Clopidogrel
Unchecked
Clopidogrel
Plavix
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Summary
Common uses
Acute coronary syndrome (with aspirin)0, Post-PCI dual antiplatelet therapy0, Secondary stroke prevention0, Peripheral arterial disease0
Pharmacy
Starting dose
75 mg PO once daily for maintenance; 300-600 mg PO loading dose in ACS or before PCI
Preparations
75 mg, 300 mg tablets
US FDA Max
75 mg/d maintenance (loading doses are single events)
Pharmacology
Routes
Oral
Onset
Antiplatelet effect within 2 hours of a loading dose; steady-state at 5-7 days of maintenance dosing
Duration
5-7 days (platelet lifespan; irreversible receptor binding)
Half-life
~6 hours (parent); active metabolite very short-lived but produces irreversible platelet effect[2]
Bioavailability
~50% (oral)[2]
Pregnancy
Limited data; weigh against alternatives (aspirin) where feasible.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Clopidogrel is a prodrug; CYP2C19 (primary) plus CYP3A4 and others bioactivate it to an unstable thiol metabolite that covalently and irreversibly binds the platelet P2Y12 ADP receptor, blocking ADP-mediated platelet activation, GPIIb/IIIa expression, and aggregation for the platelet's lifespan.0 CYP2C19 polymorphism is one of the most clinically actionable pharmacogenomic interactions in current cardiology: poor metabolizers generate insufficient active drug and have demonstrably worse outcomes after PCI; CPIC guidelines support alternative-agent therapy (prasugrel or ticagrelor) in those genotypes[1].
References
[edit | edit source]- ↑ CPIC Guideline for CYP2C19 and Clopidogrel, 2022. https://cpicpgx.org/guidelines/guideline-for-clopidogrel-and-cyp2c19/
- ↑ 2.0 2.1 FDA Prescribing Information, Plavix (clopidogrel bisulfate), Sanofi/Bristol-Myers Squibb, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020839s062lbl.pdf