,3,4
→Sulfonylureas should be taken 30 min before meals, and their dosage should be increased
every 2 weeks if glycemic control has not been reached.
→The typical starting dose should be low (for example glibenclamide 2.5 mg or glimepiride
2mg).
→Higher doses (for example more than 10mg of glibenclamide ) rarely further improve
glycemic control and should be avoided.
→Due to their prolonged biological effect, sulfonylureas are given once or twice daily.
→the maximum recommended dose is 8 mg
→After absorption, sulfonylureas bind almost completely to plasma proteins especially albumin
on average 90-99%
→The volume of distribution is about 0.2 l/kg
→The biological effect persisting 24 hr or more, and is prolonged in the presence of renal
failure .
→used as monotherapy or in combination with others
Side effects of sulfonylureas:
Sulfonylureas are usually well-tolerated
1- The most common side effect is :hypoglycemia, with all sulfonylureas and especially with
long-acting such as chlorpropamide and glibenclamide
A good way to prevent hypoglycemia is to start therapy with sulfonylureas at a low dose. The
dosage may be increased at intervals of 2-4weeks until the glycemic target is reached.
2-Weight gain: with lesser degree than insulin
3-Sulfa allergy (rare)
4-cross placenta – fetal hypoglycemia
Note: Glyburide has minimal transfer across the placenta and may be an alternative to insulin
for diabetes in pregnancy
‫عالج السكري عند الحامل هو االنسولين‬
In general oral hypoglycemia agents don’t used in pregnancy, exception: glyburide.
5-Cholestatic jaundice

→Advantages: inexpensive , effectiveness

‫بس دكاترة السكري بفضلو عليهم ال‬

DPP4-I and SLGT2--I
→In these conditions’ sulfonylureas should not be used as first line therapy, but as second or
third line agents in type 2 DM:
Old age (≥75 years)
Renal impairment
Liver disease

→Sulfonylureas act directly on B-cells, leading to progressive dysfunction and worsening of

insulin secretion. Thus despite better glycemic control in the short term, diabetes could worsen
in the long term. The clinical result of this phenomenon is known as (secondary failure)

-------
Miglitinide (Glinide): Repaglinide / Nataglinide
MOA: enhance the secretion of insulin by blocking ATP-dependent K channel
Novonorm Repaglinide NovoNordisk Tab: 0.5, 1 , 2 mg
→short duration than sulfonylureas
Short acting, act only when the level of glucose in the blood is high, so it taken 30
min before meal.
SE:
1-hypoglycemia (most common)
2-less weight gain
Note: this drug has minimal renal excretion thus useful in patients with DM and
impaired renal function.
Glinides ‫ممكن يستخدمهم مريض عنده مشاكل بالكلية اما بالكبد ال‬
Sulfonylureas ‫ما بصير يستخدمهم مريض عنده مشاكل بالكلية او بالكبد‬

Pereglinide and Nataglinide are contraindicated with Gemfibrozil (lipid-lowering

drug) because it is an metabolizim inhibitor and may significantly increase their
effects
Gemfibrozil : Lopid (Pfizer) 300mg , 600mg , 900mg OD

They are used with caution in patient with hepatic impairment

֍ Dipeptidyl peptidase inhibitor:

Sitagliptin / Vildagliptin / Saxagliptin / Linagliptin
Januvia Sitagliptin MSD Tab: 25,50,100
Juvesta Sitagliptin Jerusalem Tab:25,50,100
Sita-Glu Sitagliptin Pharmacare Tab: 50,100
 Januet Sitagliptin+Metformin MSD 50/500 , 50/850 , 50/1000
Januet XR Sitagliptin+Metformin MSD 50/1000, 100/1000
Sitaglu-Met Sitagliptin+Metformin Pharmacare 50/850 , 50/1000

Galvus Vildagliptin Novartis Tab: 50mg

Eucreas Vildagliptin +Metformin Novartis 50/850, 50/1000

Onglyza Saxagliptin Astrazeneca Tab: 2.5, 5 mg

Tragenta Linagliptin Boehringer Ingellim Tab: 5mg

Tragenta duo Linagliptin + Boehringer Ingellim 2.5/1000
Metformin
Jentadue to Linagliptin + 2.5/1000
Metformin
DPP-4-I
MOA: inhibit the enzyme that is responsible for inactivation of incretin hormones such as GLP1,
so it increase incretin levels (GLP-1 and GIP), which inhibit glucagon release, which in turn
increases insulin secretion, decreases gastric emptying, and decreases blood glucose levels.

→Orally

→Used as a second-line or later

→Used as monotherapy or in combination, they have modest capability to decrease the level of
sugar so it is better to use it with another drug

→Saxagliptin metabolism involves the action of CYP 450 isoenzymes 3A4/5, leading to the
potential for interactions with inhibitors and inducers of this system.
(Such as ketoconazole, a strong inhibitor of the CYP 450 3A4/5 and P-glycoprotein systems)
(And diltiazem, a moderate inhibitor of the CYP 450 3A4 system).

→The most common adverse reactions occurring in 5% of patients or more who received DPP-
4 inhibitors were upper respiratory tract infection, nasopharyngitis, and headache with
sitagliptin
And upper respiratory tract infection, urinary tract infection, and headache with saxagliptin.

→The incidence of hypoglycemia is reportedly increased when sitagliptin is used with a

sulfonylurea or insulin; the risk is increased when saxagliptin is used with a sulfonylurea
→Other adverse events that have been identified from post-marketing reports of sitagliptin
include serious allergic reactions, including anaphylaxis, angioedema, and Stevens–Johnson
syndrome.

→Saxagliptin may decrease the level of lymphocyte and maybe stopped to prevent the
infection

→Alogliptin and saxagliptin may worsen the HF

→Unlike incretin mimetic, these drugs do not cause satiety or fullness and are weight neutral ‫ال‬
‫يؤثر على الوزن‬

֍ Alpha glycosidase inhibitors:

Acarbose / Miglitol
Prandase Acarbose Bayer Tab: 50, 100 mg
Acrose Acarbose Rafa Tab:50, 100 mg

MOA: inhibit alpha glycosides which convert starch and complex carbohydrate into simple
sugars (prevent their break down)
→ reduce glucose absorption
→Taken at the beginning of the meal

→Maybe used as monotherapy if HbAIc around the goal and the problem is with postprandial
glucose not fasting glucose

→SE: flatulence, floating, abdominal discomfort, diarrhea

Minimized by slow dose rotation
→Not recommended in patients with inflammatory bowel disease‫تهيج القولون( القولون العصبي‬, colonic
ulceration‫ تقرحات القولون‬, intestinal obstruction ‫تلبك معوي‬
→They don't cause hypoglycemia unless given with hypoglycemia causing drugs
→In this case for the treatment of hypoglycemia, we cannot give glass of orange juice because
the enzyme is inhibited, so give dextrose or glucagon are given.

֍ Sodium-Glucose Co-transportar2 inhibitor (SGT2I):

Dapagliflozin / Empagliflozin
 Foraxiga Dapagliflozin Astrazeneca Tab: 5, 10mg
Xigduo Dapagliflozin+ Astrazeneca 5/850 , 5/1000
Metformin XR: 10/1000
Jardiance Empagliflozin Boehringer Ingellim Tab: 10, 25 mg
Jardiance Duo Empagliflozin + Boehringer Ingellim 12.5/500 , 850 ,
Metformin 1000
5/ 500, 850 ,
1000
Steglatro Ertugliflozin MSD 5mg , 15mg

SGLT-2-I
Canagliflozin / Dapagliflozin / Empagliflozin

MOA: inhibit renal reabsorption of glucose

→This drugs also decrease reabsorption of sodium and causes osmotic diuresis
→May decrease the BP, especially if it is taken with diuretic.
→Not used to treat HTN
→Doesn't cause hypoglycemia unless it is taken with sulfonylureas, insulin, meglitinides

→Used as second or third therapy

→Given once daily in the morning before the first meal
→Don't taken in stage 4 and 5 renal disease (about one third of a dose is renally eliminated)

SE:

Female genital mycotic infection(vulvovaginal candidiasis)

UTI
Urinary frequency
Hypotension particularly in the elderly or patient on diuretic
‫ لمرضى السكري‬kidney failure ‫ ألنها تحمي من حدوث‬ACEI ‫افضل دواء لعالج الضغط لدى مريض السكري هو‬

֍ Incretin Mimetics:
Exentide/ liraglutide / dulaglutide
Byetta Exentide Lilly 5 , 10 mg
Victoza Liraglutide NovoNordisk 6mg/ml pen
Saxenda Liraglutide NovoNordisk 6mg/ ml pen
Trulicity Dulaglutide Lilly 0.75mg/0.5ml
1.5mg/0.5ml
MOA:
Improve insulin secretion / slow gastric emptying time/ enhance satiety/decrease
postprandial glucagon secretion / promot B-cell proliferation.
→REDUCE: wight / postprandial hyperglycemia

Incretin hormones are responsible for 60% to 70% of postprandial insulin

secretion.
Injectable (Sc)
‫لمريض سكري النوع الثاني كدواء مساعد لألدوية الفموية‬
Control basal insulin
SE: GI: nausea/vomiting /diarrhea /constipation

Amylinomimetics (synthetic amylin analogue):

SymlinPen pramlitinide SC injection: 120mcg

→ SC injection Immediately prior to meals

Amylin: is a peptide produced by beta cells and co-secreted with insulin

→MOA:
Suppress glucagon secretion
Suppress appetite
Improve satiety
Slow gastric emptying

→Indication: in adults patient with type 1 or 2 DM if it is not adequately controlled on mealtime

insulin (an adjunct to mealtime insulin)
When given with short or rapid insulin the dose of insulin should decrease by 50% to avoid
hypoglycemia

GLP1 agonist or DPP4-I ‫ بعد الوجبة االفضل نعطي‬glucagon ‫اذا هدفنا ننزل ال‬
→SE : Nausea/ vomiting / anorexia

___________________________________________________________

Bile acid sequestrants:

Colesevelam
Decrease lipid
and sugar (unknown mechanism)
Low risk of hypoglycemia
Weight neutral (does not increase or decrease the weight)
lipid ‫بنستخدمه لما بدنا ننزل السكر شوي وننزل ال‬
SE: constipation / dyspepsia
Should be taken with large amount of water
Given with meals because the bile acid is secreted with meals
Has multiple absorption drug drug interaction

—-
Dopamine agonist
Bromocrptin : decrease the sugar by unknown mechanism
SE: Nausea/ vomiting/ constipation / fatigue / headache / dizziness / asthenia /
somnolence /orthostatic hypotension

Therapy of treatment for type 2 DM:

→If HbA1C at diagnosis is ≤ 7.5 : one drug that does not cause hypoglycemia such
as Metformin
→If HbA1C is 7.5-8.5 : monotherapy or combination
→if it higher ex: 10 : combination or insulin
→if the patient is obese : metformin is a good choice because it decrease the
weight, doesn’t cause hypoglycemia and has positive effect for cardiovascular
system.
→start with metformin for 3 months, if the target is not reached, other oral
antihyperglycemic drug should be added.
→if the target doesn’t reach after 3 months of combination of 2 drugs: give triple
therapy.
→if the target doesn’t reach after the triple therapy:
-If the drugs were oral: transfer them to the injectable form
-If one of the drugs in the triple therapy is GLP-1-agonist: add basal insulin
-If the basal insulin is already included in the triple therapy: add GLP-1agonist or
mealtime insulin.
-If the patient is refractory patient: TZD or SLGT-2-I should be included in his
therapy of treatment.
-------
Agents that increase blood glucose:
Diazoxide
Proglycem (teva)
→nondiuretic thiazide
→increase blood sugar by direct inhibition of insulin secretion.
→useful in cases of insulinoma or leucine-sensitive hypoglycemia
→SE: sodium retention / GI irritation /changes in circulating WBCs.

Evaluation of the outcomes:

1-measure HbA1c at least twice yearly

2-ask patient with type 1 about the frequency and severity of hypoglycemia
3-screen for complication
Dilated eye exam: yearly for type 2
Once in first 5 years then yearly for type 1
Feet
Sensory loss
Nephropathy: by measure microalbumin in urine

4-check fasting lipid annually if the patient is on lipid lowering therapy

5-annual influenza vaccine
6-management of cardiovascular risk factor (smoking stopping / antiplatelet)

Note: if the diabetes is not controlled in the pregnant women, hypoglycemia will occur in the
baby after birth, that’s because that high level of blood sugar in the pregnant will reaches the
fetus through the placenta, so pancreas of the fetus used to secret high level of insulin. After
delivery the pancreas will continue to secret high level of insulin until it adapts with the new
situation. (it is a reversible functional postnatal effect)
Toxicity of antidiabetic drugs:
→Hypoglycemia occurs with sulfonylureas and Meglitinide because of stimulation of
insulin secretion.
- Other antidiabetic drugs such as biguanides, alpha-glucosidase inhibitors and glitazones
are not likely to cause hypoglycemia after acute overdose, but they may contribute to
the hypoglycemic effects of sulfonylureas, meglitinides, or insulin.
- The onset of hypoglycemia is usually within 8 hours (longer if extended-release
preparations, 18 hours or up to 24 hours)
- Hypoglycemia is profound and prolonged (up to several days)
- Recent impairment of hepatic or renal function will predispose patients to hypoglycemia
even at therapeutic doses (the elderly is particularly vulnerable).

Toxic dose:
For children: one tablet can cause fatal hypoglycemia (250mg of chlorpropamide) (5mg of
glipizide) (2.5mg of glyburide)
Adults: 2 tablets of sulfonylureas is a very toxic dose and cause hypoglycemia and coma
In a 79-year-old nondiabetic person, 5 mg of glyburide caused hypoglycemic coma.
With cytochrome inhibitor drugs, the toxic dose be lesser than that.
4mg of Repaglinide produce hypoglycemia in a nondiabetic 18-year-old patient.

Sever hypoglycemic coma occurred after injections of 800-3200 units of insulin

Clinical presentation:
Manifestations of hypoglycemia include: agitation, seizure, coma, tachycardia, decrease serum
potassium and magnesium level

Treatment
asymptomatic patient should be monitored for at least 8 hours after ingestion.
When the symptoms observed the treatment should be beginning.
Dextrose: is the most important antidote and can be repeated to reach certain level of blood
sugar.
If dextrose is not enough, insulin release blockers should be used, which are Octreotide,
Diazoxide.
Note: Glucagon is not considered as first-line therapy for hypoglycemia because of its slow
onset of action and reline on glycogen stores.
Alkalinization of the urine (using sodium bicarbonate) increase the renal elimination of
chlorpropamide.
Note: Forced diuresis and dialysis procedures are of no known value for other hypoglycemic
agents.

→Lactic acidosis: is rare but potentially fatal side effect of metformin

Occurs mainly in patients with: (Metformin is contraindicated in these cases).
Renal insufficiency / alcoholism / advanced age / after injection of iodinated contrast agents
resulted in acute renal failure.
Clinical presentation:
Malaise, vomiting, respiratory distress
Mortality rate in severe cases is as high as 50%
Treatment of lactic acidosis
Sodium bicarbonate.
Hemodialysis removes metformin, and that also help correct sever lactic acidosis (when sodium
bicarbonate is not enough).

DM and Pregnancy:
Regular Insulin and NPH are the best choices for pregnant diabetic patient (glulsine and glargine
are contraindicated)
Metformin can be given for pregnant in case of insulin resistance

DM and breast feeding:

Regular insulin and NPH are the best
Metformin can be given
Glibenclamide may be taken, infant should be observed for symptoms of hypoglycemia after
the start of therapy.
Other oral antidiabetics should not be taken.
 “At the end, we will not remember the most
beautiful face and body. We will remember the most
beautiful heart and soul” ♥
 Topic 7: Body Hormones
Sex hormones:
Gonadotropin-releasing hormone (GnRH) and Analogs: GnRH: it is produces from the
hypothalamus and work on pituitary gland and stimulate it to produce FSH and LH
GnRH agonist:
Leuprolide/Gonadorelin /triptorelin/ Nafarelin /Goserelin /Histrelin
Two ways to use it:
1.short-term administration (every 1-4 hours) like in the body→this will stimulate the
synthesis of LH and FSH
This way is used to treat some type of infertility (‫)اللي هي لما تكون المشكلة بالتبويض‬
2.daily administration 2-4weeks with high doses→this reduces the production of LH and
FSH→lead to decrease production of gonadal steroids (estrogen and androgen).
This way is used to treat early puberty, hormone-dependent cancer such as prostate
and breast cancer.

