Department of Cardiology, Sarver Heart Center, University of Arizona, Tucson, Arizona, USA.
J Interv Cardiol. 2011 Jun;24(3):199-207. doi: 10.1111/j.1540-8183.2010.00613.x. Epub 2010 Dec 28.
Current clinical guidelines recommend dual antiplatelet agents namely aspirin and clopidogrel for the treatment of patients suffering from acute coronary syndrome (ACS). But the efficacy of clopidogrel is variable as it is a pro-drug, which has to be metabolized to become an active drug thus exhibiting variable platelet inhibition, increases risk of bleeding, stent thrombosis, and ischemia. To overcome this limitation, prasugrel was developed with increased antiplatelet activity thereby reducing the risk of myocardial ischemia and stent thrombosis. This action of prasugrel was associated with an increased risk of major bleeding. Finally, a novel reversible and direct-acting oral adenosine diphosphate (ADP) receptor antagonist, ticagrelor was developed that showed consistent and increased P2Y12 inhibition with similar incidence of bleeding but greater reduction in cardiac events compared to clopidogrel. The focus of this article is to review ticagrelor as a new class of P2Y12 inhibitor.
目前的临床指南推荐使用双重抗血小板药物,即阿司匹林和氯吡格雷,来治疗急性冠脉综合征(ACS)患者。但氯吡格雷的疗效存在差异,因为它是一种前体药物,必须代谢转化为活性药物,从而导致血小板抑制作用的变异性增加,出血、支架内血栓形成和缺血的风险增加。为了克服这一局限性,开发了普拉格雷,它具有更强的抗血小板作用,从而降低心肌缺血和支架内血栓形成的风险。普拉格雷的这种作用与大出血风险的增加有关。最后,开发了一种新型的可逆和直接作用的口服二磷酸腺苷(ADP)受体拮抗剂替卡格雷洛,与氯吡格雷相比,它显示出一致且更强的 P2Y12 抑制作用,出血发生率相似,但心脏事件的减少更多。本文的重点是回顾替卡格雷洛作为一种新型的 P2Y12 抑制剂。