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1 -Lactams ( Penicillins Cephalosporins Carbapenems Monobactams )

2 Macrolides

3 Ketolides

4 Lincosamines

5 Aminoglycosides 6 Quinolones
8 Tetracyclines
9 Amphenicols

7 Co-Trimoxazole

PENICILLINS

Adult dose 1 5 million unit / 6 hours IM or IV
Child dose 50.000 100.000 unit / kg / day IM or IV

1 Benzyl penicillins : (penicillin G Vial 1.000.000 unit)

2 Procaine Penicillins
Rarely used nowadays

Sustained-release preparation of benzyl


penicillins

3 Benzathine Penicillins


Bezathine penicillins (Retarpen vial 1.200.000 unit )

( Side effects b , c & d )

Adult dose 1.2 2.4 million unit IM / 1 4 weeks.


Child dose 50.000 unit / kg IM.
IT is used as a prophylactic therapy against streptococcal infection in rheumatic fever or
chronic rheumatic heart disease. Treatment is usually continued until streptococcal infection
and rheumatic fever become unlikely to occur ( usually after the age of 20 25 years ).

Natural Penicillins

It has the following side effects :


a Short duration of action = 4-6 Hours
b Acid sensitive Destroyed by gastric acidity Not effective orally
c -Lactamase (penicillinase) sensitive
d Narrow spectrum

4 Phenoxymethyl penicillins (Ospen) suspension 400.000uint/5ml


(Side effects a,c & d)
Adult dose 250 500 mg / 4 hours orally.

Tablet 1.000.000 unit


Child dose 50.000 unit / kg / day orally

5 Broad-spectrum penicillins Amino-penicillins:


a Ampicillin (Epicocillin) ( 1 2 g / day )
Incompletely absorped orally & affected by food Useful in enteritis .

But

Disturb intestinal flora

b Amoxicillin (E-mox) Similar to Ampicillin but better absorbed orally and not affected by food

- Lactamase inhibitors:
(Clavulanic acid , sulbactam & Tazobactam)
They have very weak or no anti-bacterial activity.
They protect penicillins from inactivation by -Lactamases secreted by some bacteria
Clavulanic acid + Amoxicillin (Augmentin)
Sulbactam + Ampicillin (Unasyn)
Tazobactam + Piperacillin (Tazocin)

6 Acid & -Lactamase (penicillin) resistant (cloxacillin , dicloxacillin and flucloxacillin)


They are useful as antistaphylococcal drugs
They are rarely used alone because of their narrow spectrum . They are usually used in fixed
combination with ampicillin and amoxilcillin
Amoxicillin + Flucloxacillin (Flumox)
Ampicillin + cloxacillin (Ampiclox)
Ampicillin + dicloxacillin (Dipenacid)
7 Extended spectrum (Antipseudomonal) Penicillins : (Carbenicillin, Ticarcillin and Piperacillin)
a Broad spectrum + Effective against Pseudomonas aeruginosa
b They are -Lactamase sensitive.
c Combine with Aminoglycosides Synergism & avoid resistance

Uses Of Penicillins
A) Treatment of :
1 Gram +ve Cocci

2 Gram ve Cocci

3 Gram +ve Bacilli

Pharyngitis , Abscess & Lobar


pneumonia

Meningitis(Benzyl penicillin) Anthrax , Diptheria Tetanus & Gas


& Gonorrhea
gangrene
4 Gram ve Bacilli Use Broad spectrum Penicillins e .g Ampicillin & Amoxicillin :
a Urinary tract infection
b Typhoid fever
c H-influenza : Broad spectrum penicillin + -Lactamase inhibitor.
d Helicobacter pylori Amoxicillin 500 mg tds for 2 weeks
5 pseudomonas : Anti-pseudomonal penicillin = Aminoglycoside e.g. Gentamicin.

B) Prophylaxis of :
Streptococcal infection in rheumatic fever : Benzathine penicillin 1.2 million unit IM/Month for 5 years
or up to age of 20 which is ever longer.