They are contraindicated in pregnancy and breast feeding

Menotropin (HMG) → (human menopausal gonadotropin) it is used as the source of FSH

→isolated from the urine of postmenopausal women and it is a

mixture of LH and FSH
LH→ luteinizing hormone →trigger ovulation and development of corpus luteum
→stimulate estrogen and progesterone in women and testosterone in men
FSH → follicle stimulation hormone to develop and mature of ovum in women
→stimulate spermatogenesis in men
HCG →(human chorionic gonadotropin) to maintain progesterone production of corpus
luteum during early pregnancy. (it is used as the source of LH)

HMG Menogon Amp (refrigerated) Ferring

Corresponding to 75+75 IU ‫الل توخدهم ما‬
‫ممكن ي‬
FSH + LH IM or SC ‫تحتاج ابرة‬pregnyl
(with NaCl amp as ‫النو بسد عنها‬
solvent)
Urofollitropin Fostimon Amp: 75IU IBSA
(purified FSH from
the urine of
pregnant women)
Urofollitropin Follitrin Vial: 75IU Ferring
With solvent
Coriforllitropin alfa Elnova Amp: MSD
(Long-acting FSH 150mcg/0.5ml
agonist) To treat infertility
(one injection per
week)
Follitropin alfa Gonal Pre-filled pen: 75, Merck
(recombinant FSH 300, 450, 900IU
products) To stimulate a
follicle (egg) to
develop and
mature (treat
infertility)

HMG HMG Massone Vials with solvent

Menopur Amp: 75IU Ferring
With NaCl vials as
solvent
(refrigerated)
SC
 HCG Pregnyl Amp:5000IU MSD ‫التفجي‬ ‫ر‬ ‫تسىم ابرة‬
(refrigerated) 14 ‫وتستخدم يف اليوم‬
‫من الدورة‬
IM or SC ‫بنحك‬
‫ي‬ ‫بعد ما توخد االبرة‬
‫للمريضة ما تعمل فحص‬
‫أسبوعي‬
‫ر‬ ‫حمل مدم‬
‫ه عبارة عن‬ ‫بعدها النو ي‬
‫هرون الحمل مصنع‬
‫يعط نتيجة‬ ‫ي‬ ‫فممكن‬
‫وهمية انها حامل‬
‫لحن يطلع من‬ ‫فبنستن ى‬
‫الجسم‬
Choriogonadotropin Ovitrelle Solution for Merk Serono
alfa injection
(suncutaneously) ‫لتحفي‬
‫ر‬ ‫تستخدم أيضا‬
‫االباضة‬
(refrigerated)
(in the pregnancy test, the level of HCG is detected) (it is act like LH function)
HMG or FSH products injected over a period of 5-12 days causes follicular growth and
maturation, then HCG is injected one day after the last dose of FSH to induce ovulation.
SE: ovarian enlargement.

Triptorelin Decapeptyl Amp:0.1mg/1ml Ferring Is an analog of

acetate (refrigerated) gonadotropin-releasing
hormone
Under most
circumstances, woman
is not likely to get
pregnant while using
Triptorelin Decapeptyl Vial:22.5mg , GnRH agonist, and it
should not be used in
embonate depot 3.75mg
pregnant women
because it decrease the
production of estrogen
which can cause
miscarriage.
It is used to treat
endometriosis and
fibroids in women, and
prostate cancer in men
 nafarelin Synarel Nasal spray Pfizer
To treat
endometriosis and
early puberty.

GnRH receptor antagonist:

Ganirelix / Abarelix / Cetrorelix
They are used to prevent premature ovulation (early release of eggs from the ovary) in
women having fertility treatment and who having ovarian stimulation ( stimulation of
the ovaries so that they produce more eggs), also to treat prostate, breast cancer,
endometriosis and uterine fibroids
Ganirelix Orgalutran Syringe: 0.25mg MSD
Certroliex Cetrotide Vial: 0.25mg EMD SERONO

Gonadal Hormones:
All gonadal hormones (estrogens and androgens) are synthesized from cholesterol.
They are necessary in the body for:
1-Conception ‫الحمل‬
2-Embryonic maturation ‫الهرمونات تتحكم في جنس الجنين وتطوره‬
3-Puberty

The gonadal hormones are used therapeutically for:

1-Replacment therapy ‫تعويض النقص في بعض الهرمونات‬
2-Contraception ‫منع الحمل‬
3-Management of menopausal symptoms ‫عالج اعراض ما بعد انقطاع الدورة الشهرية‬
4-Cancer chemotherapy.
Menstrual cycle (1-28 day) (4 phases):
1.Bleeding (day 1-7) low level of estrogen and progesterone
2.follicular phase (day 7-13) high level of estrogen and low progesterone
3.ovulation phase (day 14) low level of both (the ovulation occurs 10-16 hours after LH peak
which can be detected using the ovulation test (‫)افضل وقت ينعمل فيه بعد العصر‬, and the intercourse should
be done during this interval to get pregnant)

Note: Contraception is most successful when intercourse takes place from 2 days before ovulation to
the day of the ovulation).

11 ‫ من يوم‬،‫ اخر يوم مسموح يدخل فيه سبيرم هو اليوم العاشر بعد اول يوم بالدورة‬،‫في حال ما كانت بتوخد مانع حمل وما بدها تحمل‬
‫ هاد ينطبق اكتر اشي اذا الدورة كانت منتظمة‬،‫ ممنوع يدخل فيه سبيرم وبعد هيك عادي‬22 ‫ليوم‬

4.luteal phase (day 15-28) high level of both, but progesterone level is higher
Classification of estrogen:
→Natural: 17B-estradiol / Estrone / Estriol
→Synthetic:
➔ Steroidal: Ethinylestradiol / Mestranol
➔ Nonsterodial: Diethylstilbestrol (DES) / Dienestrol
Testosterone is converted to 17B-estradiol (the most potent natural estrogen) by aromatase
enzyme.
---
Selective estrogen receptor modulator (SERM):
Tamoxifen / Raloxifene / Clomiphene

Antiestrogens:
Fulvestrant /Danazol /SERM

Oral progestin:
Desogestrol / Norgestrol / Levonorgestrol/ Norethisterone
Norethindrone / Norethindrone acetate / Medroxyprogesterone
Drospirenone / Norgestimate

Only estrogen:

Estradiol as Estrofem Tab:1, 2mg Novo nordisk

(as hemihydrate)
Estradiol Progynova Tab: 2mg Bayer
(as valerate)
Estriol Ovestin Vaginal .Cream with MSD
applicator: 1mg/g

Therapeutic uses of estrogen:

1-Postmenopausal hormone therapy.
Postmenopausal symptoms: hot flashes, osteoporosis, increase the risk of
cardiovascular disease, vaginal atrophy, sever sweating
→because of decreasing the estrogen level
Using the lowest effective dose for the shortest possible time.
Progesterone is included with the estrogen therapy to reduce the risk of endometrial
carcinoma. ‫الل بدها تستخدمهم تكون قايمة الرحم‬
‫او ي‬
Amount of estrogen in the replacement therapy is less than oral contraceptive →less
side effects.
If the symptoms are only local (vaginal atrophy), then woman should be treated
vaginally.

Other uses (with progesterone)

2-Contraception ‫منع الحمل‬
3-Primary hypogonadism ‫وجي كفاية‬ ‫ى‬
‫ال يتم انتاج اسي ر‬
4-premature menopause or premature ovarian failure.
Synthetic estrogen→prolonged action, higher potency, stored at adipose tissue (slow
released)

SE of estrogen:
1-Breast tenderness (because of cell proliferation after using estrogen) (common)
2-increased the risk of MI and thrombosis (because of enhancing coagulation)
3-Edema and HTN (estrogen has some mineralocorticoid action→water retention)
4-risk of breast and endometrial cancer (so it is combined with progesterone which has
anti-estrogen effect)

SERM (selective estrogen receptor modulator)

Tamoxifen, Raloxifene, Clomiphene

Tamoxifen Tamoxifen teva Tab: 10, 20mg Teva

Nolvadex (brand) Tab:10mg Astrazenca

Raloxifene Raloxifene teva Tab: 60mg Teva

Evista Tab: 60mg Lilly

Clomiphene Clomiphene Medo Tab: 50mg

Ovaclomin Tab: 50mg Birzeit
Ikaclomin Tab: 50mg Teva
Clomid Tab: 50mg Sanofi

They work as estrogen agonist or antagonist depending on the tissue type.

→Antagonist effect in the breast tissue→they are used as chemotherapy in breast
cancer or as prophylaxis in high-risk women
→Raloxifene → agonist in bone →increase bone density →treat osteoporosis in
postmenopausal women.
→Tamoxifen (But not Raloxifene) →agonist in endometrium →increase risk of cancer.
It is used to treat metastatic breast cancer or as adjuvant therapy in mastectomy of
radiation for breast cancer.

(Raloxifene and Tamoxifen category X →fetal harm)

→Clomiphene act centrally as partial estrogen agonist→ increase the secretion of LH

and FSH (stimulate of ovulation) (to treat infertility associated with anovulatory cycles
(‫)ينشط االباضة‬.
‫ أيام‬5 ‫بيتم وصفهم لتنشيط االباضة ابتداء من اليوم الخامس للدورة حبة صباحا ومساء لمدة‬
They are used as off-label use to treat infertility in men (block estrogen action on the
pituitary gland→increase FSH and LH →enhance sperm production ( ‫يعالج قلة عدد‬
)‫الحيوانات المنوية‬
SE:
Raloxifene: hot flashes, leg cramps ‫تشنجات عضلية اسفل االطراف‬, increase the risk of
thrombus synthesis

Tamoxifen: hot flashes, nausea, increased risk of endometrial cancer

Clomiphene: flashes, visual disturbances, ovarian enlargement, increased risk of

multiple births

Antiestrogens:
Fulvestrant /Danazol/SERM
(they are not androgen nor progesterone)
MOA: block estrogen receptors
Fulvestrant Faslodex Per-filled syringe: Astrazeneca
250mg/5ml
IM
(refrigerated)
 Danazole Danol Cap:200mg Sanofi

→Fulvestrant: antagonist in all tissue

It is used to treat breast cancer after tamoxifen
→Danazol: testosterone derivative →has antiandrogen and antiestrogen activity.
It inhibits gonadotropins in men(testosterone) and women (LH/FSH)
It is used to inhibit ovarian function, treat endometriosis, treat fibro cytosis in breast.
Cat : X (cause fetal harm)
SE: edema, deepening of the voice and decrease breast size, hepatocellular disease.
Contraindication: pregnant women, patients with hepatic disease.

Progestogens
Only progesterone:
Desogestrel Cerazette Tab: 0.075mg MSD
28 tablets

Levonorgestrel Microlut Tab: 52mg Bayer

‫ حبة وتستخدم بشكل‬35 ‫يحتوي‬
‫متواصل‬
Mirena Intra-uterus device Bayer

Norethisterone Primolut Tab:5mg Bayer

Premonor Tab:5mg Birzeit

Allylestrenol Progest Tab Birzeit

It is used to treat recurrent and threatened miscarriage ‫ ثتبيت الحمل‬and to prevent premature labor in
pregnant women ‫منع الوالدة المبكرة‬

Progesterone Endometrin Vaginal tablets Ferring

 ‫لتجهيز الرحم قبل ارجاع‬
‫البويضة المخصبة‬
Utrogestan Soft Cap: 100, 200mg CTS
Oral or vaginal route
Crinone Vaginal gel Merck Serono
Ovaprost Vaginal or rectal Jepharm
supp: 400mg
Uterogestan→ it is used as ovules for prevent repeated abortion after invitro
fertilization ‫مثبت حمل خالل الثالث اشهر األولى من الحمل بعد ذلك يتم ايقافه‬

Oraly→for other uses such as irregular menstruation, bleeding…..

Medroxyprogesterone Provera Tab: 5, 100 mg Pfizer

Oralute Tab:5mg Birzeit
Depo-provera Injection: 150mg Pfizer
Hydroxyprogesterone Luterone Amp: 250, 500mg Birzeit
Progesterone Amp:500mg Bayer
retard pharlon

Dydrogesteron Duphaston Tab: 10mg Abbott

‫بالعادة يستخدم كمثبت‬
‫حمل‬

Sources of progesterone:
Female→ corpus luteum in the second half of menstrual cycle, placenta
It is important for the development of the endometrium that can accommodate
implantation of embryo.
High level of progesterone inhibits production of gonadotropins and prevent further
ovulation.
If the conception does not take place, the release of progesterone from the corpus
luteum decrease and the menstruation occur.
Male→testes
Both→ adrenal cortex
Note: it is a precursor for estrogens, androgens and adrenocortical steroids.

Therapeutic uses of progesterone:

1-Contraception (with or without estrogen)→if it is taken before pregnancy occur, by
making negative feedback and prevent the production of LH, FSH
2-Manaegment of some type of infertility → it is important for the maturation of the
endometrium if it is taken after the conception occur.
3-control of dysfunctional uterine bleeding(‫فية الدورة‬ ‫ )نزيف بغي ى‬and dysmenorrhea ( ‫الم‬
‫ر‬
‫اليوستاجالندين المسببة لالنقباضات وااللم‬
‫)الدورة الشديد النه سوف يقلل من مستويات ر‬
‫)تييل الدورة اذا تأخرت ى‬
‫فية وما كان ف حمل ى‬
4- Enhancing menstruation (‫وحن لو طلع يف حمل بتثبته‬ ‫ي‬
Dose: 5mg Q 12 hr for 5 days (oralute→ ‫ أيام‬5 ‫) حبة صباحا ومساء لمدة‬

PremoNor→

‫ حبة صباحا ومساء عل طول المدة ي‬: ‫لتأخي الدورة‬

‫الل بدها تأخر فيها ابتداء من قبل موعد الدورة بخمس أيام‬ ‫ ر‬-1
‫ مرات يوميا‬3 ‫ أيام بتوخد حبة‬5 ‫واذا كان ضايل لموعدها اقل من‬

‫ أيام وبعدها بتوقفه ورح ر ي‬5 ‫ حبة صباحا ومساء لمدة‬:‫ لتييل الدورة يف حال تاخرت‬-2
3 ‫تيج الدورة خالل يوم ل‬
‫أيام‬
‫تيج الدورة ع حسب مدة الدورة بتضل‬‫ يوم وبعدها بتوقفه عشان ر ي‬25 ‫ حبة صباحا ومساء لمدة‬: ‫لتنظيم الدورة‬-3
‫تيج الدورة وبتتكرر هاي العملية‬ ‫ى‬
‫ يوم وبتوقفه عشان ر ي‬25 ‫موقفته لما تخلص بيجع توخد حبة صباحا ومساء لمدة‬
‫ شهور ى‬6 ‫ ل‬3 ‫مدة‬
.‫لحن تنتظم‬

‫ ساعات‬8 ‫ حبة كل‬:‫لتخفيف االم الدورة‬-4

------
How does progestin work in contraception???
1- Inhibit the production of FSH,LH (estrogen also work by this mechanism)
2- Thickens the cervical mucus, thus prevent the transport of sperms

What is the advantage of synthetic progestin over natural?

They are more stable to first pass metabolism
 Oral contraceptive:
Total regimen is 28 day = (take active pills for 21 to 24 days) + (No pills or placebo for 4 to 7 days)

‫تناول الدواء يبدأ عادة من اليوم الخامس للدورة‬

The menstruation will occur during the hormone-free interval

Oral contraceptive contain:

1-progesteron only (they are used during breastfeeding because estrogen

inhabits milk production)
2-combination of estrogens (most commonly ethinyl estradiol) and
progesterone

Drug contain Combination:

Estradiol + Activelle Tab: 1+0.5mg Novo nordisk
Norethisterone Eviana Tab: 0.5+0.1mg Novo nordisk
Novofem Tab: 1 + 1 mg Novo nordisk
12 white tabs
contain
combination
16 red tabs contain
only estradiol
Note: start with red
tabs
Trisequens 28 tablets
Start with blue tabs
(2mg estradiol+1mg
northisterone)
Then white tabs
(estradiol 2mg)
Then red tabs
(estradiol 1mg)
→indicated for hormonal replacement therapy, mot as contraceptive.
Estradiol+ Progyluton 21Tabs Bayer
Norgestrel 11 white tab
contain estradiol
only, start with Biphasic pills
them
10 red tabs contain
combination
➔ It does not used as hormonal contraceptive, it is used in hormone replacement
therapy after menopause, or to treat irregularities pf menstrual cycle ‫لتنظيم الدورة‬
Ethinylestradiol+ Diane 35 Tab Bayer
Cyproterone Estelle 35 Tab Taro

→it is used to treat moderate to severe acne (related to androgens: cyproterone

is an testosterone antagonist) or hirsutism in women of child-bearing age. It is
used when other treatment such as local antibiotic have failed
Ethinylestradiol + Microdiol Tab: 0.03+0.15 MSD
Desogestrel 21 tabs
Mercilon Tab :0.02+0.15 MSD
21 tabs

Ethinylstradiol+ Yasmin Tab: 0.03 Bayer

Drospirenone 21 tabs
Yaz Tab :0.02 Bayer
21 tabs
Ethinylstradiol+ Yasmin plus 28Tabs Bayer
Drospirenone+ Yaz plus 28Tabs
Levomefolate
➔ The last 4 tabs contain only levomefolate which is the primary active form of
folate (metabolite of vit B9) for preventing neural tube defects in offspring
conceived while using the product or shortly after discontinuing it (when woman
take birth control pills, the body unable to turn folic acid into levomefolate as
easily as before)
➔ Yaz is approved for treating premenstrual dysmorphic disorder (PMDD) and for
acne for women who also need oral contraceptive (yasmin is not approved for
them)
 ➔ Drospirenone dose not has androgenic effect and it prevent salt and water
retention elicited by estrogen, thus prevent increasing in blood pressure and
body weight.
Ethinylestradiol+ Evra Patches (3) for 3 Janssen
Norelgestromin weeks, then free
week

Ethinylestradiol+ Nuvaring Vaginal ring MSD

Etonogestrel

Etonogestrel has been linked to multiple serious side effects including blood clotting.
Ethinylestradiol + Microgynon Tab Bayer
Levonorgestrel 21 tablets
From the third day Monophasic
of period

Ethinylestradiol+ Gynera Tab:0.03+0.075 Bayer

Gestodene Harmonet Tab:0.02+0.075mg Pfizer
Meliane Tab:0.02+0.075 Bayer
Minulet Tab: 0.02+0.075mg Pfizer
Minesse Tab: 0.015+0.06mg

Gestodene →has no androgenic effect.

