Cardiovascular Medicine, Queens Medical Centre, University of Nottingham, Nottingham, NG7 2UH, UK.
Expert Rev Clin Pharmacol. 2012 May;5(3):257-69. doi: 10.1586/ecp.12.17.
Agents that inhibit platelet function are used routinely in the treatment and prevention of acute coronary syndromes. The main antiplatelet treatments used combine aspirin with one of the thienopyridine P2Y(12) antagonists, either clopidogrel or prasugrel. By blocking the synthesis of thromboxane A(2) in platelets and by blocking the effects of ADP, respectively, these agents reduce platelet activity, platelet aggregation and thrombus formation. Ticagrelor (marketed by AstraZeneca as Brilinta™ in the USA, and as Brilique(®) or Possia(®) in Europe) is a cyclopentyl-triazolo-pyrimidine, a new chemical class of P2Y(12) antagonist that is now approved for use in the wide spectrum of acute coronary syndromes. In this article we provide an overview of ticagrelor. We discuss the differences in mode of action compared with other P2Y(12) antagonists, examine its pharmacodynamic, pharmacokinetic and safety profile, and summarize the various clinical trials that have provided information on its efficacy in combination with aspirin. Ticagrelor appears to overcome some of the difficulties that have been encountered with other antiplatelet treatments, clopidogrel in particular.
抗血小板药物被广泛用于治疗和预防急性冠脉综合征。主要的抗血小板治疗方法是将阿司匹林与噻吩吡啶类 P2Y(12)拮抗剂之一（氯吡格雷或普拉格雷）联合使用。这些药物通过抑制血小板中环氧化酶（COX）的作用从而抑制血栓素 A2（TXA2）的合成，并通过阻断 ADP 的作用，从而减少血小板的活性、聚集和血栓形成。替格瑞洛（阿斯利康公司在美国以 BrilintaTM 上市，在欧洲以 Brilique(®)或 Possia(®)上市）是一种环戊基三唑嘧啶，是一种新型的 P2Y(12)拮抗剂，现已批准用于广泛的急性冠脉综合征。本文将对替格瑞洛进行概述。我们将讨论与其他 P2Y(12)拮抗剂相比，其作用机制的差异，研究其药效学、药代动力学和安全性特征，并总结了各种临床试验，这些临床试验提供了关于替格瑞洛与阿司匹林联合应用的疗效信息。替格瑞洛似乎克服了其他抗血小板治疗方法（特别是氯吡格雷）所遇到的一些困难。
