新型抗血小板药替卡格雷

Novel antiplatelet agent ticagrelor

替卡格雷为第一个可逆结合的、直接起效的、口服给药的血小板二磷酸腺苷P2Y12受体拮抗剂,比氯吡格雷起效更快,对血小板凝集的抑制作用更强。2011年7月20日,美国FDA批准替卡格雷用于降低急性冠脉综合征(acute coronary syndrome,ACS)患者的血栓性心血管事件的发生率。与氯吡格雷相比,替卡格雷起效更快,对血小板聚集的抑制作用更强,能显著降低心血管死亡、心肌梗死或卒中的发生率。在有效治疗的同时,替卡格雷并未显著增加主要出血事件的发生率。联合用药时,阿司匹林的维持剂量应为75～100 mg.d-1。本文对替卡格雷药理学特性、临床价值及不良反应进行综述。

Ticagrelor is the first reversible binding, direct-acting, oral adenosine diphosphate P2Y12 receptor antagonist that has a more rapid onset and more pronounced platelet inhibition than clopidogrel. On Jul 20, 2011, the U. S. Food and Drug Administration approved ticagrelor to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndromes （ACS） cardiovascular, myocardial infarction, or stroke than clopid agrelor gave a greater reduction in the death rate from ogrel. No significant difference in the rate of major bleeding was found between the ticagrelor and clopidogrel groups. After any initial dose, use with aspirin 75 - 100 mg·d^（-1）. This article reviews the pharmacological properties, clinical efficacy and adverse events of ticagrelor.