Chlormadinone + Belara Tab: Richter

Ethinyl estradiol 21tab Pharmacare

Chlormadinone →has anti-androgen activity.

Monophasic combination pills: contain a constant dose of estrogen and
progesterone
Biphasic combination pills: contain constant dose of estrogen, but the dose of
progesterone increased about halfway through the cycle.
 Triphasic combination pills: dose of estrogen and progesterone changes every
7 days.
‫(الل‬
‫بتصي من خامس يوم بالدورة ي‬
‫ر‬ ‫اذا كانت المرأة اول مرة بدها توخد مانع حمل بتبلش من اول يوم الدورة وبعدها عادي‬
)‫تيج بعد ما توقف الدوا‬ ‫ى‬
‫يومي لحن ر ي‬‫ أيام بدون دوا النو الدورة بدها ر‬7 ‫هو نفسه بكون بعد‬
21 tablet-taking days → then 7 days pill-free days (bleeding)‫يومي من إيقاف الدوا‬ ‫ → ممكن ر ي‬start
‫تيج الدورة بعد ر‬
the next 21 tablets from the 5th day of cycle

How to calculate the ovulation day?

It is 14 days before the first days of the next cycle
Ex: (if the cycle starts at day 28 of the month, then the ovulation day is on day 14 of
that month)
‫كمان قبل االباضة بكم يوم بتبلش الحرارة تيل ف لما تحس انو يف نزول بالحرارة معناها االباضة قربت‬
There is (continuous dosage products) → taking pills for 84 days then 7 free or low-
dose. → produce 4 menstural periods per year

Lybrel → taking pills for 365 days→ suppress menstruation completely.

Note: if a pill is missed or vomited within 2 hours of taking it→take an extra

pill
Adverse effects of oral contraceptives:
→Estrogens
Breast fullness, tenderness, may be carcinoma
Fluid retention, increased HTN
Headache, nausea

→Progestins
Depression, weight gain, changes in libido, hirsutism, acne (because it has anti-
estrogen effect)
Note: disprienone, Norgestimate do not cause hirsutism and acne because they have
less androgenic activity.
Irregular and unpredictable menstrual bleeding.
Thrombotic disorders are rare side effects and more common among women over
35 and smokers.
Progestin-only contraceptive are associated with more ectopic pregnancies than
another hormonal contraceptive.

Estrogens and progesterone decrease the risk for ovarian and cervical cancer.
Contraindication of oral contraceptive:
Thrombotic disease, estrogen-dependent neoplasms, liver disease, pregnancy.
Using with precautions:
Combination pills should not be used in patients over the age of 35 and smokers
Liver enzyme inducer such as antibiotic reduce the effectiveness of contraception.
-----------

Cyproterone: it is a synthetic progesterone derivative with antiandrogenic and

progesterone-like activity.
Cyproterone Androcur 10 Tab:10mg Bayer Used mostly
acetate to treat male
characteristics
in females
‫لعالج الصفات‬
‫الذكورية وحب‬
‫الشباب المرتبطة‬
‫بارتفاع الهرمونات‬
‫الذكورية عند‬
‫النساء‬
Androcur 50 Tab:50mg Bayer Used mostly
to treat
 prostate
cancer

Antiprogestin:
Mifepristone (RU-486): progesterone antagonist with partial agonist activity→used
in early pregnancy to induce abortion
Usually with Misoprostol (prostaglandin analog) to induce uterine contraction.
SE: significant bleeding and incomplete abortion.
Misoprostol Cytotec Tab: 200mcg Pfizer
(controlled drug)

---
Hormonal contraceptive can be found in the form of:
→Transdermal Patch (contain ethinyl estradiol and norelgestromin)
3 patches applied for 3 weeks; one week is free

→progestins only pills: usually contain norethindrone

Used for beast-feeding women (because progestins do not affect milk production)
Women intolerant to estrogen ‫مش قادرة تتحمل االعراض الجانبية‬
Smokers (because the estrogen increases the risk of thrombosis)
SE: irregular menstrual cycles.

→Injectable progestin: injection every 3 months (IM/SC)

SE: weight gain (common)
Increase risk of osteoporosis and fractures (not recommended for more than 2 years).

→Progestin implants (subdermally): contain Etonorgestrel

Continuous release of drug for 3 years (the effect is totally reversible)
SE: irregular menstrual bleeding and headache

→Progestin intrauterine device: contain levonogestrel

 Effective for 3 to 5 years
It should be avoided in patients with pelvic inflammatory disease and history of ectopic
pregnancy.

→Postcoital (emergency) contraception

Uillpristal Ella Tab: 30mg CTS
(controlled drug)
Can be used for up to 120 hr (5days) of unprotected intercourse
It should be taken as soon as possible

Note: levonorgestrel can also be used for emergency contraceptive.

It can be used within 72 hours after unprotected sex ( within 24 hr is more effective).
One dose of 1.5mg

Levonorgestrel Microlut Tab: 0.03mg Bayer

Some additional information:

Human anti-D Immunorho Pre-filled syringe: KEDRION
immunoglobulin 300mcg
KamRho-D Vial : 150mcg KAMDa

MOA?
The anti-D immunoglobulin neutralizes any RhD positive antigens that may have
entered the mother’s blood during pregnancy. So the body will not produce
antibodies against positive antigens. In the next pregnancy, there this no antibodies
will attack the new fetus.
(that happened when the fetus has positive Rh and the mother has negative Rh)
 When dose it given?
Within 72 hours after the heavy bleeding starts or after an operation to remove the
miscarried pregnancy.
It is also administered routinely during the third trimester of pregnancy if the mother
has negative RhD.
It can be given by two ways:
A 1-dose treatment: during 28-30 weeks of pregnancy
A 2-dose treatment: during the 28th week and the other during the 30th week of
pregnancy.
------
Prefert Vaginal gel MEDintim

It is used on the 3 most fertile days of female cycle (time of ovulation) (day 14)
Why?
It is a lubricant to promote the motility of sperms and to make the environment (PH
and mucus viscosity) ideal for conception.
----
Dinoprostone Prostin E2 Vaginal Tab: 3mg Pfizer
Propess Vaginal tab: 10mg Ferring

It is a prostaglandin, a hormone-like substance (like oxytocin), used topically in

pregnant women to relax the muscles of cervix (opening the uterus) in preparation
for inducing labor at the end of a pregnancy.
Oxytocin Oxytocin Amp :10IU/1ml To induct and
stimulate labor

To stop
postpartum
uterine bleeding.
 Oxytocin also stimulate milk ejection from the breast.
---
Methylergometrine Methegrine Tab:0.125mg Novartis

It is a synthetic analog of ergometrine, it is used to stop uterus bleeding

It is work by increasing the rate and strength of contractions and stiffness of the
uterus muscles.
----
Aromatase inhibitor: Nonsteroidal aromatase inhibitors, decrease the amount of
estrogen in the body, to treat breast cancer.
Ex: Anastrozole, Letrozole

Anastrozole Anastrozole Teva Tab: 1mg Teva

Arimidex Tab: 1mg Astrazeneca

Letrozole Letrozole Teva Tab: 2.5mg Teva

Femara Tab: 2.5mg Novartis
Letrozole is also used to induce an egg to develop and release in women who are not ovulating
naturally.

Nonoxynol-9 Glovan Vaginal ovules Teva

It is a surfactant that destroys sperm cell walls and blocks entry into cervix. It is used half
an hour before the intercourse.

Diaphragms: intravaginally device to prevent sperms from entering, it is applied 6 hours

before the intercourse and 6 hours after (not more than 24 hours)
Cervical cap: intravaginally device it is applied 6 hours before the intercourse and 6
hours after (not more than 48 hours)

--------------------------------------------------------------------------------------------------------------

Androgens
 Testosterone→is the most important androgen.
5 alpha-dihydrotestosterone (DHT)→ the active form of testosterone.

TESTOSTERON Androgel Gel: 50mg CTS

Testoviron depot Amp:250mg Bayer
Nebido Amp:1000mg Bayer
Testomax Sachets: 25,50mg Perrigo
Sustanon Amp:250mg/ml Aspen
Androxon Cap: 40mg MSD
testocaps

Mesterolone → is an androgen and anabolic steroid medication which is used mainly

in the treatment of low testosterone levels.
Mesterolone Proviron (brand) Tab: 25mg Bayer

Nandrolone (19-nortestosterone)→is an androgen and anabolic steroid which is used in

the treatment of anemias, cachexia (wasting syndrome), osteoporosis, breast cancer.
Nandrolone Decadrol Depot Amp (IM): 25, 50mg Birzeit

Functions of androgens:
-Normal maturation in the male
-Sperm production
-Increase synthesis of muscle proteins and hemoglobin (anabolic effect)
-Decrease bone resorption.

Uses of androgens:
-Hypogonadism
(primary→caused by testicular dysfunction)
(secondary→due to failure of the hypothalamus of pituitary)
-Chronic wasting associated with HIV or cancer
-Increase body mass and muscles strength (unapproved use)

Adverse effects of androgens:

In females:
-Acne
-Voice deepening
-Facial hair
-baldness
-Menstrual irregularities.

→should not be taken by pregnant women because of possible development effects

of the female fetus.

In males:
-Impotence ‫جنس‬
‫ي‬ ‫ضعف او عجز‬
-Gynecomastia ‫زيادة حجم الثدي‬
-Baldness
-Decreased spermatogenesis

In children:
-Abnormal sexual maturation
-Premature closing of the epiphyseal plates

In athletes:
-Hepatic abnormalities
-Reduction of testicular size
-Major mood disorders and aggression ‫زيادة العصبية والتوتر‬

In general:
-Increase LDL and decrease HDL
-edema

Antiandrogens:
Finasteride, dutasteride → inhibit 5 alpha reductases resulting in the decreased
formation of dihydrotestosterone.
Use: treatment of benign prostatic hyperplasia, excessive hair growth in women.
Also finasteride can treat male pattern hair loss by blocking production of male
hormone in the scalp
Finasteride Finasteride teva Tab Teva
Finasam Tab: 5mg Sama
Prostanil Tab: 5mg Beit Jala
Fenesia Tab: 1mg Beit Jala
Propecia Tab:1 mg MSD
Pro-cure Tab: 5mg MSD
Dose: 1 mg to treat bald, 5mg to treat BPH
Dutasteride Avodart Soft cap: 0.5mg GSK
Duodart: Tab: 0.5/0.4 mg GSK
With tamsulosin
Dutasteride teva Soft cap: 0.5mg Teva

Flutamide→ receptor antagonist

Bicalutamide →androgen receptor antagonist
Bicalutamide Gasodex Tab: 50mg AstraZeneca

Use: treatment of prostatic cancer

 Phosphodiesterase inhibitors (PDE-I)
Sildenafil Sildenafil teva Tab: 50, 100mg Teva
Viagra (brand) Tab:25, 50, 100mg Pfizer
Revatio Tab: 20mg Pfizer
Sinagra Tab: 50mg Jepharm
Fortex Tab: 50mg Beit Jala
v-care Tab: 50, 100mg Pharmacare
Sil-on Tab: 50, 100mg
Duration: 4-5 hr
Tadalafil Cialis (brand) Tab: 20mg Lilly
Tada-V Tab: 10, 20mg Jepharm
Siafil Tab: 5, 20mg Birzeit
Talista Tab: 10, 20mg Pharmacare
Onset: ½ hour
Duration:36 hr

Vardenafil Levitra Orodispresible Tab: Bayer

10, 20mg

They are used to treat erectile dysfunction, prostatic hyperplasia, pulmonary arterial
hypertension.

Prolactin-releasing factor (PRF):

Secretion of prolactin from pituitary gland is controlled by both:
1.stimulation of PRF
Antipsychotic, Antidepressant, Anti-anxiety →decrease dopamine →stimulate
prolactin production →to treat lactation failure
2.inhibition of dopamine
Bromocriptine: agonist on D2 receptor (and antagonist on D1 receptor)
Cabergoline: more selective on D2 receptor
 Cabergoline Dostinex (brand) Tab: 0.5mg (2 or 4 or 8 tabs) Pfizer
Goline Tab: 0.5mg (2 tabs) Birzeit
Caberline Tab: 0.5mg (2 tabs) Jepharm
Cabotrim Tab: 0.5mg (2 or 8 tabs) Trima
Bromocriptine Parlodel Tab: 2.5mg Novartis

It is a dopamine agonist to decrease prolactin level in the body

Uses:
1-prevent feeding after labor (take 1mg once time) ‫(حبتي‬
‫ر‬ ‫لمنع الرضاعة بعد الوالدة ر‬
‫مباشة‬
)‫مع بعض خالل اول يوم بعد الوالدة‬
‫لتنشيف الحليب بعد ى‬
2-suppression of established lactation ( 0.125mg q 12 hr) ‫فية من‬
)‫ ساعة‬12 ‫الرضاعة (نصف حبة كل‬
3-for hyperprolactinemia (0.25mg twice a week) ‫والكتي خاصة‬
‫ر‬ ‫الي‬
‫لتقليل مستوى هرمون ر‬
)‫ أيام‬3 ‫لتحفي الحمل (نص حبة كل‬
‫ر‬
) high level of prolactin in the body may cause infertility)
‫طبيع‬
‫ي‬ ‫تعتي مانع حمل‬
‫الرضاعة الطبيعية ر‬

Growth Hormone
Agonist:
Somatropin, somatrem
Somatropin Zomacton Vial:12 IU Ferring
Gentropin Pen:16IU Pfizer
Vial:36 IU
Omnitrope Vial:5, 10, 15mg Sanofi
/1.5ml
Norditrop Vial: 10, Novo Nordisk
15mg/1.5ml

GH is released from pituitary gland with highest level during sleep, and its secreation
decreases with increasing age.
Administration: SC or IM , half life 25 min→sufficient to induce insulin-like growth by
the liver which is responsible for the GH-like actions
 It is used in children with growth hormone deficiency.
In adults: to treat cachexia ‫معي‬
‫فقدان الوزن والضعف بسبب مرض ر‬, AIDS wasting ‫فقدان الوزن‬
‫لدى مرض االيدز‬
‫ يزيد خطر اإلصابة بالسكري‬،‫ وجع عضالت ومفاصل‬،‫ تجمع السوائل بالجسم‬:‫من االعراض الجانبية‬
Should not be given to children with closed epiphysis (to prevent acromegaly) ‫ال يجوز‬
‫اعطاؤه بعد اكتمال نمو العظام عند الطفل‬

GH antagonist: pegvisomant
Pegvisomant Somavert Vial: 10, 15, 20mg Pfizer
Administered SC to treat acromegaly.

