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Coronary Artery Di sease

Coronary Artery Diseases


Types of angina I

IStable angina l !unstable angina ll Exercise-induced


Prinzmetal angina

Chronic angina l

~octumal Anginal

Or
Vasospastic angin
Coronary artery Diseases
The most common complications associated with Coronary artery disease include: Angina pectoris,
Myocardial infarction, post Myocardial infarction,and Ischemic stroke. Insufficient supp ly of oxygen
to heart can lead to Ischemic conditions.
Myocardial ischem ia is usually caused by coronary vessel atheroscleros is (High LDL
and high cholesterol is the most common risk facto r). As the vessel lumen nalTOws blood
flow is reduced.

Other causes that limit coronary blood How include: Arterial thrombi and Spasm

A ngina Pectoris
Angina are those symptoms of myocardial ischem ia that occur when myocardial oxygen availability
is insufficient to meet myocardial oxygen demand.
These symptoms include:
Chest discomfort often described as heaviness, pressure, and squeezing. The sensation is
localized typically in the sternal region.

Symptoms often last one to five minutes. Angina can radiate to the left shoulder, to both anns
(ulnar surfaces of the foreann and hand), and can radiate to the neck,jaw, teeth, epigastrium and
back.

Types of angina
Angina Pectoris

Severe chest pain because of inadequate coronary blood How to supply


oxygen demand.
Which is usually aggravated by exertion or stress and relieved by
nitroglycerine.
The most common form of IHD.

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Types of angina
pectoris

Nocturnal
angina (angina
decubitus)

Stable anginal Classic angina (most common-90%)


Unstable angina
Exercise induced angina
Exertion angina
Chronic angina
Prinzmetal angina
octurnal angina
Mostly secondary to atherosclerosis (high LDL)
Due to obstruction in coronary arteries
More predictable
Precipitated by exertion or emotional stress or by heavy meal.
Relieved by rest or using nitroglycerine's
The most serious one (worsening pain)
Thrombosis in a branch
Caused by formation atherosclerotic (disease of arteries, in fatty plaques
develop in inner wall), occurs at rest
ACE inhibitors are used as single treatment
Decreased response to rest and nitroglycerine
This angina occurs in the recumbent position and is not specifically related
to either rest or exertion
Nitroglycerine may relieve the paroxysmal nocturnal dyspnea

Prinzmetal
angina
(vasospastic or
variant angina)

Coronary artery spasm that reduces blood flow precipitates this angina.
Secondary to coronary artery spasm
Usually occurs at rest (pain may disrupt sleep)
Calcium channel blockers are most effective

Stable angina or
classical

Unstable
angina/resting!
Crescendo

I Vasod ilators I
INitrates I

Drugs Used In Angina Pectoris

I Cardiac depressants I

Calcium blockers, and ACE inhibitors


Nifedipine, Verapamil, Diltiazem

Short duration
Inhaled amyl nitrite
Sublingual
Nitroglycerine
Isosorbide dinitrite

Intennediate
Oral regular or sustainedrelease Nitroglycerine
lsosorbide dinitrite

~-blockers

Proponolol

Long duration
Transdermal
Ntiroglycerine patch

Treatment of angina
The following beta-blockers are used in treatment of angina:
Beta-blockers with Selective Intrins ic Sympathomimetic Activity (ISA) :
Acebutolol hydrochloride Beta-blockers with Non-I SA: Atenolol
and Metoprolol tartrate can be used.
Beta-blockers w ith Nonselective, ISA: Pindolol
Beta-blockers with Nonselective, Non-ISA: Nadolol, Propranolol hydrochloride,
Timolol maleate
Calcium Channel Blockers are used in treatment of angina:
Amlodipine besylate, Diltiazem hydrochloride, Nifedipine, Verapamil hydrochloride
The following Coronary Vasodilators, Nitrates are used in treatment of angina:
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Coronary Artery Disease

Nitroglycerin, Isosorbide dinitrate, Isosorbide5 mononilrate.

Nitrates

Ht

Nitri tes

rl t

Nitric oxide (NO)

1-+1t cGMP
~

V",So<l'l._~'

Nitrates

Organic nitrates act primarily by vasod ilation (especially venod ilation), which reduces
myocardial preload and therefore myocardial oxygen demand.
Nitrates also promote redistribution of blood flow to relative ischemic areas.
Mechanism

ft~~~;::cts\

~-""
~)
Storage
Conditions

Drug
interactions
Dosage forms

Vascular smooth muscle relaxation


Two major effects
Dil ation of the large veins (resulting of pool ing blood in veins-7 this
reduces preload and decrease work of heart.
Di lates coronary vasculature, providing increased blood supply to the heart
muscles.
The Most common side effect is headache.
Higher doses: Postural hypotension, fac ial flushing and tachycardia.
Tolerance-7 develops rapidly.
This can be overcome by usi ng "nitrate free period" and restore sensiti vi ty
to drug.
Amber color, glass and metal capped
Dispense in original container
Discard cotton present on tablets in bottle.
Drug expires after 6 months from the day bottle open.
Light sensitive, hygroscopic.
Cause hypotension with Sildenafil, Tadanafil, Verdanafil.
Additive hypotension effect
Nitroglycerine SL -7 Acute
N itroglycerine Pump -7 Acute
Nitroglycerine Patch -7 Maintenance

fU-W)

Nitrites
Therapeutic use
Side effects

DOC for hypertensive crisis


Cyanide toxicity (releases CN)
_
Sodium thiosulfite is an antidote
~ ~
(Cyanide (Intermediate) + Sodium thiosulfite -7 Sodium thiocyanate
(water soluble)
Photosensiti ve

><

Ca2+ channel Blockers


These agents are used to treat hypertension and are effective in treating angina as wel l. All musc les,
including the smooth muscle of the blood vessels, require calcium in order to contract. If the
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calcium-channel blocking agents block the entrance of calcium into the muscle, the muscle will not
contract. This will allow themuscle to relax and subsequently reduce the blood pressure. Other
therapeutic uses: angina, migraine, antiarrhythmic.

Non
dihydropyridines

Diltiazem hydrochloride
Verapamil hydrochloride

Verapamil is similar to Beta blockers in effect


Verapamil can cause bradycardia
The effect on Heart is graded from higher to lower: verapamil >
diltiazem > nifedipine
Verapamil ~ avoid using in CHF (cause -ve inotropic effect) and
constipation
Nifedipine
Dihydropyridine
Felodipine
Amlodipine
Nicardipine
Nifedipine is similar to Nitrate in effect (peripheral ~ decrease aftcrload,
dihydropyridine can cause tachycardia.
Dihydropyridines Relax and dilating arteries . The effect on vascular smooth
muscles is high with dihydropyridine: nifedipine > diltiazem > verapamil
Comparison of d ihydropyridine and Non-dihydropyridine
Mechanism

DHP

NDHP

Cause Reflex tachycardia


No heart blockade
Peripheral vasodilation
Amlodipine long half-life
(Only amlodipine does not cause
reflex tachycardia)
Can be used in asthma
Avoid CYP3A4 Inhibitorsflnducers

Cause Bradycardia
Cause Heart blockade
Myocardial vasodilation
Negative (-ve) inotropic
effect (worsening CHF)

iltiazem

Coronary Dilatation ~

(GFJ)

Side effects: flushing, profound low blood pressure, swelling oflegs and feet, constipation and
stomach upset. Ifedema (swelling) of the legs and feet occur, a diuretic may be added to the
regimen.

Nifedipine (Adalat)
Mechanism
Therapeutic use

Side Effects

A calcium blocker which interfere with conduction of signals in the


muscles of the heart and vessels.
Given regularly to prevent Angina attacks.
Reduce high blood pressure and is often helpful in improving
circulation to the limbs in disorders such as Raynaud's disease.
Blood pressure will fall too low' and sometimes causes heart rhythm.
Tachycardia, flushing, headache, dizziness, Orthostatic hypotension,
and edema

Amlodipine (Norvasc)
Mechanism

A calcium blocker which interfere with conduction of signals in the


muscles of the heart and vessels.
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Therapeutic use

Sidc Effects

Coronary Artery Disease


Angina and Chest pain
Can be safely used by asthmatic and noninsulindependent
diabetic.
Blood pressure may fa ll too low
Sometime may cause mild to moderate leg and ankle swelling

Diltiazem (Cardizem)
Mechanism
Therapeutic use
Side Effects

A calcium channel blocker that interfere with the conduction of


signals in the muscles of the heart and blood vessels.
Angina
Longer acting formulations are used to treal hi gh blood pressure
Usually well tolerated, occasional hypotension or orthostatic
hypotension, flUSh ing, arrhythmia, and bradycardia. Use with
caution in patient with CHF

Myocardial Infarction (Heart attack)


Mechanism
Drug of Choice
for Acute coronary
syndrome

ASA

Post MI

Myocardial ischemi a is usually caused by coronary vessel


atherosclerosis . As the vessel lumen narrows blood flow is reduced
Acute MI 7 ~ b l ockers, ACE, CCB,
Prophylaxis (prevention)7 ASA (608\ mg/day), Ni troglycerine
Severe chest pain-7 Morphine
Anticoagulants-7 Heparins. LMWH,
Warfarin
Antipiatelets7Aspirin, clopidogrel,

M9i01en~
tlc\opldme
~Iood
A = AnalgesIcs
.IIU
A = AntipyretIcs
Anglo1enslnl
A = Antiinflammatory
~An9~'ln

conwrtlng
A = Anllplatelets (6081 mg/day)
Kidney
fn>yMe
lung
Aspi rin decrease morbidity and mortality
AngIoIensltl ll

fj-"" "'- t

oCCB

ft

Vasocon.-"

tAldost_ _ 1on
Thrombolytic used for coronary
t ADH $Ietlon
perfusion, eg: streptok inase
lThI."
Also Glycoprotein lIB, lilA inhibitors such Ttrofiban can be used

STEMl treatment ASA, Betablockers, Nitrates, CCB, Thrombolytics


NSTEM I treatment: ASA, Betablockers, Nitrates, Heparin

Coronary Artery Disease Ti.ps


-I, () 1:> ~'M

Nitroglycerine spray storage and admin istration 7


'y-~~
"0.-
Nitroglycerine SL storage condition require-7 c..-...J.- l '('~
~ C'
Light sensitive -7
~~
Nitrates should be avoid taking with -7 .1. "
What is active moiety of nitrates 7 ~ \. \..) \ ( ~~():-
. Nitroglycerine is chemically classified as -7 l\J 1
~
Nitroglycerine + seldanafil can cause hypotens ion and this due to nitroglycerine and seldanafil.

i:.. e-..p

:::--r )

!J ~

\r

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The most common side effect ofni lroglycerine is headache; therefore nitroglycerine should be
taken while sitting position .
Nitroglycerine patch can cause tolerance, to avoid tolerance use nitrate free period.
What drugs effective in MI prevention and treatIl}ent -7 "t.,~). .f\ ')
J
What drugs should be avoided in MI -7 ~\ ?\~u..\.\IJ
~ c ~_ 1'1 _ I M Severe C.hest pain associated with Ml treatedb~ -7 \'\};~ ~
0 0 ~ -

-r\ ()

H, -) -:;.

M,

STEM] -)
~ ;":-'-~ ~
NSTEMl -) ,,",0'" S..
~ MAt what dose ASA act as Antiplatelet -7 b C> _ {1 \)
,
ASA act as irreversible Antiplatelet drug
Nitrates -7 Increase nitrites -7 Increase N itric oxide (NO) -7 vascular smooth muscle relaxation

Abbrevation and Tenninology


LDL
IHD
SL
CN
CCB
MI
ACE
ASA
STEM ]
NSTEMI

Low-density Lipoprotein

Angiotensin-Converting Enzvme
Acetyl Saliaylate
ST-Segment Elevation Ml
non-ST-Se ment Elevation MI

Generic and Brand


Verdanafil
Sildenafil
Tadanafil
Nitro russide

Levitra
Viagra
Cialis
Nitrooress

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Congesti ve Heart Failure

Congestive Heart Failure (CH F)


Drugs Used to treat Congestive Heart Failure

Positive inotropic drugs

Vasodilators

I
Cardioic
g1ycosides
Digoxin
Digitoxin
Quabain

p-agonists,
Dobutamine
POE inhibitors
Amrinone

ACE inhibitors
Captopril
Enalapril
Lisinopril

Nitrates,
Nitroprusside,
Hydralazine,
POE inhibitors
Milrinone

Congestive heart failure is characterized by reduced cardiac output so that the heart is not able to
pum p sufficient oxygenated blood strongly enough to reach the tissues. The heart beat is weak and
rapid and the heart muscles may hypertrophy (grow larger) to compensate for reduced cardiac output.
Atrial fibrillation occurs when the atria beat rapidly and out of sequence.
Cardiac Heart failure due to:
Increased sympathetic activity
Fluid retention (edema)
Decrease in heart muscle contractil ity
Due to negative (-ve) inotropic effect
Due to +ve chronotropic effects
Left systolic dysfunction
Left sided failure (systolic failure)
This is the most common type of heart failure, Often due to hypertension. Due left ventricular
(systolic) dysfunction leads to pulmonary edema; Symptoms: SOB (Dyspnea), Wheezing. Can be
treated by ACE l, and beta blockers (rarely in chronic), only carvedilol (PI , P2 and 0.1).
The Most common etiology of left sided heart failu re is:
Due to impaired pumping abi lity of the heart
Usually occurs in Left ventricular ejection fraction
May be present without CHF
Ejection fraction is lower than 35%, it is Left ventricular dysfunction (systolic failure)
Right Sided Heart failure (diastolic failure)
Due to chronic lung d isease, Diastolic filling is impaired this can leads to peripheral edema.
Symptoms: edema in veins, legs, bowel. Diuretics or Dihydropyridine cess treats ri ght-sided
heart failure.
Ejection fraction is greater than 45%, it is Right ventricular dysfunction (Diastolic fa ilure)

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The Treatment of Congestive Heart Failure (CHF)


The treatment of congestive heart failure may include: diurectics to reduce the back-up of fluids
in the lungs an the rest of the body; vasodilators that decrease vacular resistance and help improve
circulation through the heart; ACE inhibitors to improve cardiac function an y may slow the
progression ofCHF and Angiotensin n ATI receptor antagonists.

Cardiac glycosides
Mechanism

Positive Inotropic
effect

Negative
chronotropic effect

Digoxin, digitoxin, Ouaban


Cardiac glycoside increase myocardial contractility ad efficiency
Improve systemic circulations
Improve renal perfusion
Reduce edema
Inhibit the membrane bound Na+lK+ activated ATPase
Increase intracellular sodium concentration
Reduce calcium transport form cell
Facilitate calcium entry via voltage gated membrane channel
Increased vagal tone of the (SA) node
Reduced CNS sympathetic out flow
Systemic arteriolar and venous constriction

Vagomimetic effect

Increased vagal tone of the sinoatrial (SA) node.

Side effects

Early stages of toxicity:


GI: Anorexia, nausea & vomiting and diarrhea
eNS: Headache, visual disturbances (green and yellow vision) Confusion,
neuralgia, delirium

Digoxin (Lanoxin)
Digoxin

Bioavailability

Therapeutic use

Digoxin is the most widely used


cardiac g lycoside
Don' t confuse with digoxin with
doxepin, Desoxyn, or digitoxin.
75% bioavailability, 20-40%, protein
bound
T 1!2=40 hr
Urinazy excretion
CHF. Atrial fibrillation, protects ventricles

Inh ibits (slows)

+-r.~9i\""'a/K ATPase

+---;:=:f;-Na

Reduced Na
gradient ~)OW~
Caremoval

Digoxin Mechlln l~m of Action

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Side effects

Congestive Heart Failure


I" sign: 01 effects: Nausea, vomiting,
diarrhea, Blurry yellow vision,
scotoma.
CVS ~ Arrhythmias, ventricular
tachycardia
CNS ~ visual disturbances
(blurred vision)
Patient should understand the
importance offollow up laboratory
test for this medication;
Pulse

Monitor

Increased force of contractio n

Decreases and systolic volume

Decreases wa ll tension

ECG
Counselling

Increased ejection of blood

Adjust the dose with renal failure


patients
Do not take extra dose if dose missed.
Use same brand consistently.
Avoid high dose sod ium medications
Do not take with high fiber food ; fiber
diet may reduce digoxin absorption.

Improves Oxygenation

Digoxin mechanism of action


Electrolyte 'rearrangement'
(Mechanism)

j lnotropy
(Desired)

Tachyarrhythrnias
(S ide effect)

Increased Vagal tone


(Mechanism)

Bradyarrhythmias

(Side effecl)

! Heart Rate
(Desired)

Digitalis toxicity
Digitalis
toxicity

Predisposing
factors

Toxicities of digoxin
increased by renal failure
(decrease excretion)
Hypokalemia, or
hyperkalemia (potentiates
drug effect)
Hypothyroidism, hypoxia,
renal failure and myocarditis
also predisposing factors for
digitalis toxicities.

Drugs that cause digitali s toxicity


Drugs that 1 digoxin
levels
Amidome
Verapamil
Erythromycin
TetracycJin
I Quinidine

Drugs that ! K+
levels
Thiazides
Loop diuretics
Corticosteroids

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Digital is toxicity: Reduced
potassium levels
Digitalis toxicity can be
managed by: discontinue
digoxin, monitor blood
potassium levels. Sever
tachycardia may require
the use ofFAS antibodies.
Which bind to inactive
digoxin
Di gifab

Digital is
toxicity
Management

Antidote

P,_L
P

Comparison of digoxin and digitoxin


Digox.in
Digox.in has advantage
of a relatively short
half life, which allows
better treatment of
toxic reactions.

Di itoxin
Binds strongly to
proteins extravascular
space, resulting in
large volume of
distribution.

Rapid onset of act ion.

Slow onset of action

Digoxin eliminated
largely unchanged in
Urine

Extensively
metabolized by liver
before it excrete in
feces.

_u - N,

Left ventricular heart failure cause -7


-_----~ -::---0
(2,
Ri ght ventricular heart failure cause -7
..I~-..Q ~.
DOC fo rCHF 7 1\L C)
.
'", ;\.~
-\I ~L
Digoxin pharmacological action include -7 -tV
v l...~,
~
.
~
Comparison of digoxi'l. and ii,gitoxin, which is short acting and why-7 ~(j<-'Ll...I. ~ ) IL C)
Digoxin antidote -7 -tlf"flt~
Sjgnsof digoxintoxicity ~ .~ ~~. JV.J ....... }~.

-e....,

e.

li

~
Vc,....~O\.1.I""'J;c..
IJ

Abbrevation and Tenninology


CHF
ACE
CCB
CNS
SA
ECG
CYS

Congestive Heart Failure


Angiotensin-Convertin Enzyme
Calcium Channel Blocker
Central Nervous System
Sinoatrial
Electrocardio ra h
Cardiovascular System

Generic and Brand


Amidorne
Veraoamil
Erythromvcin
Tetracyclin
uinidi ne
Digoxin
Digitoxin
Ouaban

Calan Calan SR Covera-HS Isootin.lsoDtin


Emtet Panmvcin Sumycin Sumycin
uin-Tab uinadure uinaglute, Quinidex
Lanoxin
Crvstodigin

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Congestive Heart Failure

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Antiarrhythmic Drugs

Anti Arrhythmic Drugs


Antiarrhythmic Drugs Classification

T
Class II
P-blockers
Esmolol
(Propranolol)
TImolol
Atenolol
Metoprolol
Nadolol

Class I
la-Na! channel
blockers
Quinidine
Procainamide
DisoQY!iIll ide
\.;.\miodaronO
Ib: Lidocaine
Mcxilctinc
Tocainide
Ic: Flecainide
ropafenone
la

Ib
Ie
II
III

IV

Class III
K+ channel

inhibitors
Amiodarone
(Cordarone)
Bretylium
Dofetilide
Sotolol

N a+ channel blocker
N a+ channel blocker
N a+ channel blocker
Beta blockers
K+ channel blockers
Cal+ channel

Class rv
Ca 1+ channel
blockers
Verapamil
Diltiazem
Nifedipine
(procardia, Adalat)

Miscellaneous
Adenosine
Magnesium

Slows ohase 0 deoolarization


Shortens nhase 3 renolarization
Sil!nificantlv slow nhase 0 denolarization
Decrease Dhase 4 denolarization
Prolon!! nhase 3 renolarization
Shortens action notential

Arrhythmias
Arrhythmias develop because of abnormal impulse generation, propagation or both.
Cardiac arrhythmias are related to abnormal electrical activity within the heart resulting in either
altered rhythm or impulse conduction.
Dysrhythmia--disturbed heart rhythm
Arrhythmia - absence of rhythm
Bradycardia - a heart rate that is lower than nonnal 60 beats/min).
Tachycardia - a heart rate that is higher than normal (> 100 beats/min).
Paroxysmal - an arrhythmia that suddenly begins and ends (may occur with fever)
Sinus bradycardia - low sinus rate <60 beats/min ( between the pacemaker and atria).
Sinus tachycardia - high sinus rate of 100-180 beats/min as occurs during exercise or other
conditions that lead to increased SA nodal firing rate.
Atrial flutter - sinus rate of250-350 beats/min.
Sick sinus syndrome - a disturbance of SA nodal function that results in a markedly variable
rhythm (cycles of bradycardia and tachycardia).
Atrial tachycardia - a series of3 or more consecutive atrial premature beats occurring at a
frequency> I OO/min; usually due to abnormal focus within the atria and paroxysmal in nature.
This type of rhythm includes paroxysmal atrial tachycardia (PAT).
Atrial fibrillation - uncoordinated atrial depolarizations.
Junctional escape rhythm - SA node suppression can result in AV node-generated rhythm of 4060 beats/min (not preceded by p-wave).
AV nodal blocks - a conduction block within the AV node (or occasionally in the bundle of Hi s)
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Antiarrhythmic Drugs

[hal impairs impulse conduction from the atria to the ventricl es .


Types of pacemakers
Natural (main) pacemaker of heart
SA node
Latent pacemaker of heart
AV node
Bundles of His
Purkinje fibers
Pulse direction: SA node ? AV node ? His ? Purkinje fibers
Supraventricular arrhythmias (SVA)-arrhythmias develops above the bundles of Hi s
Ventricular arrhythmias (VA)-->devel ops below the bundle of Hi s
Types of arrhythmias
Supraventricular (atrial) SVA
Premature atrial contraction
Atrial flutter
Atrial fibri llation
Paroxysmal supraventricular tachycardia (PSVT)
Si nus tachycardia
Si nus bradycardia
Ventricular arrhythmias (VA)
Premature Ventricular Contraction (PVC)
Ventricular tachycardia (VT)
Ventricular fibrillati on (VF)

Heart blockade:
The el ectrical impulses are partially or fully blocked between the atria and the ventricles . The SA
node in the right atrium ' fires' at the normal rate, but the rate at which the ventricles contract (pulse
rate) depends on how many impulses get through to the ventricl es.
Three types:
1it degree ---blockage of pulsation
2nd degree ----blockage of pulsation
3rd degree---complete heart block
First-degree heart block means there is a slight delay in each impulse going from the atria to the
ventricles. But, each impulse does get through and the heart rate is nonnal.
Second-degree heart block means that some impulses from the atria are not conducted through to
the ventricles. The rate that the ventricles contract can then be slow.
Third degree or ' complete heart block' means that no impulses are conducted through. The
ventricles then comract at their own intrinsic rate of about 20-40 beats per minute. So, you have a
very slow pulse.
Myocard ial Action Potential Curve
Myocardial action potential curve reflects action potential, which describe electrical activity of five
phases.
This occurs in atrial and ventricular myocytes and Purkinje fibers

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Antiarrhythmic Drugs

Phase 0: Rapid Depolarization: Na+ enters the cell


-7All Class la drugs
Phase J: Early rapid repolarization: K~ leaves the cell
Phase 2: Plateau: Ca2+ enters the cell
Phase 3: Final rapid repolarization: K+ pumped out
of the cell
Phase 4: Slow depolarization: K* inside the cell and
Na+, Ca2+ out side the cell
Phase I to starting phase 3 is Absolute refractor
Period or Effecti ve refractory period -7 The cell
cannot respond to any stimuli
During Phase 3 is relative refractory period -7 The
cell ability to respond stimuli increases or cell can
respond to strong sti muli

mV
3

IJ,,~

"

~ '-.

~----~=~~-~~~~
Myocardial action pOlential curve

Torsade de pointes
A problem in one of the ion channels can prolong the Q-T interval. A prolonged Q-T interval can
increase ri sk for a type of arrhythmia called torsade de pointes. When torsade de pointes occurs,
heart cannot pump enough oxygen-rich blood to the rest of body, especially your brain. Torsade de
pointes can also lead to ventricular fibrillation, a dangerous fonn of arrhythmia that causes rapid,
uncoordinated contractions in the muscle fibers of the ventricles. With ventricular fibrillation, the
heart cannot pump oxygen-rich blood to the rest of the body, wh ich can lead to death.
Drugs and diseases that can lead to QT-prolongation
Phenothiazines and haloperidol -7 anti psychotics
Type III antiarrhythmic drugs
In patients with hepatic fai lure.
Electrocardiograph Wave Forms
The electrical acti vity occurred during depolarization and
repolarization transmitted through electrodes attached to
the body and transformed by an electrocardiograph (ECG)
in to series ofwavefonns;
P WAVE: indicated atrial depolarization
PR INTERVAL : indicates the spread of the impulse from the atria through Purkenje fibres.
QRS complex: indicates ventricular depolarization
ST segment: indicates phase 2 or the action potential- the absolute refractory period.
T wave: shows phase 3 of the action potential-ventricular repolarization.
Q-T interval -7 mechani cal contraction of the ventricles (Torse de pointes)
U wave -7 caused by hypokalem ia

Arrhythmias Treatment
Class I
Class la

Quinidine -7 decrease 50% digoxin, SE:Torsades de pointes


Procai namide -7 SE:Torsades de pointes
Di sopyramide -7 SE:Torsades de pointes

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Class la

Therapeutic use
Class Ib

Therapeutic use
Class Ic

Therapeutic use
Class II
Beta blockers

Therapeutic use
Class III
K ~ channel
blockers

Class IV
Ca2+ channel
blockers
Therapeutic use
Digoxin

Therapeutic use

Antiarrhythmic Drugs

Pharmacological action;
Slow the phase 0 (slow entry of Sodium ion)
Prolong re-polarization
Prolong effective refractory period
Indicated to treat SVT, VT
Lidocaine
Tocainamide
Mexiletine
Pharmacological action:
Min imal effect on Phase 0 Slow phase -III repolarization (decrease K
pump o ut)
Indicated to treat VT, VA
iv Lidocaine: used to treat cardioversion related arrhythm ias
Encainide,
Propafenone ~ decrease 25-50% digoxin
Flecainide
Pharmacological action:
Very effective on slowing phase 0 depolarization
Little effect on repoiarization
Indicated to treat VA
Propranolol
Atenolol
Timolol
Pharmacological action:
Competitively block catecholamine induced stimulation of Beta
receptor thereby
Suppress phase I V depolarization
Indicated to treat AT, SVT, VT, VA
Amiodarone ~ blue skin, photosensitivity, photophobia
Bretyl ium
Sotalol
Prolong Phase II I repolarization (Prolong QT interval) ~ Torose de
pointes
Indicated to treat VA
Verapamil
Diltiazem
Nifedipine
Pharmacological action: Shortens action potential
Indicated to treat SVA, VA
Pharmacological aClion: Effects vagotonic response (vegomimetic)
thereby increases AV nodal refractoriness.
It is contraindicated in ventricular fibrillation.
Ventricular taChycardia may result from digitalis toxicities
Indicated to treat SVA (atrial arrhythmias) only
Contraindicated in ventricular arrhythmias

Quinidine (Quinaglute)
Mechanism

Binds to sodium activated channels


Inhibits ectopic arrhythmias, VA

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Therapeutic use
Drug-Drug
interaction

Side Effects

Counselling

Antiarrhythmic Drugs
Atrial, AV junctional, and ventricular tachycardia.
Maintain sinus rhythm after direct atrial flutter or fibrillation.
Antihypertensive, Anticoagulant - Quinidine may increase the effects of
these
drugs.
Phenobarbital and Phenytoin - reduce the effect of quinidine
Digoxin-Quinidine increases the effects of digoxin (decrease 50% digoxin
dose).
SA and AV block or asystole, nausea, vomiting, diarrhea (cinchonism-large
doses-blurred vision, tinnitus, headache, disorientation and psychosis. Torsos
De pointes (VA)
Toxic level ~induce ventricular tachycardia.
Increases steady state concentration of digoxin by displacing PPB
Report tinnitus, blurred vision immediately
Avoid concurrent use of aluminum containing antacids
Keep out of reach of children
Administer after meal to minimize gastric distress
Don ' t crush tablets because drug irritates mucosa.

Procainamide (Pronestyl)
Mechanism
Side Effects

Binds to sodium activated channels


Chronic use: lupus like syndrome (25-30%), toxic levels-asystole or
induction of VA.
GI intolerance is less than quinidine.
CNS depression, hallucinations and psychosis.

Amiodarone (Cordarone)

Side effects (4P)

Amiodarone is structurally related to thyroxine, and it contains iodine.


I. DOC antiarrhythmic & recommended in more severe LVD & ifC! with I BB
2. IV Amiodarone --effec-tive in terminating VT, more so in preventing
recurrence
3. Most effective fo r thx in electrical storm
4. Usually used as an empiric therapy
,f.)
Respiratory: Pulmonary, mcluding Intererstitia~leumonitis; Respiratory
muscle impairment
GI: nausea, anorexia, constipation; hepatitis and cirrhosis;
Hypothyroidism ; hyperthyroidism; Amiodarone inhibit(fripheral conversion

ofT~ toT]

Counseling

Blue skin color gn:aentation), corneal deposits, hepatic toxicity, optic neuritis,
erectile dysfunc IOn~otophobia
Avoid exposure to sunlight, use sunscreen
Avoid grapefruit juice

Digoxin (Lanoxin)
Therapeutic use
Contraind icated

Atrial arrhythmias
Ventricular fibrillation and hypokalimic patients

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Counseling

Antiarrhythmic Drugs
May be taken with or without food
Meals wI bran fiber, antacids may reduce amt of drug absorbed
Store between15-25 0 C in a tight container and protect from light

Antiarrhythmic drugs Tips


What phases of action potential curve have no effect of stimuli 7
~e. \
~
Relative refractory period is 7
~
_ .
Phase I action potential is 40 (+ve) due to 7 '-("~
~ L. 0.. f'I_
What drug cause QT prolongation (torse des pointes) 7
. Y~Il'J~:;I({ ~ .
Digoxin is contraindicated in what type of arrhthmias 7 V.a......., . F \ b
Patient taking digoxin, the prescription is expired what will you do? ~ K
Amiodorone side effects are: Photosensitive reactions, skin pigmentation, Blurred vision.
Pulmonary toxicity, Pneumonitis.

t;

'(',,~

'A,

Abbrevation and Tenninology


SVA
PSVT
VA
VT
SVT

Supra Ventricular Arihythmias


Paroxysmal SupraVentricular Tachycard ia
Ventricular Arihvthmias
Ventricular Tachvcardic
SUDraventricular tachycardia

SA

AV
PVC
ECG
PPB
LVD
BS

Premature ventricular contraction


Electrocardiograph
Beta Blocker

Generic and Brand


Amiodarone
Digoxin
Procainamide
Diso ramide
Encainide
Ro afenone
Digoxina
I Quinidi ne
Procainamide
Flecainide

Cordarone
Lanoxin
Procaine SR
No aceCR
Enkaid
Rhythmol
Lanoxin
uinagiute, Quinidex
Pronestvl Procan Procanbid
Tambocor

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Antiarrhythmic Drugs

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MoA

(... ~ I "" &:;"", -.(J opl


\ \ <i'

P"" r l' 'V

LM\V H

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Anticoagulants

Anticoagulants
I Anticoagulants I
I

I Antithrombin III I

Mucopolysaccharide

I
",.J

Protein C

' . "'--

W -0--

Endogenous
Anticoagulant

Vitamin K
~ analogue

':>1

~ ~'~-- I Warfarin

LMWH

I
L

'~
\

IntnnSlc
"
Pal hway

1 ....

Damaged surface

l
Kininogcn,Kallikrein
XII"'"

VJ

Extrinsic Pathway
Trauma

1. .

"Xll a

XI...-..;.- ..... XI.

