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新型噻吩并吡啶类药物普拉格雷的临床概况

Clinical profile of prasugrel, a novel thienopyridine.

作者信息

Angiolillo Dominick J, Bates Eric R, Bass Theodore A

机构信息

Division of Cardiology, University of Florida College of Medicine-Jacksonville, Jacksonville, FL32209, USA.

出版信息

Am Heart J. 2008 Aug;156(2 Suppl):S16-22. doi: 10.1016/j.ahj.2008.06.005.

DOI:10.1016/j.ahj.2008.06.005
PMID:18657682
Abstract

Prasugrel (CS-747; LY-640315) is a novel, third-generation oral thienopyridine that is a specific, irreversible antagonist of the platelet adenosine 5'-diphosphate P2Y(12) receptor. Laboratory results with prasugrel support more potent antiplatelet effects, a lower incidence of interpatient variability in antiplatelet response, and a reduced time to onset of antiplatelet activity compared with clopidogrel. Phase II results indicate that prasugrel produces a greater antiplatelet effect than clopidogrel administered even at doses higher than the currently approved 300-mg loading dose and 75-mg/d maintenance dose. Recent phase III data show that prasugrel is superior to clopidogrel in preventing ischemic events in patients with acute coronary syndrome undergoing percutaneous coronary intervention, although this was associated with a greater risk of bleeding.

摘要

普拉格雷(CS - 747;LY - 640315)是一种新型的第三代口服噻吩并吡啶类药物,它是血小板腺苷5'-二磷酸P2Y(12)受体的特异性、不可逆拮抗剂。与氯吡格雷相比,普拉格雷的实验室结果显示其具有更强的抗血小板作用、患者间抗血小板反应变异性更低以及抗血小板活性起效时间缩短。II期研究结果表明,即使给予高于目前批准的300mg负荷剂量和75mg/天维持剂量的普拉格雷,其产生的抗血小板作用仍比氯吡格雷更强。近期的III期数据显示,在接受经皮冠状动脉介入治疗的急性冠状动脉综合征患者中,普拉格雷在预防缺血事件方面优于氯吡格雷,尽管这与更高的出血风险相关。

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