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新旧抗凝药物:综述

Old and new anticoagulant drugs: a minireview.

机构信息

Scientific Direction, IRCCS Cà Granda Foundation Maggiore Policlinico Hospital, Milan, Italy.

出版信息

Ann Med. 2011 Mar;43(2):116-23. doi: 10.3109/07853890.2010.539250. Epub 2011 Jan 24.

Abstract

Abstract The limits of traditional anticoagulants, such as heparin and warfarin, have prompted the search for new agents for prophylaxis and treatment of arterial and venous thromboembolism, including factor Xa and thrombin inhibitors. These agents can be given orally, and their most significant advantage is that no laboratory monitoring is needed. The anti-Xa inhibitor rivaroxaban and the direct thrombin inhibitor dabigatran etexilate are licensed for prophylaxis of venous thromboembolism (VTE) in high-risk orthopedic surgery. They are at least as safe and effective as heparins but much more expensive. Dabigatran, rivaroxaban, and other agents currently in the pipeline of clinical development have the potential to replace warfarin in the two most frequent indications for anticoagulation, i.e. secondary prophylaxis of VTE and atrial fibrillation. Prevention and treatment of coronary artery thrombosis in patients with ischemic heart disease is another area of investigation for the role of new anticoagulants. These drugs have the potential to meet some currently unmet needs of traditional anticoagulants, but available clinical data warrant confirmation and expansion. Lack of specific antidotes for anticoagulation reversal and the high cost are important limitations of their use.

摘要

摘要 传统抗凝剂(如肝素和华法林)存在局限性,这促使人们寻找新的药物来预防和治疗动静脉血栓栓塞症,包括 Xa 因子和凝血酶抑制剂。这些药物可以口服给药,其最大优势是无需实验室监测。抗 Xa 因子抑制剂利伐沙班和直接凝血酶抑制剂达比加群酯已获准用于高危骨科手术患者的静脉血栓栓塞症(VTE)预防。它们与肝素相比至少同样安全有效,但价格昂贵得多。达比加群酯、利伐沙班和其他目前处于临床开发阶段的药物有可能替代华法林,成为抗凝治疗的两个最常见适应证,即 VTE 二级预防和心房颤动。新型抗凝剂在治疗缺血性心脏病患者的冠状动脉血栓形成方面也具有一定作用。这些药物有可能满足传统抗凝剂目前尚未满足的一些需求,但尚需确认和扩展现有临床数据。缺乏抗凝逆转的特异性解毒剂和高昂的成本是其应用的重要限制。

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