IX "

.. lXa

VII

Vila

_________________--=;;;;;~:J;~j~I~la ~ssue factor +---- Trauma

...

..X a

,.
Final
Common
Pathway

Prothrombin (II)

lv.

... Thrombin (lla')


..

FibrinogTn(l)

Fibrin (La)

lXIII.
Cross-l inked
fibrin clot

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Anticoagulants

Mechanism

Therapeutic use

Drug-Drug
interaction
Side Effects

Contraindications

Monitori ng

Binds to the antithrombin III (also known as heparin cofactor) to cause a


rapid anticoagulation effect.
Heparin catalyzes the factor (thrombin activation factor) 2a, 9a, lOa,
lla, 12a, and 13a.
Major anti thrombotic drug for DVT and pulmonary embolism. To
prevent postoperative venous thrombosis in-patient undergoing surgery.
Maximum effect occurs within minutes
Do not take ASA, which may increase the anticoagulant effect of this
drug and the risk of bleeding in the intestines or joints.
Hypersensitivity reaction (chills, fever, urticaria etc),
Bleeding
Heparin induce Thrombocytopenia
Heparin An ticoagulation Mechanism
Alcoholics
Bleeding disorders
Willloul Hq>. rin
Willi HeJ>:WI
.... cIO!lIll& fac!on
Acti..e dooing r""IOI"I
Brain, eye, spinal chord surgeries. Acli
Ill, Ix.. X., XI., Xlla. Xll la 11., IX.. X.. XI .. XlIa. XlIla
Periodic blood and liver test
will be required
R.a id jAnti Thrombin lit
"
Ann_Ihrombin HI
P
.to Heparin
0
aPT[ (activated Partial
Thromboplastin Time)
7"(\C. \ u... "Ka...
after 6 hours of initiating heparin.
-\ Un,...1,:'"
In.cli .... f""I""
lnuli ....
Heparin Assay
Can be used in pregnancy
2,9,10,11 ,1 2,1 3

_I

Advantage

Low Molecular Weight Heparin (LMWH)


LMWH
(Low Molecular
Weight Heparin)
Mechanism

Therapeutic
Monitoring
Side effects

Enoxaparin
Dalteparin
Tinzaparin
Ardeparin
LMWH are not interchangeable with heparin in their actions and
use. Because these highly acidic. These administered parenterally as
sodium salt. Because poorly absorbed from Gl tract.
The prevention of DVT or PE
Does not change Prothrombin Levels
Act longer and do not require close blood monitoring as Heparin does
Hypersensitivity reaction (chills, fever, urticaria etc),
Bleeding
Heparin induce Thrombocytopenia
Osteoporosis

Warfarin (Coumadin)
Mechanism

Vitamin K antagonist producing


their anticoagulant effect
by interfering with cyclic
interconversion of vitam in K and it
2,3-epoxide (vitamin K epoxide).
Inhibition of K-dependent proteins
or cloning factors (prothrombin or
factors 2, 7, 9 and 10)

v, t 'k ~-)

ltv~

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Therapeutic

Anticoagulant used to prevent


blood clots, mainly in areas where

blood flow is slowest, particularly


in the leg and pelvic veins .
A wide variety of drugs, such
as ASA, barbiturates, oral
contraceptives, cimetidine,
diuretics, certain laxatives, certain
depressants, and certain antibiotics
interact with warfarin, either by
increasing or decreasing the anti
clotting effect.
Bleeding, Purple toe syndrome,
Skin necrosis

Drug-Drug
interactions

Side Effects

Monitoring

lI,'arfann

~.o.

isY~'hes.. of dOl""

,-

Ccfomindole

c.._

Ccf",otan
Ccfame1arole

Due 10 additm.

PT (Prothrombin Time) ratio and


INR (Intemational Normalized

<ff~

..,.",
~,~

Ratio) are performed daily upon


starting warfarin.

'T'hrornbo/y1,c
~~"

Oral amicoaguJanttherapy Warfarin


INR should be between 2 - 3

Vitamin K

Antidote

Comparison of heparin and warfarin


Henarin
Warfarin
Source :
Natura!
Synthetic
Route

Parenteral

Oral (recently IV)

Mech

Enhances the
serum protease
antithrombin
In results in
inactivation of
fators Ha, rXa, Xa,
Xla XlIa XllIa
Protamin sulfate

Inhibits the hepatic


synthesis ofvit K
dependent factors
II, VII, IX, X

Antidote

Vitamin K ,
t ohvtanadione

Site of
action

In vitro, In vivo

In vivo only (liver)

Onset of
action
Pregnancy

Faster (minutes)

Slower (6-8 hours)

Yes

NO (Terotogenic)

I Warfarin I

~r
t~

Chronic
alcohol
Barbiturates
Rifampin
Vitam in K
Dark g reen
Ve!etables

AtIJ~

~-",-/:,~~

Protamine sulfate: Works by aCid base neutrailzatlon

Anticoa ulant Practice Ti s

,)

====~~~~----------~.

p'I" o l <:,o<,

Heparin antidote -7
Patient taking heparin

1\

7- --

Y:'

monitore~ for -7 t\t:

I 1
Heparinactioninclude~ \t... V,\i,,_ \I , y "
What is the safest anticoagulant in pregnancy ~
What are the factors heparin inhibits -7 d-o, I q
Monitor warfarin through ~ I tv F.. ~
I

) IOc, I ,I c:,

~"

(y~

r lc..

" ~ ...,

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~.

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Anticoagulants

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WhatdoyoumonitorinLMWH 7 "," 0
~ lN~
Vitamin K supplements and green vegetable effect on INR by '-:"
Increase in IN R can increase risk of 7 6..L ,J.......,-, / l~A
Heparin antidote action is due to 7 (\.l...u..t-r ~&~ -l ~ --t b~
,
If patient taking warfarin and INR is 4 -~5, what is appropriat~ recommendation 7 ~
ASA interact with warfarin by 7
1 ~ ~ t~ ~
Warfarin act on what factors ~ ;). c, ) 7,\ )
I0 ~
Patient after 2 days, air flight, reports pain ?n h!s legs.. His me~ical qistory ~c1 udes , DVT and
l _~
currently using warfarin 7 "'" '"'rI \.,: <:. ~ \; l:t t< ~, '
Recurrance of~eparin induced TKrombocytop~nia syndrome can be prevented by using7

ty-

9 " -)

cv

t(up

, l.L.vVhOI ~

w~______ L~ " ' " -> L V-"L


Abbrevation and Tenninology
DVT
ASA
LMWH

PE
PT
INR

TIA
STEM]
MI
aPIT

Deep Vein Thrombosis


Acetyl Saliaylate
Low Molecular Weight Heparin
Pulmona Embolism
Prothrombin Time
International Nonnalized Ratio
Transient Ischemic attack
ST-Segment Elevation MI
Mvocardiallnfarction
activated Partial Thromboplastin Time

Generic and Brand


Di goxin
Heparin
Warfari n

Digitek, Lanoxicaps, Lanoxin


Hemochron, Hep-Lock, Hep-Lock UIP, Heparin, HepFlush-lO,
Coumadin Jantoven

,,' ,t \{ cruJ-;

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Anticoagulants

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Antiplate let Drugs

10

Antiplatelet Drugs
Antiplatelet Drugs

ASA

Dipyridamole

T '"\ """I, , ""-"<

f\L ",brb,i"

Ticlopidine
&
Clopidogrel

Glycoprotein
inhibitors

Eptifibatide
Tirrofiban

Prostaglandin

.n.IOr

Epoprostenol

("PlLbjllk
l '" l" 1,; t; "'"
Platelets, of the elements of blood cells, tend to clump together. The following drugs interfe re with
the coagulation by inhibiting platelet aggregation. Heart attacks and strokes occur when a blood
clot that forms in a narrowed portion of an artery blood flow and cuts off the supply of oxygen and
nutrients to the tissue that lies beyond the site of the clot.
ASA (Salicylates)
ClopidogreJ
Ticlopidine
Theonopyridine
Dipyridamole
Dipiperdino dinitro pyrimidine
Fab fragments of human monoclonal antibody to the Glycoproteine (GPllbIllIa) receptors
(Abciximab, tirofiban, eptifibatide).

Tielopidine (Tielid)
Mechanism
Therapeutic use
Side effects
Contraindications

Storage conditions
Dosage

Antiplatelet (to prevent blood clot)


Reduce thrombotic risk inpatient who cannot use aspirin.
Hemorrhagic: compl ications such as bruising or ecchymosis, epistaxis
Presence or history of hematopoietic disorders (such as neutropen ia,
thrombocytopenia or agranulocytosis);
Hemorrhagic diathesis or presence of hemostatic disorder;
Conditions associated with active bleeding, such as bleeding peptic ulcer
or intracranial bleeding; severe liver dysfunction.
Store at room temperature. Dispense in lighHesistant containers. Bl ister
packs should not be exposed to light
The recommended dose is 250 mg twice daily with food.

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Anti platelet Drugs


Ticlopidine should be taken with meals to minimize GI intolerance.

Food and drug


interactions

Clopidogrel (Plavix)
An antiplatelet drugs that is used to prevent blood clots from fonning.
It reduces the tendency of platelet to stick together when blood flow
disrupted.
Drug of choice for Transient Ischemic attacks (TIA), and stroke .
Bruising and nosebleeds
Increase the effects of ASA in platelets, as will the risk ofG l bleeding
when Clopidogrel is taken with ASA and other NSAID's.
Not recommended with infants and children
Bleedi ng

Mechan ism

Therapeutic use
Side Effects
Drug-Drug
interacti on
Contraindication
Monitoring

Antiplatelet summary

A,<:'", (c....-.t:.'<-~)

Drug of choice in STEMI-)


Patient cannot kake ~pf1n ~u~stomach ulcers for 111 prophylaxis, what

IS

an alternate drug

of chOice -) U--<si" ~
~ ~ ~_~
If patient is allergic to aspIrin what is alternate drug ~ C
1-\...~ ~
Drug of choice for trans ient Ischemic attack {TIA) ~ (~ L
What IS the effcct of aspirin on warfann ~ \' U 99.D"::J
a
What dose of aspirin act as Antiplatelet ~ b<...-

a.l A SA

&.'0

Abbrevation and Tenninology


ASA
TlA
NSAI D

Acetvl Saliavlate
Transient Ischemic attack
Nonsteroidal Anti-Inflammatory Drug

Generic and Brand


I Ticlopidine
Clopidogrcl

I Ticlid

Plavix

L,'", ,"l~

T icQ :ct

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Thrombolytic Drugs

11

Thrombolytic Drugs
Thrombolytic Drugs

Streptokinase
(Strepto protein from
Group CB-hemplytic
steptococci bacteria

tissue
plasminogen
activator tPA
Clot selective
Mechan ism

('

Anlstreptase Ammase)
PrOOrug of streptokinase

U ro k'mase

t~pa

(AbTlOnase)

(ti ssue type


plasminogen activator)
Alteplase (activase)
Directly degrade
Reteplase (Retevase)
fibrin and
very high affinity to
fibrinogen
plasminogen, oound to.
thrombus

Alteplase
Reteplase
Tenecteplase
Streptokinase
Urokinase
Anistreplase
Facilitate conversion of
plasminogen to plasmin that
subsequently hydrolyzes fibrin
to dissolve clots
Recombinant DNA derivatives
oftissue plasminogen activator

Side Effects

Thrombin TIa

Fibril!

,T~h;e~ra;p~e~U~I;~C____--!A~cu
~l~e~MW1~a~n~d'l!a~c~u
~,e~mJas~sl;vLe~O ~
pulmon
bolism PE D - /
<"

Prothrombin (II) _

(IPA),
They contain 527 and 355 am ino
acids of natural tPA.
tPA catalyzes the conversion of
lasminogen to plasmin

y'"
rl"-X

B<"",

_ xu.

degradation proo._.l_ .f,;;:::;;::::;:;;;:;

/.1
~

ypersensitivity reactIons
Internal GI bleeding, retroperitoneal
bleeding, superficial bleeding at catheter injection site.
Nausea and vomiting

Streptokinase (Streptase)
Mechanism

An enzyme produce by streptococcus bacteria.


Dissolve the fibrin of blood clots, especially those in the arteries of the
heart and lungs.

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Thrombolytic Drugs
Therapeutic use

Acute coronary syndrome


Deep vein thrombosis (DVT), Pulmonary Embolism ePE)
There is an increase bleeding when anticoagulants are taken at the same
time as streptokinase.
Can produce allergic reactions (urticaria) Give antihistamine before
starting the treatment.
Excessive bleeding
Branchospasm
Angioneurotic edema
Headache
Don 't give second streptokinase within 6 months of the First treatment.

D rug-Drug
interactions
Side Effects

Monitoring

Urokinase (Abbokinase)
Mechanism
Therapeutic use
Side effects

Two-chain serine protease obtained from cultured human kidney cell.

Coronary artery thrombosis, Pulmonary embolism.


All ergic reactions may lead to bronchospasm and skin rash

Anistreplase (Eminase)
Mechanism

APSAC (Anisoylated plasminogen streptokinase activator complex)


It is a complex of human Iys-plasminogen and streptokinase with anisoyl group

Therapeutic use

blocking catalyst site.


Acute MI, coronary artery emboli lysis

Thrombolytics Tips

f\ ~ ) ~~b~

I- PAsa,e -7
DOC for ST segment elevation myocardial infarction (ST EM I)

EmbOlUS -7 ~ ~ ~

Abbrevation and Tenninology


APSAC
DVT

Aniso lated lasmino en stre tokinase activator com lex


Dee Vein Thrombosis

Generic and Brand


Streotokinase
Urokinase
Anistreolase

Streotase
Abbokinase
Eminase

. ~4 -~~~

~_ ~,,~ ~,CeLh;".~ f.J)i.'l:l\- 'l .;ill ) If/J(j )X /


\ ~~ 4-'--':' - ) DV I/f!:.J MIG'\.~..t

an'}h~L"\J"'o'Ib<.li.....b .

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_ ~ 1,- ,) 0 Q

Antidepressants

12

@j l f '~

Antidepressants
Classification of Antidepressants

I
Monoamine Oxidase ( MAO)
Inhibi tors
Irreversible MAO
Phenelzine (Nardi !)
Tranylcypromine (Parnate)
Isocarboxazid
Clorgyline

I
Amine reuptake
inhibitors drugs

5HT, NE, D

I
5HT, N E
Tricyclics (TCA's)
Tertiary ami ne type (S HT<NE)
Amitripty line
Imipramine
Secondary amine type
(5HT=NE)
Desipramine
Nortriptyline

receptor inhibitors

I
Non-selective

Reversible MAOI (RIMA)


Moclobemide

(12

Mirtazapine (SA Rl)

Dual action
SNRl
Venlafaxine
sNDRl
Bupropion

5HT only
Selective serotonin
Reuptake inhibitors (SSRI 's)
Fluoxetine (Prozac)
Fluvoxamine
Paroxetine
Sertraline
Citalopram

e--ei-rnlopram

<2S (( h COP' "'-.

fI::U"i~ \-

Abbreviations : 5HT = 5-hydroxy tryptamine (Serotonin), NE = Norepinephrine,


SNRI = Serotonin Norepinephrine Reuptake Inhibitors, N DRI = Norepinephrine Dopamine Reuptake
Inhibitor; RIMAs = reversible inhibitors of monoamine oxidase, TeA = Tricyclic Antidepressants
Signs of depression include: sadness, tearfulness, dejection, sel f-critici sm, loss of abil ity to experience
pleasure, loss of appetite, inability to sleep and loss of libido. Antidepressant drugs work by altering
the concentration of neurotransmitters (chemicals) in the brain. It is believed that depression is caused
when the levels of serotonin and norepinephrine, two neurtotransmitters in the brain, are deficient, but
it is not understood wh ich one is more responsible for depression. The drugs act by causing bui ld up
of one or both of the neurotransmitters in the synapse, (the gap between two nerves) or by increasing
the nerve cel l's sensitivity to the neurotransmitters .
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Antidepressants

Classes of antidepressant drugs include: tricyclic compounds (TCAs), monoamine oxidase inhibitors
(MAOls), selective serotonin re-uptake inhibitors (SSRIs) and reversible inhibitors of monoamine
ox idase (RIMAs).

Selective Serotonin Reuptake Inhibitors (SSRI)


The SSRls are selective in blocking the reabsorption of serotonin by nerve cells by acting at the
5-HT receptors, and therefore, increasing the amount of serotonin available in the brain. This class
of antidepressants has fewer side effects than MAO!'s or TCA's. They are also used for bulimia,
obsessive-compulsive disorder and panic attacks.
SSRl

Mechanism

Citalopram (Celexa)
E-citalopram
Fluoxetine (Prozac)
Fluvoxamine (Luvox)
Paroxeline (Paxil)
Sertraline (Zoloft)
Selective serotonin reuptake inhibitors:lncrease serotonin levels

Metabolic enzymes

Most common metabolizing enzymes


SSRI inhibit ~ CYP 206
CYPJA4
CYPIA9

Therapeutic use

Antidepressant
Antianxiety
Sexual dysfunction (orgasmic delay) ~ Alprostad i l may be helpful
GI 7 Nausea (Most common)
Headache
Insomnia
ervousness
Fatigue

Side effects

Advantage

Serotonergic
syndrome
(Contraindications)
Discont inued
syndrome

151 line treatment for major depression


No Weight gain (no change in weight)
No cardiovascular side effects
Greater tolerability and ease of dosing
No hypotension
Serotonergic sy ndrome may occur if the SSRI are combined with MAO
Inhibitors, SSRl and TCA.
Do not combine with SSRI
Do not combine with TCA
FINISH
Flu like syndrome
Insomnia
Nausea
Imbalance
Sensory disturbances
Hyper activity

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Antidepressants

Tips

Most anorexic~Fluoxetine
Most nauseating ~ Fluvoxamine
Most weight gain ~ Mirtazapine
Citalopram ~ SE: Somnolence
All SSRJs have common SE: Nausea
Antidepressants with Less sexual dysfunction ~ Bupropion,
Mirtazapine, moclobemide
Onset of action
It normally takes 2-4 weeks for antidepressant to have an effect.
Wash out period
Two SSRI's or SSRl with TCA or MAOI should not combine
If switch from one SSRI to other (SS RI , TCA or MAOI), waiting period
required (washout period)
All SSRls have washout period for 2 weeks, Except: Fluoxetine (require
5 weeks)
Tramadol
Meperidine
Amphetamine
Dopamine
Cocaine
Methyldopa
MAO Inhibitors
Dextromethorphan
SS RI
Caffeine
TCA
Lithium
SSRI
MAO Inhibitors
TCAs
St.John wort

serotonergic symptoms
Hyperpyrexia (Fever)
Agitation
Neuromuscular pains/myoclonus hyper refiexia
Hypotension
Tremors I Shivering
Seizure
Coma, and death

Tricyclic Antidepressants
TCA

Amitriptyline, Clomipramine Desipramine Doxepin Imipramine,


Maprotiline, Nortriptyline Trimipramine

Secondary amine type


(NE ~ 5HT)
Tertiary amine type
NE> 5HT

Dibenzocycloheptadiene (eg : Nortriptyline)


Dibenzapine (eg; Desipramine)
Dibenzapine (eg: Imipramine)
Dibenzocycloheptadiene (eg: Amitriptyline)
More anticholinergic side effects than secondary amine

Mechanism

NE and 5HT Reuptake inhibitor

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Therapeutic use

Side effects

Contraindications
Overdose symptoms

Overdose treatment
Tips

Antidepressants
Antidepressant
Neuropathy pain ~ Amitriptyline
Enuresis in children (Bedweuing)
Anxiety disorder (OCD)

Imipramine

CVD effects ~ Orthostatic Hypotension, Tachycardia (AY blockade)


Weight Gain
Sexual Dysfunction
ConfusionlDelirium
Bone marrow depression
Mania ~ with manic depressive illnesses
Anticholinergic side effects
Constipation
Blurred vision
Urinary retention
Dry mouth
MAO inhibitors, SSRI
Nausea
Constipation
Confusion
Sleepiness
Palpitation
Dizziness
Dry mouth
Blurred vision
Fever
Contact physician immediatelyif any such symptoms appears.
ACli vated charcoal
Less hypotensive TeA -7
Nortripty line (Aventy l)
Most Anticholinergic and
sedative TC A ~ Amitriptyline
(Elavil)
Least sedative ofTCANortripty line

Less antichol inergic TCA-Nortriptyline


Take medication dai ly
Antidepressants must be taken for two to four weeks for a noticeable
effect
Continue to take medication even if you are feeling better
Do not stop taking the antidepressant without checking with the
physician

Monoamino oxidase Inhibitors


The monoamine oxidase inhibitors (MAOIs) were the first class of compounds used to treat
depression. Patients, taking these drugs, must monitor their diet for tyramine, an amino acid
present in many foods that are fennented, aged or smoked. There are a number of foods containing
tyramine and some drugs must be avoided. Monoamine oxidase is an enzyme, which inactivates the
neurotransmitters, epinephrine, norepinephrine and dopamine. These drugs inhibit the destruction
of these brain chemicals, which leads to increased concentrations of these neurotransmi tters, wh ich
may account for their antidepressant activity.
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MAO Inhi bitors
Mechanism

Therapeutic use
Side effects

Drug interactions
Can cause
Serotonergic
syndrome

Serotonergic
syndrome

Hypertensive
cris is
Food to avoid

Antidepressants

Phenel zine Tranylcypromine, Isocarboxazid


Inhibit both MAO A and MAOB.:Bl ocks deamination in brain biogenic
ammes
Clorgyline -7 MAO A selective
Selegiline -7 MAO Q selective (used as antiparkinson drug)
Antidepressant, Anti anxiety, Narcolepsy
CVS affects -7 Orthostatic Hypotension, Tachycardia, Arrhythmias, and
Stroke.
CNS effects -7 Sleep disturbances, CNS stimulations
Weight Gain
Sexual Dysfunction
Anticholinergic -7 less than TCA
Avoid concomitant use of:
Meperidine
Amphetamine
SSRI

TCA
Dopamine
Cocaine
Methyldopa
Dextromethorphan
Caffeine
Pseudoephridine
Lithium
Serotonin syndrome symptoms includes:
Hyperpyrexia
Agitation
Neuromuscular pains
Hypotension
Coma, and death
Caused by combination of MAOI's with SSRI or TCA's or narcotics
(meperidine).
Use washout period for 2 weeks before administering SSRI.
Inhibitions of MAO I in brain causes catalyze oxidative deamination of toxic
substances such as tyramine.
Tyramine is present in foods such as fermented food cheese, wine etc.
Aged cheese (cheddar, blue and Swiss), yogurt, smoked meats, wine, liquor,
yeast, raisins, chocolate, dry salami, pepperoni, sausage, bananas, figs, tea and
coffee.
Drugs: Sympathomimectis, ephedrine, pseudoephridine.

Reversible Inhibitors of Monoamine Oxidase (RlMAs)


Moclobemide are short acting, reversible inhibitors of monoamine oxidase, the enzyme which
inactivates the neurotransmitters, epinephrine, norepinephrine and dopamine. This drug inhibits the
destruction of these brain chemicals, which leads to increased concentration of these neurotransm itters,
which may account for the antidepressant activity of moclobemide. Short acting, reversible inhibitor
of monoamine oxidase, the enzyme which inacti vates the epinephrine, norepinephrine, and dopamine
Side effects: headache, abdominal fullness , GT upset, dry mouth, and sedation.

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Antidepressants

Dual action antidepressants


Dual action

Bupropion

Venlafaxine

Mirtazapine

Bupropion
Venlafaxine
Minazapine
Trazodone and Nefazadone
Serotonin (very little), Dopamine and Norepinephrine reuptake inhibitor
(sNDRI)
SE: Stimulant affect (tachycardia, agitation), aggravation of psychosis,
aggravation of seizure (Reduce seizure threshold)
Also used for sm'o king cessation (Zyban)
1" line treatment for Major depression
Least sexual dysfunction and weight gain
Inhibits Serotonin and Norepinephrine, Some degree of dopamine reuptake
inhibitor (SNRI)
Stimulant aITt::l.:l -7 Anxit::ty, agilaliulI, ht::adadLt::, ill~u lILLLia
At higher dose 225 mg / day, it has cardiovascular side effects, such as dose
dependent hypertension.
At lower dose (75 and 150mg) it acts on 5HT only, higher dose (225mg)
5HT ,NE and Dopamine.
Alph~ antagonist and potent 5HT2 receptor antagonist
Increases release of norepinephrine and serotonins.
Side effects: Increase appetite, Sedation
Increase serum cholesterol levels

Lithium (Lithobid)
Therapeutic use

Pharmacokinetics

Therapeutic levels

Dose
Side effects

Mood stabilizer drug of choice to treat manic depressions


Used prophylactically in treating manic-depressive patient and to treat
manic episodes.
Bipo lar depression (disorder)
Steady state reached in 5 days
Poor therapeutic window
Renal excretion
Acute mania: 1.0 to 1.5 mEqlliter
Maintenance bipolar disorder: 0.6 to 1.2 mEqlliter
Increasing dose 300 mg/day raises level 0.2 mEq/liter
Start: 300 mg PO bid, effective dose: 900 to 1800 mg per day divided
bid
Tremor
Polydipsia
Hypothermia or hyperthermia
Weight gain and weight loss
Nausea or Vomiting
Diarrhea
Hypothyroidism and hyperthyroidi sm

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Toxic symptoms

(Over 1.5 mEq/L)

L~-t."'~ +J....:..\A\'"'~ ~

_'

t ,::... r..

~W

Cerebellar Signs or symptoms

Antidepressants

Drowsiness
In coordination
Dizziness

Blurred vision
Confusion

Seizures
Monitoring

Fluid retenti on
Change in heart rate or rhythm
Li thium serum levels
Renal Function tests
Thyroid Function Tests

(:{~g;::t~ ,,~~'S(~~E~~i7~ ~ 1~ ~~
Antidepressant Tips

_ ',

dCt;;: () ~ u, ~ ""l=K
SSRI onset of action is ~ J - ~ I....ll./ ~\ ~

N 1\ 0 ~ A t;:::t: C;~ t ,u\-

Fluoxetine washout period ~ <;"' w i,(


Buprapion, trazadone and mirtazepine have least sexual dysfunction
Depression with sexual dysfunction -7 ~~
~
Depression with insom nia -7
r o.. 2c. ~ ~
Depression w ith diabetes -7 3 'S R- I
Take SSRl in the morning
Take TeAs in evening or bedtime
Higher dose of ven lafaxine (225mglday) have effect on ~
Il
Patient on antidepressants and shows wi,th dilated pupil, may be due to-7 0--\"1 I~~
TCA onset of action is -7 L - "
~ t--' ..)
A substance found commoflly in fermented foods which can be toxic when MAO inhibitors
are used-7 \" 't '\0..w... 1 ~

fl -..r ;

lc.J\

l' _.

MAO is classified as -7

n....t,.-., ~ ......0

-0 ~

i: '"D~

SSRI inhibit cytochrome CYP2D6


Minazepine may cause higher w~ ight gain

r.

,.... 0

Avoidcheese .with -7 H 1\0 ,'hibll't~ (~~


Milk+ MAOI -7 c...." l,... ~ ~ \"'. A 0 \"
St John won have antidepressant effect
Serotonergic symptoms-7
DOC in Bipolar disorders and manic depression -->
Nonnal blood levels of lithium in adult is 1.5 mEqlL
Lithium concentration varies with Na+ ions
Li + conc. increases with decrease N a+
Li+ cone. decreases with Increase in Na+
ACE I decrease Na+ -7
Ll'"
NSAID decrease Na+ renal perfusion is less
Thiazides deplete Na+
Fluoxetine (SSRI) increase Li+ toxicity
Renal dysfunction -7 L 1. 't
Dehydration 4
Lithium toxicity symptoms -->

~\o <..~ ... ~)

h.ilo;ttj1. i>: f'

