Department of Family and Preventive Medicine, UCSD School of Medicine, San Diego, CA 92121, USA.
Postgrad Med. 2011 Jan;123(1):73-9. doi: 10.3810/pgm.2011.01.2247.
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 P2Y(12) receptor-mediated platelet aggregation.
噻吩并吡啶类药物是血小板二磷酸腺苷受体拮抗剂，用于治疗和预防急性冠脉综合征患者的血栓事件。噻吩并吡啶类药物氯吡格雷的药代动力学特征导致其药代动力学和疗效反应高度可变。本文旨在简要概述普拉格雷和氯吡格雷的药代动力学，并讨论影响这些药物代谢的因素。临床研究表明，与氯吡格雷相比，普拉格雷与其他药物同时使用不太可能导致临床上有意义的药物相互作用。普拉格雷的变异基因型对其疗效无影响，这表明更多的患者在使用普拉格雷后将获得充分的血小板抑制作用。普拉格雷的有效代谢物的生成导致 P2Y(12)受体介导的血小板聚集的更大和更快抑制。