Anti-diuretic Hormone (ADH, Vasopressin)

It causes water retention by acting on the renal tubules.
Vasopressin: short acting(2-6hr)
Desmopressin: long acting(10-20hr)
Desmopressin Minirin Tab: 0.1, 0.2mg Ferring
Melt: 120mcg
Solution
Nasal spray

Uses of desmopressin:
1-treatment of severe central diabetes insipidus )‫السكري الكاذب بسبب نقص هرمون‬ADH)
2-noctural enuresis: by reducing nighttime urine production. ‫التبول الالرادي‬

Vasopressin used as substitute for epinephrine in cardiac arrest with asystole ‫يستخدم يف‬
‫عملية انعاش القلب‬

Thyroid Hormones
Triiodothyronine (T3)
Tetraiodothyronine (T4, thyroxine)
→they are important in regulation of growth and development, body temperature, and
energy levels.
Hypothyroidism
→Symptoms:
Cold intolerance/ weight gain / fatigue / decrease appetite
→Etiology:
Simple goiter ‫نقص اليود‬
Ablation of thyroid gland ‫استئصال الغدة الدرقية‬
‫ى‬
Congenital ‫خلق منذ الوالدة‬
‫ي‬
‫ى‬
Hashimoto disease ‫ذات يستهدف فيه الجسم الغدة الدرقية مما يقلل انتاج الهرمونات منها‬
‫مناع ي‬
‫ي‬ ‫مرض‬
→complication:

‫ تأخر ي‬/‫)لسان ورقبة سميكة‬

Cretinism in infant and child (‫عقل‬
Myxedema in adult (‫جلد سميك وجاف‬/‫باليد‬
‫الشعور ر‬/‫قلة الطاقة بالجسم‬/‫كسل‬/‫بالعينيي‬
‫ر‬ ‫)جحوظ‬
→treatment:
Levothyroxine(T4), Liothyronine (T3)
Levothyroxine Euthyrox Tab: 50, 100mcg Merck
Eltroxin Tab: 50, 100mcg Aspen
T4 converted in the body to T3 (active form) by deiodinase enzyme.
It is category A: safe in pregnancy.
------------------------------------------------------------------------------------------------------------------
Anti-thyroid drugs:
Thioamide: propylthiouracil (PTU) / Methimazole
MOA: inhibit thyroid hormone synthesis
Propylthiouracil Propyl Thiocil Tab:30mg Teva
 propylthiouracil Tab: 50mg APOTEX
Apotex

Methimazole Mercaptizole Tab: 20mg Taro

Methimazole is preferred over PTU because it has longer half life (given once daily).
PTU is recommended during the first trimester of pregnancy, because of greater risk of
teratogenicity associated with methimazole.
They are used in mild hyperthyroidism (‫)ف الحاالت المتقدمة نلجأ لالستئصال‬
‫ ي‬/ and thyroid
storm
→Symptoms of hyperthyroidism:
Heat intolerance / weight loss / increase appetite /exophthalmos ‫العيني‬
‫ر‬ ‫جحوظ‬/ increase
sympathetic activity (increase BP and other symptoms)

→Adverse effect of thioamide:

Pruritic maculopapular rash‫طفح جلدي مع حكة‬: the most common
Long use may cause thyroid hyperplasia ‫تضخم الغدة‬
Agranulocytosis (increase monocyte and lymphocyte)

Other classes:
→Iodides ‫امالح اليود‬:KI, NaI ‫صحيح اليود ضوري لتصنيع هرمونات الغدة الدرقية بس زيادة مستواه‬
‫بالجسم رح يشتغل بطريقة عكسية‬
‫يستخدم ى‬
‫اكي قبل عملية استئصال الغدة او يف حالة حدوث زيادة مفاجئة يف مستوى هرمون الغدة الدرقية‬
→Radioactive iodine (I131)
To treat thyrotoxicosis (sever hyperthyroidism ‫التات استئصالها‬
‫ي‬ ‫)او الحل‬
Contraindicated in pregnancy and breast feeding.
→B-blocker (Propranolol): to treat symptoms in thyrotoxicosis).
Life Does Not Get Easier
You Just Get Stronger ♥
 Topic 8: Drugs for Bone Disorders
Treatment of osteoporosis:
1.Bisphosphonate
Alendronate / Ibandronate / Risedronate / Zoledronic acid

Alendronate Fosalan Tab: 10,70mg MSD

Fosavance Tab: 70mg /5600 MSD
With colecalciferol
(form of vit D)
Alendronate Teva Tab: 70mg Teva
Once weekly
Osteotab Tab: 70mg Jerusalem
Alensam Tab: 70mg Sama
Maxbone Tab: 10,70mg Unipharm
Dose: 10mg →once daily
70mg → once weekly

Risedronate Risedronate Tab: 35, 150mg Pharma science

Actonel Tab: 35, 150mg Sanofi
Ribone Tab: 35, 150mg Unipharm
Dose: 35mg→ once weekly
150mg → once monthly

Zoledronic acid Aclasta Solution for infusion: Novartis

5mg/100ml
Zoledronic Acid Taro Vial: 4mg/5ml Taro
Zoledronic Acid Vial: 4mg/5ml Fresenius
Zolendronic Acid Vial: 3.5mg/5ml Accord
Accord

Clodronate Bonefos Tab: 400,600,800mg Bayer

Amp: 60mg/ml
 Pamidronate Texpami Solution for Pharmatex It is used to
infusion: trat high
30mg/10ml blood
calcium
levels and
certain bone
problems
such as
cancer or
osteoporosis.

MOA: inhibit osteoclast (‫)الخاليا الهادمة للعظم‬

They are the drug of choice to prevent and treat postmenopausal osteoporosis.
Also used in bone metastases (‫)سرطان بالجسم ووصل العظم‬, hypercalcemia of malignancy ( ‫بصير يزيد‬
‫)مستوى الكالسوم بالجسم ويقل بالعظم‬.
‫هذه العائلة يجب استخدامها بشكل متواصل النه بعد ايقافها يستمر تأثيرها لفترة معينة ثم يبدأ بالتراجع تدريجيا‬

Instructions for oral Bisphosphonate:

1.Take with 6 to 8 ounces of water ‫تناول الدواء مع كمية وافرة من المياه‬
2.Take at least 30 minutes (60 minutes for Ibandronate) before other food, drink, or
medications. ‫الصبح على الريق‬
3.Remain upright and do not lie down or recline for at least 30 minutes (60 minutes for
Ibandronate) after taking them (to prevent esophagitis and esophageal ulcers. ‫البقاء في وضع قائم‬
‫لمدة نصف ساعة على األقل بعد تناول الدواء‬
Adverse effects:
-Diarrhea, abdominal pain
-Musculoskeletal pain
-Esophagitis and esophageal ulcers.
-Rare: osteonecrosis of the jaw with IV high doses in hypercalcemia of malignancy
-Rare: Etidronate is the only bisphosphonate that causes osteomalacia following long-term,
continuous administration.
---------------------------------------------
2.Selective estrogen receptor modulators
Raloxifene →approved for osteoporosis (increase bone density without increasing the risk of
endometrial or breast cancer)

Raloxifene Raloxifene teva Tab: 60mg Teva

Evista Tab: 60mg Lilly

Alternative to Bisphosphonate
----------------------------------------------
3.Calcitonin

Calcitonin salmon Salco Amp: 100IU/ml Genmedix

(salcatonin) SC , IM

It reduces bone resorption but it is less effective than bisphosphonate and increase the risk of
malignancy. (alternative drug)
A unique property of Calcitonin (relief pain associated with osteoporotic fracture).
It is available in intranasal, and parenteral formulation (rarely used).
The most common adverse effect with intranasal: rhinitis, rhinorrhea
---------------------------------------------
4.Denosumab

Denosumab Prolia Pre-filled syringe:SC Amgen

60mg

Monoclonal antibody, target specific receptor →inhibit osteoclast formation and function ‫تمنع‬
‫انتاج وعمل الخاليا الهادمة للعظم‬
Approved in postmenopausal osteoporosis in women with high risk of fractures.
SC every 6 months
Alternative drug

Adverse effects: infections and dermatologic reactions at the site of injection, hypocalcemia,
osteonecrosis of jaw, atypical fractures ‫ حدوث كسور في عظام ال تعاني من هشاشة‬.
---------------------------------------------
5.Teriparatide
Parathyroid hormone analog

Teriparatide Forteo Pre-filled pen: 20mcg Lilly

SC

SC daily
It stimulates bone formation by enhancing osteoblast activity (other drugs inhibit bone
resorption)
The safety and efficacy have not been evaluated beyond 2 years (it increases the risk of
osteosarcoma in rats).
Should be reserve for patients at high risk of fracture and cannot tolerate other drugs.
------------------------------------------------
6.Diacerein: inhibit interleukin-1 beta: class: anthraquinone →to treat osteoarthritis

Diacerein Diatrim Cap:50mg Trima

Diacerein Teva Cap:50mg Teva
--------------------------------------------------------------------------------
Disease-Modifying Antirheumatic Drugs (DMARDs)
Methotrexate, Leflunomide, Hydroxychloroquine, Sulfasalazine, Minocycline.
Benefits of DMARDs: slow the course of disease, induce remission, prevent further destruction
of the joints.
It is better to start using them within 3 months of rheumatoid arthritis diagnosis.
NSAIDs and corticosteroids may also be used for relief symptoms if needed or until DMARDs
become effective.
Methotrexate

Methotrexate Methotrexate Ebewe Tab: 2.5mg Ebewe Pharma

Vial: 100mg/ml
Methotrexate Orion Tab: 2.5mg Orion
Abitrexate Vial:25mg/ml Teva
500mg/20ml
Metoject Pen:7.5, 10, 12.5, Tzamal Bio-Pharma
15,17.5, 20, 25mg
 MOA: antifolate (antimetabolite) that prevent synthesis of DNA which is needed for immune
cells (RA is an autoimmune disease)
Methotrexate has become mainstay of treatment in patient with rheumatoid or psoriatic
arthritis.
It can be used alone (first line) or in combination with other drugs, it take 3-6 weeks to make
response.
------------
Leflunomide

Leflunomide Arava Tab: 20mg Sanofi

Ruvar Tab: 20mg Birzeit

Antimetabolite like methotrexate and immunosuppressant.

It can be used as monotherapy or in combination with methotrexate ( ‫لما الميثوتريكسات يكون مش‬
‫)كافي بنضيفله هاد الدوا‬
It is not recommended in patient with liver disease, because of a risk of hepatotoxicity.
----------------
Minocycline

Minocycline Minocycline Rafa Cap:

50mg (30cap)
100mg (10cap)
Minocin Pfizer Tab: 100 mg

Tetracycline antibiotic
It is effective in early RA but not as first line therapy (monotherapy or in combination)
MOA: inhibit nitric oxide synthesis which responsible for collagen degradation.
--------------

Sulfasalazine

Salazopyrin Sulfasalazine Tab: 500mg Pfizer Salazopyrin is used

for ulcerative colitis
EN tab: 500mg and crohn disease
 (immunosuppressant Salazopyrin EN can
and anti-inflammatory reach the joints so it
agent) is also used in
rheumatoid arthritis
because it reduce
swelling and stiffness
in joints.

Its mechanism in treating RA is unclear

It is used in early mild RA in combination with methotrexate or hydroxychloroquine.
Onset of activity: 1-3 months.
--------------
Hydroxychloroquine

Hydroxychloroquine Plaquenil Tab: 200mg Sanofi

It is antimalarial drugs that prevent lymphocyte activation.

---------------------
Biological therapy (TNF-alpha-inhibitors):
Adalimumab / Certolizumab / Etanercept / Golimumab / Infliximab / Rituximab

Adalimumab Humira Syringe: 40mg/0.4ml Abbive

Weekly or every other week

Etanercept Enbrel syringe: 25,50mg Pfizer

Infliximab Remsima Amp: 100mg /10ml Celltrion

Remicade Amp: 100mg /vial Janssen

Rituximab Mebthera Vial:100,500mg Hoffman

Truxima Vial:100,500mg Biotec
Rixathon Vial:100,500mg Sandoz
 Golimumab Simponi Pre-filled J-C Health Care
pen:50mg/0.5ml
Pre-filled syringe:
50mg

Response can be seen within 2 weeks.

‫اذا دوا من هاي المجموعة ما زبط هاد االشي ال يمنع استخدام دوا اخر من نفس المجموعة‬
Adverse effects:
Increased risk for infections and lymphoma.
Live vaccination should not be administered while on TNF-alpha inhibitor therapy.
Should be used with caution in those with heart failure as they can cause or worsen preexisting
HF.
------------
Interleukin’s inhibitors:

Tocilizumab Actemra Vial:20mg/ml Roche

Canakinumab Ilaris Vial:150mg/ml Novartis
Secukinumab Consentyx Vial:150mg/ml Novartis

Note:
Sulfasalazine is the DMARD of first choice during pregnancy (cat:B), but high level of folic acid
should be taken with it (4-5mg/day).
-------------------------------------------------------------------------------------------------------------------------------

Drugs for Gout

Gout is an inflammatory arthritis that results from an excess of uric acid in the blood which is
come from breakdown of purines
It affects men more than women by a ratio of about 3 to 1.

Colchicine

Colchicine Colchicine Tab: 0.5mg Rafa

Goutex Tab: 0.5mg Birzeit
Colchicine-Sama Tab: 0.5mg Sama
From colchicum seeds
It is used to treat gout attack ‫وقت النوبة‬
MOA: binds with tubulin microtubules, block cells division and preventing migration of
granulocyte to the area.
Must be administered within 36 hours of onset of the attack to be effective.
Alleviating the pain of gout attack within 12 hours.
It is also used as prophylaxis with drugs that increase uric acid level in the body.
It is metabolized by CYP3A4, so CYP3A4 inhibitors such as clarithromycin, itraconazole may
increase its level and toxicity.

Other uses of colchicine:

FMF: Familial Mediterranean Fever ‫حمى البحر المتوسط‬
Pericarditis (combined with NSAID and ASA)
Adverse effects:
N /V /D and abdominal pain
Chronic administration may lead to myopathy, neutropenia, aplastic anemia and alopecia. →
so, sometimes it has been replaced by NSAIDs.

Allopurinol

Allopurinol Alloril Tab: 100, 300mg Dexcel

Uricnase Tab: 100mg Birzeit
Biloric Tab: 300mg Sama
Zyloric Tab: 100, 300mg GSK
With a full glass of water
Purine analog, Xanthin oxidase inhibitor, it reduces the production of uric acid by inhibiting the
last step which is catalyzed by xanthin oxidase.
The most common adverse effect: hypersensitivity reaction (skin rash).
The dose should be reduced in renal impairment.
It is used also to prevent calcium stones in the kidney.
Probenecid
Promote renal clearance of uric acid by inhibiting the urate anion exchanger in the proximal
tubule that mediate urate reabsorption. (block reabsorption of uric acid).
It blocks tubule secretion of penicillin and is sometimes used to increase the levels of B-lactam
antibiotics, also inhibit the secretion of methotrexate, naproxen, ketoprofen and indomethacin.
It should be avoided if the creatinine clearance is less than 50ml/min

Recommendation during pregnancy:

Probenecid →the drug of choice to eliminate uric acid (prophylaxis, chronic use).
Allopurinol →category C
Ibuprofen → the choice for pain during attack.
Colchicine → second choice during attack.

Recommendation during breastfeeding:

Probenecid →the drug of choice to eliminate uric acid (prophylaxis, chronic use).
Allopurinol → should be avoided whenever possible.
Ibuprofen → the choice for pain during attack.
Colchicine → should not be used ‫اذا قررت توخده الزم توقف الرضاعة‬
--------------------------------------------------------------------------------------------------------------
‫بسابق له"♥‬
‫ِ‬ ‫بمتأخر عن أحد وال أنت‬
‫ِ‬ ‫" إن لك ٍل منا مسلكه في هذ ِه الحياة‪ ،‬فال أنت‬
 Topic 8: Corticosteroids

Corticosteroids are synthesized from cholesterol and released from the cortex of
adrenal gland.
Two types:
1-Mineralocorticoied: Aldosterone
2-Glucocorticoide: Cortisol
Note: the medulla of adrenal gland secret catecholamines.

