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比伐芦定:药理学与临床应用综述

Bivalirudin: a review of the pharmacology and clinical application.

作者信息

Van De Car David A, Rao Sunil V, Ohman E Magnus

机构信息

Duke University Medical Center, Division of Cardiology, 2301 Erwin Road, Durham, NC, USA.

出版信息

Expert Rev Cardiovasc Ther. 2010 Dec;8(12):1673-81. doi: 10.1586/erc.10.158.

Abstract

Among the current agents in the class of direct thrombin inhibitors, bivalirudin (Angiomax(®), The Medicines Company, NJ, USA) has seen increased use in cardiovascular medicine over the past decade through its primary indication as an anticoagulant used during percutaneous coronary interventions. Bivalirudin has been further investigated and used as the anticoagulation strategy in the setting of cardiac and endovascular surgical procedures and is frequently utilized in the management of patients with heparin-induced thrombocytopenia. In comparison with heparin, bivalirudin exhibits a low immunogenic profile and provides similar or reduced major bleeding rates as well as a predictable degree of anticoagulation that is dose related. Bivalirudin primarily undergoes dual elimination via proteolytic cleavage and renal elimination, and requires dose adjustment in the setting of severe renal dysfunction. Given the body of supportive data, bivalirudin is likely to continue to figure prominently as a reliable and efficient anticoagulation strategy. Additional agents in the class of direct thrombin inhibitors are under investigation and may find increasing clinical use.

摘要

在目前的直接凝血酶抑制剂类药物中,比伐卢定(Angiomax(®),美国新泽西州医药公司)在过去十年中,作为经皮冠状动脉介入治疗期间使用的抗凝剂这一主要适应症,在心血管医学中的应用有所增加。比伐卢定已被进一步研究,并作为心脏和血管内外科手术中的抗凝策略使用,且常用于肝素诱导的血小板减少症患者的管理。与肝素相比,比伐卢定具有低免疫原性,主要出血率相似或更低,抗凝程度与剂量相关且可预测。比伐卢定主要通过蛋白水解裂解和肾脏排泄进行双重消除,在严重肾功能不全的情况下需要调整剂量。鉴于有大量支持数据,比伐卢定可能会继续作为一种可靠且有效的抗凝策略而占据突出地位。直接凝血酶抑制剂类中的其他药物正在研究中,可能会在临床上得到更多应用。

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