L\l~ \. ""'-

It-

W:iJ~R,1L ~ \90.] ~~<.f


<J

-">

Lt~~!O~? ~

~~~ o-.&. ~(HI)Nt-,

tOile. .........

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Antidepressants

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Abbrevation and Terminology


MAO
SARl
SSRl
D
NE
SNRI

NDRl
RlMA
TCA
OCD
CVD
GAD
5HT

Monoamine Oxidase
Selective serotonin reuptake inhibitor
Dopamine
Norepinephrine
Serotonin ore ine hrine Reu take Inhibitors
Norepinephrine Dopamine Reu take Inhibitor
Reversible Inhibitors of Monoamine oxidase
Tricyclic Antidepressants
Obsessive-Compulsive Disorder
Cardiovascular Disease
General Anxiety Disorde
5-hydroxy tryptamine Serotonin

Generic and Brand


Citaiopram
E-citalopram
Fluoxetine
Fluvoxamine
Paroxetine
Sertraline
Amitriptyline
Clom ioramine
Desipramine
Doxepin
Imipramine
Maprotiline
Nortriotvline
Trimi ramine
Phenelzine
Tranylcypromine
Isocarboxazid
Bupropion
Venlafaxine
Mirtazaoine
Trazodone
Nefazadone
Lithium

Celexa
Proxac
Luvox
Paxil
Zolof't
Anafranil
No ramin
Sinequan
Tofranil
Aventyl
Sunnontil
Nardil
Pamate
Wellbutrin SR
Effexor
Remeron
Desvrel
Lithobid

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Sedatives, hypnotics and Anxiolytics

13

Sedatives, Hypnotics and


Anxiolytics
Class ification of Sedative-Hypnotic Drugs

~I

Non-benzodiazepines
Zaleplon
Zopiclone
Zolpidem
Other anxiolytics:
Buspirone, Hydroxyzine

Barbiturates

Benzodiazepines

I
Long action
Diazepam
Fluorazepam
Clorazepate

[ntermediat
Alprazolam
Lorazepam
Temazepam
Estazolam

Short acting
Oxazepam
Triazulam
Midazolam

I\LT{..

~\-

Ultra-shon
action
Th iopental

Intermediate
Amobarbital
Secobarbital
Pentobarbital

Long action
Phenobarbital

Sedatives (anxiolytic agents): Reduce anxiety with linle effect on motor or mental functions.
Hypnotics: Produce drowsiness and reduce onset of sleep.
Insom nia - disturbed or fragmented sleep, often associ ated with physical or emotional illness
Anxiolytic - a drug that decreases anxiety

Sedatives

~~

Benzodinzepines

Others sedatives

Barbiturates

r-----~------_r------_.~------.

Aldehyde
derivative

Antihistamine

, :t\~ ~\'"
~Short acting
Midazolam
Estazolam
Triazolam (Halcion)

Cyc1opyrolones

Pyrazolopyrimidincs

Benzodiazepines

Hypnotic &
Sedatives

I
........ -0J.

Interm ediate acting


A1 prazolam (Xanax)
Lorazepam (Ativan)
Oxazepam (generics)
Temazepam (Reston I)
Nitrazepam

l.a

Long acting
Diazepam (generics)
Flurazepam (Dal mane)
Clonazepam,
Chlordiazepoxide

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Sedatives, hypnotics and Anxiolytics

Benzodiazepine are minor tranquilizers are used to treat insomnia and anxiety. The following are
tenns that are used to describe some conditions dealing with anxiety or sleep disorders. Anxiolytic a
drug that decreases anxiety: insomnia - disturbed or fragmented sleep, often associated with physical
or emotional ill ness: sedative - a drug which causes drowsiness but not sleep, reduces anxiety and
irritability; hypnotic - a drug which will produce sleep. Sometimes a larger dose of a sedative will
cause a hypnotic action .

Mechanism

Benzodiazepine receptors BZ I and BZ 2 are found in brain


BZ L and BZ2 are parallel to GABA receptors

Benzodiazepine
therapeutic actions

Reduce anxiety
Insomnia; Sedative and hypnotic action
Anticonvulsant action
Muscle relaxant action
Flurazepam (no rebound insomnia)
Quazt;pam (No rebound insomnia)
Temazepam
Triazolam used for insomnia ~ often rebound insomn ia
Alprazolam (used in treatment of panic disorders)
Clonazepam (useful in treating absence seizures)
D iazep am ~ status epi lepticus
D iazep am ~ muscle spasm, muscle degenerative disease
Physical and psychological dependence (at high doses)
Withdrawal symptoms upon abrupt discontinuation
Long acting withdrawal symptoms occurs after number of days
Short acti ng benzodiazepine associated wi th immediate withdrawal
symptoms if it is Slopped abruptly.
Confus ion, anx iety, agitation, restlessness, insomnia, and tension.
Rapid development of tolerance and withdraw I symptoms occurs
with short acting.
Flumazenil

Sedative and hypnotic


action

Anticonvulsant action
Muscle relaxant action
Dependence

Wi thdrawal symptoms

Benzodiazepine antidote

Other sedatives
Mechanism
Therapeutic use
Zaleplon

Zopiclone, Zaleplon, Zolpidem


ot a benzodiazepine, Acts on subset ofbenzodiazepine receptors
Insomnia
Act on benzodiazepine receptors
No anticonvulsant and muscle relaxant activity
Short half life 1 hours
Headache ~ most common
Reduce sleep latency, used in initial treatment

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Zopiclone

Sedatives, hypnotics and Anxiolytics


Act on subset benzodiazepine receptors
No anticonvulsant and muscle relaxant activity
Short half1ife 5 hours
Biner metallic taste
Bad breath
Confusion ~ most common in elderly
Do not accumulate, may cause less withdrawal effects and less rebound
insomnia:
Less tolerance
Minimal additive effect with alcohol
Acts on subset ofbenzodiazepine receptors.
It is not a benzodiazepine
It is has no anticonvulsant properties
It does not have muscle relaxing properties

Zolpidem

Zolpidem (Ambien)
Mechan ism

Therapeutic use
Advantages

Side effects

Acts on subset ofbenzodiazepine receptors.


It is not a benzodiazepine
It is has no anticonvulsant properties
It does not have muscle relaxing properties
Indicated in treatment of insomnia
Show no withdrawal effect
No tolerance with prolong use
Min imal rebound insomnia
Rapid onset of action
Elimination half life is 3hours
NlGfITmares
Dizziness Agitation
GI upset
Headache
DayTime drowsiness (hangover effect)

Barbiturates
Barbiturates

I
Ultra-short action
Thiopental

Short acting
Amobarbital
Secobarbital
Pentobarbital

Long action
Phenobarbital

Barbiturates are used much less commonly than before. They are effective only for a few weeks
since they alter the length oftime spent in R.E.M. sleep. They should only be used for short-term
therapy as sedative or hypnotics.
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Barbiturates

Mechanism

Metabolic Enzymes
Therapeutic use

Withdrawal
symptoms

Poisoning

Poisoning
management

Barbiturates
antagonist

Sedati ves, hypnotics and Anxiolytics


Phenobarbitals (Luminal, Solfoton)7 Long acting
Amobarbital (Amytal)7 short acting
Butabarbital (Butisol) 7 short acting
Pentobarbital (Nembutal)7 short acting
Secobarbital (Seconal) 7 short acting
Thiopental (Pentothal) 7 shortest acting (acts withi n second)
Primidone 7 active drug is phenobarbital (metabolite)
Two side chains in position 5 are essential for sedative hypnotic activity
Long acting have a phenyl and a ethyl group in position 5
I-Interfere with Na and K transport across membrane.
2-Potentiate GABA A action on CI- entry
3- Do not bind to BZ and BZ2 receptors
Sedation (calming effect, reduce excitement)
Respiratory depression
Barbiturates induce CYP450 in liver, reduces the effect of several drugs
that depends on CYP450.
Anesthesia
Anti seizure
Anxiety
Addiction potential
Abrupt withdrawal of barbiturates may cause:
Tremors
Anxiety
Weakness
Restlessness
Nausea
Vomiting
Seizures
Delirium
Cardiac arrest
Withdrawal symptoms are more severe than opioids, can cause death.
Severe depress ion of respiration
Cardiovascular depression
Shock like condition shallow and infrequent breathing
Artificial respiration
Purging stomach content
Hemodialysis
Alkalinization of urine for phenobarbital
Aminophylline

Miscellaneous
Non-barbiturate
sedatives

Chloralhydrate
Antihistami ne

Chloralhydrate
Alcohol
Antihistamine
Buspirone
Tri chlorinated derivative of acetaldehyde
Doxy lamine and other antihistamine are used as OTe treatment of sleep

disorders
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Autocoids

at 9 and II. Subscripts relate to the number of double bond present in aliphatic chains
Platelet aggregation, Relax bronchial and GI smooth muscles, Relax smooth muscles, Inhibit gastric
acid secretion, Pain, Edema, Inflammation

Prostaglandin analogs

1
PGF zu

PGl,

Dinoprostone

Latanoprost

Epoprostenol

Thromboxane A2

Branchial &
smooth
muscle
dilatation

Branchial &
smooth
muscle
constriction

Blood vessels
dilatation

Platelet
aggregation

PGE,

PGE,

Misoprostol
Alprastadil
Branchial &
smooth
muscle
dilatation

TxA2

Inhibit
aggrega.tion

Pharmacological actions of prostaglandins


CortitoSleraids

Receptors

PGI;:

Actions
Vasodilation
Decrease platelets aggregation
Maintaining renal blood flow
NSAID. Aspirin. coXI1

POE l

Protects gastric mucose


Inhibiton acid secretion
Stimulation of mucus secretion
Pyrogen elevate PG E2
Contraction of uterus

PGF 2

Pmstagl.aadins G

l~.--

Bronchoconstriction
Contraction of uterus
Vasodialtion
Inhibition of platelets aggregation
Increase Platelets aggregation
Vasoconstriction

ProSlaCycIill (PGIIl
'."'et aggrtgation
Vascular lone

Bnlnchiill tone
UtenDt l(lllt

IX

P'GEz &. I'Gf2

Thrombounc A

t Uterint tont
t V&SCular lOJle
t Bronchill tonc

t Pa1t:1Cl 1IggJC&
f Vascular l(IIlt

PGEAnalogs
PGE. analogs
Misoprostol (Cytotec): is used for prevention ofNSAID induced GI ulcers.
Chemically it is ecosonides
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Autocoids

Co.mbination products: Naproxen + Misoprostol, Diclophenac + Misoprostol (Arthrotec)


Alprostadil
In adults? for the treatment of impotence
Alprostadil (Caverject, Prostin VR pediatrics) is used treating impotence due to erectile dysfunction.
Alprostadil (Prostin VR pediatric) is used fortemporary maintenance ofa patent ductus arteriosus
when awaiting corrective surgery for congenital heart defects.
PGE 2 analogs
Dinoprost, Dinoprostone
Dinoprostone derovatives ~ Abortificient
Dinoprostone (Prostin E2, Prepidi l, Cervidil) are used for their abortifacient effects and to induce
cervical ripening in pregnancy.
PG F2" analogs
PGF ~a analogs are selective Prostanoid FP receptor, inhibitors that reduce lOP, and increase outflow
of aqueous humor.
Latanoprost (Xalatan)? (Used topically to lower intra ocular pressure in OAG)
Travoprost (Travatan) ~ topical ophthalmic drug
Bimatoprost (Lumigan) -7 topical ophthalmic drug
Unoprostone (Rescula) ? topical ophthalmic drug
Carboprost (Hemabate) ~ abortificient (withdrawn)
Precautions: Opthalmic solutions have been reported to cause changes to pigmentated tissue .
The changes include the increased pigmentation and and growth of eyelashes and increased
pigmentation of iris and periorbital tissue (eyelid). The increased pigmentation is pennanent.
Latanoprost (Xalatan)
Store unopened bottle under refrigeration. Protect from light. Once opended store botte in cool
place (refrigerate if possible) f,?r upto 6 weeks.
Bimatoprost (Lumigan)
Store at room temperature, no refirigeration necessary

PGI analogs (Prostacy1cin)


Epoprostenol (Prostcyclin, Flolan):
Used in the treatment of emergency pulmonary hypertension.
Prostaglandin analogs

Leukotrienes
Physiological functions
LTC and LTD antagonists
Play important role in numerous
physiological functions.
Slow reacting suhstance of anaphylaxis.
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Autocoids

Hean 7 Negative inotropic, Smooth muscles


chemotaxis (Chemotaxis = movement of cell in
response to the chemical gradient)
GI

tract ~

Neutrophil chemotaxis

Pulmonary (major)~ Bronchoconstriction,


increase permeability, and increase mucus secretion.
B lood ~

Chemotactic agent for neutrophils,


eosinophils, and modify lymphocyte proliferation
and differentiation.

Two important leukotrienes antagonists


LTC4 and LTD4
Leukotriene antagonist:

(LTC~

and LTD4 )

e. g. Zafirlukast (Accolate) and montelukast (Si ngu lair) ~ Peptid mimetic structure. Indicated in
prophylaxis of asthma.
Zafirlukast (Accolate)
Therapeutic use: For the prophy laxis and chronic treatment of asthma in adults and children
12 years of age and older. Side effects include: G I upset, liver dysfunction.
Take empty stomach to enhance it absorption
Montel ukast (Singulair)
Similar profi le to that of Zafi rlukast.
Can be used in children over 2-year age
Montelukast may be taken without regard of food.
Available as chewable tablet (once daily in the evening).
Administer granules directly into mouth or mix with teaspoon of cold or room temperature
applesauce, carrot, rice or ice cream.
Do not take aspirin or NSAlDs while on this medication.

Abbrevation and Tenninology


5HT
DHE

PGF

5-hvdroxv trvotamine Seroton in


Dihvdroenzotamine

LTC
LTD
POI
OAG
lOP

Generic and Brand


Misoprostol
Alprostadil
Dinoprostone

Cytotec
Caverject, Prostin Vi{ pediatrics
Prostin E2, Prepidil , Cerv idil

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Latanoprost
Travoprost
Bimatoprost
Unoprostone
Carboprost
Epoprostenol
Zafirlukast
Montelukast

Autocoids
Xalatan
Travatan
Lumigan
Rescula
Hemabate
Prostcyclin, Fl olan
Accolate
Singulair

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Autocoids

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Insulin and Anitdiabetic Drugs

23

Insulin a nd Antidiabetic Drugs


There are two types of diabetes mellitis, Type I and Type II. For Type I diabetes, patients need insulin
injections . Type I diabetes is known as insulin dependent diabetes mellitis (100M). It usually begins
in young people under 40 and ofnonnal weight. Onset is sudden and severe; ketones are fo und in the
blood and urine.
Types of Insulin

I Ultra rapid I

I Insulin lispro I

Rapid

I I Intennediate I

Regular
Semilente

NPH

Longacting

I
Ultralente
Protamine Zinc
Glargine

Lente

Types of insulin are categorized by their onset of action, and these relat
their effectiveness and their duration of action as well.

..

ue for

Oral Diabetic drugs


Insulin
Secretagogues

/~

r Sulfo~y[ureas l

I" Generation
Tolbutamide
Tolazamide
Chlorpropamide

I
Nonsulfonylurea insul in
secretagogue
Meglitinides
Repaglinide
Neglitinide
Biguanide
Metfonnin

2.... Generation
Glyburide
Glipizide
Gl imepiride

aglucosidase
inhibitor
*Acarbose
Thiazolidinedione
*Pioglitazone
*Rosiglitazone

Type I and Type II Diabetes Mellitus (DM)


Insulin
Duration

Humalog (H) (lispro)


synthetic

Very short
(fastest)
iv fonn

Onset
(hours)

Peak
(hours)

5-\0
min

30-40
min

Usual Effecti ve
Duration of Action
I (hours)
2-3 h

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Regular (R)
(suitabl e for iv dose). Both
human and animal source
NPH (N) Isophane
Amorphous precipitate of
insulin wI zinc ion acetate
buffer
Ultralente
Zinc suspension crystals
in acetate buffer contain
large particles that are slow
dissolve

Insulin and Anitdiabetic Drugs


Rapid (shan)
Y2 -I h
Subcutaneous
Or iv (in emergencies)
2-4 h
Intennediate
Semi lente (30%)

Long
(70%)
Slowest onset of
action but Longest
hypoglycemic effect.

Type I and Type II Diabetes Mellitus (OM)


Type I 7 Insulm dependent DM
I UIVl
(IDDM)
5- 10%

4-5 h

13 h

5-7 (dose-dependent;
may be longer)

6- 10 h

14- 18 h
not suitable for iv
dose

18-28 h

Type II 7 Non-insulin dependent DM


(NID DM)
>90%

Juvemle onset
I Adult onset (4U yrs)
Milder fonn
_
Destruction of p-cells in pancreas
No production of insulin Associated Very strong genetic predisposition
with treatment is by Diet and
Inabil ity of beta cells to produce adequate
insulin.
insulin and doesn't meet the body's
Ketoacidosis occurs
requirements.
Mainly due insul in resistance
ulet
I inSUlin
Oral hypoglyccmics
Oral hypoglycemics + insulin
I

I reatment

I ural
hypoglycemics

Suitonyl ureaS 7 StImulate Insuhn


secretions
Meglitimides 7 Stimulate insulin
secretions
Biguanides7 Inhibit gluconeogenesis in
liver, increase glucose uptake in cell.
Thiozolidinediones7 Increase insulin
sens itivity (decrease resistance) increase
glucose uptake in cell.
A lpha glucosidase inhibitors 7 Inhi bit
glucosidase in GI tract.
.

i lin.,,

. .

Diagnosis (Diabetic)
I-Symptoms
2-Random Blood sugar levels> 14.0 mmollL
3-Fasting Blood sugar levels> 11. 1mmoUL
4-Post prandial BSL > 14.0 mmollL
5-G lycosy lated hemoglobin (HbA I c) > 7%
Normal Blood sugar levels (BSL)
Fasting BSL 5-6 mmoUL
Random BSL 11.1 mmollL
Post prandial 14.0 mmollL
HbAI C is 4 - 6%
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Insulin and Anitdiabetic Drugs

Measures past three months Blood sugar levels


Used to determine antidiabetic drugs compliance of pathient
Insulin Combinations

Insulin storage conditions


Should be stored in refrigerator
Can be stored at room temperature 28 days (1 month)
Do not shake vigorously
If you notice turbidity or vapors or precipitation, do not use, discard it

Oral antidibetics
HypgJycemic drugs: Sulfony lureas, Meglitinides
Antihyperglycemics: Biguanides, Thizolinediones
Medication

Mechanism

Side effects

Contraindications

Sulfony lureas
Glyburide (DiaBeta)
Chlorpropamide
(Diabinese)
Gliclazide

Stimulate release of
endogenous insulin

Hypoglycemia
Nausea
GI discomfort
Weight gain

Meglitinides
Repaglinide (Gluconorm)

Stimulate release of
endogenous insulin
(rapid-acting, better
post-prandial glucose control): Must
take before meals,
because
Decrease postprandial glucose levels.
I-Reduce gluconeogenesis,
2-increase glucose
utilization

Hypoglycemia, especial1y if taken empty


stomach
(Less frequent than
with sulfonylureas)
Weight gain

Hepatic or renal
Impairment
Chlorpropamide not a good
choice in elderly (long half
life)
Not used in Ty pe I OM
Pregnancy
It is important to Avoid
alcohol, it can cause disulfiram tvoe reactions.
Hypersensitivity
Diabetic Ketoacidosis
(DKA)
Not indicated in type I diabetes
Contraindicated Pregnancy

Biguanides
Metformin (Gluco-

phage)

Lactic acidosis, in
hepatic and renal disease patients
GI discomfort Anorexia, nausea, diarrhea, metallic taste
Due to anorexia
caused by metformin
this drugs used for
weight loss.

Hepatic or renal
Impairment
Alcoholism
Advanced age
Previous lactic acidosi s
DOC in obese
Therapeutic uses also inelude: To treat Infertility
For weight loss

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Thiazolidinediones
Ros iglitazone
(Avandia)
Pioglitazone

(Actos)

Glucosidase
Inhibitors
Acarbose
(Prandase)

Insulin and Anitdiabetic Drugs


I-Increase peripheral Increased HDL, Increase LDL and Pioinsulin sensitivity,
2-Reduce gluconeo- glitazone (decrease
genesis
TG),
Weight gain,
Hepatotoxicity,
Anemia
Fluid retention

Decrease the absorption of carbohydrates


(thus decreasing
postprandial rise of
glucose)

Flatulence
Abdominal
Cramping, nausea
Diarrhea.
Decrease metformin
bioavailability.

Uver disease,
Congestive heart fai lure
(CHF)

Gender selective? Resume


ovulation in previously anovulatory women (example:
polycystic ovarian syndrome). Increase chances
of pregnancy, if insufficient
contraception not used.
May be taken with or without food
Hypersensitivity,

DKA,
Inflammatory Bowel

Disease (LBO)
Pregnancy & Lactation,
Li ver cirrhosis
With first bite of meaL

Skip the dose if you skip


meals.
Intestinal lipase inhibitor
Orlistat (Xenical)

Intestinal lipase inhibitor


120 mg TID with
meals

Diarrhea
Steatorrhea (Fatty
stools)
Abdominal discom-

May interfere with abdominal absorption offat soluble


vitam in ADEK

fon
Oily leakage

Chlorpropamide (Diabinese)
Mechanism
Therapeutic use

Contraindications

Side Effects

Increased insulin release from beta cells of the pancreas


To control hyperglycem ia in glyburide-responsive OM of stable,
mild, nonketosis prone, maturity onset or adult type which cannot be
controlled solely by proper dietary management, exercise and weight
reduction or when insulin therapy is not appropriate.
Patients during stress conditions such as severe infection, trauma or
surgery.
Patients with liver disease or renal impairment; or frank jaundice.
Chlorpropamide not a good choice in elderly (long half life)
Hypoglycemia, Gl discomfort: Nausea

Repaglinide (Glucononn)
Mechanism

Stimulate release of endogeneous insulin (rapid-acting, better postprandial glucose control)

Therapeutic use
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Contraindications
Side Effects

Insulin and Anitdiabetic Drugs


Hypersensitivity
Diabetic Ketoacidosis (DKA)
Hypoglycemia(les~ frequent than with sulfonylureas)

Gliclazide (Diamicron)
Mechanism
Therapeutic use
Side Effects

Drug-drug
interaction
Contraindication
Monitoring

Stimulates the production and secretion of insulin from the islet cells of
pancreas .
Treat adult (maturity-onset) diabetes mellitus
Faintness and confusion
Weakness and tremor
Sweating, constipation and diarrhea
Corticosteroids, estrogens, diuretics, rifampin, other drugs may reduce
the effect of gJiclazide.
Alcohol
Not recommended to pregnant, lactating mothers. and children.
Regular testing of sugar levels in the blood and urine is required.
Periodic assessment of the eyes, heart, and kidneys may also be
advised.

Meglitimides ( Repaglinide, Natelinide)


Mechanism
Contraindication
Side effects
Drug-Drug
interactions

Stimulates the release of insulin


Type I and pregnancy
Hypoglycemia if meal not taken
Repaglinide has weight gain side effect
-Clearance inhibited by ketoconazole, miconazole, and erythromycin
-Enhance clearance with barbiturates, rifampin, and carbamazepine

Metformin (Glucophage)
Mechan ism

Therapeutic use
Side Effects

Contraindication

Drug-Drug
interactions

Does not stimulate secretion of insulin like sulfony l ureas. Rather decreases
hepatic glucose output by inhibition of gluconeogenesis.
Reduces LDL, VLDL, cholesterol levels
To control hyperglycemia
For the treatment of obese diabetic patients.
No weight gain side effect.
Preferred in obese patients
Lactic acidosis (in hepatic or renal failure patient), metallic taste, N, D and
anorexia
Contraindicated in renal and hepatic impainnents.
During pregnancy
Patient with history of Lactic acidosis, irrespective or precipitating factors
Alcohol potentiates effects, avoid alcohol
Potentiates other oral hypoglycemics

Rosiglitazone (Avandia)
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Insulin and Anitdiabetic Drugs

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Mechanism

Increasing insulin sensitivity in type 2 OM. It improves sensiti vity


to insul in in muscle and ad ipose tissue and inhibits hepatic
gluconeogenesis.
As monotherapy, in patients not controlled by diet and exercise alone.
To reduce insulin resistance and lower elevated blood gl ucose in patients
with type II OM.

Therapeutic Effects

Pioglitazone (Actos)
Mechan ism

Therapeutic use
Contraindications
Side Effects
Drug-Drug
interactions

A Thiazolinidinedione antidiabetic agent that depends on the presence of


insulin for its mechanism of action.
Decreases insulin resistance in the periphery and liver.
Improves glycemic control whi le reducing circulating insulin levels.
Increasing insulin sens itivity in type 2 diabetes. It improves sensitivity to
insulin in muscle and ad ipose tissue and inhibits hepatic gl uconeogenesis
Serious hepatic impainnent, acute heart fa ilure.
Weight gain, fluid retention, hemodilution, varying effects on lipids:
increase HDL, Increase LOL, Pioglitazone decrease TG
Increase the risk of pregnancy, recommend adequate contraception not
used.
Resume ovulation in previously anovulatory (polycystic ovarian
syndrome).
TZDs potentiates other hypoglycemic
Combination: rosiglitazone + metfonnin (avandia)

Acarbose (Prandase)
Mechanism
Therapeutic

Inhibits alpha gl ucosidase in intestinal border thus decrease absorption of


starch and disaccharides.
For type II DM in combination with other antidiabetic drugs.

use

Drug-Drug
interaction

Dose
Side Effects
Monitoring

May decrease metform in bioavailability


Potentiates other oral hy poglycemic effects
Diuretics, cortecosteroid, estrogen, oral contraceptives, phenytoi n, and
sympathomi metics drugs may increase blood glucose level and effect diabetic
control
50 - 100 mg TID with each meal - start low and go slow.
Flatulence, diarrhea, abdominal pain, cramps, nausea
Regular testing of after meal blood sugar level.
In combination oral hypoglycem ic therapy always use agents from different
class of oral hypoglycemics.

Onistat (Xenical)
Mechani sm

Therapeutic use
Drug-Drug
interaction
Dose
Side Effects

Blocks the action of stomach and pancreatic enzymes (Iipases) that digest fats,
so fats and oiher fat so luble vitamins ADEK are not absorb in the body but pass
through and excreted in the feces.
Reduces fats stores and produce weight loss.
Orlistat increases blood levels and toxicity of pravastatin
120-360mg daily
Di arrhea, abdominal discomfort, oi ly leakage

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Insulin and Anitdiabetic Drugs

Antidiabetic drugs Tips


Acarbose mechanism 7
Orl istat mechanism 7
Difference between glyburide and glimepride7
Antidiabetic drugs taken before or after meals 7
Insulin works on cell wall
The antidiabetic drug side effect of anorexia 7
Anticholesterol DOC in diabetic patient 7
Metfonnin monitoring7
Which antidiabetic drugs are not used in type I DM 7
What antidiabetic drug of choice in pregnancy 7
If patient has admitted in surgical ward and her blood glucose levels high, what is drug of
choice7
Which of the available forms of insulin should be used IV to correct excessive preprandiai
glucose concentrations?7
8MI = weight in Kg! (height in m)2

Abbrevation and Terminology


lDDM
NPH
NIDDM
BSL
DKA
HDL
LDL
TG
ADEK
VLDL

Insulin Dependent Diabetes Mellitis


Non Insulin Deoendent OM
Blood $uQar Levels
Diabetic Ketoacidosis
Hieh Densitv Liooorotein
Low Densitv Liooorotein
Trie:lvarides
Fat Soluble Vitamins
VerY Low Densitv linonrotein

Generic and Brand


Sulfonylureas
Glyburide
Chlorpropamide
Repagl inide
Rosigl itazone
Pioglitazone
Acarbose
Orlistat
Chlorpropamide
Gliclazide
Natelinide
Metfonnin

DiaBeta
Diabinese
Glucononn
Avandia
Actos
Prandase
Xenical
Orinase, Diabinese, Insulase
Diamicron
Starlix
Glucophage

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Thy ro ids Disorders

24

Thyroid disorders
I Drugs Used In Thyroid Disease I
I
I

I Hypothyroids I

IHyperthyroids I

I
Thyroxine (T4).
Dess icated thyroi
hormone.
Svnthroid

I
ITriidothyronine CT,)I

Thioamides:
Methimazole
Propylthiouracil

Symptoms

Treatment

Monitoring

Pregnancy

I
Iodide
Lugol solution :
(lU+!)

~ I lpod," I

Hypothyroid ism
Sensitivity to cold
Constipation
Bradycardia
Weight gain
Dry flaky skin
Coarse hai r
Slowed speech
Puffy face , hands, feet
Hearing loss
Decreased libido
Slow return of deep tendon
reflexes
If untreated myxedema and coma
will develop
Thyroxin (T4)
Triiodothyronine (T])

Hvperthvroidism
Intolerance to heat
Diarrhea
Tachycardia
Weight loss
Nervousness
Heart palpitation
More common in pregnancy

Most sensitive test is :


Serum TSH assay (increase)
Decreased free T4
Decreased free T3

Serum TSH assay (decrease)


Increase Free T)
Increase T4

Thioamides
Methimazole
Propylthiouracil
Iodide
Radioacti ve iodide

PTU is drug of choice

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Thyroids Disorders

Levothyroxine (Eltroxin, Synthroid)


Mechanism
Therapeutic use
Side effects

Drug-drug
interaction

Over dose
Monitoring

Food and drug


interactions

A major hormone ofthyroid gland


Goiter thyroid cancer
Rare side effects such as
Anxiety
Diarrhea
Weight loss
Sweating
Insomnia
Muscle cramps
Antiepileptic, Cholestyramine, and sucralfate may reduce the absorption of
Levothyroxine.
Levothyroxine may increase the effects of warfarin
Glycemic control may decline with initiation ofL-T 4 potentially
necessment of antihyperglycemic Agents.
Symptoms of hyperthyroidism if over-treated; possible exacerbation of
angina.
Periodic tests of thyroid function
Monitor TSH levels to adjust initial dosage after 6-8 weeks then as
required or annually adrenal insufficiency may adrenal insufficiency may
have to be increased during pregnancy to maintain TSH in desired range;
check TSH each trimester and 4-6 wk after any dosage adjustment.
May decrease absorption oflevothyroxine by: Iron salts, Cholestyramine
Colestipol Sucralfate

Drugs used to treat Hyperthyroidism

Methimazole (Tapazo!e)
Thioamides
Mechanism

Pharmacokinetics

Similarities between
Carbimazole and
Methimazole

Do not prevent the uptake ofT by the gland they inhibit the synthesis of
T3 and T 4 by inhibiting the iodination of tyrosine in the thyroglobulin
Blocks the coupling of the iodo thyroxine
Inhibits the conversion ofT. to T J
Therefore thyroid hormone synthesis is decreased.
Obvious effects are very slow since it takes 3-4 weeks before the
hormone levels show a decrease
Well absorbed,
Slow excretion
tll2 is 6 hours
Both drugs accumulate in the plasma
Both cross the placental barrier and can accumulate in the thyroid gland
of the fetus

Propylthiouracil (Propyl-Thyracil)
Mechanism
Therapeutic use

Manage the overactive thyroid gland


Hyperthyroidism
DOC in pregnancy

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Thyroids Disorders

Side Effects

Reduction in white blood cells leading to the risk of infection


Nausea and vomiting,
Joint pain, headache,
Rash and itching,
Jaundice, fever
Propylthiouracil - rapid absorption after oral administration
Peak serum levels seen after 1 hour
t ll2 is only 2 hours
Extensive first pass metabolism
Excreted by the kidneys as glucuronide (inactive)
Preferred in pregnancy for it does not cross the placental barrier
Strongly protein bound
Secreted in breast milk less than methimazole
More agranulocytosis seen than that of Methimazole

Phannacokinetics

Disadvantage
Contraind ication

Prescribed with caution in pregnant mothers. There is risk of goiter and


hypothyroidism in the newborn infant if too high dose is used. Reduce
dose to infant and children.

Monitoring

Periodic tests of thyroid function , and blood cell counts.


Jaundice
Sore throat and fever

Thyroid drugs Tips


Calcitonin is stimulated by ~
TSH is secreted from ~
In treatment of hypothyroidism with T4 have effect on ~
Hypothyroidism is monitored by ~
DOC in pregnancy for hy perthyroidism ~
Hypothyroidism symptoms ~
Hyperthyroidism is ~
Hypothyroidism is ~
T4 metabolized to T J by deiodinase enzyme
Discontinue antithyroid ifpatient notice even a single rash
Sweating is symptom of ~
Lugol solution is?
Lugol solution can stain.
Why is it beneficial to add propranolol to a drug regimen of a patient diagnosed with
hyperthyroidism?

Abbrevation and Tenninology


TSH
HRT

Thyroid Stimulant Hormone


Hormone Receptor

Generic and Brand


Methimazole
Propylthiouracil
Levothyroxine

Tapazole
Propy l-Thyracil
Drug of Choice

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Thyroids Disorders

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Gonadal Hormone and Gonadal Antagonist

25

Gonadal Hormones And


Antagonists
Gonadal Honnones And Antagonists
I

ITestes I

I Ova')' I
Estrogen
Ethinyl estradiol
Mestranol (prodrug)

Progesterone
Norethidrone
Norgestrel
Norethynodrel
Norgestimate
-rlesogestrel

I Testosterone j I Anti -testosterone drugs I

Included in this category are: androgens (male sex hormones), estrogens (female sex hormones) and
progestins. These chemicals are needed for the development. maintenance and function of the sexual
organs and are necessary for normal pregnancy to occur, be maintained and for birth
Clinical Uses for Various Estrogen Preparations
Palliative treatment of
advanced prostate cancer

IDiethylstilbestrol
Estrogen

Conjugated estrogens
Estradiol
I Estradiol transdermal

Estrogens are female sex honnones that are used primarily to decrease bone loss and to treat the
symptoms of menopause. Estrogen is used to reduce or prevent osteoporosis in susceptible women.
Estrogens decrease the frequency and severity of hot flashes as well as the dryness in the vagina that
many post-menopausal women experience.
Estradiol ~ Exist in body in eqUilibrium with estrone
Estriol
Estrone
Ethinyl estradiol ~ 17 alpha estradiol
Mestranol
Quinestrol~ used for estrogen replacement therapy (HRT)
Diethylstilbestrol ~ Non steroidal synthetic estrogen (sti lbene derivatives)

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Gonadal HOmlone and Gonadal Antagonist

Therapo;;:utic use

Estrogen is component orall brands of oral contraceptive pi lls.


Estrogen is used to reduce or prevent osteoporosis in susceptible women.
(Both senile and post menopausal)
Estrogen is componenent of Diane 25 & 35 and Alese oral contraceptive that
are used for the treatment of acne.
HRT ?To treat menopause symptoms ? Vasomotor symptoms, vaginal
atropy, psychological disorders
To treat prostate cancer.
To treat Primary hypogonadism

Side effects

GI? Nausea and vomiting are the most common, weight gai n, d iarrhea
CNS ? Headache, Breast tenderness
CV ? Edema, Hypertension, stroke, MI, Increased risk of thromboembolic
diseases

Contraindicated in

Prolonged used of unopposed estrogens (estrogen given without


progesterone) in postmenstrual women increases the risk of endometrial
cancer.
Deep vein thrombosis or (thromboembol ic diseases)
Vaginal bleeding
Breast cancer

Antiestrogens

Mechanism

Therapeutic use

Tamoxifen
Clomiphene
Inh ibit or modify the action of estrogen
These drugs are non-steroidal antiestrogcnic compounds equally effective in
oral or injection.
Tamoxifen ? Breast cancer
Clomiphene? Fertility drugs

Tamoxifen
Mechanism
Indication
Side effects

Tamoxifen competes for binding to the estrogen receptors thereby


inhibits the action of estrogen.
Tamoxifen is indicated in advanced breast cancer in postmenopausal
women.
Hot flashes
Nausea, vomiting ~ Least nauseating anticancer drugs
Vaginal bleeding
Menstrual irregularities
Risk of endometrial cancer

Clomiphene (Clomid)
Mechanism

Clomiphene Interferes with negative feedback of estrogen on


hypothalamus and pituitary thereby increases the secretion of
gonadotropin releasing honnone (GnRH) and causes stimulation of
ovulation.

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Therapeutic use
Contraind ication
Side effects

Gonadal Hormone and Gonadal Antagonist


Clomiphene is used to treat infertility associated with anovulatory
cycles.
Not effective in women whose ovulatory disfunction is due to pituitary
or ovarian failure.
Dose related
Ovarian enlargement '
Vasomotor flushes
Visual disturbances

Selective Estrogen Receptor Modulator (SERM)


Raloxifene
Reduces bone resorption thereby decrease bone turnover
Exhibit estrogen like (agonist) effect on bones and lipid metabolism
Exhibit estrogen antagonist action on uterine and breast tissues .
Therapeutic use: Prevention of osteoporosis.

Progestins
Progestins are female sex hormones that may be used with estrogens in oral contraceptive pi lls,
hormone replacement therapy, and treat menstrual irregularities, and as cancer treatment.
Classification of progestins
Two types ofprogestins
17 -alpha hydroxyprogesterone
A. Medroxyprogesterone acetate
B. Megestrol aceta
17-alpha ethinylandrogens (more potent)
A. Norethindrone
B. Norethynodrel
Commonly used in oes
Potent oral activity
More lipid soluble
Less first pass metabolism
Progestins are produced in males from testes.
Mechanism
Adrenal cortex produced progestins in males and females.
Progestins in females promote the development of a secretor endometrium that
can accommodate implantation of newly formed embryo.
The high level ofprogestins produced in second half of menstrual cycle inhibits
the production of gonadotropins and thereby further ovulation.
Therapeutic
Major clinical use in contraception, general ly used with estrogen.
use
Not widely used as alone because of its rapid metabolism results in low
bioavailability.
Progestins are indicated in uterine bleeding, dysmenorrhea, suppress ion of
postpartum lactone, and endometrium cancer.
Endometriosis
Side Effects
Edema
Depression
Menstrual irregularities (breakthrough bleeding, amenorrhea)
Androgen like progestins can increase LDL and HDL ratio cholesterol , weight
gain and edema,
Hirsutism, and acne can cause thrombophJebitis (inflammation of wall of vein)
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Gonadal Hormone and Gonadal Antagonist

Antiprogestins- Mifepristone (RU-486)


Mechanism

Therapeutic use

Side Effects

Progestin antagonist with partial agonist activity


Mifepristone also has anti glucocorticoid property.
Causes abortion if administered in early pregnancy (85%)due to interference
with progestins and decrease in production ofhCG (human Chorionic
Gonadotropin)
Abortifacient: Administration ofmifepristone used as contraceptive
given once a month when progestin levels are high (Prostaglandin E, and
misoprostol orally after single dose ofmifepristone effectively terminates
the gestation.
Uterine bleeding, and possibility of incomplete abortion

Androgens
Testosterone is the androgen that leads to the development of male secondary sexual characteristics
and maintains the male reproductive system.
Androgens are used to treat delayed puberty in males who do not develop normal testicular function.
They are also used ill egally by athletes to build muscle mass. They are very dangerous when used for
this as they may lead to aggressive behaviour, and may cause liver and/or brain tumours and death.
Androgens

Danazol
Nandrolone
Stanozolol
Fluoxymesterone

Mechanism

Therapeutic use

Side effects

Testosterone is commonly prescribed in the treatment of female breast


cancer, androgen deficiency, and for stimulation of growth, weight gain,
and red blood cell production. Commonly known as "anabolic steroids"
because they promote muscle growth. They are also commonly used to
help patients recover from a surgery and cancer treatment that resulted in
damage to muscle tissue.
Used in males with inadequate androgen secretion
Anabolic steroids can be used in sever bums, for speedy recovery from
surgery.
Indicated in conjunction with other hormones in pituitary dwarfism.
Non approved uses: Androgenic steroids in increase of lean body mass,
muscle strength, aggressiveness in body builders and athletes
Danazol indicated in endometriosis (ectopic growth of the endometrium)
Androgens orally ineffective
In males: priapism (continuous erection), impotency, gynecomastia.
In females; masculinization, acne, hirsutism, deepening of voice,
menstrual irregularities.
Contra indicated in pregnancy.
Increase LOL, decrease HOL levels, increase Coronary Artery Disease
(CAD), fluid retention (edema)

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Gonadal Hormone and Gonadal Antagonist

Antiandrogens- Finasteride

Mechanism

Therapeutic use

Finasteride
Dutasteride
FJutamide
Cyproterone acetate
Inhibit the synthesis of androgen.
Finasteride: steroid like drug approved for BPH treatment.
Finasteride : inhibits the S-alpha reductase: Competitive and specific
inhibitor of type II S-alpha reductase
Indicated in BPH, and to treat men who have lost scalp hair.

Side effects

Decrease libido.
Sexual dysfunction
Breast tenderness
Hirsutism
Hypersensitive reactions like rashes, pruritic, swelling face and lips
Testicular pain

Dose

Smg for BPH treatment


1mg daily for 3 months for hair growth in men

Contraindication

~ofindicated

in woman and children . Woman should not hand le or


break tablet when they are pregnant.
Finasteride may cause external genitalia abnormalities in male fetus.

Endocrine disordels Tips


ACTH is secreted by ~
Example of anti androgenic drug ~
What partial anti estrogen cause hot flushes ~
Metformin + glyburide may cause -7
Increase in cortisone cause (Hypercorticoids) -7
Decrease in cortisone cause (Hypocorticoids) ~
Glutathione is -7
Diabetic Ketoacedosis (DKA) mainly occurs in -7
During ovulation increase of ~
Corpus luteum is stim ulated by ~
Purpose of freque nt glucose level monitoring ~
What steroidal hormone structure have phenolic ring ~
Decrease in cortisone cause ~
Aldosterone secreted from -7
Cortisone is secreted form ~
Hoshimoto disease ~
Example of antithyroid drugs -7
Fineseride (Proscar), Dutasteride (Avodant) is ~
Vitamin 0 3 acts as ~
Myxedema is malfunction of ~
The effect of vasopressing on kidney -7
Deficiency (absence) of Antidiuretic Hormone (AOH) or vasopressin cause
(01)
Glutathione protects-7
The endocrine gland plays important rule in calcium metabolism -7
The major factor that controls Na excretion in kidney~

Diabetes Insipidus

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Gonadal Hormone and Gonadal Antagonist

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The effect of the antidiuretic hormone is to-7


In post menopausal therapy which drugs have risk of endometrial cancer -7
The substance naturally occurs in body called -7
Thyroid is NOT a part of ~
Oral contraceptives completely contraindicated in ~
Insulin has pharmacodynamic effect on ~
Oxytosin is secreted from ~
Oxytosin is used ~
Glucogon cause ~
Calcium reabsorption of distal convoluted tubule due to.~
Normal Cholesterol =

Abbrevation and Tenninology


HRT
ADH
GnRH
HDL
LDL
BPH
ACTH
DKA

Hormone Replacement Therapy


Antidiuretic Honnone
Gonadotropin-Releasing Hormone
High-Density Lipoprotein
Low-density Lipoprotein
Benign Prostate Hyperplacia
Adrenocorticotropic Hormone
Diabetic Ketoacedosis

Generic and Brand


Tamoxifen
Clomiphene
Mifepristone
Danazol
Nandrolone
Stanozolol
Fluoxymesterone
Dutasteride
Flutamide
Cyproterone acetate
Dutasteride

Nolvadex, Soltamox
Clomid
Mifeprex
Danocrine
Durabolin, Kabolin
Winstrol
Halotestin, Android-F, Ora-Testryl.
Avodal1
Eulexin
Diane
Avodant

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Adrenal Corticosteroids

26

Adrenal Corticosteroids
The adrenal hormones, or corticosteroids, are drugs with powerful anti-inflammatory effects. These
are used for replacement therapy in conditions such as, Addisons disease, a condition of adrenal
insufficiency. In replacement therapy, the adverse effects are minimal since hormones are being
replaced and are not added to those already in the body.
Corticosteroids are used for their anti-infl ammatory, anti-allergic and anti-stress effects. Prednisone
is used 'as replacement therapy and also for its anti-inflammatory effects in many conditions, such as
arthritis, allergies and asthma.

Glucocorticoids
Classification
Short acting (812 hour)
Intermediate acting (18-36
hours)

Long acting (1 -3 days)

Mechanism

Side Effects

Drug and Food interactions

Hydrocortisone
Cortisone
Prednisone
Prednisolone
Methylprednisolone
Triamcilone
Betamethasone
Dexamethasone
Paramethasone
Promote normal intennediately metabol ism
Increase resistant to stress
Alter blood cell levels in plac;ma
Anti-inflammatory action by inhibiting IgE
High doses stimulate gastric acid and pepsin production and may
cause peptic ulcers.
Chronic use causes sever bone loss (Due to decrease in calcium)
and myopathy leads to weakness
Concentration of topical Glucocorticoids depends on site of use
on the body.
Take with food
Should not be stopped suddenly, taper off or gradually decrease
dose.
Diabetic drugs ~ glyburide, chlorpropamide, gl ipizide,
tolbutamide, and tolzamide.
Can rise blood sugar noticeably
Monitor blood sugar levels

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Therapeutic use

To treat severe allergic reaction


To treat chronic ulcerative col itis
To treat nephrotic syndrome and renal diseases
Topical agent to treat diaper rash and dermatitis
Topical agents for ophthalmic disorders
To treat rheumatic carditis
To treat severe arthritis
To treat acute and chronic adrenal deficiencies
To treat Nausea and vomiting associated with cancer
chemotherapy
01 -7 peptic ulcer, hemorrhage, acute pancreatitis, ulcerative
esophagitis
CNS-7 headache, [ncreased lOP, muscle weakness, euphoria
and dysphoria
Hormonal -7 We ight gain, osteoporosis, hyperglycemia
(Diabetes), flushing of face and neck, cushingoid (moon face
and buffalo hump) and increase risk of infections.
CY-7 edema and hypertension
Skin thinni ng

Side effects

I Adrenal
Corticosteroid

I L-ortlcoster010
biosynthesis
inhi bitors

I Mccnamsm

InD icatIOns
of Adrenal
corticosteroids

Adrenal Corticosteroids

Cortisone
Hydrocortisone
Betamethasone
Beclomethasone
Prednisolone
Prednisone
Triamcilone
Methylprednisolone
tl..etoconaZOle
Spi ronolactone
Mifepristone
Metyrapone
Aminoglutethimide
l'or antl-mnammatory cortlco~as: .li lucocOrtlCOIOS cnccts on mc o~ stfloutJon,
concentration, and function of leukocytes. These include decrease in
concentration oflymphocytes T and B cell s) and increase in concentration of
neutrophils.
Decrease basophils, eosinophils and monocytes, and inhibition of the ability
ofleukocyte and macrophages to responds mitogen and antigen.
The above Inhibitory response also results in reduce the amount of histamine
release from basophil s to inhibit kinins.
InDIcatIOns ot aDrenal cortlcoster01DS
Addison's disease (caused by dysfunction of adrenal cortex}-hydrocortisone.
Cushing' syndrome (caused by hypersecretion of glucocorticoids that is due
to excess secretion of corticotropi n by anterior pituitary to adrenal tumor. dexamethasone test is used in diagnosis .
Congenital adrenal hyperplasia (CAH}-results from enzyme defectsadministration of sufficient corticosteroids .
Indicated in inflammatory symptoms of rheumatoi d arthritis, osteoarthritis,
skin condition. Redness, swelling, heat, and tenderness that commonly treated
by adrenal corticoids
Indicated in treatment of allergies.

Opyfl glll 11.0' .LOuv 'UV,- J Jr.;:) mc. unaUUlOflzeu reOfUUUClion


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Adrenal Corticosteroids

I FormulatIOns

. Systemic:
lM -7 Cortisone, triamcinolone, desoll.ycorticostt:rum::
IV and 1M -7 Dexamethasone, hydrocortisone, methylprednisolone,
prednisolone.
Inhaled -7 Aerosol -7 Beclomethasone, flunisolide. fluticasone, triamcinolone
Topical -7 Hydrocortisone, beclomethasone, dexamethasone, triamcinolone,
Oral: All corticosteroids can be administered orally.
I Long term use OsteoporosIs --> IS due negative calcIUm balance
Side effects
Increase risk of infection due to impaired wound healing and immunosuppression
associated with Diabetes -7 due to hyperglycemia SE
oral steroids
Increased appetite can cause we ight gain
Hypertensi on is due to increase water retention (Edema)
Peptic ulcers
Euphoria
Psychosis
Immunosuppression -7 due to suppression ofh!:E.

Adrenocorticoids Tips
Increase in cortisone cause -->
Decrease corticosteroids Gause~>
What is steroid sparing drug -->
Aldosterone are secreted from -->

Abbrevation and Tenninology


eNS

Centa[ Nervous S stem


Intra Ocular Pressure

lOP

Generic and Brand


Cortisone
Hydrocortisone
Betamethasone
Beclomethasone
Prednisolone
Prednisone
Triamcilone
M ethvTrll-edn iso lone
Ketoconazole
Snironolactone
Mife ristone
Me ra ne
AminO-;;-' utethi m ide

Cortone
A-hvdroCort, Ala-Cort, Ala-Scalpt, Anu-Med HC
Oi rosone. Oi rolene
Beclovent Beconase A Beconase. var Vancenase
AX-Pred Bubbli-Pred Econo red Econo red Plus
Oeltasone. Predone. Stera red Stera red OS
A-Methanred Cortimed De medalone De o-Medrol Medralone
Extina Kuric Nizoral Shamnoo Nizoral Nizoral A-D Xolepel
Aldactone Snirono
Mife rex
Meto irone
Amino lutethimide

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Oral Contraceptives

27

Oral Contraceptives
Oral contraceptives (birth control pills) are combinations of estrogen and progestins.
The combination preparations may be monophasic, biphasic or triphasic. They contain various
estrogens and progestins . Some common ones are listed:
Drugs that Causes Of
OC Failure

Contraindications

Precautions

Starting Hormonal
Contraceptives

Alcohol excessive chronic,


Anti biotics (ampicillin, cotrimoxazole, griseofulvin, metronidazole,
nitrofurantoin, neomycin, penicillin, rifabutin, rifampin &
tetracycline),
Anticonvulsants (carbamazepine, ethosuxim ide, oxcarbazepine,
phenobarbital, phenytoin, primidone & topiramate l dose),
Antivirals (nelfinavir & ritonavir), modafinil, red clover & St. John's
wort.
Active thromboembolic disease
-undiagnosed vaginal bleeding
Acute or chronic obstructive liver disease
Known or suspected breast cancer
Known Or suspected pregnancy
Hypertension may use OCs if hypertension controlled
CVD, hyperlipidemia OCs with new progestins preferred because of
more favorable lipid profile
Diabetes -low dose OCs unlikely to affect glucose control but
estrogen may complicate vascu lar disease
Epilepsy - some anticonvulsants ! oes efficacy due to l metabolism;
may require use ofOCs with >35ug EE
Hepatitis, cirrhosis - avoid OCs if active disease; may use if liver
enzymes have returned to normal
Gallbladder disease - iIlay be exact:rbatt:d by Des
Migraine - avoid OCs if classic, complex, age ~35 (lstroke)
Inflammatory bowel disease - active diarrhea may reduce absorption
and efficacy of OCs and require backup method
Systemic lupus erythematosus - avoid ~C 's as estrogens can
complicate vascular disease
Smoking women over age 35 - if light smoker \5cigs/day) or on
nicotine patch, can use 20 Jlg EE product but l risk ofDVT.
Starting Combined Des:
Most effective ifstarted Day I of menstrual period can be started any
day up to Day 6
To avoid weekend periods, start on I S1 Sunday after period begins
If started after Day 5 use backup method for first 7 -10 days as
ovulation may not be suppressed
Starting Progestin-only Pill (PO P):
Start on Day 1 of menstrual period an~ daily thereafter
Use backup method for first month

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Starting Hormonal
Contraceptives

Side Effects & Their


Management

Miss pills

Plan B (Levonorgestrel
O.7Smg per dose)
Or Minipill
Or Morning after pill
or
Emergency
contraception
Side effects plan B

Oral Contraceptives
Starting Depo-Provera: im
Should be inj ected during the first 5 days of menstrual cycle rule out
pregnancy
Repeat injection ql2 weeks - effective for up to 14 wks
Breakthrough bleeding - most common in 1st 3 months; if persists
beyond 3-6mon check for other causes (eg. chlamydia). Change to
oe with 1 estrogen/progestin depending on when BTB occurs in the
cycle; may also be related to poor compliance, smoking, DIs
Breast tendemess - if persists beyond 1st 3months rule oul pathologic
causes; change to oe with! estrogen/progestin
Weight gain - may i appetite in 1st month but overall weight gain is
minimal with low dose oes & within nonnal limits for age-related
gain; may be cyclical due to Na & H20 retention
Nausea - often subsides within 3 months; take at hs with food or change
to lower estrogen content
Headache - tension headaches unaffected but honnone related or
vascular migraines may i!; if precipitated or exacerbated by oes
should avoid their use
Acne - sometimes worsens initially but usually improves in the long
tenn; change to ! androgenic OC or use topical therapy
Chloasma - irreversible and idiosyncratic; exacerbated by sunlight so
use sunscreen and reduce exposure; ! estrogen dose
Miss one pill: Take as soon as you remember and take usual pill next
day. This means that you might take two pills in a day.
Miss two pills in a row:
First two weeks : Take two pills the day you remember and two pills
next day. Then take one pill until you finish pack.
Use back up method of birth control, if you have sex in next seven
days of missing pill.
Third week: Safely dispose remained pills and start new pack same day.
(If you're on Sunday start schedule continue one pill until Sunday).
You may not have periods this month.
If you miss two periods in a row call doctor.
Progestin only
Very efective within 24hrs and can be used upto 5 days unprotected
inter course.
Schedule 2 (Phannacist intervention)
Contains 2 pills (use 2nd pill after 12 hours of I " pill)
To treat Nausea and vomiting associated with this pill can be treated
by Gravol (dimenhydrinate)
Nausea (23.1%), Vomiting (5%), Dizziness, fatigue

Abbrevation and Tenninology


DC

DVT
BTB

Oral Contraceptive
Deep Veinthrombosis
Break Through Bleeding

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Oral Contraceptives

Generic and Brand


Levonorgestrel, Ethinyl Estradi ol
Ethinvl Estradiol, Norethindrone

Alesse
Brevicon
Demulen
Diane35
Ortho Cept
Marvelon
Ortho
M inOvral
Triphasil
Svnphasic

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Oral Contraceptives

;;>

O--~

M'J~ ~ ~~
\-1et-~o tra~

~~ \v,1:)~ ~

4 'l.--<-:J

~ if J
J. ('

-~

Mo.Yc_-/~'

"t () fr.-vo.!

sf

D1rj. 6j
'b~;

\)
L~

l"" """ '" 0 ~ ~

~-"-h

; <>-- S

II

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Osteoarthritis

~,-,l."'~
~ I", -h ,; """"--t, .

28

0",

Osteoarthritis
1Osteoarthritis I

Nonsteroidal Anti~
inflammatory Drugs

Pain Therapy,
Topical

Tonical

Synovial Fluid
Replacement

Corticosteroids

Betamethasone valerate

Dic10fenac sodium

Capsaicin

Hylan GF 20

(pennsaid)

Methy l salicylate
Menthol
Triethanolamine

Hyaluronic acid sodium

salicvlate

Sodium hyaluronate

Viscous supplements
Intraarticular injections

~ , "'~ \~,-b,
Glucoconiooids

Cortisone acetate
Dexamethasone
Dexamethasone sodium
phosphate
Methyl prednisolone
acetate
Prednisolone
Triamcinolone
Triamcinolone diacetate

t Prostaglandins

of C}1otoxic .

t Cytokines

T cells

~.

r.-\ ~S
.L' "'\~..\,
\
J-

Activation of
B cells

Production of

IgRF

autoimmune

complex

Joint
inflammation
Synoviocytc
prolifcrnlion,
Bone and
cartilage
destruction

antibodies

Diclofenac (Voltaren)
Therapeutic use

Side Effects

Relieves mild to moderate headache


Menstrual pain
Pain following surgery
Acute attacks of gout
Relieves pain and stiffness associated wI rheumatoid arthritis and
osteoarthri tis (when given regularly)
OI disorders

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Drug-Drug
interaction

It interacts with NSAlDs, oral anticoagulants, and corticosteroids, risk of

Contraind ication
Monitoring

Osteoarthritis

bleeding and ulcer may increase


Cyc1osporin with dic10fenac may increase the risk of kidney problems
Not usually prescribed in the last month of pregnancy as it may increase the
risk of affecting baby's heart and promote prolong labour.
There is an increase risk of bleeding from peptic ulcers and in bowel w ith
prolonged use.

Osteoarthritis Tips
Allergic to aspirin -7
Aspirin use in children with flu symptoms can cause -7
Peptobismol (Bismuth subsalicylate) can cause Rye syndrome in childrem.
Ibuprofen is safe in children under 12 years (No Rye syndrome)
Misprostol is -7
Azotemia -7
Topical pain relievers -7
Hylorunan injections (synovial fluid replacement) act as viscous supplement given -7
Misoprostol is -7
What type of exercise in osteoarthitis -7
Acetaminophen is least used in -7
Risk factors for renal toxicity associated with NSAIDs and COX II inhibitors include -7 .
Counseling of Capscicin -7
Corticosteroids are used primarily for their action as -7
Symptoms
Stiffness
Localized
Pain

lnftammation
Risk factor

Osteoarthritis
Morning or after inactivity (l ast 30
min)
Limited affected joints.
Worsens With Activity Or
After Prolong Use, (weight bearing
activity) .
Uncommon
>65 years
Degenerative joint disease caused
by breakdown of the cartilage b/w
bones, degradation of articular
cartilage in ~ynov ialjoints

Rheumatoid Arthritis
In the morning (last I hour)
Not localized
Worsens with prolong inacti vity. (Usually
improves with activity).
Common
Autoimmune inflammatory condition
Chronic systemic
Symmetrical synovitis affecting similar
joints bilateral.

Abbrevation and Tenninology


I Cylco Oxygenase

Generic and Brand


I Diclofenac

Cataflam, Solaraze

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Desease Modifying Antirheumatic Drugs

M~"'OL~() ..
LC)

ll~
/ --:-,

<:.- 1

'-'-

29

O :~ ,

, '""""'

Disease Modifying Antirheumatic


Drugs
Disease Modifying Antirheumatic Drugs (DMARD's)

DMARD'S

r
Gold preparations

Cytotoxics

Other DMARDs

:\

Aurothioglucose
Sodium
aurothioglucose

Azathiopnne
Methotrexate
sodium ~ Gold
Standards for
treatment ofRA

""Cyclosponne
Hydroxychloroquine--,.
sulfate ~ SE: Corneal &
retinal deposition

Biological response
modifiers

Adalimumab
Anakinra
Etanercept
lnflixirnab