Side Effects Of Penicillins


1 - Allergic Reactions : Urticaria , angiodema & Anaphlylactic shock.
a - Avoid by :
Ask for previous history .
Dermal sensitivity test.
b - Treatment of Anaphylactic shock : Adrenaline + cortisol + Antihistaminic.
c - Never reuse penicillin again.
d - cross allergy with Cephalosporins (10 %).
2 Diarrhea due to superinfection , specially after oral Ampicillin :
a - Candida albicans Monilial thrush & Diarrhea . Treat by Nystatin.
b - Antibiotic associated ( pseudomembraneous ) colitis .

3 -CNS irritation Seizures may occur if Large dose or intra-thecal of penicillin.


4 Usually we use Na+ or k+ salts of penicillins . Large dose of penicillins Na+or k+ over load ,
which could be dangerous in patients with renal or cardiac problems .
5 Benzathine penicillin Pain , enduration & tenderness at site of injection.
6 Ampicillin induces skin rash in 10 % of patients & in All patients with infective mononucleosis ,
leukemia & taking allopurinol
7 Carboxy-penicillins e.g Carbenicilin Platelet dysfunction bleeding .

CEPHALOSPORINS
First Generation

Second generation

Third generation

Forth Generation

Cefixime (Ximacef)
Cephalexin (Ceporex) Cefaclor (Bacticlor)
Cefadroxil (Duricef)
Cefuroxime (Zinnat)
Cephradine (Velosef) Cefprozil (Cefzil)

Cefpodoxime (Cepodem)

Ceftriaxone (cefaxone)

Cefepime (Maxipime)

Cefoperazone (Cefobid)

Cefotaxime (Cefotax)

First Generation :
1 Broad spectrum Active mainly against
Gram +ve organisms.

Second Generation :

2 Resistant to -Lactamase enzymes.

1 Broad spectrum. Similar to first generation


But less active against Gram +ve &more active
against Gram ve
2 More resistant to -Lactamase enzymes.

3 Do Not pass BBB . Not effective in meningitis.

3 Do NOT pass BBB. Except Cefuroxime

Third Generation :
1 Broad spectrum against Gram +ve & -ve
aerobes & anaerobes.
2 More Resistant to -Lactamase enzymes.
3- Excellent pass BBB

Forth Generation:
1 Similar to 3rd generation Ceftazidim, But More
resistant to -Lactamase enzymes.

Ceftriaxone and Cefoperazone are excreted mainly in bile, so allowed in renal patient without
readjusting the dose.
Cefoperazone Less BBB Less effective in meningitis .

Uses of Cephalosporins
1 Infections resistant to penicillins
2 Pseudomonal infections : Cefoperazone & Ceftazidime
3 Gram ve Meningitis : Cefotaxime & Ceftriaxone
4 Respiratory tract infection
5 Typhoid fever Ceftriaxone & Cefoperazone
6 - Urinary tract infection specially Gram ve
7 Gonorrhea Ceftriaxone
8 pre- & post-operative First or second generation Cephalosporins

Side effects of Cephalosporins


1 Allergy & partial Cross-allergy with penicillins (10%)
2 GIT upsets and super infections.
3 Irritant : - I.M. painful , so add lidocaine. - I.V. Thrombophlebitis
4 Nephrotoxicity.
It is augmented by concurrent use of Frusemide and Gentamicin.
5 Ceftriaxone + calcium Insoluble salts in Bile Biliary Sludge
6 Cefoperazone Hypoprothrombinemia
( can be prevented by vit k 10 mg twice weekly )

MONOBACTAM
Aztreonam (Azactam) 1-2g / 6-8 hours IV
1 -Lactamase resistant.
2 Not effective against Gram +ve or anaerobes.
3 100 % bioavailability after IM. Depend on renal excretion.
4 USES Gram ve infections specially is patients allergic to penicillins.
There is no cross allergy with penicillins.

CARBAPENEMS
1 - Imipenem (Tienem)

2 - Meropenem (Meronam)

Very wide spectrum, Gram +ve & Gram ve and aerobes, & anaerobes
1/2 1 g / 6 hours

1/2 1 g tds I.M or I.V

Polymixin B :
Used only locally :
A Topically (usually + Neomycin) as eye drops or skin preparations.
B Orally (Not absorpes) to sterilize the gut.

Bacitracin:
Used topically in staph aureus infections.

