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替格瑞洛:用于治疗急性冠脉综合征的综述。

Ticagrelor: a review of its use in the management of acute coronary syndromes.

机构信息

Adis, a Wolters Kluwer Business, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, North Shore 0754, Auckland, New Zealand.

出版信息

Drugs. 2011 May 7;71(7):909-33. doi: 10.2165/11206850-000000000-00000.

DOI:10.2165/11206850-000000000-00000
PMID:21568367
Abstract

Ticagrelor (Brilique™; Brilinta™), a cyclopentyl-triazolo-pyrimidine antiplatelet agent, is the first oral antagonist of the P2Y(12) receptor to offer reversible receptor binding. It is indicated in the EU for the prevention of atherothrombotic events in adults with acute coronary syndromes (ACS) [unstable angina pectoris, ST-segment elevation myocardial infarction [STEMI] or non-STEMI), including those managed medically or with percutaneous coronary intervention or coronary artery bypass grafting (CABG). Ticagrelor provides selective and reversible inhibition of adenosine diphosphate-induced platelet aggregation, with a faster onset and offset of action than that of clopidogrel, and is effective in the treatment of patients with ACS, with or without ST-segment elevation. In the large, randomized, double-blind, multicentre PLATO trial conducted in this patient population, ticagrelor was more effective than clopidogrel in terms of preventing ischaemic events over 12 months, providing a significantly lower risk of the primary composite endpoint of myocardial infarction, stroke or death from vascular causes, and was associated with an overall mortality benefit. The risk of major bleeding with ticagrelor, including bleeds related to CABG, did not differ from that seen with clopidogrel in this study, although ticagrelor was associated with more non-CABG-related major bleeds and fatal intracranial bleeding, albeit the latter bleeding events were rare. Further long-term and comparative efficacy and tolerability data are required to definitively position ticagrelor with respect to other antiplatelet agents, including prasugrel. However, the clinical data currently available indicate that ticagrelor is a promising option for the treatment of patients with ACS and may be of particular use in those at high risk of ischaemic events or unresponsive to clopidogrel.

摘要

替格瑞洛(Brilique™;Brilinta™),一种环戊基三唑嘧啶抗血小板药物,是第一个提供可逆受体结合的 P2Y(12)受体的口服拮抗剂。它在欧盟被批准用于预防成人急性冠脉综合征(ACS)[不稳定型心绞痛、ST 段抬高型心肌梗死[STEMI]或非 STEMI]的动脉血栓栓塞事件,包括接受药物治疗或经皮冠状动脉介入治疗或冠状动脉旁路移植术(CABG)的患者。替格瑞洛可选择性、可逆性抑制二磷酸腺苷诱导的血小板聚集,作用起始和消除快于氯吡格雷,对 ACS 患者,无论是否存在 ST 段抬高,均具有治疗作用。在这项针对该患者人群的大型、随机、双盲、多中心 PLATO 试验中,替格瑞洛在预防缺血事件方面优于氯吡格雷,12 个月时主要复合终点(心肌梗死、卒中和血管原因导致的死亡)的风险显著降低,且总体死亡率获益。在这项研究中,替格瑞洛与氯吡格雷相比,大出血风险(包括与 CABG 相关的出血)无差异,但替格瑞洛与更多非 CABG 相关的大出血和致命性颅内出血相关,尽管后者出血事件罕见。还需要进一步的长期和比较疗效和耐受性数据来明确替格瑞洛相对于其他抗血小板药物(包括普拉格雷)的地位。然而,目前可用的临床数据表明,替格瑞洛是治疗 ACS 患者的一种有前途的选择,可能对缺血事件风险高或对氯吡格雷无反应的患者特别有用。

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