Short acting glucocorticoids: (1-12 hr)

Cortisone/ Hydrocortisone
Its anti-inflammatory effect = salt-retaining effect
Solu-Cotref Hydrocortisone Vial: 100, 500mg Pfizer
Floxin-HC otic Hydrocortisone + Ear drop Jepharm
Ciprofloxacin
Hydrocortisone Hydrocortisone Tab: 10mg Rekah

Birzeit
Corten Hydrocortisone Cream Beit Jala
Mico-cort Hydrocortisone + Cream Jepharm
Daktacort Miconazole Cream Janssen
Refrigerated
Hydroagisten Hydrocortisone + Cream Perrigo
Mycoten HC Clotrimazole Cream Beit Jala

Fucidin H Hydrocortisone + Cream Leo

Fusylin H Fucidic acid Cream Jepharm
Zydex HC Cream Beit Jala
Hemoral-HC Hydrocortisone + Ointment Beit Jala
Lidocaine + Supp
Zinc oxide

Virax HC Hydrocortisone + Cream Birzeit

 Acyclovir
Novocort Hydrocortisone + Eye,ear,nose Beit Jala
Neomycin ointment
Ramacetine HC Hydrocortisone + Eye ointment Birzeit
Chloramphenicol

Intermediate acting glucocorticoids: (12-36hr)

Prednisone / Prednisolone / Methylprednisolone / Triamcinolone / Flucinolone
/Fludrocortisone
There anti-inflammatory effect much more than salt-retaining effect.
Prednisone Prednisone Tab: 1,5,20mg Rekah

Prednisolone Prednitab Tab: 5,20mg Birzeit

Prednisolone Tab : 5, 20mg Rekha
Prednilet Syrup : 15mg/5ml Birzeit
Allow Syrup: 15mg /5ml Jepharm

Pred forte Prednisolone Eye drop Allergan

Aflumycin Prednisolone + Cream Perrigo
Gentamicin
Neo-Medrol acne Methylprednisolone + Lotion Pfizer
lotion Neomycin
Sulfur
Aluminium
chlorohydroxide
Depo-Medrol Methylprednisolone Injection: Pfizer
alone or with 40mg/1ml
lidocaine 1, 2, 5ml
Solu-medrol Methylprednisolone Vial: Pfizer
40,125,500,1000mg
Medrol Methylprednisolone Tab: 4mg Pfizer

Triamcinolone Sterocort Tab: 4mg Taro

Cinolone Tab: 4mg Birzeit
 Mioret Tab: 4mg Sama
Kenacort Amp: 40mg/ml
IM or intra-articular
Oracort / Oracort E Cream Taro
Steronase Nasal spray
Skinolone Cream / ointment Beit Jala
Triamcinolone Decomb Cream Birzeit
Neomycin Dermacombin Cream / ointment Taro
Nystatin
Gramicidin

Fluocinolone + Proctocare Cream Pharmacare

Lidocaine
Fluocinolone Synalex Cream / gel / Pharmacare
ointment

Fludrocortisone Astonin Tab: 0.1mg Merck

Long-acting glucocorticoids: (36-55hr)

Betamethasone / Dexamethasone
Betamethasone Betacort Tab: 0.5mg Beit Jala
Diprospan Injection: 1ml , 2ml MSD
Betacort V Cream Beit Jala
Tabetan Cream Sama
Betacorten Cream / ointment Trima
Betnovate Ointment /Scalp GSK
application
Betacare Cream Pharmacare
Betamethasone + Betacorten G Cream / ointment Trima
Gentamicin Betacare-G Cream Pharmacare
Diprogenta Cream /Ointment MSD

Valecort G Cream / ointment Birzeit

Betamethasone + Triderm Cream MSD

Gentamicin +
Clotrimazole
Betamethasone + Diprosalic lotion Lotion MSD
Salicylic acid
Betamethasone + Fucicort Cream Leo
Fucidic acid
Betamethasone + Daivobet Ointment Leo
Calcipotriol Xamiol Gel Leo

Dexamethasone Decort Tab: 0.5, 0.75, 2mg Birzeit

Amp: 4mg
Dexamethasone Tab: 2mg Rekah
Dexamethasone Amp: 4mg Rompharm
Rompharm
Dexasone Amp: 4mg Jerusalem
Dexa-Alison Amp:4mg Alison
Novodexon Syrup Beit Jala
Sterodex Eye drop Dr.Fischer
Dexamethasone Neodex Ear drop Beit Jala
Neomycin Dexamycin Eye drop Teva
Dethamycine Eye, ear, nose drop Rekah
Dexamethasone Otodex Ear drop Birzeit
Neomycin Dex-otic Ear drop Teva
Polymyxin B Neocort Ear drop Beit Jala
Desoren Ear drop Rekah
Maxitrol Eye drop Novartis
Eye ointment
Dexamethasone Medihist Cream Birzeit
Neomycin Polycutan Cream Perrigo
Clotrimazole Tevacutan Cream Teva
Dexamethasone Dexefrin Eye drop Dr-fischer
Neomycin Refrigerated
Phenylephrine
Dexamethasone Dexacol Eye drops Birzeit
Chloramphenicol Refrigerated
Dexamethasone Chloroson Eye drop Birzeit
Chloramphenicol
Polymyxin B Refrigerated
According to the anti-inflammatory potency (highest→lowest)
Orally:
Betamethasone →dexamethasone →triamcinolone →prednisone and prednisolone
→cortisol

Topically:
Highest potency Betamethasone
Clobetasol
Halobetasol
High potency Amcinanide
Fluocinonide
Triamcinolone
Medium potency Beclomethasone
Fluticasone
Hydrocortisone
Low potency Dexamethasone
Desonide

Clobetasol Dermovate (brand) Cream GSK

Ointment
Scalp application
Closol Cream Sama
Dermacare Cream Pharmacare
Clobetasone Eumovate Cream GSK
Ointment
Clobetasole is a medicine used on the skin to treat swelling, itching and irritation. It can
help with skin problems such as: eczema, contact dermatitis, psoriasis.
Fluocinolone + Comagis Cream Perrigo
Bifonazole
(antifungal)

Beclomethasone + Foster Inhalation solution Chiesi

Formoterol
 Flumethasone+ Topisalen Cream Trima
Salicylic acid

Fluticasone Flixotide Inhalation GSK

Nebulization
Fluticasone + Flutiform Inhalation Rafa
Formoterol suspension
Fluticasone + Seretide Inhalation powder GSK
Salmeterol

Mometazone Elocom Cream MSD

Ointment
Lotion
Nasotrex Nasal spray Birzeit
Montazone Cream Birzeit
Topocort Cream Beit Jala

Mineralocorticoids: Fludrocortisone
→use: as a replacement therapy in regulation of electrolyte and water balance in
hypoadrenalism by modulating ion transport in the epithelial cells of the collecting ducts
of the kidney.
---------------------------------------------------------------------------------------------------------------------
Glucocorticoids are a group of drugs structurally and pharmacologically similar to the
endogenous hormone cortisol with various functions like anti-inflammatory (reduce
erythema, swelling, pain, and heat), immunosuppressive, anti-proliferative, and
vasoconstrictive effects.
→How glucocorticoids give anti-inflammatory effect?
-Inhibit antigenic response of macrophage and leukocyte
-Inhibit vascular permeability
-Decrease circulating WBC
-Inhibit cytokine production
-Inhibit arachidonic acid and prostaglandin production by inhibition of phospholipase A2 and the
cyclooxygenases.
Indications:
➔ As a replacement therapy in adrenocortical insufficiency (Addison disease),
congenital adrenal hyperplasia.
➔ Systemic symptomatic treatment
Acute use:
1.in allergic reactions and anaphylactic shock (for their vasoconstrictive effects, Na
and water retention)
2.In asthma (for broncho dilatory effect)
3.Anti-emetic treatment for example to treat nausea due to chemotherapy.
4.Acute exacerbation of autoimmune disease such as multiple sclerosis ‫التصلب‬
‫ن‬
‫اللويح‬, vitiligo ‫ البهاق‬, uveitis ‫التهاب القزحية‬, rheumatoid arthritis ‫الروماتيم‬, Systemic
lupus erythematosus……
5.Cerebral and pulmonary edema.

Note:
Rheumatoid arthritis is an autoimmune disease that affect mainly flexible
(synovial) joints.
Systemic lupus erythematosus is an autoimmune disease that attacks normal
healthy tissues including joints, skin, kidney, blood cells, heart and lungs.

Long-time use:
1.chronic, inflammatory diseases (asthma, COPD, inflammatory bowel disease)
2-Rheumatic disease (sarcoidosis, gout, Sjogren syndrome, SLE)
3-Graves’ ophthalmopathy
4-leukemia in adult and children.

➔ Locally to treat dermatologic disorders: Eczema, Psoriasis…etc.

➔ Prophylactic:
-Organ transplant (to prevent rejection due to their immunosuppressive action)
-Preterm delivery (to stimulate surfactant production and to accelerate fetal lung
maturity) → 12mg of dexamethasone as IM injection Q 12hr
It is better to use the lowest possible dose and for the shortest possible time to prevent
suppression of the adrenal-hypothalamic pituitary axis, also we can use it as alternative day
therapy to prevent adrenal crisis.
Patients removed from long-term glucocorticoids therapy must be weaned off the drug several
days to allow recovery of adrenal responsiveness.
Adverse effects of glucocorticoids after long term use:
1- Osteoporosis: is one of the well-known adverse effect, up to 40% of patients on
long-term glucocorticoids develop bone loss leading to fractures
How? By activation of osteoclast, inhibition of osteoblast and decreasing intestinal
absorption of calcium.
2- Cushing syndrome: moon face, fat deposition on face and back of shoulders, thin
extremities, thin skin, bruises, gynecomastia in males, amenorrhea and hirsutism
in females
3- Sodium and water retention, potassium loss, edema, HTN
4- Adrenal suppression
5- Hyperglycemia and steroids-induced diabetes mellitus
6- Weight gain
7- Peptic ulcer
8- Cataract and increasing of intraocular pressure leading to glaucoma
9- Muscle weakness and tissue loss
10- Increased susceptibility of infection and poor wound healing.

-------------------------------------------------------------
Note:
Prednisone and Prednisolone are the corticosteroids of choice for systemic treatment
during pregnancy and breastfeeding.
‫رعايته" ♥‬ ‫"واألمرُ حني تَستودعَهُ اهلل يفرُّ من ضَعفِ حيلتك إىل أمنِ‬
 Topic 10: NSAIDs
NSAID (nonsteroidal anti-inflammatory drugs):
MOA: inhibiting prostaglandins by inhibiting cyclooxygenase.
Functions of prostaglandins in the body:
1.Modulating pain, inflammation and fever.
2.Reduce acid secretion and stimulate mucus and bicarbonate production in the GI tract
3.Control uterine contractions
4.Control renal blood flow
-----------------------
PROSTAGLANDINES
Alprostadil: PGE 1 that is naturally produced in tissues
Alprostadil Caver Ject Amp: 10,20mcg Pfizer
Prostin VR Amp for IV infusion Pfizer
Uses: to treat erectile dysfunction, or to keep the ductus arteriosus (between the aorta and
pulmonary trunk) open in neonates with congenital heart conditions until surgical correction is
possible.

Lubiprostone: simulate chloride channels in the intestine →increase intestinal fluid

secretion → it is used to treat constipation
SE: nausea (can be decreased if taken with food) , diarrhea.

Misoprostol: PGE 1 analog: to protect stomach from ulcer during chronic NSAID
treatment.
Misoprostol Cytotec Tab: 200mcg Pfizer
(controlled)
Misoprostol + Arthrotec Tab: 200mcg + Pfizer
Diclofenac sodium 50, 75mg
Prostaglandin F2alpha analog: Bimatoprost, Latanoprost, Tafluprost, Travoprost.
→they are used as ophthalmic solution to treat open-angle glaucoma by increasing
outflow of the fluid so decreasing intraocular pressure.
Note: they are more effective than timolol because it prevents the production of the
fluid only without increasing outflow.
Bimatoprost Lumigan Eye drop: 0.3mg/ml Allergan
Note: it is approved to treat eyelash hypotrichosis because it increases eyelash
prominence, length and darkness. ‫بس ال تستخدم لتطويل الرموش بسبب االعراض الجانبية التي تسببها‬
Latanoprost Lataro Eye drop Taro
Xalatan Eye drop Pfizer
Tanup Eye drop Birzeit
Latanoprost + Lataro-Tim Eye drop Taro
Timolol Xalacom Eye drop Pfizer
Tanup plus Eye drop Birzeit

Travoprost Travatan Eye drop Novartis

Travoprost + Duotrav Eye drop Novartis
Timolol

SE: blurred vision/ iris color change / ocular irritation / foreign body sensation / increased
number and pigment of eyelashes.

Prostacyclin (PGI2) analog: Epoprostenol, iloprost, Treprostinil.

They are potent pulmonary vasodilators that are used to treat pulmonary arterial hypertension.

SE: bronchospasm and cough after inhalation, dizziness, headache, flushing.

-----------------------------

NSAID
inhibition of Cyclooxygenase-2 →Lead to the anti-inflammatory and analgesic actions by
inhibiting prostaglandin production
inhibition of COX-1 → responsible for prevention of cardiovascular events and most
adverse events.

Non-selective NSAID:
→Salicylates: Aspirin / Diflunisal
Aspirin Aspirin Tab:100mg Birzeit
Aspirin cardio Tab:100mg Bayer
Cartia Tab:100mg Aspen
Godamed Tab:100mg Godamed
Tevapirin Tab:100mg Teva
Baby Aspirin Tab:100mg Beit Jala
Micropirin Tab:100mg Dexcel

At this does (75-325mg) it prevents platelet aggregation by inhibiting COX-1 mainly.

It exhibits anti-inflammatory activity only at relatively high dose that are rarely used
(from 500mg).
Aspirin is often differentiated from other NSAIDs, since it is an irreversible inhibitor of
cyclooxygenase activity.
It should be avoided in patients less than 20 years with viral infections such as
chickenpox or influenza to prevent Reye syndrome (fulminating hepatitis with cerebral
edema, often leading to death).

Diflunisal Dolocare Cap: 250, 500mg Pharmacare

The suggested dosage range for osteoarthritis and rheumatoid arthritis is 500mg to 1000mg
daily in two divided doses (dose over 1500mg daily is not recommended)
Note: this drug does not have antipyretic effect.

→Acetic acid derivatives: Diclofenac / Indomethacin / Sulindac / Etodolac / Tolmetin

Diclofenac sodium Betaren SR Tab: 100mg Dexcel
Voltaren SR Tab: 100mg Novartis

Voltaren emulgel Emulgel

Abitren Amp 75mg/3ml Merckle
Supp: 50
Rufenal SR Tab: 100mg Birzeit

Rufenal DS Emulgel
 Diclofen SR Tab: 100mg Jepharm
Supp: 12.5, 75,
100mg
Amp
Voryn Tab: 50mg Pharmacare
Gel
Diclo-Sama Tab: 50mg Sama
Supp:12.5, 100mg
Gel
Swiss relief Spray gel 4% Temmler Werke
Dicloren gel Gel Trima

Diclofenac Cataflam Tab: 50mg Novartis

Potassium Joflam Tab: 50mg Jepharm
Anaflam Tab: 50mg Beit Jala
Toleran Tab: 50mg Birzeit
Diclofenac is more potent than ibuprofen
Indomethacin Indocaps Cap:25mg Beit Jala
Supp: 100mg
Indolin Cap: 25mg Birzeit
Supp: 100mg
Indovis Cap: 25mg CTS
Indogel Gel Beit Jala

Sulindac Mobicol Tab: 100, 200mg Birzeit

Etodolac Etodolac Teva Tab: 400mg Teva

ER tab: 600mg
Etopan Tab: 200, 400, 500, Taro
600
XL tab: 400, 600mg
Dote Tab: 400mg Sama

This class of NSAID may cause upper GI disturbances

They have long half-life permits daily or twice daily dosing.
→Propionic acid derivatives: ibuprofen / Fenoprofen / Ketoprofen / Naproxen
Ibuprofen Nurofen LC: 200mg Reckitt
Forte: 400mg
Forte LC: 400mg
Quick: 512, 256 mg (sodium ibuprofen)
Susp: 100mg /5ml
Child Supp: 60, 125mg
Gel

Nurofen plus: Tab: 200+12.8mg

With codeine

Nurofen cold and flu: Tab: 200mg+30mg

With pseudoephedrine
iBOO Susp:100mg /5ml Teva
200mg/5ml
Ibufen Caplet: 400, 600mg Dexcel
Trufen Tab: 200, 400, 600mg Jepjarm
Susp: 100mg /5ml

Trufen plus: Tab: 200+30mg

With pseudoephedine Susp: 100+15mg /5ml

Ultrafen Caplet: 200, 400, 600mg Birzeit

LC: 400mg
Quick: 512mg
Susp: 100mg/5ml
Supp: 60, 125mg

Ultrafen plus: Tab: 200mg+30mg

With pseudoephedrine Susp: 100+15mg /5ml
Spirifen Cap: 400mg Birzeit
Algofen Tab: 400mg Birzeit
Extrafen Susp: ibuprofen + paracetamol Birzeit
Isofen Tab: 400mg
Susp: 100mg /5ml
Emulgel
Ibusama Tab: 200,400,600,800mg Sama
Susp: 100mg/5ml
Susp forte: 200mg/5ml
OTC: 200-400mg q 4-6hr (not to exceed 1200mg /day)
Prescription: 400-800mg q 6hr (not to exceed 3200mg /day)

For children:
Less than 6 months→safety not established
More than 6 months →5-10mg /kg/dose q 6 hr (not to exceed 40mg/kg/day)
Supp:
1-2 year: 60mg supp q 6 hr
2-6 year: 125mg supp q 6hr
Naproxen Naprex Tab: 250, 500mg Birzeit
Naxyn Tab: 500mg Teva
Naproxen sodium Naproxen Tab:275mg Birzeit
Narocin Tab:275mg Teva
Point Tab:275mg Trima
For pain: 250mg q6-8hr or 500mg q12hr (not to exceed 1250mg/day)

This class of NSAID has lower toxicity and better acceptance in some patients
Naproxen is considered by some experts as one of the safest NSAIDs.