~~~LeflunOmide-7 ~

pregnancy

H~~ 'i

Penic;lIamme
Sulfasalazine ~ ell: ASA

& Sulfa allergy

."

~"up

A chronic inflammatory disease with frequent acute attacks. The immune system is involved in
attacking the joints and surrounding structures such as muscle tendons and most other connective
tissue. There is inflammation of the synovial membrane.
Biological
Response Modifiers

:::':,

"

...."

""

lnflix.imab

Etanercept

lnfliximab

lnflix.imab (Remicade)
Etanercept (Embrel)
Anakinra (Kineret) .
Binds to the Tumor Necrosis Factor (TN Fa.)
Inhibit interleukin- l (IL-!), a key mediator of inflammatory NF
synoviti s as well as bone and cartilage destruction.
Improve the sign and symptom of active RA
Must be given with Methotrexate to prevent fonnatian of antibodies.
Binds to the Tumor Necrosis Factor (TNF alpha and beta)
Given SC twice weekly
Side effects: Most common: Respiratory tract infections
Given every 8 week by iv
Most common SE is Respiratory tract infections (Pneumonitis)
Storage: Refrigerator (2 - 8OC)
~
Do not freeze

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Desease Modifying Antirheumatic Drugs

Methotrexate (Rheumatrex)
Mechanism
Therapeutic use

Folic acid antagonist


Treat Rheumatoid arthritis
An anticancer drug, and used together with other anticancer drugs in the
treatment of Leukemia, Lymphoma, and solid cancers such as Breast,
bladder, head, and neck.
Treat uncontrolled psoriasis until less potent drug can be re-introduced.

Side effects

Nausea, diarrhea
Flu-like aches
Oral ulcers (mouth ulcer): Treated by folic acid or folinic supplements.
Bone marrow and liver toxicity
Immunosuppression
Hepatotoxicity
Renal failure
Leukopenia
Abnormal LFT
Pulmonary toxicities in children
Susceptible to Infections (P. carinii)
Starting 7. 5 - 15 mg po Q wk. Increase by 2.5 - 5 mg Q 2 - 4 wk.
Maximwn 25 mg! wk
Maintenance dose: 7.5 - 20 mg po, sc or 1M Q wk (s ingle dose if
tolerated or divided in 2 or 3 doses Q 12 h)
Effectiveness seen after 2- 6 weeks
Administer; PO, 1M, SC
IfG] upset occurs: 2.5 mg start ~ (12 h after) 2. 5 mg ~ (1 2 h after) 2.5

Dose

mg

Monitoring

Methotrexate weekly doses 20-25 mg (orally or parenteral) for at least


three months.
Concurrent use of fo lic acid reduces oral ulcers side effect.
Alcohol restriction may minimize hepatotoxicity.
Regular monitoring is mandatory:
Baseline hepatitis Band C serology
Chest X-ray

CBC
LFT's
Creatinin Q 1-2 months

Azathioprine (Imuran)
Refractory RA
Mefabolism
Therapeutic use
Side effects

Azathioprine is cleaved in vivo to mercaptopurine


Drug interaction with allopurinol (indicated in gouty arthritis), decrease
one th ird dose of azathioprine
H ematolog i c~ Leukopenia and/or thrombocytopenia and rarely as
agranul ocytosis
GI effects ~ Nausea and vomiting
Hepatic: Hepatotoxicity

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Contraindications

Desease Modifying Antirheumatic Drugs


Pregnancy
Children
Patients with rheumatoid arthritis previously treated with alkylating
agents (cyclophosphamide, chlorambucil, melphalan or others) may
have a prohibitive risk of neoplasia iftreated with azathioprine.

Hydroxychloroguine (Plaguenil)
Therapeutic use
Side Effects

Overdose
management

Treat Rheumatoid arthritis, Malaria


Retinopathy -7 Irreversible retinal damage (but is rare. In its early form, it
appears reversible upon discontinuation of the drug)
Skin rashes
G I disturbances
For management of a suspected drug overdose, CPhA recommends that you
contact your regional Poison Control Centre

Sulfasalazine (Azulfidine)
Mechanism

Therapeutic use
Side effects

Dose
Pharmacokinetics
Contraindications

Allergies

A chemical combination of sulfonamide and salicylate (S-ASA)


Sulfasalazine is axelatLvely weak. inhibitor o(the cycle-oxygenase
enzyme, but a potent inhibitor of IS-prostaglandin dehydrogenase
(pGDH), which is the main metabolic pathway for the prostaglandins
Second line therapy in ulcerative colitis (UC)
Blood Dyscrasias: aplastic anemia, agranulocytosis, purpura,
thrombocytopenia and hypoprothrombinemia, pancytopenia, macrocytosis
Hypersensitivity: erythema multifonne (Stevens-Johnson syndrome)
Skin: facial edema,
Gastrointestinal: hepatitis, pancreatitis
Nervous System: smell and taste disorders
PO or rectally
About 20% of sulfasalazine is absorbed in the small intestine after oral
administration
In patients with hypersensitivity to component of the product,
sulfonamides, or salicylates. In patients in whom acute asthmatic attacks,
urticaria, rhinitis or other allergic manifestations are precipitated by
ASA or other nonsteroidal anti-inflammatory agents. Fatal anaphylactic
reactions have occurred in such individuals.
In patients with intestinal and urinary obstructions.
In patients with porphyria, as these drugs have been reported to precipitate
an acute attack.
Infants under 2 year age
If allergic to the following drug avoid sulfasalazine

ASA
Furosemide
Thiazide diuretics
Carbonic anhydrase inhibitors,
Sulfonamides -7 sulfapyridine

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Counselling

Desease Modifying Antirheumatic Drugs


Discolors urine and May color skin orange yellow.
May pennanently stain soft lenses
Take drug after meals to reduce GI distress and to facilitate passage into
intestine.

Leflunomide (Arava)
Mechanism
Therapeutic use
Side Effects

Monitoring

Washout

Isoxazole immunomodulator, inhibits dibydro orate dehydrogenase.


It reduces pain and inflammation and slow progression of structural damage
Di arrhea. Nausea
Weight Loss
Flu like syndrome
Skin rash
Alopecia
Hypokalemia
Male patient have poss ible male mediated fetal toxicity. Reliable
contraception during treatment should be guaranteed.
Pregnancy must be avoided if either partner receiving lefluno mide.
Leflunomide should be administered to patients only under careful
medical supervision .
For men having received leflunomide and w ishing to have children.
Plasma levels of active metabolite should be less than 0.02 mgIL
Using Cholestyramine resin

Cyclosporine (Neoral)
Cyclosporin PO

Neoral or Sand immune I. V

3- 10 mg/Kg/day for RA
Therapeutic use

Side effects

Precautions

Drug interactions
(Cyclosporin is
metabolized by
CYP3A4)

Kidney transplantation
Organ transplantation rejection
PsoriasislRheumatoid Arthritis/Nephrotic Syndrome
Renal 7 Very common : renal dysfunction
Cardiovascular 7 Very common: hypertension (particularly in heart
transplant patients)
Nervous System7 Very common: tremor, headache
Metabolic7 Very common: hyperlipidemia
NSAlD therapy should be discontinued where possible. As nonsteroidal
anti-inflammatory drugs alone can have an adverse effect on renal
function, addition of these drugs to N eora! or Sandimmune LV. therapy
or an increase in their dosage should be accompanied by particular close
monitoring of renal function .
Drugs that increase cyclosporin serum concentration :
Ketoconazole
Fluconazole, Itraconazole
Macrolide antibiotics (mainly erythromyci n and c\arithromycin)
Corticosteroids, Oral contraceptives
Norethisterone or danazo l
Calcium channel blockers: Diltiazem, Verapamil, N icardipine
Metoclopramide

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Desease Modifying Antirheumatic Drugs

Drug interactions
(Cyclosporin is
metabolized by
CYP3A4)

Drugs that decrease cyclosporin serum concentration


Phenytoin or phenobarbital, Rifampin Lv. Sulfadim ine i.v. and trimethoprim
Lv. Nafci!lin, Carbamazepine, Octreotide, Barbiturates, Metamizole,
Probucol, Orlistat, Hypericum perforatum (St. John's wort), Troglitazone

Food and drug


Interaction

Grapefruit juice should be avoided

Minocycline (Minocin)
Minocycl ine
Therapeutic use

Side Effects

Contraindication

Drug and food


interactions

Broad spectrum antibiotic


Rheumathoid arthritis
Acne
Chlamydia (lymphogranuloma, Psittacosis)
Rickettsia (Rocky mountain s potted feve r)
Mycoplasma pneumonia
Lyme disease
Less phototoxicity than tetracycline
CNS 7 Vestibular problems: dizziness, nausea, vomiting
GI effects 7 anorexia, nausea, vomiting, diarrhea, stomatitis, glossitis,
enterocolitis, pancreatitis, pruritus ani, constipation
Skin7 maculopapular and erythematous rashes, SJS
Pregnancy, children under 13 yrs, breast-feeding.
Newborns, Infants and Children: The use o f tetracycline's, including
minocycline, during tooth development in last half of pregnancy.
Teeth and Bone: Dental staining (yellow-gray-brown) in infants of patient
who have last halftenn of pregnancy
Antacids containing aluminum, calcium or magnesium and oral iron
preparations impair absorption and should not be given to patients taking
oral minocycline.

D-penicillamine (Cuprimine)
Mechanism

Chelating agent

Therapeutic usc

Wilson's disease (excess copper)


Chronic lead poisoning
Active Rheumatoid arthritis
For refractory RA, if other drugs fail.

