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用于治疗缺血性心脏病患者的新型抗血小板疗法:血小板糖蛋白IIb/IIIa整合素受体抑制剂

Novel antiplatelet therapies for treatment of patients with ischemic heart disease: inhibitors of the platelet glycoprotein IIb/IIIa integrin receptor.

作者信息

Frishman W H, Burns B, Atac B, Alturk N, Altajar B, Lerrick K

机构信息

Department of Medicines, Albert Einstein College of Medicine/Montefiore Medical Center, Bronx, NY, USA.

出版信息

Am Heart J. 1995 Oct;130(4):877-92. doi: 10.1016/0002-8703(95)90091-8.

Abstract

Blood platelets play essential roles in normal coagulation and in coronary atherosclerotic disease and its complications. Various antiplatelet therapies, including aspirin, ticlopidine, and dipyridamole, have been developed for use in patients with known coronary artery artery disease to prevent ischemic complications. More recently a more complete anti-aggregation effect has been accomplished by the use of monoclonal antibodies and specific peptide and nonpeptide compounds that bind to the platelet GP IIb/IIIa surface receptor. This receptor becomes activated by platelet stimulation and binds fibrinogen molecules between platelets in the aggregation process. These new antiplatelet drugs are now being evaluated in clinical trials in patients undergoing balloon coronary angioplasty, in whom fewer ischemic events occur when the receptor blocker is used intravenously than with standard therapy, and in patients with stable and unstable angina. Excessive bleeding is an important problem with these agents, and efforts must be made to eliminate this side effect.

摘要

血小板在正常凝血以及冠状动脉粥样硬化疾病及其并发症中发挥着重要作用。已经研发出多种抗血小板疗法,包括阿司匹林、噻氯匹定和双嘧达莫,用于已知患有冠状动脉疾病的患者以预防缺血性并发症。最近,通过使用单克隆抗体以及与血小板糖蛋白IIb/IIIa表面受体结合的特定肽和非肽化合物,实现了更完全的抗聚集效果。该受体在血小板受到刺激时被激活,并在聚集过程中结合血小板之间的纤维蛋白原分子。目前正在对接受球囊冠状动脉成形术的患者进行这些新型抗血小板药物的临床试验评估,在这类患者中,静脉使用受体阻滞剂时发生的缺血事件少于标准治疗,同时也在对稳定型和不稳定型心绞痛患者进行评估。这些药物存在一个重要问题,即出血过多,必须努力消除这种副作用。

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