→Oxicams: piroxicam / meloxicam

Piroxicam Pirox Cap:10,20mg Jepharm
Amp:20mg
Supp:20mg
Emulgel
Brexin Tab: 20mg Taro
Pixam Cap: 10,20mg Sama
Exipan Gel Perrigo
Roll on
Feldene Gel Pfizer
 Meloxicam Movalis Tab: 7.5, 15mg Pharmacare
Moxicam Tab: 7.5, 15mg Beit Jala
Mexilon Amp: 15mg Medicuse

Tenoxicam Reutenox Tab: 20mg Rubio

Lornoxicam Xefo Tab:8mg CTS

Amp: 8mg/2ml
Oxidure Tab:8mg Birzeit

→Fenamates: Mefenamic acid / Meclofenamic acid

→Cox-2 inhibitors: Celecoxib / Etoricoxib
Celecoxib Celecox Cap: 200mg Trima
Coxib Cap: 100, 200mg Jepharm
Celex Cap: 100, 200mg Beit Jala
Celebra Cap:100,200mg Pfizer
Celecoxib Teva Cap:100,200mg Teva

Etoricoxib Arcoxia (brand) Tab: 60,90,120mg MSD

Coxitor Tab: 60,90,120mg Sandoz
Tericox Tab: 60,90,120mg Birzeit
Etoflam Tab: 60,90,120mg Beit Jala
Acro-Teva Tab: 90mg Teva

Nimesulide Mesulid Cap: 100mg Rafa

Nimesulide →preferentially inhibits COX2 enzyme
They are used for rheumatoid arthritis, osteoarthritis, and acute mild to moderate pain.
Less GI irritation than aspirin, but has potential for increasing myocardial infarctions and
strokes.
Half-life for celecoxib: 11 hours → given once or twice daily
The dose should be reduced in patients with hepatic impairment because it is
extensively metabolized in the liver
Celecoxib should be avoided in patients with severe hepatic or renal disease because it
is excreted in urine and feces.
-----------------------
Nabumetone Nabuco Tab:500mg Trima
Is a nonacidic NSAID prodrug that is rapidly metabolized in the liver to the active
metabolite (6-methoxy-2-naphthyl acetic acid)
Dipyrone Optalgin Teva Tab:500mg Teva
(Metamizole) Oral drops
Amp
Dipyraz Oral drops ABC
Amp
Novagesic Amp Birzeit
Metamizole Amp Kalcex
sodium-Kalceks
Dipyrone→Class: pyrazolone

They have 3 therapeutic actions:

Anti-inflammatory / Analgesic / Antipyretic
→Not all NSAID are equally effective in each of these actions
‫ال تعالج المرض وانما تقلل االلتهاب وتؤخر او تمنع ظهور مضاعفات المرض وتعالج االالم المصاحبة له مثل‬
‫التهاب المفاصل‬
→they are used in mild to moderate pain such as musculoskeletal disorders, menstrual
pain, toothache (opioid for more severe pain)
Ketorolac →it is an NSAID that can be used for more severe pain but for short duration
less than six days.
Ketorolac Acuavil Vials used as eye Allergan
drops

→They reset body temperature to the normal level when it is elevated due to
prostaglandin synthesis because of pyrogens
As antipyretic: ibuprofen and naproxen can be used.
Note:
Salicylic acid is used topically to treat acne, corns, warts, celluses. →Keratolytic effect
Pitrisol Benzoic acid Topical To treat topical fungal infections (ringwarms)
Salicylic acid solution especially during its chronic hyperkeratotic
Lidocaine stages and for other skin disorders
characterized by itchiness and thickening.
Spirit Salicylic Salicylic acid Topical Floris
Ethanol solution To treat seborrhea, acne and mycoses
Salikaren Salicylic acid Ointment
Diprosalic Salicylic acid Ointment MSD
Betamethasone Lotion To treat eczema and psoriasis
It reduces redness, itching and swelling
It removes dead skin cells and helps in
softening the skin.
Topisalen Salicylic acid Ointment Trima
Flumethasone The same uses as diprosalic
Cornex Salicylic acid Ointment Pella
Lactic acid For corns and warts
Timodore Salicylic acid Plaster To remove corn and warts
Ointment
Liquid
Salatac Salicylic acid Gel To remove corns and warts

--------------------
Adverse effects of NSAID:
→The most common adverse effects of NSAIDs are GI related, ranging from dyspepsia
to bleeding (more selectivity to COX-1→more GI SE by decreasing prostaglandins)
Note: NSAID should be taken with food or fluid to prevent GI upset.
If NSAIDs are used in patients with a high risk for GI events→ PPI should be used
concomitantly to prevent NSIAD-induced ulcers.
→Increased risk of bleeding
`Inhibition of COX-1 →inhibit thromboxane-2 formation →antiplatelet effect
Note: Aspirin is often stopped at least 1 week prior to surgery.
NSAIDs other than Aspirin are not utilized for their antiplatelet effect, but can still
prolong bleeding time.
Patients who take aspirin for cardio protection should be avoid concomitant NSAID use
if possible because they can block aspirin binding to cyclooxygenase.

→Action on the kidney

NSAIDs prevent prostaglandin production which are responsible for maintain renal
blood flow.
Patients with kidney disease are at high risk
COX-2 inhibitors such as celecoxib may have the same potential for adverse renal effects
as traditional NSAIDs.

→Sodium and fluid retention →elevate blood pressure and may cause edema.
COX-2 inhibitors such as celecoxib may affect blood pressure less than traditional
NSAIDs such as ibuprofen and diclofenac.

→increased risk of cardiovascular events has been associated with all NSAIDs except
aspirin (especially selective COX-2 inhibitor, because they inhibit prostacyclin production
which inhibit platelet aggregation)
Note: among NSAIDs, naproxen appears to be the least harmful on CVS, it should be
used for shortest duration and with lowest dose)
→NSAIDs should be used with caution in patients with asthma because inhibiting of COX
pathway will enhance lipoxygenase pathway and produce leukotrienes which are
bronchospasm.
→Patients with severe hypersensitivity to aspirin should avoid using NSAIDs
→Drug-interaction:
Aspirin bind roughly with albumin →may be replaced by other drugs and increased the
level of salicylate
Also, aspirin may replace other agents which also bind with albumin such as warfarin,
valproic acid, and phenytoin resulting in higher free concentration of these agents.

→Aspirin toxicity (salicylism) causes nausea / vomiting / tinnitus ‫ طنين باالذن‬/confusion/

dizziness / hallucination / coma / respiratory and metabolic acidosis /respiratory failure
/ death.
Ingestion of as little as 10g in children can cause death in children.
→COX-2 inhibitors SE: headache/ nausea / diarrhea and abdominal pain are the most
common adverse effects. (but not ulcer or bleeding).
Celecoxib, when used without concomitant aspirin, is associated with less GI bleeding
and dyspepsia, but this benefit is lost when aspirin is added to celecoxib therapy.

Note: patients who are at high risk of ulcers and require aspirin for cardiovascular
prevention, celecoxib should be avoided as anti-inflammatory because it is no longer
very effective.
Note: patient who is allergen to aspirin or nonselective NSAID may be at risk for similar
effects with celecoxib.
Fluconazole and Fluvastatin (CYP2C9 inhibitors) may increase level of celecoxib.
----------------------------------------------------
Acetaminophen (Paracetamol)
Paracetamol Acamol Tab:500mg Teva
Acamoli Syrup: 250mg/5ml Teva
Supp: 80,150,250mg
Dexamol Tab:500mg Dexcel
Panadol Tab:500mg GSK
Otamol Tab:500mg Jerusalem
Syrup:125mg/5ml
Supp: 150,300mg
 Febramol Tab:500mg Birzeit
Syrup:125mg/5ml
Supp:150,300mg
Sedamol Caplet: 500mg Birzeit
Paramol Tab:500mg Beit Jala
Syrup:125mg/5ml
250mg/5ml
Supp:150,300mg

Paramol extra Tab:1000mg

Tailol Tab:500mg Pharmacare
Syrup:125mg/5ml
250mg/5ml
Molpar Tab:500mg Sama
Syrup:125mg/5ml
Supp:80,150,250mg
Novimol Oral drops: 100mg/ml CTS
Abrol Tab:500mg Rekah
Abrolet Supp:150
Supp Forte:250mg/5ml
Syrup:125mg/5ml
Paracetamol Taro Vial Taro
Paracet Elixir:120mg/5ml Vitamed
Paracetamol Extrafen Syrup Birzeit
Ibuprofen
Paracetamol Dexamol cold Cap Dexcel
Dextromethorphan
Guaifenesin
Paracetamol Acamol focus Tab:250+250+65mg Teva
Aspirin
Caffeine
Exidol Tab:250+250+65mg Perrigo
Sedaprin Tab:250+250+65mg Birzeit
Paracetamol Paramol plus Tab Beit Jala
Caffeine
Paracetamol CodAcamol Tab Teva
Codeine
(controlled)
Rokacet Tab Taro
Paracod Tab Pharmacare
 Algonal Tab
Codaprol Tab: 325+15mg
Paracetamol Spasmalgin Tab Sam-on
Codeine (controlled)
Papaverine
Atropine
Paracetamol Zoldiar Tab: 325+37.5mg
Tramadol (controlled)
Paracetamol Muscol Tab:500+30mg Teva
Orphenadrin
Relaxon Tab:500+30mg Beit Jala
Balgesic Tab:450+35mg Jerusalem
Paracetamol Scobutyl-CO Tab Jerusalem
Hyoscine N-butyl
bromide
Paracetamol Spasmin Tab Jerusalem
Homatropine
Allobarbitone
Papaverine
Paracetamol Emegrain Tab: 500+5mg Beit Jala
Metoclopramide
Paracetamol Coldex Tab Teva
Chlorphenamine
Caffeine
Phenylephrine
Paracetamol Dexamol sinus Cap Dexcel
Chlorphenamine
Pseudoephedrine
Paracetamol Paraflu Tab Beit Jala
Chlorphenamine
Caffeine
Phenylephrine
Ascorbic acid
Paracetamol Flu Tab Jerusalem
Pyrilamine
Phenylephrine
Paracetamol Decongex cold Syrup Birzeit
Chlorpheniramine
Pseudoephedrine
Phenylpropanolamine
Paracetamol as IV is called perfalgan 10mg/1ml
It is not an NSAID because it is antipyretic and analgesic but not anti-inflammatory.
MOA: it works centrally not peripherally by inhibiting prostaglandins
It does not have anti-inflammatory effect because it has less effect on cyclooxygenase in
peripheral tissue.
It does not affect thromboxane 2 enzyme so it does not affect on platelet aggregation.

Uses:
It is the choice for reducing temperature and reducing pain particularly in patients with
gastric complaint, and when there is no need for anti-inflammatory effect, also for
children with viral infection or chicken pox (to avoid using NSAIDs because of Reye
Syndrome)

Pharmacokinetic:
N-acetyl-P-benzoquinonemine (NAPQI) is highly active metabolite for paracetamol that
can react with sulfhydryl groups and cause liver damage.
At normal doses, NAPGI react with sulfhydryl group of glutathione in liver and it is
excreted in urine, but the risk is at toxic doses.

SE:
At normal doses→ no SE
At toxic doses: Hepatic necrosis and death
Patient with hepatic disease or viral hepatitis are at risk for toxicity.

N-acetylcysteine is the antidote for acetaminophen which contain sulfhydryl groups.

Normal dose for children: 10-15mg/kg/day every 4-6 hours as needed
(Maximum:5doses in 24 hours).
‫ ساعات بين جرعة الباراسيتامول والتروفين (يعني‬4 ‫اذا ضلت حرارة الطفل مرتفعة ممكن نعطيه معه تروفين بس شرط يكون اقل اشي‬
)‫ ساعات واحد فيهم‬4 ‫كل‬

Toxic dose of paracetamol: (cause hepatotoxicity)

For healthy people → children: more than 200mg/kg
→Adult: 6-7g (12 tablets)
(‫ غرام‬4 ‫ حبات باليوم يعني‬8 ‫)ممكن نصرف الباراسيتامول لحد‬
--------------------------------------------------------
In pregnancy:
-Paracetamol is the analgesic and antipyretic of choice; it can be used at usual doses and
at any stage of pregnancy.
-Low doses of aspirin (antiplatelet activity) are good at pregnancy, to prevent increasing
blood pressure and eclampsia, thus preventing preterm delivery, but it should not be
given at time near to birth to prevent excessive bleeding.
‫ انما يستخدم اذا كانت هناك دواعي الستخدامه‬،‫استخدامه بالحمل مش ضروري لكل النساء‬

-High doses of aspirin (more than 500mg)

→Before week 28: good to relax the uterus and it has not any effect on ductus
arteriosus.
→After week 28: it should not be used, because it reduces uterus muscles contraction,
thus causing aging of the placenta ‫هرم المشيمة‬without delivering the baby.
Also, this cause closure of ductus arteriosus early which leading to pulmonary
hypertension.

-Aspirin is the analgesic and antipyretic pf second choice in pregnancy after

paracetamol.
-For anti-inflammatory indications, NSAID such as Ibuprofen are preferable.
-Combination preparations are not recommended with the exception of paracetamol
plus codeine. (before week 28, a combination of paracetamol and ibuprofen can be
used).
-NSAIDs are not used after week 28, unless they are required to close the ducts, in this
case the baby will be delivered by caesarean section.
Indomethacin is the best studied agent in this respect.
-Use of the more established NSAIDs like Ibuprofen and Diclofenac can be considered in
the first two trimesters for anti-inflammatory therapy.
-Selective COX-2 inhibitors are not recommended during pregnancy because of the lack
of data.

In lactation:
Paracetamol is the first choice as analgesic during breastfeeding.
Low dose of aspirin in not recommended during the first month of breastfeeding
High dose of aspirin is not acceptable during breastfeeding.
Ibuprofen is the choice as anti-inflammatory agent.
Among NSAIDs: ibuprofen and Flurbiprofen.
 ‫ُ‬ ‫ُ‬ ‫ى ا‬
‫تأت إّل بعد ان يخت ري ص ريك" ♥‬
‫" خبايا هللا العظيمة ال ي‬
 Topic 11: Opioid Analgesics
Extracted from: Papaver Somniferum
MOA: bind with opioid receptors (mu, kappa, delta) in the CNS and mimic the action of
endogenous painkiller
Acting on mu and delts is responsible for analgesic effect, and cause respiratory
depression and physical dependance.
Acting on kappa receptor cause spinal analgesia and sedation
They can cross the placenta.
Metabolized by the liver (morphine and meperidine give active metabolites)
They eliminated by the kidney (morphine and meperidine are not suitable to use in
renal impairment) (the best choices in this case are methadone and fentanyl).

Morphine:
Morphine Oramorph Oral solution:
(controlled drugs) 10mg/5ml
Morphine kalceks Amp Kalceks

Onset of action:
Immediate release (IR): 30min
Extended release (ER): 90min

Metabolites:
Morphine-6-glucuronide: more potent than morphine /produce analgesia/ responsible
for respiratory depression.
Morphine-3-glucuronide: lack affinity to receptors.
Actions of morphine: analgesia / euphoria / respiratory depression / antitussive action /
miosis (pinpoint pupil) / nausea and vomiting /urinary retention and constipation (by
decreasing GI motility). / hypotension and bradycardia.
It is contraindicated in head trauma or severe brain injury because of vessel dilation in
increased intracranial pressure.
It is used with caution in patient with asthma because of histamine release resulting in
urticaria, bronchospasm.
Using near to term in pregnancy may cause neonatal respiratory depression and long-
term use may lead to withdrawal symptoms. Category C

Codeine

Paracetamol CodAcamol Tab Teva

Codeine
(controlled)
Rokacet Tab Taro
Paracod Tab Pharmacare
Algonal Tab
Codaprol Tab: 325+15mg
Paracetamol Rokacet plus Tab: 500+50+15mg Taro
Caffeine
Codeine
Paracetamol Spasmalgin Tab Sam-on
Codeine (controlled)
Papaverine
Atropine
Codeine Nurofen plus Tab: 200+12.8mg Reckitt
Ibuprofen
Codeine Codivis Tab: 30+10mg CTS
Phenyltoloxamine

Codeine Pulmadrin Syrup Birzeit

Pseudoephedrine Compound
 Triprolidine
Tussibal Co Syrup Jerusalem
Codeine Broncholate forte Syrup Meditic
Pseudoephedrine
Diphenhydramine

Weak analgesic
Metabolized to morphine
Used as antitussive
May be used as analgesic for pregnant women if paracetamol is not sufficiently
effective.