Side Effects

Urticaria, Pruritis, Rashes, Bone marrow depression,


Thrombocytopenia, Leucopenia, Tinnitus, Proteinuria
Diarrhea ( 17%)
5-10 mg of copper can administered as 5-10 drops of Copper sulphate
solutions in fruit juice twice daily (do not use in Wilson disease patients).
Penicillamine should be given empty stomach. (increase absorption)

Non Wilson disease


patients

Gold sodium thiomalate


Therapeutic use

Treat Rheumatoid arthritis

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Desease Modifying Antirheumatic Drugs

Side Effects

Most common
Skin rashes
Proteinuria (after 1M admin.)
Nitritoid reaction (low blood pressure and syncope after injections)
Pruritis (pruriginous), dermatitis
Angioedema
Thrombocytopenia
Aplastic anemia
Diarrhea
Stomatitis
Proteinuria

Post dose reactions

Arthralgias, flushing, hypotension

Rheumathoid arthritis Tips


Drug of choice (DOC) in RA is DMARDs (Methotrexate)
Which DMARD cannot be given for life7
lnfiiximab mechanism 7
lnfliximab storage conditions7
ASA antipyretic mechanism due to 7
ASA toxicity 7
N utropin is 7
Methotrexate used for 7
Mucositis (Stomatitis) is Side effects of 7
Patient taking methotrexate, to prevent bucal ulcer, should recommend 7
Shorter onset of action in DMARDs -->e
Osteoporosis associated with the use of which of OA drug -->
Which DMARDs require ophthalm ic examination monitoring- >
Mucositis is side effect of 7
Pannus means7

Abbrevation and Tenninology


DMARD
RA

ASA
TNF

LFT

esc
uc

NSAID
SJS

OA

Disease Modifying Antirheumatic Drugs


Rheumathoid Arthritis
Acet 1 Salia late
Tumor necrosis factor
Liver Funtion Test
ComDlete Blood Count
Ulceralive Colitis
Nonsteroidal Anti-Inflammatory Drug
Steven Johnson Syndrome
Ostreoarth itis

Generic and Brand


Arava
Leflunomide
Cyc1osporine
Neoral
Minocycline
Cleeravue-M Dynacin Minocin Myrac
0 - enicillamine
Cuprimine
Infliximab
Remicade
Embrel
EtanerceDt
Anakinra
Kineret
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Gout and Hyperuricemia

~ 30
Gout and Hyper uricemia
I

I Gout attack therapy

Hyperuricemia
TheraDV

Antimitotics and
anti-inflammatory
action

Colchicine

Corticosteroids

Nonsteroidal
Anti-inflammatory
Drugs (NSA IDs)

UricosuricS71ncrease
excretion of uric acid

Xanthine oxidase
inhibitors " prevents
conversion of purine to
uric acid

Indomethacin 7 Highest anti


inflammatory NSAID
Phenylbutazone
Sulindac

Dexamethasone
Dexamethasone sodium phosphate
Hydrocortisone sodium succinate
Methylprednisolone acetate
Prednisone
Triamcinolone

Probenecid" Take with full glass

H,O
SuJfinpyrazone7 Take with full
glass of HP

Allopurinol" Take
with full glass of HP

Basics of Gout arthritis


Gout is a d isease in which monosodium urate monohydrate (MSU) crystal deposit in joints, soft
tissues such as cartilage, tendon and bursa or renal tissues such as glomeruli, interstitium tubules.
Gout arthritis involves 4 Stages
Asymptomatic hyperuricemia
Acute gouty attacks
Intercritical gout
Tophaceous gout
Asymptomatic hyperuricemia
Nonnal serum urate levels:
Woman 360 mmollL
Men 420 mmollL

r...........

lL

/-M-o-r-e-c-o=m::'m~o-n-=:in~:~M::e~n~o:v~e~r-4-0-y-e-a-r~o=f=a:g=e~;;~

t< /ri: R...cO, lh X 14. .V'~~

R~

..-.

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Gout and Hyperuricemia

Hereditary metabolic disease that is a fonn of acute arthritis and is marked by inflammation of the
- Joints.
Gout is associated with increased body stores of uric acid.
Acute attacks involve joint inflammation caused by precipitation of uric acid crystals.
Hyperuricemi a ~
Urate crystal in joints -?
inflammatory response
Acute gout arthritis
Abrupt onset of excruciating pain and inflammation of joint during the night or early morning.
Patient cannot tolerate even light pressure such as a bed sheet on the affected j oint.
Attacks often resolve spontaneously over 3- 10 days. J.IIline treatment is N SAID's
For sever pain a Intra-articular inj ection of corticosteroid. (especially in patient with polyarticular
gout)
Colchicinea It relieves pain withjn 24 hours in 90% patients if treated within few hours of attacks.
Side effects: Gl ~ abdominal pain, cramps, diarrhea, N and V
Rarely a Neuropathy, myopathy, bone marrow suppression
Intercritical gout: Most patient have second attack within 6 - 24 months .
Chronic tophaceous gout: May occur after 12 year of first attack.

Colchicine - "'> .v> J


c::C>~
~ t.-r \:,

3~ '~

Mechanism

Colchicine is as selective inhibitor of microtubule assembly, reduced


leukocyte migration and phagocytosis: the drug may also reduce
production ofleukotriene B4
Because it reacts with tubulin and interferes with microtubu le
assembly, this is general mitotic poison. Tubul in is necessary for
nonnal cell division, motility and much other process: therefore,
colchicine has systemic side effects if used in excess

Therapeutic use

Used only for GOUl, can be used as IV


Antiinflammatory action only
No analgesjc effect No J![jrp5uric effect

Side effects

Diarrhea, nausea, and abdominal pain .


Chronic use can produce hemorrhagic gastroenteritis, hematuria,
alopecia, agranulocytos is and peripheral neuropathy

Drug-Drug
interactions

Taking cyclosporine with colchicine may lead to adverse effects on the


kidneys.

Indomethacin (Indocin)
Mechanism

Potent NSA1D's such as indomethac in also effective (but not as


selective) in inhibiting the inflammation of acute gouty arthritis.
NSA1 D's acts through prostaglandin formation and through inhibition
of crystal phagocytosis by macrophage

Therapeutic use

Use to treat gout arthritis

Side effec ts

Indomethacin may cause renal damage or bone marrow depression .

Probenecid (Benemid)
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Gout and Hyperuricemia

Mechanism

Uric acid is both actively secreted and actively reabsorbed in the


kidney. Probenecid partially inhibits both the active secretion and the
active reabsorption.
Uricosuric agents are weak acids that compete with uric acid, in the S2
segment of the proximal renal tubu le, for reabsorption by weak acid
mechanism
Gout
Before using probenecid check to see that the patient is not a high
excreter of uric acid, otherwise the use of drug may precipitate uric
acid crystals in the kidney

Therapeutic use
Side effects

Counselling
Take plenty of water

Sulfinpyrazone (Anturane)
Mechanism

Allopurinol (Zyloprim)

Metabolism
Therapeutic
use
Side effects

C 1.< . ; : " , ,,

&" .~"'~ ~,

." , AZo " ,0 I'r """ --. """t ~ e.

Sulfinpyrazone partially inhibits both the active secretion and the active
reabsorption
Inhibits platelet aggregation
Gout arthriti s
Urate crystal formation
Take plenty of water

Therapeutic use
Side effects
Counselling

Mechan ism

""'-,,-X'c"'-r-\.o~ ~~ 'r "';;4;' Y~

en ~

Rlbo," -

Allopurinol is a suicide inhibitor of


xanthine oxidase (XO)
Purine a uric acid
Allopurinol aoxypurinol
Reduce uric acid pool

P + ATP

s - Ph"pho"bo,yl - 1 - PY'TO'h'" (pRPp) + GI,"ml"

Inosinic Acid
j

Hypersensitivity rashes
Inosine
Peripheral neuritis and necrotizing
j 1
vasculitis
Hyroxilnthinp
GI intolerance, diarrhea
Ir.X~M-'~h~I"-,-o-xo~d-,,'eI
In condition with large purine turnover xanthine
Xanthine
stone formation may occur
Ir.X~M----'th~'"-,-o-xo~d-,,'eI
Alkalinize the urine to increase solubi lity
With 6~merca topurine (but not thioguanine)
Uric Acid
Must decrease by 2 I use Wit a opurm .
Xanthine oxidase is main biotransforming enzyme for 6-mercaptopurine.
Example of6-mercaptopurines is azathioprine, an anticancer drug
Take plenty of water

!
!

Counselling

Gout arthritis Practice Tips

T}>~"--.A
a

~,}

t'"

Not. used in acute gout a~ack7A\ 0 - 1'\4.


Punnestructurepresentm 7
~\f,

l\~t,,,J:)
<;Jf"'V'o""'~
-J
,
~ ,

f l' \ ~

~ ~ o...L..o-...C;~l 0

Takeplentyoffluids(water)~ith7 <;~: ~t1'fo-.L~ ..(

"'l

,0

'j
'"'.(1<1)

Co

l'\. _ ~

'1'J4-

Colchicine act as 7 "-"i\;" \~) 0..",-\, "'-I \:~t\ ( ) ""'" ~q..., 1 c:


The end product of purine metabolism 7 Iv..r I
0.... c..l
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o!

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-Lj)

Gout and Hyperuricemia

www.PhannacyPrep.Com

Sulfinpyrazone is used as ~
A uricosuric drug is one that -7
Colchicine is mainly used for ~

Abbrevation and Tenninology

I xo

I xanthine oxidase

Generic and Brand


Colchicine
Indomethacin
Probenecid
Sulfinpyrazone
Allopurinol

lndocin
Benemid, Probalan
Anturane
Zyloprim

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Osteoporosis

31

Osteoporosis
I

Osteoporosis Treatment

I
Calcium Supplements

Anti parathyroid
Hormones

calcitoni~

Bisphosphonates

Benzothiophene

"\
Parathyroid hormonesl

Alendronate

- l-

~tidronate

Non Modifiable

I
Selected Estrogen
Receptor Modul ators
"(SERM s)

Calci um carbonate
Calcium gluconate

Risedronate

Age> 65 y
Vertebral compression fractures
Postmenopausal woman (not on estrogen
therapy)
Premature menopause 45 years)
Gender (Female)
Family history
Thin and small boned (overweight is NOT a
risk factor)
Hypogonadism
Race: Caucasians, Asians
Hyperparathyroidism
Hypocalcemia

In esled

I S-Dib ydrox ychole<:a1ciferol

Teriparatide

Raloxifene
hydrochloride

Modifiab le
Low calcium intake 1000 mg
elemental calcium per day)
Inadequate sun exposure.
Gigarette smoking
Excessive Alcohol intake ~
Caffeine contai ning beverages.
Sedentary life sty le
Excessive heparin therapy
Oral Corticosteroid therapy

V.'t D

( )

) ~.~~~

(
(

(~ )
Fe<:al
Ca"

_s,_cro_;_,,_---'

LI

Filtration

Reabsorptl

~
I'TH

~rmary Ca'-excretlon

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0 2,

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ac Pre .Com

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'~'1J ~,-\' J ~ ~~

Osteoporosis

Calcium and Vitami


o supplements

CalcIUm carbonate (40% Elemental calcium).-? Provides most


calcium, usually require requires an acidic environmenl for absorption.
Tricalcium phosphate (Calcium phosphate, tribasic) 39%
Calcium chloride 27%
Calcium citrate (21 %)-7 good choice for seniors
Calcium lactate ( \ 3%)
Calcium gluconate (9.3%)-7 least elemental calcium
Dose of Calcium
4 - 8 Year: 800mglday
9 - 18 year 1300 mg/day
Perimenopausai woman: Not less than 1000mglday
Men 18 - 50 year 1000mglday
Men over 50 year 1500mglday
Pregnant and lactating woman> 18 year: 1000mg/day

Dose of Vitamin D

Men and woman over 50 year: 800 IV (20mcg) day


Men and woman under 50 year: 400lU (lOmcg) day
Active Vitamin D is -7 Vitamin D3 (Cholicalceferal)

s\::::

Bisphosphonates
L-.". ~ ~

l' ~ Y) r s 'v,.~ -~

"C<A..
! \ I.) <.l""'O

'r~ -?t"-V4-2>~po<...toi.s

Bisphosphonates

Alendronate (Fosamax) = Increase bone mass, and reduce Non


Vertebral fracture or decrease vertebral fractures)
Etidronate (Di dronel) = Decrease vertebral fractures only
Risedronate (Actonel)
Fosavance (Alendronate + Vitamin D 2800 IU)

Mechanism

Decrease bone resorption via several mechanisms


Inhibition of the osteoclastic proton pumps necessary for dissolution of
hydroxyapatite.
Decrease osteoclastic fonnation or activation.
Increase osteoclastic apoplosis (cell death)-7Decrease resorption
Bisphosphonates act as a potent, specific inhibitor of osteoclast
mediated bone death.
Bisphosphonates arc synthetic analog of pyrophosphate that bind to the
hydroxyapatite that found in bone.

Therapeutic use

Osteoporosis Prevention
Treatment of post menopause bone loss
Treatment of osteoporosis
Treatment of Glucocorticoid induced osteoporosis
Paget's disease = Excessive activity of osteoclasts.
Metastatic bone cancer
Bisphosphonates have decreased rate of bone fracture in osteoporosis
and Paget's disease patients
Bisphosphonates have anti resorptive activity.
Risedronate has highest anti resorptive activity and than alendronate.
Etidronate has lowest anti resorptive activity

Side Effects

Di arrhea, Nausea., Altered taste, Abdominal pain, Night time leg


cramps,
Esophageal ulcers
Osteomalacia (etidronate only) (osteomalacia = softening of bones due
to vitamin D deficiency

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Dose

Alendronate
Counseling

Osteoporosis
Alendronate (Fosamax) available in a once weekly 70mg tablet
Available dosage forms: 5 mg, IOmg, 35 mg, 40 mg, 70 mg
Prevention of osteoporosis in postmenopausal women - once 5 mg
daily
Treatment of osteoporosis in women 10 mg once daily or 70 mg tablet
once weekJy
Treatment and prevention of glucocorticoid induced osteoporosis in
men and women- 5 mg once daily
Treatment of osteoporosis in men one 10 mg tablet once daily or 70 mg
once a week.
Risedronate (Actonel) = Available dosage forms: 5 mg, 35 mg,
Take first thing in the morning empty stomach
Take with plenty of water
Do not lie down for 30~45 min after medications (slay upright)
Calcium supplements should be separated by 2hours before or after

Raloxifene (Evista)
Mechanism

Selective Estrogen Receptor Modulator (SERM)


Estrogen like action on bone and lipid metabolism
Estrogen antagonist action in breast and endometrium

Therapeutic use

Prevents postmenopausal bone loss, increases bone density


approximately 3%, decrease vertebral fractures
Has estrogenic and antiestrogenic activity
It does not have effect on endometrium like tamoxifen and estrogen,
therefore may not predispose uterine cancer.
Lower cholesterol and LDL but no effect on HDL and TG .
For prevention of osteoporosis in postmenopausal

Side Effects

Increase risk of Deep vein thrombosis (DVT)


Avoid in who are pregnant and planning to become pregnant.
Aggravate hot flushes
Coadministration of cholestyramine reduces absorption up to 60%. Do
not take together.

Calcitonin salmon
Calcitonin is a hormone secreted from thyroid gland
Calcitonin hormone helps bone formation by transporting Ca from blood to bones
Mechanism: Directly effect on osteoclast and decrease bone resorption through direct effect.
Two products are available
Miacalcin
200 JU/day intranasally
Common SE is nasal irritation
Calcimar, caltine
50 - 100 JU sc/day or Q 2,.j day or 5days/wk
Not approved for osteoporosis

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Osteoporosis

Osteoporosis Tips

present~ 0 ~ ft- ~ _n

_r
rO~4~ ~
Riskfactorsofosteoporosis~ ~ost_~ ~.- ~Ot>~_-' \_- ',t:
~e!~

Bone remodeling occurs, when whi lj;h.is


Osteoporosis is caused by ~ Q... ~~ )

Androgendeficiencycause~ t\'1pDoc~~ d {~J~) ~


What is NOT risk factor ofosteroporosis ~ 0 ~ S ii:y
Recommended daily allowance of vitamin D is 7 40 0

o....~

OJ

Ff 0 I 4
Elderlymayabsorbcalciumpoorlydueto \~ ~ o....<'l'd... ~ ~~~ ~j\\I.Q \J~
Calci u~ supplement in elderly ~ C6..... (
Paget O>sease-7 D
~ -l

lh ~t- ~ c c:.....

c.c ~

_0-::\ '< .
~"- '""~ J l>'("'4l!.:. '\:)

~~

.~

V t

~
..,
(..

n.

M ~.

Abbrevation and Tenninology


Selective Estrogen Receptor Modulator
Low Densitv Liooorotein
Hi gh Densitv Liooorotein

SERM

LDL

HOL
TO
OVT

Deep Vein Thrombos is

Generic and Brand


Raloxifene
Alendronate
Etidronate
Risedronate
Fosavance

s-J 1~ '" Ptr'-'"-~~


U,"\

t. O<;.IAY;

Evista
Fosamax
Didronel
Actonel
Alendronate

-')

--:::,

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Asthma and COPO

32

Asthma and COPD


~lr1~~~\~GC==J~~=r~~
OI(~'==~--~==~__~

Bronchodilators

Methyl
xanthene

Mast cell
stabilizers

Aerosol
corticos-

teroids
'5t \. yo d.
~--:-::-:-~~/ a. V., La:

~eophylli.ne

Fluticasone
Beclamethasone

antagonist

Ipratropium .-Tiotropium (Spirival..

PR~r'-I-----"';;;=;-----J

Leukotriene
receptors
antagonist
Inhibitory
of5-lipo /

'" Cromolyn sodium


Nedocromi l

Ammophyll~

rM-u-sc-ar-;--'n-;c'

I Leukoteine antagon ists

~2-adrenergic

agonist

Anti-inflammatory drugs

ox~enas~
enZ)'

2...~ l( S
()\.os.~

\0'0

Ii

Zafirlukast
Montelukast

I z;yu~
,

S~>-t

:,nort actmg
Albuterol (salbutamol)
Isoproterenol
Isoetharine
Metaprotereno]
T

Long acting
Fonneterol
Salmeterol

Asthma Triggers (factors that increase risk of asthma)

~Tj]jrigi9giOi.rs"---------------lN~,,\vvrtlt< ~ CO P D
Early asthmatic response- Symptoms only (i.e., bronchoconstriction)
Cold ai r
Exercise
Emotional stress
Late asthmatic response- Worsening asth ma
Allcrgens (Pollens. cockroach, molds, animal dandur)
Respiratory viruses
Occupational chemicals
Drugs - ASA, NSAIDs
Food additives - sulfites, tartrazine
Air pollution (including cigarette smoke)

GERD
Sinusitis

Treatment for chronic asthma

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Asthma and COPD

Beta? agonist drugs


Be~Agonist

Short acting beta., agonist (SABA)


Albuterol (S-albutamol)
Terbutaline
\,..,...
1.
Metaproterenol
~.. \ ~ Co...~
Pirbuterol
C
~ acting bet~ agonist (LABA)

~ ~~

c.....tto

~'--'
Q(5

c::::::

-.

Salmeterol
""~
Fonnoterol (short ~ I- 3 min and long duration 12 hours)

Mechanism

Bronchodilation
Vasodilatation
Slightly decrease peripheral resistance
Increase muscle and liver glycogenolysis
Relax uterine muscles
Increase release of glucagon

Therapeutic use

Treat Asthma

Short acting beta 2 agonist:


Albuterol, terbutaline,
pirbuterol

Rapid onset of action and provide relief for 4 to 6 hours.


Indicated in symptomatic treatments, rescue agents, combat
acute bronchoconstriction
Albuterol, terbutaline, pirbuterol has little alpha-I and beta -I
effects.
Does not effect by COMT enzymes because these are acti vated
by non COMT
Inhalation route has less toxic side effects than systemic routes.
Have less tachycardia, hyperglycemia, and hypokalemia effects
with inhalations routes.
Short acting are best reserved for treatment of acute
exacerbations and prophylaxis o f exercise induce asthma (EIA)

Long acting bela 2 agonist:


Salmeterol

Salmeterol has long duration of action, providing bronchodilation


for at least 12 hours, and slow onset of action.
Indicated in maintenance treatment in combination with
corticosteroids especially for nocturnal asthma, EIA, and COPD
Not indicated in acute asthmatic attacks

SE

Tremors (shaking) ~ due to effect on bet~ receptors of muscles


Cardiovascular SE (tachycardia, palpitation) due to effect on
Beta I receptors

Salbutamol (Ventolin)
Mechanism

Sympathomimetic bronchodilator that relaxes the muscle surrounding


the bronchioles

Therapeutic use

Relieve symptoms of Asthma, chronic bronchitis and emphysema.

Side effects

Fine tremor of the hands


Anxiety, tension restlessness

Recommendation

Inhalation is considered more effective because drug is delivered


directly to the bronchioles

Contraindication

Caution in diabetes, Hyperparathyroidism, CV disorders

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Asthma and COPD

Onset ofbronchodi lation

10-20 minutes

Duration of
bronchodilation

4-5 hours

Salmeterol (Serevent)
Mechanism

A Sympathomimetic Bronchodilator, And Relaxes The Muscle


Surrounding The Airways In The Lungs But Because It Has A
Slow Onset Of Effect, It Is Not Used For Immediate Relief Of
Symptoms Of Asthma.
It Has Longest Duration OfBronchodiiation

Therapeutic use

Indicated In COPD And Emphysema


Prevention Of oClumal Asthma
Prevention Of Exercise Induced Asthma

Side effects

Dry And Irritated Nose, Throat (Inhalations), Tremors,


Nervousness, Cough Wheezing

Drug-drug intemclion

There is an increase risk of low blood potassium levels when high


doses of salmeterol are taken with corticosteroids, Theophylline
And Diuretics

Metaproterenol (Alupent)
Mechanism

Produces dilatation of the bronchioles and improved airway funct ion

Therapeutic use

Asthma
5-10 Minutes

Onset of
bronchodilation
Duration of action

4-5 Hours

Terbutaline (Bricanyl)
Mechanism

A sympathomimetic bronchodilator that dilates the small ain'lays of the


lungs

Therapeutic use

Treatment and prevention of the bronchospasm occurring with asthma,


chronic bronchitis, and emphysema
Bronchodi lator and reduce uterine contractions in premature labor.

Side effects

Muscle tremor, especially of the hands


Nervousness and restlessness

Drug-drug
. interaction

Administered subcutaneously and orally.


Terbutaline may intemct with MAOIs to cause a dangerous rise in
blood pressure

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Asthma and COPD

Corticosteroids
Corticosteroids

Mechanism

Therapeutic use

Side effects

Recommendation
Combination
products

Prednisone - PO, Prednisolone PO,


Beclomethasone
Budesonide
Fluticasone
Triamcilone
Steroids have no effect on the airway smooth muscles; rather decrease
the number and activity of cells involved in airway inflammation.
(Macrophage, eosinophiis, and T-Iymphocytes).
Prolonged use for several months reduces the hyperresponsiveness of
smooth muscles.
Antiinflammatory response reduced by reversal of mucosal edema
Asthma
Allergic rhinitis
lnhaled glucocorticosteroid are the drug of choice in moderate to
severe asthma that req uires bet~ agonist more than once daily.
Inhaled corticosteroids are deposited in the airway and mouth
Severe asthma systemic glucocorticoids (short time use only)
Glucocorticoids most effe ctive when taken conti nuous
Oral thrush (candidiasis): Can be reduced by rinsing mouth or using
spacer
Spacers: reduces systemic side effects and reduces thrush.
Nasal sprays : systemic absorption is minimal and side effects are
localized nasal irritation, nosebleed, sore throat, rarely cand idiasis
To red uce corticoids side effects rinse and gargle mouth after inhalations.
Adviar = Salmeterol (LABA) + Fluticasone (steroid)
Symbicort = Formeterol (LABA) + Budesanoide

PrednisoneJPrednisolone (Inflamase)
Mechanism
Therapeutic use
Side effects
Drug-Drug interaction
Recommendation

Predn isolone is the active form of Prednisone, is a powerful


corticosteroid
Skin diseases, rheumatic disorders, and certain blood disorders.
Long term treatment with high doses can cause fl uid retention,
indigestion, diabetes, hypertension and acne.
It may increase the adverse effects of Diuretics
Prolonged systemic use can lead to such adverse effects as diabetes,
glaucoma, cataracts, and fragile bones, and may retard growth in
children.
Dosages are usually tailored to min imize these effects.

Fluticasone (Flovent)
Mechani sm

A corticosteroid drug used to control inflam mation in asthma and


allergic rhinitis.

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Asthma and COPD

Mechanism

It does not produce relief immediately, so it is important to take it


regularly.

Therapeutic use

Prevent asthma attack (by inhaler)


Prevent allergic rhinitis

Side effects

Fungal infection causing irritation of the mouth and throat (inhaled


form)
To minimize side effects thorough rinsing the mouth ang gargling with
water after inhalation is recommended

Monitoring

Periodic checks of adrenal funct ions may be required if large doses are
being taken.

Budesonide (Pulmicort, Rhinocort)


Mechanism

A corticoisteroid in a form of slow release capsule that reduces


inflammation of whether nose, lungs, or intestines

Therapeutic use

Prevent attacks of asthma but not stop an existing attack.


Enema to treat ulcerative colitis
Rel ieve symptoms ofCrohn's disease

Side effects

Fewer and less serious side effects

Drug-Drug
interaction

Ketoconazole and other azole antifungals can increase the blood level
of oral Budesonide.

Monitoring

When taking in a large dose, period ic checks may be needed to insure


the adrenal glands are working properly
Chi ldren inhalers may have their growth (height) monitored regularly.

Beclomethasone (Qvar)
Mechanism

A corticosteroids that controls nasal symptoms by reducing


inflammation and mucus production in the nose.

Therapeutic use

Relieve the symptoms of allergic rhinitis and to control asthma


Helps to reduce symptoms such as wheezing and coughing
Given to people whose asthma is not responding to bronchodi lators
alone.

Side effects

Fungal infections causing irritation of the mouth and throat (inhalers)

Recommendation

Rinse mouth and gargle with water after each inhalation.

Monitoring

When large doses are being used, periodic checks is required to ensure
that the adrenal glands are functioning healthy.

Anticholinergics
Ipratropium Bromide

Atrovem

Mechanism

An anticholinergic bronchodi lator that relaxes the muscles surrounding the


bronchioles. Has longer effect but slower onset.

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Therapeutic use

Maintenance treatment of reversible ainvay disorders, particularly Chronic


Bronchitis
Runny nose due to allergy (nasal spray)
T he drug of cho ice for COPD

Side effects

Anticholinergic s ide effects


Has rare side effects

Onset of effect

515 minutes

Duration of action

8 hours

Tiotropi um (Spiriva)

Long acting muscarinic blocker


Administered by special devise handihaler
Available as capsule

Combivent

Ipratropium bromide + Salbutamol (MO l) and Nebul izers

All MDI

Should shake before use

Leukotriene inhibitors
Zafirlukast
Mechanism

Leukotriene inhibitors
Inhibitors ofLTC 4 and LTD4 receptors
Steroid sparing properties

Therapeutic use

Have anti-inflammatory and bronchodilator activity


Reduce bronchospasm and associated symptoms that are mediated
through leukotrienes.
Used fo r exercise induced asthma
DOC for aspirin induced asthma

Side effects

Sudden withdrawal of corticosteroid patient taking Zafirlukast


precipitated ChurgStrauss syndrome (Severe asthma with increase
eosinophil count in blood).
Vasculitis angiitis: A patchy inflammation of the walls of small blood
vessels

Drug.Food
interaction

Zafirlukast-Food reduces bioavailability take I hour before or 2 after


meals
Take empty stomach
Oral tablets
Used in 12 year or Over 12 year old only

Montelukast

Singulair
Chewable tablets and G ranules

Mechanism

Inhibitors of LTC 4 and LTD4 receptors

Therapeutic use

Have antiinflammatory and bronchodilator activity


Reduce bronchospasm and associated symptoms that are mediated
through leukotrienes.
Used in Exercise induced asthma

Side effects

Headache
Nausea and diarrhea
Abdominal pain

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Asthma and COPD

Drug-Food
interaction

Montelukast may be taken without regard to food.


Chewable tablet
Powder
Over 2 year old can be used

Theophylline and Aminophylline


Mechanism

(A minophylline will breaks down to Theophylline in the body)


Induce phosphodiesterase (POE) inhibition
Alter intracellular calcium
Adenosine antagonisms
Increase circulating catecholamines

Therapeutic use

Antiinflammatory action
Chronic asthma----mainly decreases symptoms
Bronchitis and emphysema
Use as a preventive measure, and is added to standard therapy

Side Effects

GI effects -7 Nausea, vomiting, abdominal cramps, Diarrhea,


headache,
CVS -7 Palpitation
CNS effects -7 Insomnia, seizures, dizziness, nervousness, restlessness
Overdose causes seizures, and arrhythmias.
Dosage should be adjusted based on serum levels
Sustain release theophyllines allow for a longer dosing interval and
improve compliance. Compliance to oral theophylline also may better
than that inhaled bronchodilators and corticosteroids
Oral therapy: Sustained released theophylline allows for longer dosing
interval and improve compliance

Recommendation

Monitoring

Factors that alter


theophylline
clearance

-.

Periodic checks on blood levels are requires especially the Serum level
Theophyllines are contraindicated in patients with hypersensitivity to
xanthine compounds.
Cuation in patient with peptic ulcers and seizure diseases
Increase theophylline clearance (decrease levels): age: 1-9 years, '::,
High protein diet, smoking (tobacco, Qlarijuana), fever, drugs such as
carbamazepine, Phenobarbital, phenytoin and nfampl~
.
Decrease theophylline clearance (Increase levels): Age (elderly,
infants, under 6 months age, premature neonates), CHF, Fatty food,
High carbohydrated diet, Liver dysfunction and Drugs such as: Oral
contraceptives, Non selective beta blockers, CCBs, Macrolide antibiotics,
Clindamycin, Zafirlukast, Allopurinol.

