clopidogrel

Pharmacokinetics

Absorption: Well absorbed following oral administration; rapidly metabolized to an active antiplatelet compound. Parent drug has no antiplatelet activity.

Distribution: Unknown.

Protein Binding: Clopidogrel—98%; active metabolite—94%.

Metabolism and Excretion: Rapidly and extensively converted by the liver (CYP2C19) to its active metabolite, which is then eliminated 50% in urine and 45% in feces;2% of Whites, 4% of Blacks, and 14% of Asians have CYP2C19 genotype that results in reduced metabolism of clopidogrel (poor metabolizers) into its active metabolite (may result in ↓ antiplatelet effects).

Half-life: 8 hr (active metabolite).

TIME/ACTION PROFILE (effects on platelet function)