Macrolides
Erythromycin
(Erythrocin)

Azithromycin
(Zithromax)

Clarithromycin
(Klacid)

Spiramycin
(Rovamycin)

Erythromycin absorbed orally, but acid sensitive. Used as enteric coated or as an esteolate ester.
Distribution all over the body but not CSF & concentrated in prostatic fluid
Hepatic metabolism Excreted in bile
Azithromycin & Clarithromycin Similar to Erythromycin but longer duration of action and
Less side effects.

Uses of Macrolides
1 Drug of choise in chlamydial infection : Respiratory, Genital & Ocular specially in neonates & pregnancy

2 Sexually transimitted diseases : Gonorrhea, Syphilis & Chlamidia


3 Penicillin substitute in Staph, Strept & pneumococcal in patients allergic to penicillin.
4 In rheumatic patients taking penicillin as prophylaxis prior to dental procedures to avoid bacterial
endocarditis
5 Topically in Acne vulgaris
6 Clarithromycin is used to eradicate Helicobacter pylori infection in peptic ulcer

Side Effects of Macrolides


1 Most common is Epigastric pain . Erythromycin > Others.
2 Cholestatic Jaundice.
3 Large dose of erythromycin Reversible Ototoxicity .
4 Drug Interactions :
a - Erythromycin & Clarithromycin (not Azithromycin) inhibit Cytochrome p 450
Metabolism of Theophylline ,Carbamazepine &Warfarin Toxic concentration
Metabolism Of Terfenadrine & Astemizole Cardiac arrythmias
b - Erythromycin inhibit intestinal flora Metabolism of Digoxin Its absorption

Ketolides
Telithromycin (Ketek) 800 mg/day for 5 10 days orally
Semisynthetic derivative of Erythromycin.
Similar mechanism and spectrum to Erythromycin
Used mainly in respiratory tract infections
Adverse Effects Visual disturbances , Cardiac arrhythmia, GIT disturbances, Pseudomembranous
colitis & worsens myasthenia gravis

Lincosamines
Lincomycin (Lincocin)

Clindamycin (Dalacin-c) : 300 mg/6 hours orally

Uses : 1 Bone and Teeth infections


2 Intra-abdominal anaerobic infections (Add aminoglycoside)
3 Locally in acne vulgaris
Side Effects : 1 Fatal pseudomembranous colitis treated by Vancomycin or Metronidazole
2 GIT disturbances and impaired liver function

Fusidic Acid
Uses : 1 Orally & IV in severe Staphylococcal infection including osteomyelitis
2 Ointment and gel for Staphylococcal infection
Side Effects : Mild GIT upsets

Aminoglycosides
Drug

Uses
1 Serious Gram ve Infection, and Staphylococcal & Enterococcal infections
2 Severe infection : Pneumonia , Ut , Osteomyelitis & Septicemia

Gentamicin

3 Pseudomonal infections. Add Carbenicillin or Ticariciilin

(Garamycin) 4 Bacterial endocarditis. Add Benzyl Penicillin


5 Methicillin-resitstant Staph.aureus (MRSA)
6 Topically (Cream, Ointment or solution) in burns , wounds & Skin lesions.

Tobramycin
(Nebcin)
Amikacin
(Amikin)

Similar to Gentamycin but more effective against p.aeruginosa

Useful in Gentamicin-resistant infections.


1 Used for Local use only

Neomycin

2 Orally as intestinal antiseptic before intestinal operations acute intestinal


infections & Hepatic coma (Add lactulose).
3 Orally in Hyperlipidemia Absorption of cholesterol
4 Topically on skin & Mucous membranes.
5 Inhalation in chest infections.

Side Effects Of Aminoglycosides


1 Ototoxicity
a - Irreversible damage of vestibule-auditory 8th Cranial nerve Deafness
b - Toxicity increased with increased doses , duration and age , impaired renal function and
concurrent use of loop diuretics , Salicylates & Chloroquine.
2 Nephrotoxicity:
a - Usually reversible
b - Increases in patients with poor kidney function
3 Skeletal muscle Relexation
4 Allergic manifestations e.g. contact dermatitis
5 Drug Interactions:
a - Polymixins , Cephalosporins & Frusemide increase their Nephrotoxicity
b - Loop diuretics , Chloroquine & Aspirin increase their Ototoxicity
c - Aminoglycosides + Penicillins Synergism.But Never mixed in same container
d - Chloramphenicol Bacterial Uptake of Aminoglycosides