~obllr1J

tartmmillipirle
RrtamplCln

cyt:losporin

l'

Theophylline

ke:Dc~naztll
~,~

smoking

U
phenytoin
anbcoagulam

~~~nitidlne

ropilll'(Jloi

"

ftuconilzol
obesity
lmonary aedema

COf'

allopurinol
uncosul'llic drugs
Erylhromyt:in

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Asthma and COPD

Cromolyn and nedocromil


Mechanism
Therapeutic use

Side Effects

Mast cell inhibitors


Has Anti-inflammatory Action
Effective in prophylactic, has anti-inflammatory effect.
Not used in acute asthmatic attacks
Cromolyn administered by inhalation of micro fine powder or as an
aerosol solution.
Cromolyn poor absorption causes more side effect that can be reduced
by powder or aerosol formulations .
Internasal cromolyn reduces allergic rhinitis symptoms
Bitter taste
lrritation of nasal mucosa, pharynx, larynx

Chronic Obstructive Pulmonary Diseases (COPD)


CO PD : Chronic Obstructive Pulmonary Di seases; COPD is due to chronic obstruction in airway
passage. COPD is two types:

Emphysema (high altitude sickness)


Chroni c bronchitis .

EMPHYSEMA is a disease in which the small air exchange sacs (alveoli) in the lungs become
permanently enlarged and damaged (alveoli walls destroyed) decreas ing oxygen absorption and
resulting in shortness of breathe.
CHRONIC BRONCfITTIS is an inflammation of the airways in the lungs that causes your lungs to
produce excessive amounts of mucus (phlegm). This reduces the flow of air to the lungs .
Onset age 45 years
Risk Factors that Cause COPD
Smoking (8090%)
Family History
Occupational exposures to ceI1ain ducts and fumes
Air Pollution
Second Hand Smoke
Asthma
Drug used for the treatment of CO PO

Beta adrenergic agonists


COI1icosteroids
Ipratropium (Atrovent)
Theophylline

Asthma and COPD Tips

PDt:.
Theophylline inhibit activity of -7
Leukotrienes are chemical derivatives of -7

""L,,<J::;;:;

!\ y<>--.i.; JO",I'C

AuJ

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Asthma and COPD

Leukotrienes are produced from arachidonic acid by catalization of-7

Long te,nn use

l~ t 01-\..\ O~ t:..4 ~

ofor~l corticosteroi~may cause -7 0 c:;i:Q.~ ~orc..._'i~S ) U ~,,~ ) c:\....~_ '\ \...\Q~""

Leukotnene antagonist act on -7 L: \ <=- '-1 L T () ~


- - ~y d"DOC for aspirin induced asthma -7

Patient has COPD and pneumonia, what is DOC -7 O()"'\'\'0 ~~: -4 0'- "2...~ ~'( v \0....."" "KOral contraceptive effect on theophylline -7
l-.Q.~.J~
Dry cough is caused by accumulation of -7 ~T ......J,.qk\'" 1l-\3
What is differentiating symptoms of-asthma from CO'P'D -7
'.J ~<....t. L.. J;
Smoking is very high risk factor for -7 COPD
U
What asthma devices do not require shaking 7, 1I \ c:;, I< ~ ~ '\::"''':r
~ 0
Polycythemia -7
R. I!>c-'> ll..,,,,,,boV, ~ OL str.,.Q,(
<..
~
Asthma exacerbations are NOT triggered by~ H
1\ t....Y' ~
Q..
Obstruction of airways in lungs is referred as~ \'ry <;. ~
Pennanent enlargement of alveoli is referred as ~ Q...."-. P\..Q ~
Highest clearance of theophylline in which Me $fouP~rt l ~ q 'f r $
When can we use leukotriene inhibitors ~ '" '!Il::-QY'O\Q d.o~
What is important to counsel in patient using steroid inhalers ~ 'c
So--e....
Histamines are released from ~ ""o...~ ~
ba..\o~~,~What kinds of changes can you expect to see in aminophylline solutions exposed to air? ~ C \'\l~ 3u~

Uq:

l'

b _) l . . . t

l'

crt

\th

Abbrevation and Tenninology


ASA
NSAlDS
SABA
LABA

COMT
EIA

CO PO
CHF
CCB

Acetyl Saliay late


Non-Steroidal Anti-infl ammatorv Drue:s
Short Actinp Beta Aponist
Lam)" Actinp Beta Ap"onist
Catechol -0 -meth I transferase
Exercise Jnduce Asthma
Chronic Obstructive Pulmonarv Diseases
Coneestive Heart Failure
Calcium Channel Blocker

Generic and Brand


Salbutamol
Salneterol
Meta roterenol
Terbutaline
Prednisone!Prednisolone
Fluticasone
Budesonide
Beclomethasone

Ventolin
Advir, Serevent
Alupent
Brenthin Bricanv l
Inflamase Pedia ril Win red
Flonase Flovent
Entocort Pulmicort Rhinocort Rh inocortA ua
Ati-Beclomethasone var Rivanase A

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Anticancer Drugs and Chemotherapy

33

Anticancer Drugs and Chemotherapy


Classification of Anticancer drugs

Action of DNA

Damage DNA

I
I

Alkylation:
Mechlorethamine
Cyclophosphamide
Ifosfamide
Chlorambucil
Melphalan
Busulfan
Lomustine
Cannustine
Streptozolin
Cisplatin
Carboplatin
Dacarbazine
Procarbazine
Altretaminel
Hexamelhylmelamine
Mitomycin

Others
Actinomycin 0
Etoposide
Teniposide
Amsacrine

I Free
radicals: I
Bleomycin

Inhibit
synthesis or
functions

A,,~ b;~IC

Topoisomerase
inhibitors
Doxorubicin
Daunorubicin
Topotecan
lrinotecan

I
Antimetabolites
5f1uorouracil
Cytarabine
Mercaptopurine
Thioguanine-Thioguanine
Methotrexate

Action on steroid
Hormones

Agonists
Androgens
Estrogens
Progestins
Lcuprotide
Goscrclin
Narfarclin

Atagonist
Tamoxifen
Toremifcnc
Flutamide
Anastrozole
Letrozole

Cancer estimated
deaths in men

Lung cancer 3 I% - ' " " " -..,>j(


Prostate cancer 1I %

Cancer estimated
deaths in women

Lung cancer 25%


Breast cancer 15%

Warning signs of
cancers

C- change in bowel o r bladder habits


A a sore that does not heal
u- unusual bleeding o r discharge
T T hickening or lump in breast
1--- Indigestion or difficult in swallowing
0- Obvious change in wart or mole
N.----- Nagging cough or hoarseness

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Cell Cycle Phases

Anticancer Drugs and Chemotherapy


All cells must traverse the cell cycle phases before and during cell divis ion.
Anticancer drugs may act on specific phase. Tumor cells are more
responsive to specific drugs
Go phase - Resting phase
G l phase - Synthesi s of enzymes needed for DNA synthesis
S phase - DNA replication (DNA synthesis)
G 2 phase - Synthesis of components needed for mitosis.
M phase - Mitotic tubule form ation 7 Vincristine and vinblastine

Cell cycle phase


specific drugs

Cell cycle specific


drug (phase-non
specific)
Cell cycle non
specific agents

More active against cells that are specific phase of cycle:


G-1 phase7 L-aspraginase and prednisone
S phase7 Methotrexate, 6-thioguanine, cytarabine
G2 specific7 Bleomycin and etoposide
M phase ~ Vincristine and vinblastine, peclitaxol
Alkylating agents, Antitumor antibiotic, Cisplatin

Effective whether cancer cells are in cycle or resting


nitrosoureas, mechlorethanime
AJ : mitotic
phase where
cell divides

G1 : synthesis of
cellular componenlS
required for mitosis

I s:replicated
DNA is

phase ~

radiation,

G,: resting
state where cell
is not dividing

h/1

G/ : synthesis
of ellZ)mes
necds for DNA
smthesis

~
~

Class

Examples

Mechanisms

Alkylator and alkyl atorlike drugs

Melphalan, Chlorambucil,
Cisplatin, Carmustine

Covalent bonds break with DNA


bases; strand breaks

Antimetabolites

Fl uoroucil, Methotrexate
cytarabine, Mercaptopurine
fludarabine

Inhibit DNA synthesis by inhibiting


enzymes or incorporating into DNA
and RNA.

Antibiotics

Doxorubin, Bleomycin,
Mitomyci n C, Dacti nomycin

Intercalate DNA strands and


produce oxygen free radicals

Mitotic inhibitors

Vincristine, Vinblastine,
Paclitaxel . Docetaxel

Vi nca's inhibit microtubule


formation
Taxanes stabilize microtubules so
can' t rearrange

Topoisomerase
inh ibitors

Etoposide, lrinotecan, Topotecan

Inhi bit unwinding and winding of


double helix; can 't form or repair
DNA

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Anticancer Drugs and Chemotherapy

Alopecia is a counseling issue! The extent of hair loss varies, but is usually starts at 2-4 weeks and
is reversible when the drugs are discontinued. Doxorubicin and paclitaxel tend to cause the most
alopecia, but it is common with most combination regimens. Patients may wear wigs, hats, or may
just go bald.
Neurotoxicity: Vincristine has as its dose-limiting toxicity autonomic dysfunction and peripheral
neuropathy, both sensory and motor.
Pulmonary toxicity; Bleomycin causes a generally irreversible pulmonary fibrosis at higher lifetime
doses.

Clophosphamide (Cytoxan)
Mechanism

An Alkylating agent use to treat cancer.

Therapeutic use

Lymphomas (lymph gland cancers)


Leukemia
Solid tumors (breast and lung)
Also use for autoimmunediseases

Side Effects

Nausea, vomiting, and hair loss


Irregular menstruation
Can affect heart, lungs, and liver (acute hemorrhagic cystitis)
Bladder damage in susceptible people

Drug-Drug
interaction

Phenytoin can increase the breakdown of cyclophosphamide


Allopurinol and phenothiazines can inhibit breakdown of
cyclophosphamide.

Contraindication
Monitoring

Not advisable for pregnant and lactating mothers.


Periodic checks on blood composition and on all effects of the drug are
usual ly required.

Mercaptopurine, 6-MP (Purinethol)


Mechanism

Inhibits purine synthesis


Analog of hypoxanthine
Structurally similar to allopurinol (purines)
Azathioprine an immunosuppressant exert effect after converting 6-MP.
Causes RNA and DNA dysfunction

Side effects

GI ., Nausea, vomiting, diarrhea


Bone marrow depression
Hepatotoxicity

Doxorubicin (Adriamycin)
Mechanism

Effect maximal at Sand 02 phase


Anticancer antibiotics

Therapeutic use

Widely used anticancer drug (breast, lung etc)

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Anticancer Drugs and Chemotherapy

Side effects

Irreversible cardiotoxicity
Myelosuppression
Stomatitis
Alopecia
Nausea and vom iting

Compounding

Should be carried in Vertical laminar air flow hood

Dactinomycin (Cosmegen)
Mechanism

Anticancer antibiotics
Form stable DNA complex and interfere with DNA dependent RNA polymerase

Side effects

Major dose lim iting toxicity-bone marrow depression.

Mechlorethamine (Mustargen)
Mechanism

Alkylating agent

Therapeutic use

Primarily used in Hodgkin's disease (malignant disease of lymphatic tissue) as


part ofMOPP regimen (Mechlorethamine, Oncovin, Prednisone, Procarbazine)

Side effects

Severe nausea and vomiting


Sever bone marrow depression
Myelosuppression
Anorexia
Gonadal dysfunctionz

Vincristine and vinblastine


Mechanism

Mitotic spindle is part of cytoskeleton and essential for internal movement


occurring in the cytoplasm of all eukaryocytic.cells.
Mitotic spindle is essential for partition ing two DNA daughter cells.

Side effects

Myelosuppression
Paralytic ileus
Alopecia
Stomatitis

Paclitaxel (Taxol)
Mechanism

Reversible microtubule inhibitor.


Obtained from Yew plants (from Himalayas)

Side effects

Serious hypersensitivity reaction,


Patient should be premedicated with dexamethasone and
diphenhydramine as well as H2 blockers.
Myelosuppression
Peripheral neuropathy
Alopecia
Mucositis

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Anticancer Drugs and Chemotherapy


Anaphylaxis
Dyspnea

Chemotherapy

c9.J

The treatment of cancer with drugs is called chemotherapy. Antineoplastic drugs, also referred to as
chemotherapeutic agents, are drugs that are used to treat cancer.
Side effects of chemotherapy:
Acute:
Extravasation (effects the adjacent tissue)
Vessicant drugs (damage to tissue / necrosis) Example: Bleomycin, cisplatin,
dactinomycin, domorubicin, vincri stine, vinblastin etc.
Thrombophlebitis (inflammation associated with thrombus): Patient with cancer can
develop thrombosis after chemotherapy. Due to activation of fibrinogen.
Hypersensitive reactions. Example: Etopisi de, peclitaxol, ritux.imab, trastuzumab.
Rapid tumor lysis syndrome
Nausea and vomiting

Chronic, organ s pecific:


Skin ~ alopecia,

dry skin, riail changes, pigmentation (melanoma), Xerostomia

Alopecia is the loss of hair: Drug that cause alopecia is doxorubicin, daunorubicin,
cyclophosphamide, vincristine, and paclitaxel.
Vessicant agents include: dactinomycin, doxorubicin, mechlorethamine, mitomycin, vincristine, and
vinblastine.
Hair regrowth occurs after \-2 months after stopping chemotherapy.
Xerostomia: Dry mouth is one of the most common complication associated with radiation therapy.
Reversible after 6-12 months of therapy.
Can be managed by: Sugar free hard candy, chewing sugar free gum stimulate salivation.
Commercially available saliva substitute. Ice chi ps . Cholinergic agonist ~ Pilocarpine Smg tab.
Bone marrow depression (Myelosuppression):
Bone marrow depression ~ Neutropenia, Thrombocytopenia
Neutropenia 7 treated by colony stimulating factors (O-CSF and OM - CSF): Filgrastim or
pegfiJgrastim
Thrombocytopenia ~ for prevention use Oprelvekin (Inerleukin-ll)
Complications: Bone marrow suppression is the most dose limiting side effect of cancer
Myelosuppression in general the onset is 7 ~ 10 days and peak is I 0 ~ 14 days. Recovery count
occurs usually occurs in 2 ~ 3 weeks.
Megaloblastic anemia by methotrexate ~ Fo l inic acid (leucovorin, 5-fonnyltetrahydrofolic acid)
Neutropenia associated anticancer drugs ~ can be treated by filgrastim (human granulocyte
colony stimulating factor)
Least bone marrow depression anticancer drugs is: Bleomycin
Cancer patient with anemia -7 Erythropoeitins are useful

Cardiotoxicity:
Ri sk ofC HF, commonly seen with doxorubicin, daunorubicin. epirubicin, mitoxantrone.
5-FU, capecitabine; Cause coronary spasms, mimicking a myocardial infarction (avoid in know
coronary artery disease patients)
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Anticancer Drugs and Chemotherapy

Cardiotoxicity can prevented or lessen by using cardioprotective agent: Dexrazoxane

Pulmonary toxicity:
Pneumonitis, pulmonary fibrosis commonly seen with Bleomycin, Cannustine, Cyclophosphamide,
Mitomycin, Methotrexate, vinca alkaloids,
Symptoms of pulmonary toxicity include: SOB, non-productive cough, and rarely low grade fever.

Neurotoxicity:
Common with vincristine, vinblastine, Cytarabines, Methotrexate (very little), 5FU, interferon
alpha
Peripheral neuropathies associated with: Vincristine, peclitaxel: Peresthesia (numbness and
tingling) can occur with vincristine, which often appears within few weeks of therapy.
Hi gh dose of cytarabin may produce cerebllar toxicity that manifest initially as loss of eye-hand
coord ination and progress to coma.
Fludrabine cause severe neurotoxicity
Caramustine and other alkylating agents cause little or no neurotoxicity.

GI toxicity
Mucositis or stomatitis:
Mucositis: Generalized burning, and pain on the ventral surface of tongue. Floor of tongue, mouth
looks erythromatus.
Stomatitis: generalized inflammation of oral mucosa.
Mucositis or stomatitis: Common with Doxorubicin, Methotrexate, 5-Huorouracil, Actinomycin,
Bleomycin capecitabine.
Recommend mouth hygiene, xylocaine, viscous sucralfate, nystatin, sod ium bicarbonate, for
severe cases pelifonnin (growth factor) can be used.
Avoid alcohol, antihitamine, steroids, spicy food
Mucositis treatment and prevention:
Topical anesthetics: Viscous Lidocaine, or dyclonineHCL 0.5 or 1%
Corticosteroid provide anti-inflammatory action
Capscisin: Produces burning and pain and ultimately desensitizes pain.
Sucralfate suspens ion may provide benefit by coating.
-For Localized effect: use benzocain in orabase
Mucositis prevention:
Chlorhexidine gluconate 0.12% (peridex, Periogard) may reduce severity and frequency
of mucositis infections.

Nausea and vomitinga


Very high emetics anticancer drugs
Cisplatin
Streptozocin
Cyclophosphamide
High emetics anticancer drugs
Doxorubicin
Methotrexate (250 mg to 1000mg)
Cytarabine
Lowest emetic anticancer drugs
Bleomyc in
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Anticancer Drugs and Chemotherapy

Methotrexate (under 50 mg)


Vincristine
Vinblastine
Tamoxifen
Management of Nausea and vomiting associated with cancer chemotherapy:
Lowest emitogenic drugs Nausea and vomiting can be treated by 7 Metoclopramide
High and very high emitogenic drugs associated Acute: nausea and vomiting can be treated bY7
Dexamethasone
DOC for delayed nausea and vomiting 7 Dexamethasone

Hepatotoxicity
Hepatotoxicity monitor LFT, jaundice, or hepatitis: Asparaginase, cytarabine, mercaptopurine, and
methotrexate.

Nephropathy:
_

Elevate BUN and electrolyte abnonnalities: methotrexate may precipitate in kidney. Cisplatin and
streptozocin. Amifostine..may be used to protect the kidney from the...nephrotoxicity associated
with cisplatin.

Sexual dysfunction:
Cyclophosphamide, melphalan, and procarbazine associated with significant infertility in men and
women.

Hemorrhagic cystitis G-It is a bladder toxicity that is seen most commonly after administration of cyclophosphamide and
ifosfamide.
These drugs produce a metabolite called acrolein, w~ ich cr u ~e chemical irritation in bladder
mucosa, resulting in bleeding.
\.--"J b~
Hemorrhagic cystitis caused by Acrolein can be prevented by excessive hydration and subsequent
frequent urination. The other method is by administering uroprotecting agent called MESNA,
which bind acroleine and prevent from contacting the bladder mucosa.

Pulmonary toxicities:
The most common with bleomycin, mitomycin, cannustine
Rationale for combination therapy: Overcoming or preventing resistance, Cytotoxicity to resting and
dividing cells' Biochemical enhancement of effect. Beneficial drug interactions' Rescue host cells
Some agents can be administered intrathecally: Methotrexate, Cytarabine' Thiotepa
Warning: Vincristine should be labelled as Intravenous only. Intrathecally vincristine causes death.

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Anticancer drugs Tips

'S\.(~~

Melonoma is ?
r
Metoc!opramide and dexamethaso,(lc are more effective Rausea r~lated, to ? e.o
~ ~ "
Methotrexate is used for ?
t\ 1 c........ ~) ,~S uT , c... S. i .s
f
Which anticancer d..(ugs cause pulIl,lonary fibrosis~ ~~:..- ~ u:J.....-4Il _ ~ 0 . f\
Hypenropy is -7
L.Q.~'"'~ ~~SI:;"'O -. r --::;~
Hyperplasia is -7 l'
'#-_
~
.
J ,,--, \.0 .....
Least emetic anticancer drug is ~ l'
0.' {o.......... I:l~
Cancer patient on cancer fihemotherapy, reports shortness of breath, non productive cough, she
may be using drug ~ b~
DOC for delayed Nausea and vomiting ~
Mesna is ~
Doxorubicin preparation should be perfonned in ~
Hypertrepy-is -7
1iyperpIasia..i.s ~
Melatonin ~
Peclitaxel and docetaxel act on ~

c..

fl.--

'l'''''-U s,

<..o..U...

e, . .

'0" ,"-

Abbrevation and Tenninology


MOPP
GM

Mechlorethamine Oncovin Prednisone Procarbazine

CSF
LFT
MESNA

Li ver Funtion Test

Generic and Brand


Mel halan
Chlorambucil
Cisolati n
Cannustine
Fluoroueil
Methotrexate
Cvtarabine
Fludarabine
Bleomycin
Mitomycin C
Vincristine
Vinblastine
Docetaxel
Etoposide
lrinotecan
TODQtecan
Vincristine
Cyclophosphamide
Mercaptopurine 6-MP
Doxorubicin
Dacti nomvcin
Mechlorethamine
Pac1itaxel

Alkeran
Leukeran
Platinol
BiCNU
Adruc il Carae Efudex Fluoronlex
Rheumatrex TrexaJl
Cvtosar
Fludara
Btenoxane
Mitozytrex Mutamycin
Oncovin Yincasar PFS
Velban
TaxotereT
Etopophos Toposar VePesid
Camotosar
Hvcamtin
Oncovin
Cytoxan Procytox
Purinethol
Adriamycin Rubex
Cosmegen
Mustargen
Taxol

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Gastrointestinal Drugs

34

Gastrointestinal Dru s
GERD
Mild GERD, relief of symptoms is with antacids, algi nates or non-prescription strength H1 RA.
Severe GERD: PPI are the Drug of choice. Use PPJ for 2 - 4 weeks
The goal is to raise the intragastric pH 4 during periods when reflux is likely to occur.
peptic ulcer.;
Gastric ulcers - Due to reflux since has weak pyloric sphincter
Duodenal ulcers - Excessive secretion from parietal cells
Acute stress ulcers (Curling's ulcer) - Tumors
Pathologic acid-hypersecretory states (Zollinger- Ellison syndrome)
Treatment of peptic ulcers
Neutralization of gastric acid a Antacids
Reduction of gastric secretion a H. antagonist, Proton Pump Inhibitors (PP I)
Cytoprotection a Sucralfate
Eradication of Helicobacter pyloria 2 Antibiotics + PPJ (triple therapy)
To eradicate H. pylori
Triple therapy: 2 antibiotics + 1 PPJ
Losee 1-2-3 A: Amoxicillin + Clarithromycin + Omeprazole
Losee 1-2-3 M: Metronidazole + Clarithromycin + Omeprazole
Quadruple therapy: Tetracycline+ Metronidazole + Bismuth subsalicylate + Omeprazole

Antacids
Antacids are used to treat stomach upset, acid indigestion (heartburn) and sometimes ulcers. They
are simple chemical compounds that are mildly alkaline, and some also act as chemical buffers. They
act by neutralizing stomach and coating the mucosal lining of the stomach. Simethicone is an agent
added to antacids that helps relieve gas.
Types of antacids

.
.

Aluminum
compounds

Aluminum compounds, Magnesium compounds, Combined


preparations
(e.g. Aluminum hydroxide, Calcium carbonate, Mg hydroxide, Mg
trisilicate, Na carbonate). Antifoaming agent (Simethicone)

Has prolonged action and widely used especially for the treatment of
indigestion and dyspepsia.
Side effects: constipation.

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Mg bicarbonate

Has prolonged action.


Side effects: in large doses they cause diarrhea
In patient with impaired kidney function, a high blood Mg level may build
up causing weakness, lethargy, and drowsiness.

Na bicarbonate

The only sodium compound used as antacid


Acts quickly but its effect soon passes.
It reacts with stomach acids to produce gas, which cause bloating and
belching
Recommendation: not advisable to patients with kidney disease, as it
can lead to water accumulation (edema) in the legs, and lungs, or serious
changes in acid-base balance in blood .

Combined
preparations

Antacids combined with Alginates or anti foaming agents.


ALGINATES are intended to float on the content oflhe stomach to
produce a neutralizing layer to subdue acid that can otherwise rise into
esophagus, causing heartburn.
ANTIFOAMING agents are intended to relieve flatulence

Calcium Carbonate

Constipation

Drug interactions with Antacids:


Tetracyclins: Tetracyclin binds with bi and trivalent ions, thereby this can reduce absorption of
tetracyclins.
Ketoconazole: The antifungal ketoconazole require acidic medium for absorption. Concomitant use
of antacids can reduce absorption ofketoconazole.

H?receptor antagonists
A,"

_r_

Gastrin

Histamine
AUOPine

M~receptor

Cimetidine
H , receptor

H2-receptor antagonists inhibit the action of a special type of histamine receptor present in the
stomach. Th is reduces the amount of gastric acid production, which helps heal ulcers.
H2 receptor
antagonists

Cimetidine (Tagamet)
Ranitidine (Zantac)
Famotidine (pepcid)
N izatidine (Axid)
Acid must be produced to digest protein
Gastric acid secretion is controlled by histamine from enterochromaffin-like
cells, acetylcholine neurons and gastrin-G cells in the antrum

Therapeutic use

90% reduction in acid secretion


Useful in promoting healing of gastric ulcers
Preventing reoccurrence of ulcers
Management of Zollinger-Ellison syndrome
Gastric hypersecretory states in systemic mastocytosis which is a rare
disorder with increase number of mast cells systematically and in skin

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Gastrointestinal Drugs

Side effects

Gynecomastia - e levation of prolactin (cimetid ine)


H eadache~ - famotidine ::ind ranitidine
Hematologic abnonnalities
Decreased hepatic microsomal metabolism of some drugs like c imetidine
which dec reases the metabolism of warfarin, theophylline, diazepam and
phenytoin
Diarrhea
Constipation
Fatigue
Confusion
Cardiac effects
Diarrhea, constipation, fatigue, headache and confusion are more common
in elderly and decrease renal function patients.

Tips

Nizatidine is preferable used in elderly and renal disorder patients


Cimetidine and famotidine are now available without prescription in some
countries for the treatment of dyspepsia (2 weeks supply)

Ranitidine (Zantac)
Mechanism

Reduces the amount of stomach acid produced, allowing ulcers to


heal

Therapeutic use

Ulcers cause by H, pylori


Protect against duodenal ulcers in patients taking NSAIDs.
Reduces discomfort and ulceration of reflux esophagitis; and may
prevent gastric bleeding

Side Effects
Drug-drug
interaction

Headache; nausea and vomiting; constipation; diarrhea; jaundice

Contraindication

Avoid alcohol (may aggravate underlying condition and reduce


drugs effects)
Reduce dose to children and infants, and it may pass into beast
milk.

Advantage from
other drugs

Not like Cimetidine. it does not! blood levels of other drugs


such as anticoagulants, anti-convulsants, which might reduce the
effectiveness of treatment.

Call physician NOW

Sore throat/fever

Ranitidine may reduced the absorption of Ketoconazole


High doses (2g) of Sucralfate may reduce the absorption of
Ranitidine.

Cimetidine
Mechanism

Is an Anti-ulcer drug that reduces the secretion of gastric acid and


pepsin in the duodenum and stomach, and promotes the healing of
ulcers.

Therapeutic use

Treat stomach and duodenal ulcers


Used for reflux esophagitis

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Gastrointestinal Drugs

Side Effects

Diarrhea
Dizziness

Drug-Drug
interaction

Increases the e ffects of anticoagulants. Inhibit CYP 3A4 metabolism,


thereby inhibit metabolism of warfarin, phenytoin, theophylline .

Contraindication

Discuss with physician about using the drugs for pregnant and
lactating mothers.

Mo nitori ng

It is prescribed with caution to people who are receiving


anticoagulants and anticonvulsants
This drug wi ll mask the symptoms of cancer, and delay diagnosis.

Proton pump Inhibitors


Omeprazole, esomeprazole, pantoprazo!e, lansoprazole and rabeprazoie are proton pump inhibitors,
powerful anti-ulcerogenic drugs that work by stopping the production of stomach acid completely.
Eradication of H . pylori is considered to be a major factor in the treaUTIent of duodenal ult;er disease.

PPJ

Omeprazole
Lansoprazoie
Rabeprazole
Pantoprazole

Mechanism

Irreversible inhibition of gastric parietal cell proton pump W/K+ATPase

Therapeutic use

Prevention of reoccurrence of duodenal ulcers and esophagitis


Pathology hypersecretory states
Multiple endocrine neoplasias
Healing ofNSAID induces peptic ulcers
Systemic mastocytosis
A part of the eradication of H. pylori therapy
Drug of choice for Ellison Zollinger Syndrome

Duration

Short term treatment ( 4-8 weeks)

Side effects

Abdominal pain
Diarrhea
Headache

Omeprazole (Losee)
Mechanism

It reduces (about 70%) the amount of acid produced by the stomach.

Therapeutic use

Treat peptic ulcer


Can be given w ith antibiotics to kill H. py lori (bacteria that cause gastric ulcer)

Side Effects
Drug-drug
interaction

Headache, diarrhea, nausea, and constipation


Warfarin and Phenytoin = t the effects by omeprazoie
Bl ood levels of cyclospori ne may raised by omeprazole

Contraindication

Not recommended to infants and children


Alcohol

Stop taking drug


NOW

Rash

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Gastrointestinal Drugs

Lansoprazole (Prevacid)
Mechanism
Therapeutic use

An anti-ulcer drug belongs to proton pump inhibitors group.


Peptic ulcer
Gastroesophageal reflux
Zolli nger-Ell ison syndrome (large quantities of stomach acid are
produced)

Side Effects

Headache and dizziness


Diarrhea and constipation
Flatulence/abdominal pain
No clinical interaction with Lansoprazole however this may reduce the
effects of oral contraceptives, phenytoin, carbamazepine, warfarin, and
theophylline.
Antacids and sucralfate should not to be taken within an hour with
lansoprazole (Lansoprazole wi ll reduce the absorption ofthese drugs)
Avoid alcohol
Not recommended with infants and ch ildren

Drug-drug
interaction

Contraindication

Esomeprazole (nexium)., no clinical significant interaction

Cytoprotective Agents (Mucosal Protective Sulfate)


Sucralfate binds to the ulcer site by forming a viscid sticky gel that coats the ulcer si te and acts as a
protectant.
Sucralfate

Alum inum sucrose sulfate is a Sulfated disaccharide

Mechanism

Selectively binds to necrotic ulcer tissues (Acts as a barrier to acid,


pepsin and bile)
Directly absorb bile thus has chelating property
Stimulates endogenous prostaglandin synthesis.
Stimu lates mucus secretion
Effective in the healing of duodenal ulcers
Requires acid pI-I to be activated
Reduces the number of H. pylori

Therapeutic use

Side effects

Causes constipation

Dose

Dose Ig qid

Drug interactions

Should not be administered with antacids, H2 antagonists or proton


blockers

Bismuth Compounds
Mechanism

Selectively binds to necrotic ulcer tissues


Stimulation of mucous production
Inhibition of pepsin activity

Therapeutic use

Possess anti-microbial activity against H. pylori


When combined with antibiotics like metronidazole and tetracycline has
98% healing rate for ulcer

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Gastro intestinal Drugs

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Shoul d not be given in renal disease and pregnancy

Contraindications

GI disorder Tips
Lactulose is used in what type of chronic liver disorder ~
An example of ecosanide is~
Misoprostol is ~
Type of pain in GERD is ~
Increase in bilirubin cause ~
Aluminum salts can cause SE ~
Magnesium antacids cause SE ~
H pylori will cause ~
What type of hepatitis is chronic ~
What is treatment of hepatitis ~
NSA lDs induced ulcers can be treated by ~
Independent risk factors for peptic ulcers are: H.pylori and NSAI Ds
Chronic hepatiris?
Epsom salt is?
Ul cerative colitis occurs at?
Antiftatulance agent?
What vaccine can be used for traveler 's diarrhea?
Na bicarbonate is contraindicated in-patient with hypertension, CHF, severe renal disease,
and edema. This also contraindicated in ulcers.
CaC03 antacids have rebound acidity due 10 stimulation of acid secretion.
CaCOJ antacids avoid in hypercalcemia patients .
Hypophosphetemia and osteomalacia can occur with long-tenn use of Aluminum containing
antacids.
Antacids bind with Tetracyclins, and fluroqu inolone and reduce absorption.
Antacids may destroy coating of enteric-coated drugs.
Mg antacids can cause cathartic SE.

Abbrevation and Tenninology


IBD
IBS
IFN alfa

GERD

Inflammatory Bowel Disease


Inflammatory Bowel Syndrome
Interferon alfa
Gastro Esopho eal Reflux Disease

Generic and Brand


Omeprazole
Lansoprazole
Cimetidine
Nizatidine
Ranitidine

Losee
Prevacid
Tagamet
Axid
Zantac

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Cell Wall Synthesis Inhibitors

35

Cell Wall Synthesis Inhibitors


Antibiotics classifications

I
Cell Wall synthesis
inhibitors
Peni cillins
Cephalosporins
Vancomycin

Protein Synthesis
inhibitors
Am inoglycosides
Macrol idcs
Tetracycline 's
Lincosamide

I
DN A Synthesis
inhibitors
Quinolonesl
Fluoroquinolones
Metronidazole

Folate Inhi bi tors


Su lfonamid es
Trimethoprin

Penicillins
Acid labile (ac id sensitive)
Penicillin G ......... J!-lactamasc sensitive
Methicillin ........ . ~- lactamase resistant
Nafcillin .... .. ... .... ~-lactamase resistant

Acid stable (acid resistant)


Pen ici llin V ......... ~- lactamase sensitive
Oxacillin ... .. ... .. .. ~- Iac tamase resistant
