*Note increased bleeding risk is a potential side effect of all*
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Pharmacodynamics: Mechanism of action (MoA) Side effects (SE) |
Pharmacokinetics: Metabolism (M) Excretion (E) Duration (D) |
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Aspirin (irreversible) |
· MoA: Irreversible COX1&2 acetylation · ↓TXA2 production in platelet · Minimal effect on endothelial PGI2 at low dose · SE: bleeding peptic ulcer, nausea, Reye’s syndrome, toxicity -> metabolic acidosis |
· M: 80% (liver) · E: 20% (kidney) · D: 7 days (new platelets) |
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Dipyridamole |
· MoA: PDE inhibition -> ↑cAMP · MoA: potentiate PGI2 · SEs: bleeding headache, hypotension |
· M: live · E: bile · D: t1/2β 10 hours -> BD dose |
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Clopidogrel |
· Prodrug with active thiol metabolite · MoA: irreversible P2Y12 ADP receptor antagonist (ADPRA) · SE: bleeding, risk of failure (2C19 polymorphism) |
· M: 50% (2C19) · E: 50% (renal) · D: 7 days |
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Ticlopidine |
· Prodrug · MoA: irreversible P2Y12 ADPRA · SE: bleeding, TTP |
· M: liver · E: urine > bile · D: 7 days |
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Ticagrelor |
· MoA: Reversible P2Y12 ADPRA · Has an equipotent metabolite · SE: bleeding, dyspnoea (esp if asthma) |
· M: hepatic CYP3A4, 3A5 · E: bile > urine · D: 2 days |
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Abciximab |
· MoA: GPIIbIIIa mAb antagonist · SE: bleeding, ↓plt |
· M&E: reticulo-endothelial system · D: 2 days (prolonged binding) |
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Tirofiban |
· MoA: GPIIbIIIa inhibitor · SE: bleeding, ↓plt |
· M: nil · E: 66% urine, 33% bile · D: 8 hours |
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Prostacyclin |
· MoA: Gs GPCR -> ↑cAMP -> inhibit activation |
· M: liver, kidney, lung · D: very short (t1/2β 6 minutes) |
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Dextrans |
· MoA: ↓von Willebrand factor · SE: anaphylaxis, impair blood cross matching |
· M: nil? · E: renal · Duration: 6-8 hours for volume expansion, ? antiplatelet duration |