Quinolones
Ciprofloxacin

Gatifloxacin

Norfloxacin

Levofloxacin

Lomefloxacin

Moxifloxacin

Gemifloxacin

Moxifloxacin

Ofloxacin

Nalidixic acid

Uses Of Quinolones
Urinary Tract Infection , Prostatitis , GIT infections ,Typhoid fever & Respiratory Tract Infection

Side Effects Of Quinolones


1 Allergy & Photosensitivity , use sun-screen & sun-blocks.
2 CNS : Headache , dizziness & confusion Avoid driving .
Seizures specially if used with NSAID Avoid in epileptics .
3 GITupset
4 Chondrolytic Reversible Arthropathy Avoid in pregnancyLactation and in children
up to age of 18 years
5 Nephrotoxic &Crystaluria
6 Rupture of tendons ( Achilles tendon ) in elderly taking glucocorticoids.
7 Drug Interactions :
a - Ciprofloxacin , Ofloxacin Enzyme inhibitors Metabolism of Theophylline , Warfarin &
Sulfonylurea
+3
+2
+2
+2
b - Sucralfate , Antiacids ( AL & Mg ) Food supplements ( Fe & Zn )
absorption of Fluoroquinolones.
C - Fluoroquinolones + NSAID Seizures.

Co-Trimoxazole
Sulphamethoxazole + Trimethoprim (Sutrim)

Uses Of Co-Trimoxazole
1 Respiratory tract infection
2 Urinary tract infection and Prostatitis
3 Gonococcal infection (Urethral & Oropharyngeal)
4 Shigella & Salmonella enteritis
5 Systemic salmonella (Typhoid fever )
5 Prevention & Treatment of Toxoplasmosis

Side Effects Of Co-Trimoxazole


1 Allergy ( Hypersensitivity
a - Manifestations : Fever , photosensitivity & Steven-johnson syndrome.
b - Cross-Allergy with other Sulfonamides e.g. Diazoxide , Sulfonylureas &
Diuretics (Thiazides,Frusemide,Bumetanide & Carbonic anhydrase inhibitor)
2 Blood dyscrasis:
a - Hemolysis in patients with G6PD deficiency.
b - Bone marrow inhibition.
3 Crystaluria: Avoided by , Fluid intake & alkanization of urine.
4 Diarrhea GIT disturb ances & Superinfection.
5 Hepatotoxicity & Nephrotoxicity
6 Drug interactions:
a - Displace Warfarin & Tolbutamide initial increase in their activity
b - Methenamine (Urinary antiseptic) Releases Formaldhyde Inactivate sulfa
7 Megaloblastic anemia
8Displace bilirubin avoid during pregnancy &Lactation

Amphenicols
Chloramphenicol (Cidocetine)

Thaimphenicol (Thiophenicol)

Uses Of Chloramphenicol
1 Typhoid fever & Paratyphoid fever : Start by 750 mg / 6 hours till fever subsides then
250-500 mg / 6 hours for at least 10 14 days
2 Topically in eye and ear infections
3 Vancomycin-resistant enterococci
4 Bacterial meningitis
5 Other bacterial infections : ENT , Respiratory, Urinary & GIT

Side Effects of Chloramphenicol


1 Bone marrow inhibition
2 Gray baby syndrome: in premature neonates , Chloramphenicol is not properly metabolized
Cummulation Toxicity Vomiting , hypotension , hypothermia , hypotonia , shock , collapse &
Gray discoloration of skin
3 GIT upsets & Superinfection.
4 Hepatic microsomal enzyme inhibition potentiate Phenytoin , Theophylline & Warfarin

Tetracyclines
Low to moderate lipid solubility
High lipid solubility
Tetracycline (Tetracid)
Doxycycline (Vibramycin)
Oxytetracycline ( Oxytetracid)

Uses Of Tetracyclines
1 Enteritis
2 Bacillary infections : Brucelosis & Tularemia
3 Urinary tract infections
4 Sexually Transmitted diseases Syphilis and Gonorrhea
5 Skin infections : Acne vulgaris
6 Eye infections : Topical tetracycline
7 Intestinal Amebiasis