Hydrocodone
Available in combination with paracetamol and codeine
Metabolized to active hydromorphone
IR (immediate release): 4-6hr
LA (long acting): 12-24hr

Oxycodone
Analgesic activity is twice as that of morphine
Formulated with aspirin or paracetamol
Oxycodone OxyContin Tab: 10,40,50mg

Oxymorphone
10 times more potent that morphine
Not affected by liver enzyme
Little histamine release
Hydromorphone
Preferred over morphine in renal failure
Hydromorphone Palladone Tab:
4,8,16,24,32mg

Methadone
Resimac mixture (R form more potent) (S form for neuropathic pain)
It is used for patient with morphine allergy and renal failure.
Lake euphoria effect
Methadone Dolestine Amp: 50mg Teva
Physeptone Tab: 10mg Aspen

Fentanyl
Fentanyl Fentora Buccal tablet: 100,
200, 400,600,
800mcg
Alfentanil kalecks Amp: 0.5mg/ml
Actiq Tab: 600,1200mcg Teva
Fentadol Transdermal Sandoz
patches:
12.25,50,75,100
mcg
Penfent Spray: 400mcg
Fentanyl Amp Amp Birzeit

100 times more potent than morphine as analgesic

Available IV, transdermal (apply q 72hr), trans buccal.

Tramadol
Centrally acting analgesic
Risk of serotonin syndrome if accompanied with antidepressant (because it has
serotonin and norepinephrine activity)
Tramadol Tramal Oral Crunenthal Strong analgesic
drops100mg.
Cap: 50,100
Supp: 100mg

Ketamine (NMDA receptor antagonist→has analgesic and anesthetic effect)

Ketamine Ketalar Injection: 50mg/ml Anesthetic

Others:
Tapentadol
Mepiredine (Pethidine): epidural analgesia, it can be used during labor when therefore
are critical indications for it.
Dextropropoxyphene
Heroin

Antidotes for opioids: Naloxone and Naltrexone (more potent)

Patient controlled analgesia (PCA): it is a method to allow patient in pain to

administer their own pain relief depending on the pain sensation (demand). The
infusion is programmable by the prescriber.
 Topic 12: Headache and Migraine
Migraine: throbbing headache, sometimes is felt on one side of the head, because of
vasodilation of cerebral and cranial blood vessels then migration of pro-inflammatory
mediators.
Other symptoms: nausea / vomiting / sensitivity to light and sounds.

Non-specific (symptomatic) treatment of migraine:

NSAIDs as analgesic
Antiemetic such as prochlorperazine to control vomiting.
Opioids when other drugs are not successful.

Specific migraine therapy:

1.Triptan 5-HT receptor agonist (serotonin type 1 agonist).
Sumatriptan / Almotriptan / Frovatriptan / Rizatriptan / Eletriptan

Sumatriptan Sumatridex Tab: 50, 100mg Dexcel

Imitrex (brand) Tab: 50, 100mg GSK
Migratan Tab: 50, 100mg BeitJala

Rizatriptan Rizalt Tab: 10mg MSD

Wafer tab: 10mg
(rapidly dissolved)

Eletriptan Relert Tab: 20, 40, 80mg Pfizer

MOA: Vasoconstriction and inhibit the release of pro-inflammatory mediators.

Adverse effect:
Elevate blood pressure (should not be used in patient at risk to heart disease without
evaluation the case)
Pain and pressure sensation in chest, neck, throat and jaw.
Cause less nausea
2.Ergot alkaloids 5-HT receptor agonist.
Ergotamine

Drugs for prophylaxis:

-Beta-blockers are the drug of choice: Propranolol, Metoprolol, Atenolol and Nadolol.
-CCB: alternative
-Antidepressants: especially useful in patient with comorbid depression such as Amitriptyline.
- Topiramate: anticonvulsant approved for prevention of migraine headache
Analgesic such as NSAIDs (ex: Ibuprofen, naproxen), acetaminophen and aspirin used for
symptomatic relief of tension headache.
Acetaminophen and aspirin may be combined with caffeine (it increase their effectiveness)

Paracetamol Acamol focus Tab:250+250+65mg Teva

Aspirin Exidol Tab:250+250+65mg Perrigo
Caffeine Sedaprin Tab:250+250+65mg Birzeit
2 tabs q 6 hr
They can be used for patients older than 18 years old.

Barbiturate + aspirin / acetaminophen +- caffeine → for tension headache.

Inhalation of 100% O2 and somatotropin → for cluster headache.

Paracetamol Emegrain Tab: 500 +5mg Beit Jala

Metoclopramide
For migraine accompanied with nausea and vomiting.

Paracetamol Migraleve Cap Manonpharm

Codeine
Buclizine
(antihistamine)
 Clonidine Clonnirit Tab: 0.025mg Rafa
It is indicated to prevent migraine and headache due to narrowing or dilation of blood vessels.
In addition, this drug is indicated for the treatment of flushing and other vascular effects
associated with menopause.

Note: estrogen has been liked with migraine headache (it controls chemicals in the brain that
affect the sensation of pain)→ it is better to use contraceptive with low level of estrogen or
without it (only progesterone).

Migraine and pregnancy:

Migraine attack is most commonly occurred during the first trimester.
The analgesic of choice: paracetamol (perhaps combined with caffeine or codeine).
Ibuprofen can also be used (before third trimester).
Meclizine the drug of choice for nausea and vomiting, Metoclopramide also can be given before
analgesia.

Sever attacks can be treated with Somatropin

As prophylaxis: propranolol, metoprolol.
Ergot alkaloids are contraindicated during pregnancy.
“Your flaws are perfect for the heart that is meant to love you” ♥
 Topic13: Other drugs which are not included in the previous systems:

Name Active Form and Company Indications

ingredients dose

ALA 300 Alpha lipoic acid cap:300 mg adipharm Antioxidants protect against
damage to the body's cells.

Alkasolve potassium citrate Tab:330+300mg urinary alkalizer

Sodium citrate

Artrosamine Glucosamine Sachets adipharm ‫مكمل غذائي يحتوي على حموض امينية‬
plus Aquamine ‫ضرورية للجسم وبخاصة للعظام‬
Lysine ‫والمفاصل‬
‫يذوب الكيس في كوب ماء ويشرب‬
‫صباحا على الريق‬

Arthryl Glucosamine sachets Rottapharm //

Baclosal Baclofen Tab: 10,25 mg Unipharm skeletal muscle relaxant

Brintellix Vortioxetine Tab:10mg

B-card Vit B6,9,12 cap floris ‫المستورد‬

New Bio-flora acidophilus and Cap Ambrosia ‫بكتيريا نافعة تعيد التوازن الطبيعي في‬
others supherb ‫االمعاء‬

B-Neural Vit B1, 6,12 Cap floris ‫المستورد‬

B-Six Pyridoxin (Vit B6) Tab:300mg Meditic

Calcimore calcium carbonate chewable tablet: Taro -calcium supplements

600mg -Antacid

Condylox Podophyllotoxin Genital solution Takeda to treat genital warts in

women and men

Cupripen Penicillamine Tab:250mg Rubio It works to treat Wilson's

disease by binding to the
extra copper in the body and
causing it to leave the body
through the urine.
is also used for people with
kidney stones who have
high urine cystine levels,
 rheumatoid arthritis, and
various heavy metal
poisonings.

Cobra Dietary Cap ‫ ازالة‬،‫تعزيز انتاج الطاقة في الجسم‬

supplement for ‫ رفع مستوى االداء الجنسي‬،‫التوتر‬
men

Curatane isotretinoin Cap:10,20,40mg Taro For acne treatment

Dantrium Dantrolene Cap: 25mg NORGINE Skeletal Muscle Relaxants

sodium used to treat the symptoms
of Malignant Hyperthermia

Detrusitol Tolterodine Tab: 4mg Pfizer Antimuscarinic to treat

overreactive bladder (urinary
incontinence).

Endoxan Cyclophosphamide Tab: 50mg Baxter is in a class of medications

(cytotoxic) called alkylating agents.
When cyclophosphamide is
used to treat cancer, it works
by slowing or stopping the
growth of cancer cells in
your body. When
cyclophosphamide is used to
treat nephrotic syndrome, it
works by suppressing your
body's immune system.

Fampyra Fampridine Prolonged Biogen K+_channel blocker for

release improving walking ability in
tab:10mg adults with multiple sclerosis
who have a walking
disability.

Hydroxy hydroxucarbamide cap:500mg also known as hydroxyurea,

Carbamide is a medication used in
sickle-cell disease, chronic
myelogenous leukemia,
cervical cancer, and
essential thrombocythemia.
In sickle-cell disease it
increases fetal hemoglobin
and decreases the number
of attacks.

Imuran Azathioprine Tab: 25,50mg Aspen Immunosuppressant

Mestinon Pyridostigmine Tab: 60mg MEDA Acetylcholinesterase

Inhibitors
 used to treat myasthenia
gravis.

MAR- Midodrine Tab Alpha agonist (vasopressor)

MIDODRINE To treat orthostatic
hypotension)

Provigil Modafinil caplet:100mg Teva wakefulness promoting

(brand) agents
to treat sleepiness due to
narcolepsy, shift work sleep
disorder, or obstructive sleep
apnea

Pyridostigmine pyridostigmine Tab: 60mg Rafa Acetylcholinesterase

Inhibitors
used to treat myasthenia
gravis. It is also used
together with atropine to end
the effects of neuromuscular
blocking medication of the
non-depolarizing type.

Spasmex Trospium Chloride Tab: 15mg antimuscarinics. It works by

relaxing the bladder muscles
to prevent urgent, frequent,
or uncontrolled urination

Sirdalud Tizinadin Tab:2, 4mg Novartis Is a short acting muscle

relaxant, which is used to
treat muscle spasticity by
blocking nerve impulses that
are sent to brain, also used
to relief the spasm and
increase muscle tone in
multiple sclerosis

Ursolit ursodeoxycholic Tab: 100,300mg CTS Dissolution of gallstones and

acid treatment of some liver
diseases

Ursofalk ursodeoxycholic cap:250mg Rafa

capsules acid

Venoruton O-(beta- Cap:300mg 1-2 capsules daily with

hydroxyethyl)- meals
rutosides (HR) To treat of varicose veins
and chronic venous
insufficiency
Vesicare Solifenacin Tab:5,10mg CTS It is a medicine used to treat
(Brand) overactive bladder and
neurogenic detrusor
overactivity. It may help with
incontinence, urinary
frequency, and urinary
urgency.

Nostensyl Dicyclomine Tab: 10,20mg / CTS Anticholinergic

syrup (Antispasmodic such as in
irritable bowel syndrome)

Neotigason Acitretin Tab:25mg Teva Oral retinoid (vit A

derivative) used to treat
severe psoriasis

Toviaz Fesoterodine Tab: 4,8 mg Pfizer Antimuscarinic

To treat over reactive
Encytol Tolterodine Tab: 1, 2 mg Beit Jala bladder (urinary
incontinence).

Mycosod Mycophenolic acid Tab: 360mg Birzeit Immunosuppressant

medication used to prevent
rejection after organ
transplantation

Dermalux Calamine lotion Jerusalem ZINC OXIDE is used to treat

Zinc oxide or prevent minor skin
Lidocaine irritations such as burns,
cuts, and diaper rash.
Calamine, is a medication
used to treat mild itchiness.
This includes from sunburn,
insect bites, poison ivy,
poison oak, or other mild
skin conditions. It may also
help dry out skin irritation

Dermagesic Calamine lotion Beit Jala

Zinc oxide

Uroclean Hexamine powder for oral Beit Jala is used to suppress or

Sodium Benzoate use eliminate urinary bacteria
associated with chronic or
recurrent infection.
helps to acidify the urine and
maintain a low urinary pH.

Neurovit vit B1,6,12 Tab Beit Jala Vitamin B complex play a

role in cellular energy
production, growth of blood
 cells, healthy brain function,
proper nerve functions…etc.

It is better to take water-

soluble vitamins on an
empty stomach (30 min
before breakfast).

Xaprine Cyclobenzaprine Tab: 5, 10mg Beit Jala Short acting muscle relaxant
by blocking nerve impulses
sent to brain.
Adrenaline Adrenaline Amp S.A.L,F It is used in emergencies to
S.A.L.F IV, IM, SC treat very serious allergic
reactions of insect, food,
drug or other.
It acts quickly to improve
breathing, stimulate heart
rate, raise a dropping blood
pressure, reduce swelling.

Arthro Hyal Sodium Intra-articular gel To increase the viscosity of

hyaluronate the synovial fluid, which
helps lubricate, cushion and
reduce pain in the joints.

Betrimine B1,6,12 AMP (IM) Help Vitamin B complex play a

role in cellular energy
production, growth of blood
cells, healthy brain function,
proper nerve functions…etc

D3-Vicotrat Vit D3 Amp:100 000 IU It aids in the absorption of

(colecalciferol) calcium and may be helpful
in the prevention of
osteoporosis and
osteomalacia

Konakion MM Phytomenadione Amp: 2, 10mg Also known as vitamin k1 or

paediatric Oral, IM, IV phylloquinone.
It is used to treat bleeding
disorder such as warfarin
overdose, vitamin K
deficiency and obstructive
jaundice.

Oral D Vit D3 Amp: 15000 IU Birzeit

Oral use
Venofer Iron sucrose Amp: 100mg/5ml Vifor To treat iron deficiency
anemia in people with
kidney disease.

Neupogen Filgrastim Pre-filled syringe Amgen It is a colony-stimulating

Solution for factors, it is used to treat low
injection neutrophil count

(refrigerated)

Havrix 720 Hepatitis A virus Suspension for GSK Vaccine against hepatitis A
Havrix 1440 Antigen IM injection virus
(inactivated)
(refrigerated)

IMOVAX D.T Active substances Suspension for Sanofi Vaccine against Diphtheria
of Diphtheria injection in a and Tetanus
toxoid and Tetanus prefilled syringe
toxoid (refrigerated)

Act-HIB Haemophilus type Powder and Sanofi Haemophilus type b vaccine

b conjugate solvent for
vaccine solution for
injection in pre-
filled syringe:
10mcg/0.5ml

(refrigerated)

Nimenrix Neisseria Powder and Pfizer Neisseria meningitis vaccine

meningitis group solvent for
A,C, W-135 and Y solution for
polysaccharides. injection in pre-
filled syringe:
IM
(refrigerated)

Pneumovax Pneumococcal Powder and MSD Pneumococcal vaccine

vaccine solvent for
solution for
injection in pre-
filled syringe:
IM, SC
(refrigerated)

UMAN Albumin Human albumin Solution for KEDRION It is used to treat low serum
from human infusion albumin in hypovolemia,
plasma (refrigerated) pulmonary edema, renal
failure, burns and others.
Octanate Human blood Vial It is used to treat and
coagulating factor prevent bleeding in patient
VIII with hemophilia A

Aransep Darbepoetin Pre-filled syringe Amgen It is a re-engineered form of

erythropoietin
It is used to treat anemia

----------------------------------------------------------------------------------------------

Topic 14: Some important eye drops and ointments:

Name Active ingredients Classes of active Company Indication

ingredients
Antivine Naphazoline Decongestant Beit Jala ،‫الزالة احمرار العين‬
Zinc sulfate Astringent ‫االحتقان الحكة والتهيج‬
‫البسيط‬

Refrigerated

Azolin Tetrahydrozoline Decongestant Dr.Fischer Relief of red,

burning and
irritated eyes

Alphagan Brimonide tertrate Alpha agonist Allergan Reducing

intraocular
pressure

Allnex Olopatadine H1-blocker Birzeit Treatment of

(antihistamine) signs and
symptoms of
allergic
conjunctivitis

Allervin Antazoline Anti Allergic Jerusalem Relief of red,

Naphazoline Decongestant burning and
irritated eyes

Atrospan Atropine sulfate Anticholinergic Dr.Fischer Mydiatric ‫توسيع بؤبؤ‬

‫العين‬

Alifresh Carboxymethylcellulos Lubricant Alison Relieves dry and

e irritated eye
 Smooth and
moisturize the
eye

Basilox Moxifloxacin Fourth generation Birzeit Treatment of

Fluoroquinolone bacterial
Antibiotic conjunctivitis

Blink intensive PEG Lubricant AMO Ireland Lubrication

tears Sodium Hyaluronate ‫تلطيف العيون الجافة‬
0.2% ‫والمجهدة‬

Blink Contact Sodium Hyaluronate Lubricant ‫مخصصة لمرتدي‬

‫العدسات الالصقة العادة‬
‫النضارة لها وترطيبها‬
‫مناسبة لجميع انواع‬
‫العدسات الالصقة دون‬
‫الحاجة الى خلع العدسات‬
‫من العين‬

