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血小板抑制药物:当前及未来的P2Y12受体拮抗剂

Platelet Inhibition Agents: Current and Future P2Y12 Receptor Antagonists.

作者信息

Tang Jie, Li Mu-Peng, Zhou Hong-Hao, Chen Xiao-Ping

机构信息

Department of Clinical Pharmacology, Xiangya Hospital, Central South University; Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University, Changsha, Hunan, 410008, P.R. China.

出版信息

Curr Vasc Pharmacol. 2015;13(5):566-77. doi: 10.2174/1570161112666141127162209.

Abstract

Percutaneous coronary intervention is widely used to reduce the risk of death or cardiovascular events in patients with acute coronary syndromes. Dual antiplatelet treatment with aspirin and clopidogrel has become routine practice to prevent thrombotic events after coronary surgery. Despite advances of significant reduction of thrombotic complications in this adjunctive therapy, major adverse cardiovascular events still occur, suggesting the need for development of novel antiplatelet agents that act as superior alternatives to current standard regimen. Recently developed antiplatelet agents (prasugrel, ticagrelor, cangrelor and elinogrel) efficiently antagonize P2Y12 receptor, a key platelet activating signaling pathway, and thereby inhibit aggregation induced by mediators such as ADP, collagen, thrombin and TXA2. We provide an evidence-based review on the pharmacological and clinical performance of clopidogrel and novel antiplatelet agents that antagonize P2Y12 receptors.

摘要

经皮冠状动脉介入治疗被广泛用于降低急性冠状动脉综合征患者的死亡风险或心血管事件风险。阿司匹林和氯吡格雷的双联抗血小板治疗已成为冠状动脉手术后预防血栓形成事件的常规做法。尽管在这种辅助治疗中血栓形成并发症显著减少,但主要不良心血管事件仍会发生,这表明需要开发新型抗血小板药物作为当前标准治疗方案的更优替代方案。最近开发的抗血小板药物(普拉格雷、替格瑞洛、坎格雷洛和依利格雷)可有效拮抗P2Y12受体,这是一条关键的血小板激活信号通路,从而抑制由ADP、胶原、凝血酶和血栓素A2等介质诱导的聚集。我们对氯吡格雷和拮抗P2Y12受体的新型抗血小板药物的药理作用和临床性能进行了循证综述。

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