Side Effects Of Tetracyclines


1 Teeth & bone Abnormalities: if Tetracyclines are taken during pregnancy & early childhood
chelated by Ca+2 & deposited in newly formed teeth & Bone
a Teeth: Permanent yellow-brown discoloration & Enamel dysplasia.
b Bone: Deformity & inhibition of growth.
c should be avoided during pregnancy , lactation & in children up to 8 years.
2 Teratogenicity
3 G.I.T. irritation: Nausea , vomiting , epigastric pain & diarrhea
4 Inhibit intestinal flora VitB & K deficiency
5 Large doses especially during pregnancy Hepatotoxicity Jaundic e.
6 Nephrotoxicity especially if they used after their expiry date
7 Hypersensitivity
8- Photosensitivity

Doses Of Antibiotics for pediatrics


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ORAL DRUGS

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20 40 mg/kg/day in divided doses every 8 hours

amoxicillin

Amoxicillin+ 25 50 mg/kg/day of the 4 parts amoxicillin , 1 part clavulanic acid preparations (which
corresponds to a daily dosage of the equivalent of 20-40 mg/kg of amoxycillin and 5-10
clavulanic acid mg/kg of clavulanic acid) to be taken in divided doses every 8 hours at the start of a meal
50 100 mg/kg/day in doses divided every 6 hours

Ampicillin

25 50 mg/kg/day in 3 4 divided doses

& Cephalexin
Chloramphenicol

25 50 mg/kg/day in divided doses every 8 hours

Cephradine

25 50 mg/kg/day in asingle dose or in divided doses every 12 hours

cefadroxil

20 40 mg/kg/day in divided doses every 8 hours

Cefaclor

20 40 mg/kg/day in asingle dose or in divided doses every 12 hours

Cefprozil

20 40 mg/kg/day in divided doses every 12 hours

cefuroxime

8 mg/kg/day in divided doses every 12 hours

Cefpodoxim

14 mg/kg/day in asingle dose

Cefdinir

8 mg/kg/day in asingle dose dose or in divided doses every 12 hours

Cefixime

= * ) ( / / 30 50 mg/kg/day in 3 4 divided doses

Erythromycin

= / / 10 mg/kg/day in asingle dose

Azithromycin

Clarithromycin

15 mg/kg/day in divided doses every 12 h

Sulphamethoxazole+
Trimethoprim

( / ) ( / ) * =

0.5 1 ml / kg /day in divided doses every 12 hours

Parenteral
Amoxicillin

50 100 mg/kg/day in divided doses every 8 hours

Ampicillin

100 150 mg/kg/day in doses divided every 6 hours

Sultamicillin
(Unasyn)
Co-Amoxiclav
(Augmentin)

150 mg/kg/day 3 4 divided doses


3 months-12 years: --> Usually 30mg/kg every 8 h. (In more serious infections,
increase frequency to every 6 h)
0-3 months: in premature (less than 4kg) --> 30mg/kg every 12 hrs

Cephradine

Cefotaxime

50 - 100 mg/kg/day in 4 equally divided doses.


Children and infants
50-100 mg/kg/day in 2-4 divided doses. A maximum dose of 200 mg/kg/day in 2-4
divided doses may be given in exceptional cases.

0 - 1 week of age
50 mg/kg IV every 12 h
1 - 4 weeks of age

Cefoperazone

50 mg/kg IV every 8 h
25 -100 mg/kg every 12 hours

Infants and young children may receive from 20-80 mg per kg body-mass daily;
depending on the severity of the infection, usually 12-24 hourly.

Ceftriaxone
Ceftazidime

In cases of premature babies, the daily dosage should not exceed 50 mg per kg body
mass on account of the immaturity of the infants enzyme systems.
50 - 100 mg/kg/day in 2 divided doses.
Patients 2 months of age with body weight <40 kg: 50 mg/kg q12h for 10 days. For more
severe infections, a dosage schedule of q8h can be used.

Cefipime

Gentamicin
Amikacin

Experience with the use of MAXIPIME in paediatric patients <2 months of age is
limited. While this experience has been attained using the 50 mg/kg dose, modelling of
pharmacokinetic data obtained in patients >2 months of age suggests that a dosage of
30 mg/kg q12h or q8h may be considered for patients aged 1 month up to 2 months.
3 5 mg/kg/day in divided doses every 8 hours
15 mg/kg/day divided into 2 or 3 equal doses. Treatment should preferably not continue
for longer than 7 to 10 days, and the total dosage in adults should not exceed 15g .