Pharmacokinetics, Drug Metabolism, and Safety of Prasugrel and Clopidogrel

Abstract

Thienopyridines are platelet adenosine diphosphate receptor antagonists used in the treatment and prevention of thrombotic events in patients with acute coronary syndrome. The pharmacokinetic profile of the thienopyridine clopidogrel has resulted in highly variable pharmacokinetics and efficacy responses. The purpose of this review is to provide a brief overview of the pharmacokinetics of prasugrel and clopidogrel and discuss factors that would influence the metabolism of those drugs. Clinical studies have shown that the coadministration of prasugrel with other drugs is less likely to result in clinically relevant pharmacokinetic drug interactions compared with clopidogrel. The lack of effect of variant genotypes on the efficacy of prasugrel suggests that more patients will receive adequate platelet inhibition after administration of prasugrel. The efficient generation of the active metabolite of prasugrel results in greater and more rapid inhibition of P2Y12 receptor-mediated platelet aggregation.

Keywords:

• clopidogrel
• drug interactions
• metabolism
• pharmacokinetics
• prasugrel