Danielak Dorota, Karaźniewicz-Łada Marta, Główka Franciszek
a Department of Physical Pharmacy and Pharmacokinetics , Poznan University of Medical Sciences , Poznań , Poland.
Expert Opin Pharmacother. 2018 Feb;19(2):103-112. doi: 10.1080/14656566.2017.1421634. Epub 2017 Dec 27.
Ticagrelor is a first drug of a new chemical class cyclopentyltriazolopyrimidines. It is an antiplatelet agent with a unique mechanism of action, allowing a direct and reversible competitive inhibition of P2Y receptor. According to newest guidelines, it is recommended for prevention of thrombotic events in patients with acute coronary syndromes. Moreover, it is preferred over clopidogrel, an older generation antiplatelet drug, and therefore gains more interest in modern cardiology and vascular medicine.
This review is a comprehensive and thorough summary of the most important findings on ticagrelor. Pharmacokinetics, pharmacogenetics, drug-drug interactions, adverse effects, efficacy in specific patient populations and off-label properties of ticagrelor are discussed in this paper. Moreover, the results from pivotal clinical trials are presented.
Introduction of ticagrelor, a first directly-acting and reversible P2Y inhibitor, gave some new possibilities as the efficacy of older drugs was often insufficient. Despite some drawbacks, such as a risk of bleeding events or dyspnea, a rapid onset of action, consistency in the antiplatelet effect and reports on pleiotropic properties make this drug a promising candidate for a first-choice antiplatelet agent in patients with acute coronary events.
替格瑞洛是新型化学类别环戊基三唑并嘧啶类的首个药物。它是一种具有独特作用机制的抗血小板药物,能直接且可逆地竞争性抑制P2Y受体。根据最新指南,推荐其用于预防急性冠状动脉综合征患者的血栓形成事件。此外,相较于 older generation 抗血小板药物氯吡格雷,它更受青睐,因此在现代心脏病学和血管医学中受到更多关注。
本综述全面且深入地总结了替格瑞洛的最重要研究结果。本文讨论了替格瑞洛的药代动力学、药物遗传学、药物相互作用、不良反应、在特定患者群体中的疗效以及超说明书用药特性。此外,还展示了关键临床试验的结果。
首个直接作用且可逆的P2Y抑制剂替格瑞洛的引入带来了一些新的可能性,因为 older drugs 的疗效往往不足。尽管存在一些缺点,如出血事件风险或呼吸困难,但起效迅速、抗血小板作用的一致性以及有关多效性的报道使该药物成为急性冠状动脉事件患者首选抗血小板药物的有前景候选者。