Aspirin-as an Antiplatelet

drug

-Dr. Bindira Maharjan

1st yr resident
Dept. of Clinical Pharmacology
Role of Platelets in Coagulation

• At sites of vascular injury, platelet aggregates

form the initial hemostatic plug
• Contribute to pathological thrombi that leads to
myocardial infarction, stroke and peripheral
arterial thrombosis
 Damage to
vascular PLATELET
endothelium ACTIVATION

Reactive proteins React with platelet

like collagen---- surface Glycoprotein Release of
exposed receptors (1a and 1b) proaggregatory
and
Binding of vasoconstrictory
Formation of fibrinogen and GPIIb/IIIa receptor mediators: TXA2,
Platelet plug vWF undergoes ADP, 5-HT
Platelet conformational
aggregation change
• In veins, due to sluggish blood flow a fibrinous tail is formed—traps
RBCs

• In arteries, Platelet mass the main constituent of the thrombus

• Antiplatelet drugs – most useful in arterial thrombosis

• Anticoagulants----venous thrombosis

• PGI2----synthesized in the intima of blood vessels : strong inhibitor of

platelet aggregation
Aspirin-as an antiplatelet drug

• Blocks the production of TXA2

• Irreversible Acetylation of serine residues near the active site of

platelet cyclooxygenases (COX-1)

• Action of aspirin on platelet COX-1 lasts for the lifetime of platelets

i.e 7-10 days

• Repeated dosed of aspirin------ cumulative effect on platelet function

• At 75 mg---- complete inactivation of platelet function

• Lower doses: Maximally effective as an antithrombotic agent

(50-325 mg/day)

• Higher doses: Anti-inflammatory effect .Inhibition of

Prostacyclin production (PGI2)

• Increase toxicity---- risk of bleeding

• Doses of 100 mg or less used for most indications

Bibliogaphy

• Brunton LL, Knollmann BC, Hilal-Dandan R. Goodman & Gilman’s: :

The Pharmacological Basis of Therapeutics /. 13th edition. New York,
N.Y.: McGraw-Hill Education LLC.; 2018.
• Tripathi KD. Essentials of medical pharmacology. Eight edition. New
Delhi: Jaypee Brothers Medical Publishers (P), Ltd; 2013. 1002 p.