Blink Intensive PEG Lubricant ‫ترطيب اعلى‬

plus Sodium Hyaluronate
0.38%

Collihist Pheniramine Antihistamine and Birzeit Reduce of

Naphazoline decongestant redness and
Benzalkonium itching
chloride

Combigan Brimonidine Alpha-agonist Allergan Reduce high

Timolol Beta-Blocker blood pressure

Chlorosone Dexamethasone corticosteroids BirZeit ‫لمعالجة التهابات العين‬

Chloramphenicol Antibiotics ‫السطحية والتهاب ملتحمة‬
Polymyxin B ‫العين وااللتهابات التي‬
‫تسببها البكتيريا‬

Refrigerated

Cosopt Dorzolamide -Carbonic anhydrase Rafa Reduce high

Timolol inhibitor blood pressure
-Beta-blocker and treatment of
glaucoma

Ciloxan Ciprofloxacin Antibiotic Novartis treatment of

bacterial infection
of the eye

ciclopentolat Ciclopentolat Muscarinic antagonist Rompharm It is used during

eye examination
to dilate it.
 Rifregerated

Clarastill carboxymethylcellulos Lubricant Bruschettini protect and

e moisturize the
eye

Comfort Shield Hylan A fluid Lubricant I.Com ‫يتكون من مواد طبيعية‬

MDS ‫تشبه الموجودة على سطح‬
SD ‫العين فهي تؤدي وظيفة‬
‫الدموع لذلك فهي ال‬
،‫تسبب الحساسية للعين‬
‫تحمي وترطب العين‬
‫وتوفر حماية طويلة‬
‫المدى‬

Dethamycin Dexamethasone -Corticosteroid Vitamed treatment of

Neomycin - inflammation with
Antibiotic(aminoglycosid probable
e) secondary
bacterial infection

Dexefrin Dexamethasone Dr.fischer Rifregerared

Neomycin
Phenylephrine

Dexacol Dexamethasone corticosteroid Birzeit ‫لعالج التهابات العين‬

Chloramphenicol Antibiotic ‫والتهاب الجفن‬
Refrigerated

DuoTrav Travoprost prostaglandin analoug Novartis reduce intaocular

Timolol that increase aqueous pressure
humor

Beta-blocker

Epihist Epinastine Antihistamine Beit Jala treat symptoms of

seasonal allergic
conjunctivitis
(watery, itchy, red
eye)

FML Liquifilm Steroid Allergan treat inflammation

(Fluorometholone) in the eye

Gentacol Gentamicin Antibiotic Birzeit treatment of

infection

Ganfort Bimatoprost Prostaglandin analog Allergan For reducing

Timolol Beta blocker intraocular
pressure
Hylo-Comod Sodium hyaluronate Lubricant Kalema solution for
rinsing and
wetting contact
lenses inside and
outside the eye
Also, improving
hydration of the
eye.

I-Clear Polyvinyl alcohol Lubricant BeitJala relieve dryness

and irritation
caused by a
reduced flow of
tears.

Izilack Hypromellose lubricant and wetting Birzeit relieve dryness

and discomfort

I.O.P Dorzolamide carbonic anhydrase Birzeit treatment of

inhibitor intraocular
pressure

I.O.P Plus Dorzolamide carbonic anhydrase Birzeit treatment of

inhibitor intraocular
pressure
Beta-Blocker
Timolol

Isomar euritalia ‫تخفيف سريع لحاالت‬

pharma ‫االحمرار او االلتهابات او‬
‫الشعور بجسم غريب‬

Isomar plus euritalia ‫لعالج العيون الجافة‬

pharma

Ketofen ketotifen antihistamine Beit Jala elevate symptoms

of allergic
conjunctivitis

Lacromycin Gentamycin Aminoglycoside Dr.Fischer ‫لعالج التهاب العين‬

antibiotic

Localin Oxybuprocaine local anesthetic Dr.Fischer ‫تخدير موضعي للعين‬

Lyteers Hydroxyethylcellulose lubricant Dr.Fischer ‫ترطيب العين في حالة‬

‫الجفاف عندما ال يكون‬
‫انتاج الدموع كافيا‬

Lotemax Loteprednol Anti-inflammatory Teva ‫اللتهاب العين‬

corticosteroid
 ‫مثال بعد اجراء عملية‬
‫جراحية للعين‬

Lomixin chloramphenicol Antibiotic Beit Jala Refrigerated

Lacri-Vision Hydroxyethylcellulose lubricant Bruschettini ‫ترطيب للعين‬

Lumigan Bimatoprost Prostaglandin analog Allergan ‫تقليل ضغط العين‬

Murine Dry & ‫للعين الجافة‬

Tired

Murine ‫للعدسات الجافة‬

Contact ‫ال حاجة الزالة العدسات‬

‫للعين الجافة والمتهيجة‬

Murine Bright ‫ دقيقة‬١٥ ‫توضع العدسة بعد‬
& Moist
‫للعين التي تصاب بالجفاف بشكل‬
Murine ‫متكرر‬
Advanced

Mydramide Tropicamide Anticholinergic Dr.Fischer Mydriatic effect

‫لتوسيع البؤبؤ إلجراء‬
‫فحص للعين‬

Nevanac Nepafenac NSAID Novartis It is used to treat

pain and
inflammation
associated with
cataract surgery.

Neodex Dexamethasone steroid BeitJala ‫لعالج التهاب العين‬

Neomycin Antibiotic ‫البكتيري‬

oflox ofloxacin antibiotic Allergan ‫لعالج التهاب العين‬

OftaMed Alovera gel extract lubricant Framac- ‫حماية وترطيب العين‬

Hyaluronic acid Zabban

Ocutacin Tobramycin Antibactetial agent Birzeit treat eye

(amino glycosides) infection

Pilocarpine Pilocarpine Myotic Vitamed treatment of

Vitamed glaucoma

Pred Forte Prednisolone corticosteroids Allergan for short-term

treatment of eye
 inflammation
when the
presence of viral,
fungal and
bacterial agents
have been rules
out.
It reduces the
irritation, burning,
redness and
swelling of the
eye caused by
chemicals, heat,
radiation or
foreign objects in
the eye.

Relestat Epinastine Antihistamine Allergan treat symptoms of

seasonal allergic
conjunctivitis
(watery, itchy, red
eye)

Rufenal Diclofenac NSAID Birzeit treat of eye

inflammation after
surgery or other
causes

Sterodex Dexamethasone corticosteroid Dr.Fischer to treat eye

inflammation

Sulfacid Sulfacetamide Antibiotic Dr.Fischer treat infections

sensitive to it

Tetrin tetrahydrozoline decongestant Birzeit ‫الزالة احمرار العين‬

Tericin Ofloxacin Antibiotic Beit Jala ‫لعالج التهاب العين‬

Timolin Timolol Beta Blocker Jerusalem ‫لعالج ارتفاع ضغط‬

‫العين‬

Tanup latanoprost prostaglandin analog Jerusalem ‫لعالج ارتفاع ضغط‬

‫العين‬
Refrigerated

Travatan Travoprost prostaglandin analog Novartis ‫لعالج ارتفاع ضغط‬

‫العين‬
Tears Natural 2 Hypromellose lubricant Alcon ‫لعالج اعراض جفاف‬
Dextran ‫العين ونقص افراز‬
‫الدموع‬

Ultracin ofloxacin Antibiotic Birzeit ‫لعالج التهاب العين‬

UnodropsHy eyedrops with Lubricant Maeshal ‫ترطيب للعين‬

hyaluronic acid

Vigamox Moxifloxacin Antibiotic Novartis ‫لعالج التهاب العين‬

Voloxal levofloxacin Antibiotic Birzeit

Vivaxin Levofloxacin Antibiotic Beit Jala

Zymaxid Gatifloxacin Antibiotic Allergan

Xalatan latanoprost prostaglandin agonist pfizer ‫لعالج ارتفاع ضغط‬

‫العين‬
Refrigerated

xalacom Latanoprost prostaglandin agonist pfizer ‫لعالج ارتفاع ضغط‬

Timolol ‫العين‬
Refrigerated

Eye ointments:
Duratears Anhydrous liquid lubricants Alcon ‫مرهم لمنع جفاف العين‬
lanolin
Mineral oil
White petrolatum

Fucithalmic Fucidic acid Antibiotic Amdipharm ‫مرهم لعالج التهاب العين‬

Jordacycline Oxytetracyclin Antibiotic Beit Jala ‫مرهم لعالج التهاب العين‬

Maxitrol Dexamethasone corticosteroid Novartis

Neomycin Antibiotic
Polymyxin B Antibiotic

Novocort Neomycin Antibacterial Beit Jala ‫مرهم للعين واالنف واالذن‬

Hydrocortisone Anti- ‫يستخدم لعالج التهابات العين‬
inflammatory ‫الناتجة عن بكتيريا تتأثر‬
 ‫بمكونات العالج وتشمل‬
‫ملتحمة العين او القرنية‬
‫لعالج التهاب الجفون والتهاب‬
‫القرنية البكتيري‬
‫يستعمل لعالج التهابات االذن‬
‫الخارجية واالنف‬

Oxycin Oxytetracycline Antibiotic Birzeit

Ramacetine chloramphenicol Antibiotic Birzeit

Ramacetine chloramphenicol Antibiotic Birzeit ‫عالج حساسية وااللتهابات‬

HC Hydrocortisone Anti- ‫رالمصاحبة لعدوى بكتيرية او‬
inflammatory ‫معرضة لالصابة بالبكتيريا‬

Synthomycine chloramphenicol Antibiotic Rekah

Tobrex Tobramycin Antibiotic Novartis

-------------------------------------------------------------------------------------------
Topic 15: Controlled drugs available in the pharmacy:
Name Active Form and dose Company Indications
ingredients
Alpralid Alprazolam Tab: 0.5mg CTS For the relief of States of
anxiety and tension
Clonex Clonazepam Tab: 0.5, 2mg Teva For the relief of States of
anxiety and tension
Frisium Clobazam Tab: 10mg Sanofi For the relief of States of
anxiety and tension
Phenobarbitone Phenobarbitone Tab: 15,100mg Rekah Belongs to the
phenobarbiturate group
Act as sedative and
hypnotic in short-term
treatment of insomnia

Razin phentermine Tab: 15mg CTS Appetite suppressants

that work via the central
nervous system: for
severe obesity not
respond to appropriate
dietary treatment
Spasmalgin Paracetamol Tab: 150+80+10+ Sam-on Analgesic and
Papaverine. 0.4mg antispasmodic for the
Codeine. digestive system, the
Atropine. kidney and the
gallbladder
Sinufed Pseudoephedrine Tab: 60mg Trima For the symptomatic
Syrup: 30mg/5ml treatment of nasal
congestion and relief of
eustachian tube
congestion due to ear
infection

Partane Trihexyphenidyl Tab: 2mg, 5mg Trima Anticholinergic, anti-

parkinsonism
For all types of
Parkinson and for extra
pyramidal symptoms.
Lorocare Lorazepam Tab: 1, 2.5mg Pharmacare Anti-anxiety
Zaldiar Tramadol Tab: 37.5 + 325mg Pharmacare Strong analgesic
Paracetamol
Rivotril Clonazepam Oral drops: Roche Anti-anxiety
2.5mg/ml
Rokacet plus Paracetamol Tab: Taro Strong analgesia
Caffeine 500+50+15mg
Codeine
Paracode Paracetamol Tab: 325 + 20mg Pharmacare Strong analgesia
Codeine
Cytotec Misoprostol Tab: 200mcg Pfizer Prostaglandin analog
To protect stomach
To contract uterus
(abortion).
Lyrica Pregabalin cap Pfizer A gamma-aminobutyric
25,50,75,100,150, acid analog
200,225,300 mg For the treatment of
neuropathic pain in
adults and for
fibromyalgia.
Tramal Tramadol Oral Crunenthal Strong analgesic
drops100mg.
Cap: 50,100
Supp: 100mg

Drug-Drug interaction:
Cytochrome inhibitors and inducers:
 →CYP450 3A4:
Inducers: carbamazepine, St johns wart
Inhibitors: azole antifungal, clarithromycin, grape fruit
Substrates: simvastatin, atorvastatin, cyclosporin

→CYP450 2D6:
Inducers: No inducer
Inhibitors: paroxetine, fluoxetine, quinidine, Terbinafine . . .
Substrates: codeine, risperidone

→CYP450 2C9:
Inducers: carbamazepine, phenobarbital, phenytoin, valproic acid.
Inhibitors: fluconazole, Metronidazole . . .
Substrate: warfarin

→CYP450 1A2:
Inducers: carbamazepine, phenobarbital, rifampin, tobacco
Inhibitors: cimetidine, amiodarone, ciprofloxacin, fluvoxamine
Substrate: theophylline, clozapine.

Examples:
→Aspirin compete with warfarin by binding with albumin
→Antibiotic increase warfarin effect by decrease vit K production.
→Avoid citalopram and escitalopram with omeprazole because of risk of QT prolongation.
→Fibrates and sulfonylureas →delay hypoglycemia
→warfarin and fibrate compete for albumin
→Valproic acid + Lamotrigine →increase the level of lamotrigine cause life-threatening rash.
→carbamazepine decreases the level of ethinylestradiol which may lead to pregnancy.
→clarithromycin increases the level of simvastatin which may lead to myopathy and
rhabdomyolysis.
→fluoxetine increases the level of haloperidol which may lead to extrapyramidal side effect
→Metronidazole increases the level of warfarin which may lead to bleeding.
→Terbinafine increase the level of Amitriptyline which may cause dizziness and dry mouth.
→carbamazepine is both a substrate and an inducer of CYP3A4, thereby inducing its own
metabolism.
→Tobacco decreases the level of clozapine which lead to the failure of the treatment.
→probenecid decreases the clearance of penicillin.
→Alkalization of urine PH decrease the reabsorption and increase the clearance of barbiturate.
→tetracycline and fluroquinolone →chelation with calcium, magnesium, aluminum
→cholestyramine and fibers can bind with digoxin and warfarin
→the reduction of GI normal flora could result in contraceptive failure because contraceptives
undergo enterohepatic recycling.
→digoxin metabolized by bacteria into active metabolite→so co-administration of antibiotics
can cause an increase in digoxin levels.
→high level of protein in food may affect on the transporter of levodopa

Note: most protein binding interactions are not clinically significant.

----------------------------------------------------------------------------------------------------------------

Pharmacognosy:

Active Ingredient Plant extracted from Example of drugs

Hydroxychloroquine Cinchona Bark Plaquenil
Pilocarpine Jaborandi Leaves Pilocarpine Vitamed eye drops
Salicylate Willow Bark Aspirin
Ephedrine /pseudoephedrine Ephedra Sinica Decongex /Clarinase/Sinufed . . .
Atropine Atropa Belladonna Spasmalgin / Atrospan eye drops
Colchicine Colchicum Seeds Colchicine / Goutex
Pyridostigmine Calabar Beans (Physostigma Pyridostigmine Rafa
Venenosum)
Digoxin Digitalis Leaves Lanoxin elixir / Digoxin-Kern Pharma
Tab
Codeine/ Papaverine / Opium Poppy Capsule Spasmalgin /Roacet plus/
Hyoscyamine /Hyoscine kolic/Scobutyl
Caffeine Tea leaves/ coffee seeds Flu / Teva-Cold /Acamol Focus /Exidol
/Cacao seeds It potentiates the effect of analgesic
and it is CNS stimulant
Diprophylline / Theophylline Tea Leaves Dyphylline Supp/ Theotrim /Theotard
Tannic acid Tea leaves Gingipant / Dequabal
Activated Charcoal Pine wood Eucarbon / Gas Clear / NoGasDual
Eucalyptus oil Eucalyptus Leaves Albocal / Strepsils
Clove oil Clove Buds Dento
Isoflavonoids Leguminous Plants Vagilact vaginal supp
Ivy leaves extract Ivy leaves Cofspan / Prospan
Marshmallow White marshmallow root Apipol syrup
Thyme extract Thyme leaves Pikta forte
Sodium alginate Sea weeds Gaviscon
Passiflora extract Passiflora valerian Relaxin / Calmanervin
Hyroquinone Bearberry
Chestnuts Veno-Kashtan cream to improve the
elasticity of vessels to treat varicose
veins
 ‫ل‬ ‫ل‬ ‫م‬‫ُ‬
‫" يا سخر ات ر ِادك‪ ،‬أ ر ا "‬
‫ب‬ ‫م‬ ‫ك‬ ‫ب‬ ‫ع‬‫ل‬ ‫ب‬ ‫ج‬ ‫ا‬ ‫ظ‬‫ح‬
‫ل‬ ‫أ‬ ‫ت‬
‫ي‬‫ط‬ ‫ل‬
‫" أرسلوأ لي دعوأ م فة "‬
‫ك‬

‫يفين شفبرأت ♥‬