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ANTIPLATELETS

By Gurleen

©PharmacologyCMC2008
INTRODUCTION

These are drugs which interfere with


platelet function.

Useful in the prophylaxis of


thromboembolic disorders.

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Formation of Platelet Plug

Platelets in contact with damaged vessel wall

Contractile proteins release granules (active subs)

Adhere to von Willibrand factor + Secretion of ADP


and TXA-2

Activation of other platelets Platelet plug

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Role of Platelets

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Platelet ADP receptors P2Y1 and P2Y12
play a vital role in platelet aggregation.

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DRUGS

Aspirin and other NSAIDS


Dipyridamole
Ticlopidine
Clopidogrel
Abciximab

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ASPIRIN
Acetylates and inhibits irreversibly the
enzyme Cyclooxygenase and TX-
synthetase.

TXA-2 formation suppressed at very low


doses (75-150 mg/day).

Higher doses (>900 mg/day) suppress


both TXA-2 and PGI-2 production.
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Continued…..

Other NSAIDs – reversible inhibitors of


COX , short lasting action.

Available as Colsprin, Disprin, Loprin,


Ecosprin

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Adverse effects of Aspirin

GI effects – Nausea , vomiting, epigastric


distress , peptic ulcer
Hypersensitivity – asthma, angioedema,
rashes.
Electrolyte imbalance
Reye’s Syndrome in children –
Encephalopathy and liver damage

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DIPYRIDAMOLE
Vasodilator .

Inhibits Phosphodiesterase and blocks


the uptake of adenosine , to increase
cAMP.

Hence increased PGI2 formation.


(PGI2 is an inhibitor of platelet aggregation)

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Continued……
Little clinical significance alone,
hence used with Warfarin.

Half life is 10-12 hrs , hepatic


metabolism

Dose- 75-100 mg 4 times/day .

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TICLOPIDINE
Alters surface receptor (Gi coupled P2Y-
12) on platelets .

Inhibits ADP and fibrinogen induced


platelet aggregation.

Synergistic effect on platelets with


Aspirin.

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Continued……
Well absorbed orally, metabolized in liver.

Half life is 8 hr after single dose ; 8 days


after multiple doses.

ADRs – Diarrhoea , vomiting, abd pain,


headache, tinnitus, skin rash, bleeding,
thrombocytopenia.
Dose – 250 mg twice daily
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Drug interactions of
Ticlopidine

 Anticoagulants or other antiplatelet


agents may increase the risk of bleeding

 Increases blood levels of Theophylline


and carbamezpene

 Decreases blood levels of Digoxin,


cyclosporine.
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CLOPIDOGREL
Similar mechanism of action as
Ticlopidine.

Lesser Side effects.

ADRs – diarrhoea , epigastric pain,


rashes.

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Drug interactions of
clopidogrel

 Macrolide antibiotics and Atorvastatin


may decrease the effects of clopidogrel

 Rifampicin increases the effect .

Dose - 300 mg loading dose  75 mg once


daily
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ABCIXIMAB
Glycoprotein IIb / IIIa antagonists.

GP IIb / IIIa is an adhesive receptor for


fibrinogen and von Willebrand factor.

Action exists for 12-24 hrs.

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Continued……..

ADRs – Hemorrhage, thrombocytopenia,


dyspepsia,constipation, ileus,
arrhythmias

Dose – 0.25 mg/kg iv

Other drugs – Eptifibatide, Tirofiban

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USES OF ANTIPLATELETS

Myocardial Infarction

Unstable Angina

Cerebrovascular Disease

Coronary bypass implants


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Continued………..

Prosthetic heart valves

AV shunts

Venous thromboembolism

Peripheral Vascular disease

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Thank You……

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