Amoxicillin .. ....... ~-lactamase sensitive
Ampici ll in . .......... ~-lactamase sensiti ve

Tips: PAPA is sensitive to beta lactamases


Beta-Lactam ase Inhibitors
Clavulanate
Sulbactam
Tazobactam
Clavulanic acid
Beta-lactamase inhibitors such as clavulanic acid can be combined with sensitive Beta-lactams to
yield an active combination with resistant organisms
Penicillins

Penicillin G
Penicill in V
Methicillin
Nafcill in
Oxacillin
Carbenicillin
Ticarcillin
Piperacillin

Aminopcnicillins

Amox icillin
Ampicillin

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Mechanism
Therapeutic uses
Side effects

Cell Wall Synthesis Inhibitors


Cell wall synthesis inhibitors
Gram + ve and Gram - ve
Hypersensitive reactions, rash,
Nausea & Vom iting,
Pseudomembranous colitis ~ diarrhea
Intestinal nephritis

Penicillins G
Mechan ism
Therapeutic uses
Side effects

Side effects
management
Drug interactions

Cell wall synthesis inhibitors


Gram

+ ve (all of them), Gram -ve for Neisseria

Hypersens itive reactions, rash,


Nausea & Vomiting
Pseudomembranous colitis ~ diarrhea
Intestinal nephritis
Take empty stomach
Interferes and alters test results for urine and serum protein levels. It
does not interfere with test using bromophenol blue.
Aminoglycoside causes synergistic effect. Most effective endocarditis
infections.

Penicillin V
Mechanism

Cell wall synthesis inhibitors

Uses

Gram + ve (all of them)


Gram - ve for Neisseria

Side Effects
SE management
Drug interactions

Hypersensitive reactions, rash,


Gl effects ~ Nausea & Vomiting, Pseudomembranous colitis
Give 1 hour before or 2 hour after meals for max absorption.
Interferes and alters test results for urine and serum protein levels. It
does not interfere with test using bromophenol blue.

Piperacillin and Carbenicillin


Therapeutic use

Gram - ve (E. coli, Enterobacter, Klebsiella, Pseudomonas.

Side Effects
Drug interaction

Used combination w ith ~- lactamase inhibitors.


Often mixed with aminoglycoside (not in same IV bag)

Amoxicillin (Amoxil)

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Cell Wall Synthesis Inhibitors

Therapeutic use

Gram + ve (mainly)
Gram - ve Ne isseria
Synergi stic effect with aminoglycoside

Side Effects

Hypersensitivity, Anaphylaxis
GI affects ~ Nausea& Vomiting, P Colitis (diarrhea).
Blood related ~
Thrombocytopenia
Leucopenia
Agranulocytosis

Drug interaction

Allopurinol-Increases rashes
Honnonal contraceptive-Decreases contraceptive effect.
Methotrexate-effects renal tubular absorption.

Ampicillin (Principen)
Clinical use

Gram + ve (mainly)
Gram -ve Neisseria

Drug interaction

Allopurinol- Increases rashes


Honnonal contraceptive-Decreases contraceptive

- Side Effects

Hypersensitivity, Anaphylaxis
Gl -7 Nausea & Vomiting, P colitis (diarrhea).
Blood related ~ Thrombocytopenia
Leukopenia
Agranulocytosis

Cephalosporins
1 a.generation

Cefazolin

Long duration of action in I $ gen.

Cephalothin
Cephalexin

Oral (DOC pharyngitis, cellul ites)

Cephapi rin

Renal and hepatic elimination


Shortest half life (0 .6 - 0.8 h)

Cephrad ine
f.Dd.generation

Ccfadroxin

Oral

Cefaclor

Oral (Associated with serum sickness)

CefamandoJe
Cefoxitin
Cefuroxime
sodium

Can cross BBB, can be used in commun ity aquired


bronchitis or pneumonia in elderly

Cefuroxime
auxetil

oral

Cefotetan
Cefproxi l

Oral

Cefonic id
Loracarbef
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Cell Wall Synthesis Inhibitors

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lni.generation
Contain
methy lthiotetrazo le
side chain. Can cause
hypoprothrombonemia
and bleeding problems

Ilh.generation

Cefixime
Cefoperazone

Oral
Hepatic elimination only

Cefotaxime

Renal and hepatic elim ination, Can penetrate in CSF.

Cefpodoxime
Ceftazidime
Ceftriaxone

Longest half life (8 hours)

Cefdinir

Oral

Ceftibuten

Oral

-+ Single dose

Cefepime

Cephalosporins _1 st Generation
I II Generation

Therapeutic use
Side effects

Dose

Cefazolin
Cephalothin
Surgical prophylaxis (best for Gram + ve)
Allergic reaction (5- 15%)
Anaphylaxis
Skin rash
Fever
Hemolytic anemia
Granulocytopenia
Local irritation at site of injection.
Seizure in high doses in IV form
IV and PO

Cephalosporins - 2nd Generation


2nd Generation

Clinical use
Side effects

Dose

Cefaclor
Cefamandole
Cefoxitin
Cefuroxime
Gram Ave coverage.
Parenteral administration except cefaclor
Allergic reaction (5 -15%)7 Skin rash, Anaphylaxis
Fever,
Local irritation at site of injection
Blood related 7 Hemolytic anemia, Granulocytopenia
IV and PO

Cephalosporins-3 rd Generation
3'" Generation

Cefixime
Cefoperazone
Cefotaxime
Cefpodoxime
Ceftazidime
Ceftriaxone

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Clinical use

Cell Wall Synthesis Inhibitors


Gram negative only
Reserved for serious infections (bacterial meningitis)
These drugs can penetrate Cerebrospinal fluids (CSF) thereby it indicated
for bacterial meningitis infections.
Nosocomial infections (hospital acquired infections),
Unknown origin infections Sepsis in immunocompramized patients .
Allergic reaction (5 -15%) ~ Skin rash, Anaphylaxis
Fever, Local irritation at site of injection
Blood related ~ Hemolytic anemia, Granulocytopenia
IV and PO

Side effects

Dose

Cephalosporins - 4th Generation


4th Generation
Clinical use

Cefepime
Best for Gram -ve
Higher potency

Side effects

Allergic reaction (5- 15%)7 Skin rash, Anaphylaxis


Fever, Local irritation at site of injection
Blood related 7 Hemolytic anemia, Granulocytopenia

~ose

LVand~

Vancomycin (Vancocin)
Mechanism
Therapeutic use

Cell wall synthesis inhibitor


A very important drug for treating meth ici llin-resistant staphylococcus
aureas infections (MRSA), and it is an alternate drug for treating
superinfection (Superbug) by Clostridium difficile in patients with P. coliti s.
Narrow spectrum of activity - active against Staphylococcus, Streptococcus
and Clostrid ium sp. (Gram + ve bacteria)
Chill s, Fever
Ototoxicity
Nephrotoxicity

Side effects

Precautions

Rapid administration causes red man syndrome (flushing)


In renal failure patient drug will accum ulate
IV and Oral
Renal elimination
Oral is used in only treatment of P. Colitis
Halflife6-8h

Dosage

Abbrevation and Tenninology


PAPA

Penicillin G, Amoxicillin, Penicillin V, Ampicillin

GI

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Cell Wall Synthesis Inhibitors

Generic and Brand


Penicillins G
Penicillins V
Piperacillin
Carbenicillin
Amoxicillin
Ampicil lin
Ce halos orins
Vanconvcin
Cefazolin
Cephalothin
Cefac10r
Cefoxitin
Cefuroxime Sodium
Cephradine
Cefadroxil
Cefamandole
Cefoxitin
Cefuroxime axeti l
Cefotetan
Ceti roxil
Cefonicid
Loracarbef
Cefixime
Cefoperazone
Cefotaxime
Cefpodoxime
Ceftazidi me
Ceftriaxone
Cefdinir
Ceftriaxone
Ceftibuten
Cefcpime

Pfizerpen
Beepen-VK, V-Cillin-K, Veetids
Pipraci l
Amoxi!, Dipermox, Trimox
Principen
Vancoc in, Vancol ed
Ancef, Kefzol
Keftin
Cec1or, Ceclor CD, RanicJor, RanicJor
Mefoxin
Alti, Ceftin, Kefurox, Zi nacef
Velosef
Duricef
Mefoxin
Ceftin
Cefotan
Cefzil
Lorabid
Suprax
Cefobid
Claforan
Banan, Vantin
Ceptaz, Fortaz, Tazicef, Tazidime
Rocephin
Omnicef
Rocephin
Cedax
Maxipime

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Protein Synthesis Inhibitors

36

Protein Synthesis Inhibitors


Protein Synthesis
Inhibitors

50 S Anti bacterial Agents

30 S Anti bacterial Agents

I
I

Chloramphenicol
Lincosamides
Clindamycin
Lincomycin

Aminoglycosides
Gentamycin
Streptomycin
Kanamycin

Macrol idcs
Erythromycin
Azithromycin
Clarithromycin

TEST CC: T = tetracycline, E = erythromycin S =-Sulfadrugs. r


are baclereostatic.

Tetracyclines
Oemec1ocycline
Doxycycline
Minocycline

trimethoprin, C= clindamycin C "" Chloramphenicol,

Aminoglycosides
Gentamicin, Streptomycin, Tobramycin, Kanamycin, Amikacin
Phannacokinetics
All am inoglycosides renally eli minated
Halflife 2 - 4 hours .
Post dose antibiotic effect (PDAE)
Only k anamycin and neomycin have oral and topical
Commonly aminoglycosides used as 1M or IV
Streptomycin has only 1M
Pharmacokinetics is not completel y understood
Contain aminosugars structures and have low bioavailablity
Pri marily used in infections associated w ith gram - ve.
Aminoglycoside have little activity against anaerobic.

Gentamicin (Garamycin)
Therapeutic Uses

Gram-ve
Drug uptake depends of oxygen: active against aerobes
Second line treatment for tuberculosis (mainly streptomycin)
Treatment for plague (streptomycin).
Pseudomonas (streptomycin)
Combined with cephalosporins (2nd and 31d) to reduce resistance

Side Effects

Respiratory paralysis (decrease Ach at NMJ)


Nephrotox icity (prox imal tubular cell)
Ototoxicity (also occurs in unborn fetus)

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Protein Synthesis Inhibitors

Streptomycin
Uses

Gram -ve
Second line treatment for tuberculosis (mainly streptomycin)
Treatment for plague (streptomycin).
Pseudomonas (streptomycin)
Combined with cephalosporins (2nd and 3rd ) to reduce resistance

Side Effects

Otic nerve toxicity-8 th cranial nerve (mainly streptomycin)


Hi ghest ototoxicity
Least Nephrotoxic

Ototoxicity
Streptomycin = Kanamycin> amikacin = gentamycin = tobramcycin > netilmycin

Tobramycin (Tobrex)
Uses

Gram -ve
Second line treatment for tuberculosis (mainly streptomycin)
Treatment for plague (streptomycin).
Pseudomonas (streptomycin)
Combined with cephalosporins (2nd and 3rd ) to reduce resistance

Side Effects

Respiratory paralysis (decrease Ach at NMJ)


Nephrotoxicity (proximal tubular cell)
Ototoxicity (also occurs in unborn fetus).

Amikacin (Amikin)
Uses

Gram -ve
Second line treatment for tuberculosis (mai nly streptomycin)
Treatment for plague (streptomycin).
Pseudnmnna.~ (streptomycin)
Combined with cephalosporins (2 nd and 3rd) 10 reduce resistance

Side Effects

Respi ratory paralysis (decrease Ach at NMJ)


Nephrotoxicity (prox imal tubular cell)
Ototoxicity (also occurs in unborn fetus)

Ami noglycoside summary


Side effects
A = Allergy
M = neuroMascular Blockade
I = Inactivated when physically mixed with p-lactams
N = Nephrotoxicity
0 = Ototoxicity, Optic nerve toxicity
Half life is 2 -4 h
Aminoglycoside have post antibiotic effect
Highest ototoxicity is with -+ Streptomycin
Highest nephrotoxic is 7 Neomycin
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Protein Synthesis Inhibitors

Ototoxicity symptoms associated with gentamycin and streptomycin are: Vestibular damage this
can cause T innitus, vertigo, and ataxia.
Ototoxicity symptoms associated with ami kacin and kanamycin are: Auditory damage this can
cause hearing loss.
Tobramycin can cause both vestibular and auditory damage
To prevent serious side effects associated with aminoglycosides monitor: Blood drug levels,
BUN, Serum creatinin levels
Blood levels are monitored by peak and trough levels:
Trough levels of gentamycin greater than 2mcglml can cause nephrotox ic .

Macrolides
Erythromycin. C larithromycin, Azithromycin
Pharmacokinetics:
All of macrolides hepatical ly eliminated, except: clarithromycin, which is renally el iminated.
All macrolides have oral dosage and erythromycin gluceptate and lactobionate is IV.
Azithromycin has long half-life 68h and used single daily doses.
Erythromycin has short half-life 1.2 - 2 .6 hours .
Erythromycin are preferred drug for treatment of Mycoplasma infection.
Important alternate in patient allergic to penicill ins
Erythromycin estolate may cause cholestatic jaund ice in-pati ent used more than 10-14 days.
( Resolved after d iscontinued treatment)
Erythromycin is inhibitor ofCYP3A4, thereby potentiates toxicities of drugs that are metabolized
by CYP3A4. eg: digoxin, corticosteroids, lovastatin or CALS), Carbamazepine.
Clarithromycin increase warfarin INR (monitor PT), increases digoxin and theophylline levels.
Azithromycin is more active against gram - ve H .influenza than erythromycin.
Clarithromycin is effective for H .pylori (used along with PPls in triple therapy)

Erythromycin
+ ve (all of them), Gram -ve for Neisseria

Use

Gram

Side effects

Epigastric distress (poor compliance)


Cholestatic jaund ice (in estolate fonn) :
Estolate is salt of lauryl ester.
Ototoxicity (more with erythromycin)

Drug
Interactions

Contraindicated in patient with hepatic dysfunction (it accumulate in liver)


Theophylline, Warfarin, Terfenadine, Statins

Clarithromycin (Biaxin)
Use

Same as erythromycin: H. influenza, Chlamydi, Legionella

Side Effects

G I7 Epigastric distress (Nausea, vomiting, Burning stomach, Diarrhea),


Renal (azotemia), Liver 7 Hepatitis

Contraindication

Patient with hepatic dysfunction

Azithromycin (Zithromax)
Use

Less active for Staph. and Strep than Erythromycin


Far more active H. influenza, Moraxella catarrhalis
Mycobacterium avium, except I-UV

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Protein Synthesis Inhibitors

Side Effects

Epigastric distress.
Oral has less N and V.

Contraindicated

in patient with hepatic dysfunction

Counsell ing

Suspension do not refrigerate

Tetracycline
Tetracycline

Broad spectrum antibiotics

Therapeutic Uses

Acne treatment
Chlamydia (lymphogranuloma, Psittacosis)
Rickettsia (Rocky mountain spotted fever)
Mycoplasma pneumonia
Lyme disease

Side Effects

Tetracyclines should not be treated to renally impaired patient.


(Accumulated increase azotemia.

Contraindication

Pregnancy, breast feeding, children under 8 old,

Counselling

Must take empty stomach with glass of water.


Tetracycline may stain teeth and fo r topical can stain cloth
Avoid prolong sun exposure.
Topical: Can continue use of cosmetics.
Stinging may occurs and that may resolve shortly.
Tell patient to report continuous nausea, vomiting,
Yellowing of eye and skin.

Doxycycline
Uses

Broad spectrum
Prophylaxis in travellers diarrhea
Lyme disease, Chlamydia (lymphogranuloma, Psittacosis), Rickettsia (Rocky
mountain spotted fever)
Mycoplasma pneumonia

Side Effects

Gastric discomfort.
Effect on calcified tissues (deposition in the bone and primary dentination
occurs during growing children.
Discoloration and hypoplasia of the teeth and temporary stunting of growth,
Fetal hepatotoxicity
PhototoxicitySevere sunburn
Super infection (over growth of candida in vagina or resistance to
Staphylococcus in intestine)

Contraindication

Pregnancy, children under 8 old, breast feeding

Counseling

Take entire medication even if you feel better


Oral: take with or after meal with glass of water.
(Food decreases GI side effects ~ avoid milk, antacids, iron)
Tell patient to check tongue for fungal infection.
Stress good oral hygiene.
Avoid prolong sun exposure

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Protein Synthesis Inhibitors

Minocycline
Minocycline

Broad spectrum antibiotic

Therapeutic use

Acne, Rheumatoid anhritis

Side Effects

Less phototoxicity
Vestibular problems: dizziness, nausea, vomiting
Pregnancy, breast-feeding, children under 8 old

Contraindication

Take with or without food

Clindamycin
Clindamycin

Lincosamides class of drug

Uses
Side Effects

Gram +ve anaerobic bacteria Bacteroidfragilis (abdominal infection)


Diarrhea (c. difficile - is resistant to clindamycin.,treatmentTreatment: Discontinue medication, and stan vancomycin or
metronidazole (oral)

Contraindication

History of colitis, regional entities, or antibiotic associated colitis.

Counseling

Take With or without food (Discourage with food)


Capsule: take with full glass (240 ml) of water to prevent dysphagia.
Do not refrigerate the reconstituted solution since under condition of low
temp, the solution may thicken and difficult to pour.
Stable at room temp for 14 days.

Precaution

I.M injection may be painful

Abbrevation and Tenninology


PDAE
NMJ
AcH
ALS
INR
PT

Post Dose Antibiotic Effect

Generic and Brand


Gentamicin
Stre tom cin
Tobramvcin
Amikacin
Ervthromycin
C larithromvcin
Azithromvcin
Tetracycline
Doxycycline
Minocvcline
Clindamvcin

Garamycin, Genoptic, Gentacidin


Ak-Tob Nebcin Tobi Tobrex
Amikin

Biaxin
Azasite Zithromax Zmax
Emtet Panmycin Sumycin Tetra 250
Adoxa Pak Atridox Bio-Tab Doxy
Cleeravue Dvnacin Minocin Mvrac
Dalacin Clinacin Cleocin Evoclin

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Quinoiones and fluroquinolones

37

Quinolones & Fluoroquinolones


Quinolones & Fluoroquinolones
Quinolones
Nalidixic acid (disinfectant)
lSI Gen
Fluoroquinolones
Nalidixic acid
Norfloxacin
Ciprofloxacin
Oflaxacin

3"'
Gatifloxacin
Moxifloxacin
Levofloxacin
4th Travofloxacin

Ciprofloxacin (Cipro, Cipro XR )


Mechanism

Inhibits DNA replication of bacterial DNAg (gyrase)

Therapeutic Uses

UTI 7 E.coli
STD -7 Gonorrhea
Respiratory 7 alternate to ampicillin in pneumonia
G I infections 7 E.coli travellers diarrhea
Nephrotoxicity
Cartilage toxicity-Avoid under 18years and pregnancy
Tendonitis/tendon rupture-common in elderly and renal failure patient
Most common: Nausea and Vomiting, light-headedness.

Side Effects

Counseling

Cipro otic suspension:


Store cipro otic suspension at room temp (15 to,25C).
Do not use otic suspension under 2 year of age

Auxi liary labels

With or without food. The preferred time is 2 hours after meal (for faster
absorption)
With full glass of water. (avoid dairy products)
Avoid taking with antacid, iron, or calcium together

Phototoxicity

Sunscreens may not effective; drug should be discontinued at the first of


sign of toxicity-sun bum like rashes.

Ofloxacin (Floxin)
Mechanism

Inh ibits DNA replication of bacterial DNA gyrase

Uses

Mainly for E. coli in UTI and STD with exception syphi lis.
Alternate in gonorrhea

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Side effects
Counseling

Quinolones and fluroquinolo nes


Hypoglycemia, Leukopenia, Neutropenia
Tell patient to drink fluids liberally.
Separate doses of vitamins, antacids by 2 hours.

Gatifloxacin (Tequin)
Mechanism

A quinolone, use to treat several types of bacterial infections.

Therapeutic use

Chest infections (pneumonia), Sinus infection, Urinary tract infection

Side Effects

Q-T prolongation

Drug-drug
interaction
Contraindication

Oral iron preparation and antacids containing magnesium and aluminum


can interfere the absorption of gatifloxacin
Not recommended in children

Monitoring

Metronidazole (Flagyl)
Metronidazole

Classified as antiprotozoal drug and has antibiotic actions (anaerobic)

Mechanism

Mode of action is thought to be breakage of cell DNA.

Therapeutic use

Indicated in anaerobes such as Bacteroides, C. difficile, C.vaginalis


Protozoans (Entamoeba, Giardia, Trichomonas)
Th is drug is also active against trophozoites in the intestinal lumen and
walls.
Metronidazole has direct anti-inflammatory effect (antioxidant action that
contributes to its anti-inflammatory activity).
Giardiasis and trichomoniasis metronidazole used oral ly

Side effects

Metallic taste, furry tongue, glossitis,


Must avoid taking alcohol while on this drug can cause disulfiram like
reactions
Rarely be neurotoxic.

Drug-Drug
interaction

Cimetidine - prolongs metronidazole half-life and decrease its plasma


concentrati on
Warfarin: Potentiates effects rcsulting in prolongation of prothrombin timc.
Disulfiram: Causes acute psychosis ever if taken within two weeks.
Phenobarbitone: Increases metronidazole metabolism

Precautions

It can cause dark urine


Do not mix i.v metronidazole with any other drug.

Pregnancy and
lactations

Caution require in pregnancy and lactation

Dosage

Inj ection: to treat anaerobic infections and protozoal infection


Oral capsul e
Oral tablets
Vaginal cream and insens, vaginal gel: for treatment of bacterial vaginitis
Topical cream or gel: Drug of choice for Rosacea applied effected twice
daily morning and evening for 9 weeks, then as needed.

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Quinolones and fluroquinolones

Abbrevation and Tenninology


I UTI
STD

I Sexually Transmitted Disease

Generic and Brand


Ciprofloxacin
Oftoxacin
Gatifloxacin
Metronidazole

Cipro, Cipro XR, Proquin XR


Floxin, Tarivid
Teauin, Zvrnar
Flagyl, Metrocream. Metron, Vandazole

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Folate Antagonist Su lfa Drugs

38

Folate antagonist Sulfa drugs


Sul fa drugs

Sulfamethoxazole
Sulfadiazine
Sulfisoxazole
Sulfasalazine
Trimethoprim

Combination
drugs

Cotrimoxazole

Mechanism

Folate Antagonists

Therapeutic Use

UTI ~ E. coli
Drug of choice in Traveller diarrhea
Trachoma-chlamydia trachoma-most
common cause of preventable blindness
Topical: Bums and wounds

Side effects

Crystalluria: adequate hydration and


alkalinization prevent this problem
Hypersensitivity; rashes, StevensJohnson syndrome-occurs with longer
acting agents: (diuretics, acetazolamide,
thiazide, furosemide, bumetanide,
diazoxide).
Hemolytic anemia-G6 PD defi ciency
Kernicterus: newborns because sul fas
displace bi lirubin from binding

Counseling

Sulfasalazine: drugs colors urine and may


color skin orange yellow.
May pennanently stain soft lenses
Take drug after meals to reduce G I
distress and to facilitate passage into
intestine.
Stevens-Johnson syndrome

Ptcridinc + PABA

1--Dihydroptcroic acid

1-

Dihydrofolic acid

""=;:

=-:':::::i.

T etrahydrofolic acid en-IF)

1
l ~;on;~

THF cofactors

Thymine

DNA

Purines

DNA

Glycine
f-mct-tRNA

Proteins

Sulfa Drugs = Antiseizure drugs; Allopurinol


Management ofSJS: by discontinuing medication .
Folate antagonist Mechanism

Sulfasalazine (Salazopyrin)
Mechanism

A combi nation of sulfanamide and salyc ilate, is use to treat two


inflam matory disorders affecting the bowels

Therapeutic use

Ulcerative Colitis (mainly affects the large intestine); Crohn's disease


(usually affects small intestine)

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Fo late Antagonist Sulfa Drugs

Side effects

Stomach irritation (can be avoided by taking the coated tabled fonn)


Allergic reactions, such as fever and rash (can be avoided or minimized by
low initial doses followed by gradual increases).
Nausea and vomiting
Aplastic anemia

Drugdrug
interactions

Sulfasalazine inhibits the absorption offolic acid


Decrease the bioavailability of digoxin
Choleslyramine decreases the metabolism of sulfasalazine

Monitoring

Periodic test of blood composition and liver function are usually required.
Blood disorders may occur with prolonged use of this drug.

Cotrimoxazole (SMX + TMP)


Therapeutic Use

Chronic treatment of UTI


Gram - ve : H influenza, Gonorrhea, E. coli, Klebsiella, Salmonella, shigella
sp. V. cholera
Gram +ve: S. pyogenes (GAS), S. viridans, S. aureus
UT IAcute, recurrent, chronic.
Upper and lower rasp----chronic bronchitis.
immunocompromised children: P. carin ii
Not indicated in infections assoc iated with pseudomonas, mycoplasma.

Side effects

Skin reaction (severe in elderly)


GI --> N and V
Blood related: Megaloblastic anemia, Thrombocytopenia, Leukopenia: The
above three effects can be reversed by concurrent administrati on of folinic
acid.
Hemolytic anemia G6 PD deficiency due to SMX

Counseling

Drug is not for 1M


Shake oral suspension thoroughly before use
Take drug as prescribe even feel better
Take oral dose with full glass of water.
With or without food. (tOOd decreases Gl side etfect)
Store in amber glass of bottle.
Store at room temp until expiry and protect from moisture.

Contraindications

Last trimester of Pregnancy, lactation.


Children under 2 months. May cause kernicterus

Antibiotics Tips
Steven-johnson's Syndrome: Rash, sk in peeling, and sores on the mucus membrane. In Steven
Jhonson's syndrome, a person has blistering of m ucus membrane, typical ly in mouth, eyes and
vagina. Patchy areas of rash. SJS can occur in all age groups .
Due to: SASPAN
Sulfonylurea
Anticonvulsant (phenytoin)
Sulphonamide
Penicillin
Allopurinol
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Folate Antagonist Sulfa Drugs

NSA lDs
Sulfa drugs ~ Stevens Jhonsons Syndrome
Topical sulfa is contraindicated because it may cause disease like SJS, this disease is life threaten ing.
Treatment of SJS is Cortisone
Summary of Cell wall synthcsis inhibitors
Methicillin is only IV and 1M
Penicillin G benzathine has long half life ~
Naficillin is mainly hepatic elimination
Beta lactamase sensitive drugs: Pen G, Amoxi, Pen V and Ampicillin
Endocarditis prophylaxis is (Dental extraction prophylaxis) ~
A child less than 2 y allergic penicillin, what is the drug choice for otitis media treatment ~
A patient has heart diseases and undenvent prostatic valve surgery. Dentist plans to tooth
extraction, what antibiotic is suitable for endocarditis prophylaxis ~
Chewable antibiotics ~
Beta lactams that should be taken empty stomach ~
Aminopenicillins are:
Penicillin allergic patient, alternate drug of choice is?
Penicillins are ineffective in treatment of bacterial infections associated with ~
MRSA infections are treated by ~
P.colitis associated diarrhea is treated by ~
Bacteria is inhabitant in GI, what location ofGl tract is commonly fou nd ~
Type of bacteria mainly present in colon is ~
Macrolides Practice Test
Azithromycin suspension stored at 7
Clarithromycin suspension stored at -7
Which macroli de suspension have to refrigerate after reconstitution ~
What antibiotics should caution and require monitoring in patient receiving warfarin What antibiotic potentiate the effect of digoxin and can cause digitalis toxicity 7
Azithromycin is the drug of choice in traveler diarrhea for patient travel ing to ~
Tetracyclin Practice Tests
Tetracyclin are contraindicated are contraindicated in pregnancy and children.
Tetracyclin can stain teeth and discoloration.
Oral or topical tetracycline are drug of cho ice for acne treatment
Tetracyclin MUST BE taken empty stomach.
Tetracyclin binds ~
GI distress (abdominal discomfort, diarrhea) most common SE. This can be resolved by taking
with food or decreasing dose.
Expired tetracycline can lead 7
Doxycyclin is the DOC ~
Doxycyclin should be taken ~
Minocyclin may take with or without food.
Phototoxic reactions (sever skin lesions) can develop with exposure to sunlight. Photoxicity is the
most common with doxycyc1in or demec1ocyc1in.
Epimerization is a ~
Tetracyclins = Take empty stomach
Doxycyclins = Take with or after food
Minocyclins = Regardless of food

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Folate Antagonist Sulfa Drugs

Clindamycin Practice Tests


Most common compl ication of clindamycin is 7Clindamycin active against 7Pseudomembranous colitis symptoms include: fever, abdominal pain, bloody stools.
Clindamycin can cause 7Clindamycin drug associated diarrhea is treated bY 7Clindamycin suspension stored at 7Clindamycin should taken 7Quinolone and fluroquinolone Practice Test
Fluroquinolones are indicated for UTI, Infectious diarrhea (Travellers diarrhea), lower respiratory
tract infections, bone and joint infections (osteomy litis).
Gatifloxacin, Moxifloxacin SE are 7FluroquinolonesContraindicated in children, under 18 y, pregnant women due to i15 7Antacids, bivalent and trivalent ions significantly decrease absorption of 7Fluroquinolone increase INR in patient receiving warfarin, therefore monitor -7
Fluroquinolones can cause hypo or hyperglycemia, therefore monitor -7
Fluroquinolones at higher alkaline pH can cause -7
Cipro is the drug of choice in -7
Metronidazole Practice Tests
Alcohol with metronidazole can cause -7
Metronidazole is classified as: Antiprotozoal drug
Metronidazole is effective against -7
Metronidazole discolor urine
Metronidazole caution in pregnancy
Sulfadrugs Practice Test
Sulfamethoxazole + trimethoprim have -7
A 22 year old patient currently using cotrimoxazole for UTI, reported sever rashes on anns, neck
and back, what are the possible reactions-7
What are the folic acid synthesis inhibitors-7
Patient with G6PD defic iency, takes sulfadrugs can cause -7
Hypersensitive reactions of sulfadrugs most commonly invol ve -7
Life threatening hepatitis caused by sulfadrug toxicity or sensitization rare SE, the signs and
symptoms include-7
Sulfamethoxazole have high frequency of skin hypersensitive reaction in patient with
If used in last trimester of pregnancy, can cause kemecterus in new born.
Cotrimoxazole suspension stored at room temperature in amber color glass bottle.
r carinii pneumonia (PCP) drug of choice is Cotrimoxazolc.

Abbrevation and Tenninology


SIS

THF
SMX

TMP
UTI
GAS
1M

JNR

Generic and Brand


Sulfasalazinc
Cotrimoxazole

Salazo rin Salazo


Se trin Bactrim

rin EnTabs

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Antifungals

39

Antifungal agents
Mechanisms of Action and Classification of Antifungal Agents
Antifu gat Agents
After cell me1brane permeability

Azolr5

AlIyl. mint

Terbinafine
Nftftifin"
lm idazoles
.. Ketoconazole
.. Miconazole
- ClouimazoJc

Systemic
antifungals

Topical
Antifungals

Tria7.oles

Block nuclei acid synthesis

P oly tnt
mRnol idt
a ntibiotic

Pyriml din t
An a log

Disru pt microtubul function

I
I

Aucytosinc

Ptnir ill in
dtriva li vt

I
I

Griseofulvin

.. Amphotericin B
-Nystatin

Auconawlc
Itraconawle

Ally lami nes

Terbinafine hydrochloride

Antifungal Antibiotics

Amphotericin B
Amphotericin B (lipid-based)
Griseofulvin

Echinocandins

Caspofungin acetate

Imidazole

Ketoconazole

Pyrimidi nes

Flucytosine

Triazoles

Fluconazole
Itraconazole

Allylamines

Naftifine hydrochloride
Terbinafine hydrochloride

Antifungal Antibiotics

Nystatin

Imidazoles

Clotrimazoles
Econazole nitrate
Ketoconazole
Miconazole nitrate
Oxiconazole nitrate
Tioconazole

Other topical antifungals

Chlorphenesin
Ciclopirox olamine
Clioquinol
Selenium sulfide
Tol naftate
Undecylenic acid

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Antifungals

Amphotericin 8 (Fungicidal)
Therapeutic use

Widest of any agent, systemic funga l infections; candidiasis; cryptococcos;


blastomycosis; histoplasmosis; coccodiodomycosis; aspergillosis;
sprorotichosis; mycO!>,is; leishmaniasis
Availability: 3% cream/lotion/oral suspension
Not absorbed in the G IT

Mechanism

Bind to ergosterol from pores resulting in the leakage of cell ular contents

Side effects

Infusion related fever and chills; anorexia; muscle pain; headache


Non-infusion related: nephrotoxic, hyperkalemia, hypomagnesemia,
tachycardia, anemia, thrombocytopenia, arrhythmias, YF, HTN, tachypnea,
leukoencephalopathy, dry skin, skin discoloration, SJS, toxic epidermal
necrolys is, agranulocytosis, jaundice, hemorrhage, sore throat

Contraindication

Allergies

WARN ING

Apply only to patients with progressive, potentially fatal infections and


should not be used to treat non-serious infection
Monitor Lab test sp. Renal function (frequently), liver function, serum
electrolytes particularly magnesium and potassium, blood count, Hgb conc.
Not use for dosage adj ustment
