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Prasugrel: a new antiplatelet drug for the prevention and treatment of cardiovascular disease.

机译:普拉格雷:一种用于预防和治疗心血管疾病的新型抗血小板药物。

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摘要

Prasugrel, trade name Effient, is an investigational new antiplatelet drug currently under review for clinical use by the Food and Drug Administration. It is a thienopyridine analog with a structure similar to that of clopidogrel and ticlopidine. Thienopyridine derivatives inhibit platelet aggregation induced by adenosine diphosphate by irreversibly inhibiting the binding of adenosine diphosphate to the purinergic P2Y12 receptor on the platelet surface. Prasugrel has been shown to be a potent antiplatelet agent with a faster, more consistent, and greater inhibition of platelet aggregation compared with clopidogrel. It is debatable, however, how effectively these pharmacologic benefits will translate to clinical benefits. The results of the large TRITON-TIMI 38 trial, which compared prasugrel and clopidogrel in patients with acute coronary syndrome who were scheduled to receive coronary stents, demonstrated a significant reduction in ischemic events, including stent thrombosis, with prasugrel, but with an increased risk of major bleeding. The exact role of prasugrel in the management of ischemic heart disease is still being defined, but the risk:benefit ratio will likely play a major role in directing the best place for therapy with this new agent.
机译:普拉格雷(Prasugrel),商品名Effient,是一种正在研究中的抗血小板药物,目前正在由美国食品药品管理局(FDA)进行临床审查。它是噻吩并吡啶类似物,其结构类似于氯吡格雷和噻氯匹定。噻吩并吡啶衍生物通过不可逆地抑制二磷酸腺苷与血小板表面嘌呤能P2Y12受体的结合来抑制由二磷酸腺苷诱导的血小板聚集。与氯吡格雷相比,普拉格雷已被证明是一种有效的抗血小板药物,对血小板聚集具有更快,更一致和更大的抑制作用。然而,这些药理学益处如何有效地转化为临床益处尚有争议。 TRITON-TIMI 38大型试验的结果比较了普拉格雷和氯吡格雷在计划接受冠状动脉支架的急性冠脉综合征患者中的发生,结果表明普拉格雷可显着减少缺血事件,包括支架血栓形成,但风险增加大出血。普拉格雷在缺血性心脏病治疗中的确切作用仍在确定中,但是风险:获益比可能会在指导使用这种新药物的最佳治疗位置方面发挥重要作用。

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