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新型抗血小板治疗药物。

Novel agents for anti-platelet therapy.

机构信息

Department of Hematology, QiLu Hospital of Shandong University, Jinan, China PR.

出版信息

J Hematol Oncol. 2011 Nov 4;4:44. doi: 10.1186/1756-8722-4-44.

Abstract

Anti-platelet therapy plays an important role in the treatment of patients with thrombotic diseases. The most commonly used anti-platelet drugs, namely, aspirin, ticlopidine, and clopidogrel, are effective in the prevention and treatment of cardio-cerebrovascular diseases. Glycoprotein IIb/IIIa antagonists (e.g., abciximab, eptifibatide and tirofiban) have demonstrated good clinical benefits and safety profiles in decreasing ischemic events in acute coronary syndrome. However, adverse events related to thrombosis or bleeding have been reported in cases of therapy with glycoprotein IIb/IIIa antagonists. Cilostazol is an anti-platelet agent used in the treatment of patients with peripheral ischemia, such as intermittent claudication. Presently, platelet adenosine diphosphate P2Y(12) receptor antagonists (e.g., clopidogrel, prasugrel, cangrelor, and ticagrelor) are being used in clinical settings for their pronounced protective effects. The new protease-activated receptor antagonists, vorapaxar and atopaxar, potentially decrease the risk of ischemic events without significantly increasing the rate of bleeding. Some other new anti-platelet drugs undergoing clinical trials have also been introduced. Indeed, the number of new anti-platelet drugs is increasing. Consequently, the efficacy of these anti-platelet agents in actual patients warrants scrutiny, especially in terms of the hemorrhagic risks. Hopefully, new selective platelet inhibitors with high anti-thrombotic efficiencies and low hemorrhagic side effects can be developed.

摘要

抗血小板治疗在血栓性疾病患者的治疗中起着重要作用。最常用的抗血小板药物,即阿司匹林、噻氯匹定和氯吡格雷,在心脑血管疾病的预防和治疗中有效。糖蛋白 IIb/IIIa 拮抗剂(如阿昔单抗、依替巴肽和替罗非班)在减少急性冠脉综合征中的缺血事件方面显示出良好的临床获益和安全性。然而,在使用糖蛋白 IIb/IIIa 拮抗剂治疗时,已报告与血栓形成或出血相关的不良事件。西洛他唑是一种用于治疗外周缺血(如间歇性跛行)的抗血小板药物。目前,血小板二磷酸腺苷 P2Y(12)受体拮抗剂(如氯吡格雷、普拉格雷、坎格雷洛和替格瑞洛)在临床中因其显著的保护作用而被使用。新型蛋白酶激活受体拮抗剂,沃拉帕沙和阿托伐沙班,在不显著增加出血率的情况下,降低缺血事件的风险。一些正在进行临床试验的其他新型抗血小板药物也已被引入。事实上,新型抗血小板药物的数量正在增加。因此,这些抗血小板药物在实际患者中的疗效需要仔细研究,特别是在出血风险方面。希望能开发出具有高抗血栓形成效率和低出血副作用的新型选择性血小板抑制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/977a/3224753/879450628522/1756-8722-4-44-1.jpg

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