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Updated: Feb 23 2020

Antiplatelet Drugs

  • Aspirin (ASA)
    • Mechanism
      • acetylates and irreversibly inhibits cyclooxygenase in platelets
        • both COX-1 (more important) and COX-2
        • prevents conversion of arachidonic acid to thromboxane A2 (normally secreted by active platelets)
        • decreases platelet activation
      • ↑ bleeding time
      • PT and PTT unchanged
    • Clinical use
      • prevent MI
      • prophylaxis against clotting in atrial arrhythmias and stroke
      • analgesic
      • antipyretic
      • anti-inflammatory
      • low dose reduces the incidence of colon cancer
    • Toxicity
      • GI bleeding
      • Reye's syndrome
      • hyperventilation
      • tinnitus
        • affects CN VIII
  • ADP receptor antagonists (thienopyridines)
    • Drugs
      • ticlopidine
    • Mechanism
      • blocks ADP-mediated platelet aggregation which decreases Gp IIb/IIIa expression via the P2y12 receptor
        • via irreversible block of ADP receptors
          • activated platelets secrete ADP
      • prevents expression of glycoprotein IIb/IIIa by platelets
        • inhibits binding of fibrinogen and clot formation
    • Clinical use
      • alternative to ASA
        • reduce risk of thrombotic stroke
        • post-stent surgery
        • post-MI
        • acute coronary syndrome
        • unstable angina
    • Toxicity
      • neutropenia (ticlopidine)
      • thrombotic thrombocytopenic purpura (ticlopidine)
  • IIb/IIIa inhibitors
    • Drugs
      • abciximab
      • eptifibatide
      • tirofiban
    • Mechanism
      • monoclonal antibody antagonizes IIb/IIIa glycoprotein receptor on activated platelets
        • prevents platelet aggregation
    • Clinical use
      • acute coronary syndromes
      • percutaneous transluminal coronary angioplasty
    • Toxicity
      • bleeding
      • thrombocytopenia
  • PDE III inhibitors
    • Drugs
      • cilostazol
      • dipyridamole
    • Mechanism
      • phosphodiesterase III inhibitor
        • ↑ cAMP in platelets
          • inhibits aggregation
        • direct arterial vasodilation
    • Clinical use
      • intermittent claudication
      • prevention of stroke and TIA with aspirin
      • angina
    • Toxicity
      • nausea
      • headache
      • GI upset
      • palpitations
      • facial flushing
      • hypotension
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