Dhillon Sohita
Springer, Private Bag 65901, Mairangi Bay, 0754, Auckland, New Zealand,
Am J Cardiovasc Drugs. 2015 Feb;15(1):51-68. doi: 10.1007/s40256-015-0108-5.
Ticagrelor (Brilique™, Brilinta®), a cyclopentyl-triazolopyrimidine, is an orally active, reversible, and selective adenosine diphosphate (ADP) receptor antagonist indicated for use in patients with acute coronary syndromes (ACS). Ticagrelor has a faster onset of action and provides greater inhibition of platelet aggregation than clopidogrel. In the large well-designed, PLATO study in adult patients with ACS, 12 months' treatment with ticagrelor was more effective than clopidogrel in reducing the incidence of the primary composite endpoint of myocardial infarction, stroke, or cardiovascular (CV) death. Ticagrelor also reduced all-cause mortality relative to clopidogrel, although statistical significance of this was not confirmed in hierarchical testing. Benefit with ticagrelor was seen both in invasively and noninvasively managed patients. Ticagrelor was generally well tolerated and was not associated with an increased risk of major bleeding relative to clopidogrel. However, the incidences of non-coronary artery bypass grafting (CABG)-related bleeding, and major or minor bleeding, as well as some non-hemorrhagic adverse events, including dyspnea (usually of mild or moderate severity) and ventricular pauses (largely asymptomatic) were higher with ticagrelor. In addition, the ATLANTIC study showed that although pre-hospital administration of ticagrelor did not improve pre-percutaneous coronary intervention (PCI) coronary reperfusion in ACS patients relative to in-hospital administration, ticagrelor was safe in both instances, with no significant between-group differences in non-CABG-related major and minor bleeding events. Although further comparative studies with other antiplatelet agents, including prasugrel, are required to position it more definitively, current evidence indicates that ticagrelor is a useful option for the prevention of thrombotic CV events in ACS patients managed invasively or noninvasively.
替格瑞洛(倍林达™,Brilinta®),一种环戊基三唑并嘧啶,是一种口服活性、可逆且选择性的二磷酸腺苷(ADP)受体拮抗剂,适用于急性冠脉综合征(ACS)患者。与氯吡格雷相比,替格瑞洛起效更快,对血小板聚集的抑制作用更强。在针对成年ACS患者进行的精心设计的大型PLATO研究中,替格瑞洛治疗12个月在降低心肌梗死、中风或心血管(CV)死亡的主要复合终点发生率方面比氯吡格雷更有效。与氯吡格雷相比,替格瑞洛也降低了全因死亡率,尽管在分层检验中这一点未得到统计学证实。在接受侵入性和非侵入性治疗的患者中均观察到了替格瑞洛的获益。替格瑞洛总体耐受性良好,与氯吡格雷相比,未增加大出血风险。然而,替格瑞洛导致的非冠状动脉旁路移植术(CABG)相关出血、大出血或小出血的发生率,以及一些非出血性不良事件,包括呼吸困难(通常为轻度或中度)和心室停搏(大多无症状)均较高。此外,ATLANTIC研究表明,尽管相对于院内给药,院前给予替格瑞洛在ACS患者经皮冠状动脉介入治疗(PCI)前并未改善冠状动脉再灌注,但在这两种情况下替格瑞洛都是安全的,在非CABG相关的大出血和小出血事件方面组间无显著差异。尽管需要与其他抗血小板药物(包括普拉格雷)进行进一步的比较研究以更明确地定位它,但目前的证据表明,替格瑞洛是预防接受侵入性或非侵入性治疗的ACS患者血栓性CV事件的一个有用选择。