Does not penetrate CSF

Drug interaction

Antineoplastic= increase renal toxicity, bronchospasm, hypotension


Corticosteroids/ACTH= increase. amphotericin B-induced hypokalemia,
renal toxicity;
Nephrotoxic agents (Cisplatin, pentamidine, aminoglycoside, cyclosporine=
increase renal toxicity
Digitalis glycosides= Amphotericin B-induced hypokalemia, increase
digitalis toxicity
Skeletal muscle relaxants= enhance cureiform
Others: AZT, chloramphenicol, antithyroid, colchicine, deferoxamine,
streptozocin, plicamycin, lithium, penicillamine
Overdose : cardiorespiratory arrest

Prccauti"on

Storage of dry powder; 2-8 deg, protect from light


Give slow IV infusion

Counselling

When applying topicals on the skin, protect nails and clothes as it may stain

References

CPS 2004, 854-855,


Comprehensive Pharmacy Review, 5th Ed. Page 795,

Nystatin
Category
Therapeutic use

Mechanism
Side effects

Polyene antibiotic, structurally similar to Amphotericin B, fungicidal,


fungistatic
Active against Camlitia ~p. Primarily use as a topical agent in vaginal
and oral candidiasis
Not very effective against dermatophytes (Tinea)
Inhibit growth of yeast, binds to sterol in the funga l cell membrane,
increasing permeability and causing leakage of intracellular components
Irritation e.g. mild digestive upset, Nausea & Vom iting diarrhea; creaml
vaginal tablet- itching, burning, irritation

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Antifungals

Advantage
Drug interaction

Can be use by pregnant women

Precaution

Application of vaginal tablet

Counselling

Nystatin liquid-3-5x a day by mouth for mouth infections, intestinal


infection-3x per day. Shake bottle well before each use. Place half of the
liquid on one side and the other half on the other side. Hold; swish it
for several times in the mouth before swallowing. For intestinal use, just
swallow liquid.
Skin ointment or cream. Use several times a day. Wash thoroughly the
affected area. Apply a small amount of the cream or ointment and gently
massage it. Keep away from eyes .
Powder. Dust the powder inside shoes and socks.
Nystatin vaginal tab and cream. Use 001 BID as directed for vaginal
infections. Use vaginal tab or cream for two week in women who are not
pregnant and 3-6 weeks before delivery in pregnant women. Continue to
use medication even if symptoms improve for a few days.

Reference:

CPS 2004 1308- 1309


Comprehensive Pharmacy Review, 5th Ed. Page 795.
Comparison of FJuconazol And Ketoconazol
Fluconazol

Triazole type antifungal


Inhibitors of Ergosterol synthesis by
binding to CYP
Single doses
Penetrate eNS (AIDS chemotherapy)
CNS SE: dizziness
No interaction with cimetidine, antacids
For systemic infection UTI , peritonitis,
pneumonia

Potent inhibitor of CYP 2C9 (high) and


CYP3A4

Fluconazole taken with or without food.

Ketoconazo!
Imidazole type antifungal
Inhibitor Ergosterol synthesis
Not a single dose
Doesn't penetrate eNS
SE: Hormonal effects such as gynecomastia and
menstrual disturbances
Interaction with cimetidine, antacids
Require acidic conditions for absorption (avoid
antacids concomitantly)
Potent inhibitor ofCYP 3A4 (high) and CYP
2C9
Ketoconazole taken with food or after food
(with cola beverage if achlorhydric or on acid
secrete suppressor)

Ketoconazole (Nizoral)
Ketoconazole (Imidazole type)

Miconazole; Clotrimazole

Therapeutic use

Chronic mucocutaneous candidiasis, systemic and vaginal


candidiasis, Tinea corporis (ringworm), T. cruris Gock itch),
T. pedis (Athlete'S foot), Tinea versicolor (sun fungus),
histoplasmosis, blastomycosis, paracoccidioidomycosis, oral
thrush
Relative bioavailability: 75 % with meals
Available as tablet, cream

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Antifungals

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Mechanism

Block the symhesis of ergosterol 14a demethylase in the


fu ngal CYP 450 complex; hepatic elimination

Side effects

Honnonal effects ? Decreased male libido and potency,


gynecomastia, decreased plasma testosterone levels, affects
female menstrual problems, Cardio effects ? hypertension,
fluid retention,
GI effects ? GI upset, hepatotoxicity, dizziness, anorexia,
Nausea & Vomiting

Contraindication

Hypersensitivity; teratogenicity

WARNING

Rebound effect. Apply mild topical corticosteroids in the


morning and ketoconazole at night and gradually decrease
steroid over a period of2-3 weeks. Cross sensitivity

Precaution

Allergies with imidazoles

Counsell ing

Increased absorption on an empty stomach.


Shampoo, I %: Wet scalp and work lather. Massage . Leave
for 3-5 minutes then rinse zwell w ith wann water. Repeal
application. Rinse and dry hair. Wash eyes if shampoo gels
into them. Treatment is 2x a week for 2-4 weeks whereas as
a prophylaxis, use once every 1-2 week; Shampoo, 2% : Wet
hair and scalp.
Apply shampoo the affected area. Work up lather and leave for
5 minutes. Rinse hair and scalp well. Dry hair. Protect eyes.
Cream: Apply Ketoconazole cream to cover affected area and
surrounding ski n areas. Rub gently. Keep using cream for the
fu ll treatment even if symptoms begin to clear up after a few
days to several weeks. Recurrent infection if you stop meds
too soon . Do not miss a dose

References

CPS 2004, 1379-1380


Comprehensive Phannacy Review, jlh Ed . Page 794-795,

Fluconazole (Diflucan)
Mechani sm

Block The Synthesis Of Ergosterol By Inhibit 14A-Demethy lase In The


Fungal C YP450 Complex

Therapeutic use

Mucocutaneous Candidiasis (Esophageal); Alternative For


Amphotericin B For Treatment Of Systemic Candidiasis, Cryptococcal
Meningitis, Coccidioidomycosis, Cryptococcosis, HIV Associated
Infections
aRelati ve Bioavailability: 85- 92% With Meals

Side effects

Skin Rash
GI Effects ? Nausea, Vomiting Diarrhea Or Commonly Causing G I
Disturbances.
Liver Effect ? Increase Liver Enzymes, Yellowing Of The Skin, And
Eyes, Flu-Like Symptoms,
CNS ? Dizziness, Headache, Exfol iative Skin Reactions, Altered Taste
Buds, Extreme Tiredness, Seizures.

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Antifungals

Drug interaction

Decrease Levels With Carbamazepine, H2 Blockers, TN H, Phenytoin;


Increase Levels Of Phenytoin, Warfarin, Sulfonylureas; ROH ;
Anticancer Drugs, Amiodarone, Astemizole, Benzodiazepi ne,
Cyc losporine, Disopyramide, OCP, D iuretics, Moxiftoxacin, Sotalol,
Terfenadine, Quinidine, Valproic Acid, Thioridazine And Tacrolimus

Precaution

Decrease Elimination O f Enzyme Inducers Like Rifampin, Al lergies To


Fluconazole And Other Antifungals, Irregular Heart Beat; Kidney Or
Heart Disease

Reference:

Applied T. Handbook; Chapter. 67, Pp. 67.4 - 67.5


TC Page 4th Ed Page 1056.

Itraconazole (Sporanox)
Therapeutic use

More active treatment against Aspergill us spp.; blastomycos is; other


mycosis like mucor,Jusarium pseudoallescherria boydii; HIV associated
infections; invasive and non-invasive pulmonary aspergi llosis;
oral and esophageal candidiasis; chronic histoplasmosis (acute
immunocompromised, an alternative to am photeri cin); cutaneous and
lymphatic sporotrichosis; paracoccioi domycosis; chromomycosis
Dose Aspergillosis: ;lOOmg IV Q8H X 12 H then 200mg IV Q l2H
Blastomycosis; 200mg po BID
Histoplasmosis: 200-400mg QD po
Take wi th meals fo r adequate absorption

Mechanism

Bl ock the synthes is of ergosterol 14a demethylase in the fungal CYP 450
complexz

Side effects

Nausea, epigastric pain rash, headache, edema, hypokalemia, loss of


appetite, shaking, dyspnea, bl eeding gums, yellowing of eyes and skin ;
hypertriglyceridemia; decrease libido

Contraindication

CHF; Ventricular dysfunction

Warning

Cause CHF; heart attack; irregular heart beat! dse; lung! kidneylliver
disease or other serious problems; SOB; coughing up white phlegm;
weakness; excessive tiredness; fast heart beat; swelling ofthe feet, ankle or
leg; sudden weight gain

Drug interaction

Cisapride, pimozide, dofet ilide, ergot meds, tri azolam, midazolam,


quinidine, - all may cause irregular heart beat
Take antacid one hour before or two hours after itraconazole

Drug interaction

Increased by Itraconazole: antiarrhythm ics, anticonvulsants-

CBl, antimycobacterial-ri fab utin, antineoplastics, antipsychotics,


Benzodiazepine, Ca-channel bl ockers, gastrointestinal motil ity agents,
HMG-CoA reductase inhibitors, Immunosuppressants, oral hy poglycemics,
protease inhibitors, buspirone, macrolides;
Decrease by Itraconazole anticonvulsant, anti mycobacterial, gastric acid
suppressants, NN RTI

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Antifungals

Counselling

Oral solution: Sw ish 10ml (2tsp) in the mouth for a few seconds and
swallow. Repeat is necessary until entire dose is taken. The solution is
usually taken on an empty stomach once daily or 8lD for 1-4 weeks .
Tell Doctor if taking Itraconazole. Do not substitute the capsules for the
liquid because they have different use .

Reference:

CPS 2004, page 1973- 1978


Comprehensive Phannacy Review, 5111 Ed. Page 794-795

Clotrimazole
Therapeutic use

Yeast infection, skin infections, high concentration needed in bacterial


infection
Availability: cream, lotion or solution- dennatophytes (ski n infections);
intravaginal suppositories for vaginal candidiasis, lozenge

Mechanism

Block the synthesis of ergosterol 14a demethylase in the fungal CYP 450
complex
Topical: blisters, edema, pruritus, burning, stinging, peeling skin tissue,
increase urinary frequency
Abdominal pain
Irritation
Abnormal liver function test in patient taking lozenge

Side effects

Contraindication

Not for first tri semester of pregnancy

Management

In case of vaginal infection, refrain from sexual intercourse cause an


ingredient in the cream may weaken certain latex condoms / diaphragms .
If first time of vaginal itching and discomfort. see a doctor. Do not use
products within 72 hours of this med. Wear cotton unden . . ear and loose
fitting pants; no lozenge for children under 3y/o
Pregnancy

Precaution
Reference

CPS, 2004 , 36\-362;


Comprehensive Phannacy Review, 5111 Ed. Page 797

Miconazole
Category

Broad spectrum fungistatic

Mechanism

Block synthesis of ergosterol by inhibiting 14a-demethylase in the fungal


cytochrome P450 complex; selective inhibition of RNA & DNA and
mucopolysaccharide precursor

Therapeutic use

Covers both dennatophytes and candidiasis (Advantage Over Tolnaftate


and Nystatin; Also, effective against Tinea infections by T. pedis, T cruris,
T. corporis, T. versicolor

Side effects

Itching, skin rash,


Nausea &Vomiting, burning on the site of application

Contraindication

Sensitivity to any of the components of Miconazole, not for chi ldren> 2y/o
unless directed by a doctor, do not use for the infection of the nail

Drug interaction

Anticoagulants,
Phenytoin,
Terbinafine,

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Antifungals

Drug interaction

Atypical anti-psychotics,
Cyclosporins
Some statins

Availability

Topical 2%, aerosol powder, 2 % cream, a kit-2% powder 2y/o and 2%


tincture, 2% vaginal cream and 100 and 200 mg vaginal suppositories
Aerosol powder
Cleanse skin with soap and water.
Dry thoroughly.
Shake aerosol well before using.
Apply or spray a thin layer over the affected area in the morning and up to
bedtime.
Do it from a distance of 6-10 inches to the affected area of the feet. Do not
inhale powder.
rf no improvement in 2 weeks time, see doctor But continue fir 1-2
weeks after symptoms disappear to a maximum of 4 weeks. Jock itch and
ringworm is 1-2 weeks resolution; athlete's foot-4 weeks.
Cream Apply sparingly, smoothen well and avoid maceration. Massage
area gently. Athlete's f09t: dry feel, wear cotton socks
CPS, 2004, page 1246

Application

Reference

Tolnaftate
Category

Fungistic, fungicidal

Mechanism

Damage hyphae and stunt mycelial grO\vth in susceptible fungi

Therapeutic use

Jock itch, athlete's foot, ringworm ; T. pedis, M. canis, Aspergillus niger,


C. a/bieans, M. gypseum, M. audounii, M.japonieum, T. rubrum, T,

Side effects
Administration

Administration
Warning
Contraindication

mentagrophytes, T. sehonleinii, A./umigatus


Slight irritation, sting (aerosol solution), burning and itching of athlete's
foot and jock itch should decrease with in 2-3 days
Do not apply dressings, or mix cosmetics or other skin medications with
tolnaftate treatment.
Powder: Clean and dry affected area. Sprinkle it bIn toes and in socks and
shoes treated lightly.
Spray should be shaken well before use. Apply it from a distance of at
least six inches away. Continue treatment until symptoms disappear. A
total of 4-6 weeks necessary. Do not inhale powder, bring close to a hot
object or flame
Cream. Thoroughly clean the infected area. Allow it to dry and then rub
gently the medication until most of it disappears. Use sufficient quantity
to cover the affected area. Wash hands after application.
Solution. If it solidifies, dissolve by warming the closed container in
warm water then follow dosage as directed.
Usually, applied in affected areas 2x a day. Ifno effect in 4 weeks, check
with health care professional.
Aeroso ls: Flammable
Allergies to tolnaftate or any preservatives, dyes; pregnancy; children, 2

y/o
Reference:

Comprehensive Pharmacy Review, 5th Ed. Page 80 I

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Antifungals

Antifungals Tips
Nystatin is indicated -7
Ketoconazole require acidic conditions for higher bioavai lability therefore -7
Meningitis fungal infections other eNS infections can be treated bY-7
If a chi ld swallowed 5g of nystatin, and parents are panic, comes to your phannacy, what is
appropriate action -7
Nystatin is ineffective for -7
DOC for oral thrush-7
DOC for vaginal candidasi s
Topcal Drug of choice for Atheletes foot -7
Nystatin suspension counseling-7
Amphotericin - B is -7 act by inhibiting the cell membrane function

Abbrevation and Tenninology


GIT
YF

HTN
SJS
CSF
ACTH
AZT
OCP
NN RTI
IV
CYP
SOB
CBZ
BID
CPS

Generic and Brand


Amphotericin B
Nystatin
Fluconazole
Itraconazole
Clotrimazole
Miconazole
Tolnaftate

Fungistic, Fungicidal
Tri-Statin, Mycolog, Mytrex
Diftucan
Sppranox
Clotrimazole Cruex Lotrimin M celex
Aloe Vesta Cruex Desenex Jock Itch
Asorbine Afate. Genas ore Pitrex

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Ami-Mycobacterial Drugs

40

Anti-Mycobacterial Drugs
Antimycobacterial drugs
Isoniazid
Rifampin
Streptomycin
Pyrazinamide
Ethambutol
Capreomycin
Rifabutin
Tuberculosis treatment:
Goal of treatment is must eradicate mycobacterium.
Important issues in tuberculos is treatment are resistance to drugs .
.-Drugs that haveJowest resistancejs:lsoniazid, rifampin, streptomycin and combination of these
drugs with pyrazinamide, or ethambutol.
Drug of choice is combination of Isoniazid + rifampin + pyrazinamide.
Antimycobacterial Drugs
Rifampin
Chemical structure ofrifampin is a macrocyclin.
This drugs is bactericidal
Inhibits RNA synthesis
Mechanism
Therapeutic Use
Effective against M. tuberculosis, and M. leprae
Prophylactic for house hold members of exposed to meningitis caused by
meningococci or H. influenza type b
Side Effects
Seri ous liver toxicity (hepatotoxicity) thereby LIT should be performed
regularly
Gr SE: nausea, vomiting, abdomil!al pail!
CNS SE: Headache, drowsiness, confus ion, fatigue
Rifampin discolor urine, sweat, tears, saliva and feces to orange-red .
Drug interactions
Rifampin is inducer ofCYP IA2, 206, 2C9, 2C19, 3A4
Reduce efficacy oral contraceptive.
Isoniazid (INH)
Mechanism
Therapeutic Use
Side Effects

Chemical structure is hydrazide of isonicotinic acid.


Targets enzyme responsible for mycolic acid synthesis
First line treatment for tuberculosis
Most common: Peripheral neuritis (because of pyridoxine deficiency)
Vitamin 8 6 supplements. Skin rash, jaundice and fever are common SE.
Supplementing breast fed mothers can provide pyridoxine deficiency in
ch ildren.

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Side Effects

Anti-Mycobacterial Drugs
Most common: Hepatitis: Most severe-fatal, the risk of hepatitis increases
with patient age and alcohol abuse. Monitor LFT
Blood dyscariasis (agranulocytosis, aplastic anemia, hemolytic anemia
Thrombocytopenia) thereby monitor CBC routinely
eNS toxicity due to decrease in pyridoxine levels: Administer 15 -50 mgldy
pyridoxine to minimize the peripheral neuropathy.
Symptoms of CNS toxicity are: insomnia, restlessness, hyperreflexia, and
convulsions.

Pyrazinamide (ZIN)

It is pyrazine analog of nicotinamide

Mechanism

Pyrazinamidase enzyme converts into pyrazinoic acid (active fonn)

Therapeutic Use

Combination with INH and rifampin. Pyrazinamide has activity only against
M.Tuberculosis
Liver dysfunction
Urate retention .
May precipitate gouty attacks

Side effeclS

Antimycobacterials Tips
Drugs that discolor urine, tears, saliva, feces, sweat ?
Drug of choice to treat tuberculosis ?
Peripheral neuritis caused by isoniazid can managed by administering ?
XDR TB = Extensive Drug Resistance Tuberculosis.
All antitubercular drug should be taken on :

Abbrevation and Tenninology


TNH
LFT

Isoniazid
Li ver Funtion Test

XDRTB
ZIN

Extensive Drug Resistance Tuberculos is.


Pyrazinamide

CYP

Generic and Brand


Isoniazid
Ri fampin
Streptomycin
P razinamide
Ethambutol
Capreomycin
Ri fabutin

Isoniazid INH Nvdrazid


Ri fadin Rimactane
Myambutol
Mycobutin

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Anti-viral Drugs

41

Anti-viral Drugs
Antiviral Agents

Amant.din<

~Iovir

lidovudine

Ne,u apint

Rimantadirr

VolK)'Clow
Ganciclo, u

Didano<int

Delavitdint
Efavirenz

Neuroamindiase inhibitor
Osaltamavir
ZarJalllavir

Sl.wdin<

Antiretroviral

Amantadine
Ribavirin
Rimantadine
Zidovudine
Didanosine
Zalcitabine
Stavudine
Lamivudine
Nevirapine
Nucleoside Reverse
Transcriptase
Inhibitors (NRTI)

Foscarnet
Ribavirin

ACyclovir (zovirax)

Retrovirus are the vi rus the consist of


reverse transcriptase enzyme, reverse
transcriptase helps to copy vi rus.
For HTV treatment
Reverse transcriptase enzyme
present in H]V
There are three types of antiretroviral
drugs

NRTI
NNRTI

For DNA viruses Acyclovir


Ganciclovir
Famciclovir
For RNA and
DNA viruses

Lami" ..dint

Vidanbft

At.ca ....

Antivirals Drugs classifications


-PofRNA viruses

Zalcilabino

TriOuridin<

lndina ....

Soquinaw
RitolUlvir
Ampre"" .....

Protease inhibitors
Zidovudine (AZT)
Stavudine
Lamivudine
Didanosine
Zalcitabine

Non-Nuc leoside
Reverse Transcriptase
Inhibitors (NNRTI)

Nevirapine
Efavirenz
Delavirdine

Protease Inhibitors

Saquinavir
Ritonavir
Indinavir

Mechanism

Guanosine analog and lacks true sugar moiety

Therapeut ic use

Herpes Simplex Virus (HSV-I)


Herpes Simplex Virus (HSV-2)
Varicella zoster (VericeJla is referred chicken pox and zoaster is referred as
Shingles)
Epstein-Barr virus

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Anti-viral Drugs

Side effects

Depends on route of administration


Topical ~l ocal irritation
Oral-nausea, vom iting
IV- transient renal dysfunction in dehydrated patients

Advantage

Greater specificity fo r herpesvirus.


Sensitive to HSV-J and HSV-2, Epstein-Barr virus, Varicella zoster,
Drug of choice for HSV.
Most commonly used in genital herpes.

Dosage

Oral
Topical (5% cream, ointment)7 Recurrent orolabial herpes infections

Antiretroviral drugs:
Retrovirus: Virus that contain reverse transcriptase enzyme such as HIV is referred as retrovirus
There are three classes of antiretroviral drugs: NRTl, NNRTI and Protease Inhibitors;
Nucleoside reverse transcriptase inhibitors (NRTI) phosphorylate by human cellular kinases .
Non nucleoside reverse transcriptase inhibitors (NNRTI}- phosphory late by human cell ul ar kinases.
Protease inhibitors : ! viral protease

Zidovudine (AZT)
Mechanism

AZT is converted to the nucleoside triphosphate and incorporated into


growing chain of virus DNA by reverse Transcriptase. Thus synthesis of
DNA is tenninated.
Chemically it is synthetic thymidine analog (Azidothymidine: AZT)

Therapeutic use

Only cl inical use in HlV

Side effects

Most common SE is Bone marrow toxicity: Bone marrow toxicity can


be treated by antianemic supplements: Erythropoeitins (stimulates RBC
production)
Reversible neuropathy
Sever anemia
Leukopenia
Headache
Seizure

Didanosine (ddl)
Mechanism

It is a synthetic purine analog.


Biolransfonned into didanosine ATP, through several reactions and
incorporated into viral DNA.
Long intracellular half-life 8 - 24 hours.

Therapeutic use

Dose dependent activity against Hl V- 1 as result decrease in production of


virus.
This drug also increases in appetite and weight gain and energy.

Side effects

Pancreatitis (which of may be fatal) 7 major Black Box warning.


Avoid drug that cause pancreatitis: Sulfonamides, Zalcitabine
Peripheral neuropathy
Require acidic content in stomach for absorption (like ketoconazole)

Monitor
Monitor 7 serum amylase and triglyerides
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Anti-viral Drugs

Zalcitabine (ddc)
Mechanism

Synthetic pyrimidine analog acti ve against mv

Therapeutic use

Indicated in patient advance HI V disease (Serum CD4 count <300/mm2),


and combined with Zidovudine

Side effects

Rash and stomatitis (pin feeling)


Peripheral neuropathy (major)
Pancreatitis
Neuropath ic pain
High triglyceride levels

Monitor
Avoid

Drugs that cause peripheral neuropathies: Cisplatin, isoniazid, ethambutol,


metronidazole, phenytoin, dapsone, ribavirin, vincristine, nitrofurantoin,
lithium, and chloramphenical.
Do not take with Mg, Ca, and Al antaci ds
Do not combine with stavudine, didonasine, lamivudine

Stavudine (d4T)
Mechanism
-Side-effects

Monitor

A synthetic thymidine neucloside analog acti ve against H1V


Peripheral neuropathy-(21 %)
Pancreatiti s
Drug is not affected by food
Do not combine with zidovudi ne and zalzitabine

Lamivudine (3TC)
Mechanism

Synthetic neucloside analong structurally similar to zalcitabine

Therapeutic use

Indicated to treat HIV and chronic hepatitis B in patients with active liver
inflammation

Side effects

CNS toxicity: dizziness, insomnia, neuropathy

Monitor

Pancreatitis toxicity in children

A ntiviral drugs TIps


CD4 count 100 patient require prophylaxis for the infections of ~
Pancreatitis is SE of ~
Peripheral neuropathy is SE of ~
Didanosine should be avoi ded with what are the other antiretroviral drugs ~
Flu season in Canada ~
Fl u immunization in Canada ~
Who should get flu vaccination ~
Who is vector (carrier) of flu ~
Zidovudine induced anemia may be treated by ~
Acyclovir is the DOC for HSV-J and HSV-2 infections
Famcyclovir and Valacycyclovir are alternate treatment for HSV-I and HSV-2
Cold sore can be treated by calamine lotion, oatmeal bath, and antihistmines.
Genetal herpes:
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Antiviral Drugs

Keratoconguntivitis: Trifturohexidine ophthalmic or acyclovir.


l nfluen7.a A and R virus causes flu:
Amantadine: for Influenza A
Rimantadine: fo r influenza A
Neuroarninidase inhibitors: Oselatarnavir (Tamiflu): for influenza A and B
Zanamavir: for influenza A and B
Herpes simpex virus causes infections of Genital herpes, Keratoconjuctivitis, Cold sores

Abbrevation and Tenninology


NNRTI
NRTI

NonNucleoside Reverse Transcriptase Inhibitors


Nucleoside Reverse Transcriptase Inhibitors

HIV
AZT
HSV
RBC

ATP
RBC

Generic and Brand


Acyclovir
Zoviraxc
Didanosine ddl
Zalcitabine ddc
Stavudine d4
Lamivudine 3TC
Oselatamavir

Zovirax
AZT Retrovir
Videx Videx EC
Hivid
Zedt
Eoivir
Tamiflu

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Anti-Malarial Drugs

42

Anti-Malarial Drugs
Malaria is infection of red blood cells with the single-celled parasite Plasmodium, which causes
fever, an enlarged spleen, and anemia.
Four species of malaria parasites--Plasmodiumja[ciparum, Plasmodium vivax, Plasmodium ovale,
and Plasmodium mal(Jriae--can infect people.
Fa1ciparum malaria, caused by Plasmodium falciparum, is the most dangerous fonn of malaria and
can be fatal.
Blackwater fever is an uncommon complication of falciparum malaria.
Chloroquine is the drug of choice for treatment in a person who has malaria caused by Pl asmodi um
vivax, Plasmod ium ovale, or Plasmodium malariae--except in a very few areas where resistance to
chloroquine in people with Plasmodium vivax has been reponed.
Chloroquine is the preferred drug for prevention of malaria caused by Plasmodium falciparum in
Mexico, areas of Central America west of the Panama Canal, Haiti, the Dominican Republic, and
some areas of the Middle East.
Primaquine is added to kil! persistent parasites in the liver of a person infected with Plasmodium
vivax or Plasmodium ovale. Before primaquine is given, a blood test is done to look for a relatively
common enzyme deficiency (G6PD defic iency). People with G6PD deficiency who are given
primaquine may have a breakdown of their red blood cells.
Treatment of malaria
Prophylaxis
P. falciparum

Pyri metham inels ul fadoxi ne

P. malariae

Chloroquine
Chloroquine

P. vivax

Chloroquine + primaquine

P. ovale

Chloroquine + primaquine

Chloroquine res istant


prohylaxis

Primaquine, Quinine + doxycycl ine: Mefloquine, atovaquone


proguanil.

Treatment

Quinine or mefloquine or pyrimethamine/sulfoxine

Side effects of antimalarial drugs


Mefloquine

Retinopathy
Nausea, dizziness, and trouble sleeping, may rarely produce seizures
or psychiatric problems. Should al so be avoided in people with
certain heart conditions.

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AntiMalarial Drugs

Quinine

Headache, nausea, vomiting, visual disturbances, and ringing in the


ears-a condition known as cinchonism
Retinopathy

Atovaquone-proguanil

Nausea, vomiting, or abdominal pain and is not used in people with


poor kidney function, pregnant women, or infants.

Prevention: pyrimethamine-sulfadoxine or atovaquone-proguanil

Anti-malarial drugs Tips


Mefloquin prophylaxis:
Chloroquin resistant area prophylaxis is:
Chloroquin resistant area treatment:.
Plasmodium vivax and ovate infections, treatment must include
Cinchonism is caused by?
Chloroquine side effect include :

Abbrevation and Tenninology


I G6PD

I Glucose-6-phosphate dehydrogenase

Generic and Brand


Chloroquine
Prima uine
Oox c ckine
Meflo uine
Atovaauone- ro uaniJ.
Pvrimethamine

Ara;em
Radical cure
Adoxa Pak Adoxa. Alodox . Atridox Bio-Tab
Lariam
Malarone Malarone Pediatric
Oaraorim

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Travellers Diarrhea

43

Traveller's Diarrhea
Travellers diarrhea also known as infections diarrhea. Organisms commonly implicated in the
cause of Traveller's Diarrhea:
Escheri chia col i.
Shigella sp.
Compylobacter jejuni
Shigella diarrhea diarrhea characterized as dysentery (bloody diarrhea).
Effective drugs in the prevention of Traveller's Diarrhea:
Ciprofloxacin is the DOC for traveler's diarrhea.
Alternate DOC is Cotrimoxazole
Prevention~ Doxycycline or ciprofloxacin
Traveller to Thailand: Azithromycin is the DOC for traveler 's diarrhea
The antibiotic most commonJy recommended is ciprofloxacin.
Non prescription drugs:
Bismuth subsalicylate, a nonprescription drug. Causes black stools and tongue.
Loperamide (immodium): Treatment ofdiarrh"ea.
Bismuth subsalicylate can be used as prophylaxis or treatment. However loparamide is only used
upon appear of symptoms of diarrhea
When symptoms occur, treatment includes drinking plenty of fluids and eating a bland diet (for
example, cooked cereals, bananas, rice, applesauce, and toast). In addition, antib iotics (such as
ciprofloxacin) and antidiarrheal drugs (such as Lopramide or bismuth) are usually recommended.
Travelers are encouraged to seek medical care if they develop fever or blood in the stool.

Travellers diarrhea Tips


Travellers diarrhea commonly caused by
Prophylaxis of traveler d iarrhea include:
Ifpatient allergic to aspirin, what antidiarrheal drug should be avoided:
Loperamide belong what class of drug:
A patient currently taking over the counter antidiarrheal medication and notice black stools
and tongue, which drug can cause these symptoms?
What is the vaccine for traveler'S diarrhea and cholera?

Abbrevation and Tenninology


I DOC

I Drug of Choice

Generic and Brand


I Loperamide

I lmmodium

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AntiHelments Drugs

44

Anti-HelminthicDrugs
Helminthic
Spec ies

Diseases and medication


Common infections

Mode of
transmission

Treatment

Ascaris
lumbricoides

Round wonn

Ingestion

Pyrantel pamoate,
mebendazole

Necator
americanus

Hook wonn

Percutaneous

Pyrantel pamoate,
mebendazole

Trichuris trichuria

Whipwonn

Ingestion

Mebendazole

Enterobius
vermiculars

Pinwonn

Ingestioniinhalation

Strongyloides

Threadwonn

Ingestion

Pyrantel pamoate
Mebendazole
Thianendazole

Wuchereria
bancrofti

Filariasi s

Percutaneous

Diethylcarbamzine

Onchocerca
volvulus

River blindnessl
onchoceriasis

Percutaneous

Livermectin

Tri chinella spiral is

Trichinosis

Ingestion

Thiabendazole

Taenia solium

Pork

Ingestion

Niclosamide

Taenia saginata

beef

ingestion

Niclosamide

Diphyllobothrium
latum

Fish

ingestion

Niclosamide

Hymenolepis nana

Dwarf

Intestinal
nematodes

Tissue nematodes

Ceslodes
(tapewonns)

Praziquantel, niclosamide

Trematodes
(flukes)

Schistosoma
mansoni
Schistosoma
haematobium

Blood

Clonorchis sinesis

Liver

ingestion

Praziquantel

Fasciolopsis

Intestinal

Ingestion

Praziquantel

Pragonimus

Lung

Ingestion

Praziquantel

Percutaneous

bilharziasis

Praziquanlel
Praziquantel

Mebendazole:
Mechanism: Inhibits microtubule synthesis and glucose uptake in nematodes
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Anti-Helments Drugs

Clinical Use: Pinworm and wh ipworm infections


Contraindicated in pregnancy
Pyrantel pamoate:
Mechanism: Depolari zing neuromuscular blocker, which causes paralysis of nematodes.
Clinical use: Hookworm infections, pinworm infections, Roundworm.
Caution.:.Red color urine, feces, stains on vomiting.
Praziquantel:
Mechanism: Increase membrane pemteability to Ca2+ using muscular contraction and paralysis oflhe
nematode muscles.
Clinical Use: Drug of choice for Schistosomiasis, clonorchiasis, and pranom iasis.
Niclosamide:
Clinical Use: Infections from ingestion of beef, pork, and fish.

Anti-Helminth Drugs Tips


Pinworm infections cnn treated by:
Non-medical recommendation in patients with pinwonn infection include: Bathing every
morning, regular cleaning of undergannents, bedding etc. Handwash, during the fol lowing week
of treatment all family members should wear cotton underpants. Frequent wash ing oftoileLseats.
Which antihelmenthic drug can cause red color body fl uids, such as urine, saliva etc? Pyrantel
pamoate

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