Nemets Anatoly, Lishner Michael, Lugassy Gilles
Department of Hematology, Barzilai Medical Center, Ashkelon.
Harefuah. 2011 May;150(5):458-62, 490.
Anticoagulant therapy is based on two veteran drugs, which have been in use for over 60 years: heparin and warfarin. Due to the limitations of these agents, new parenteral anticoagulants have been introduced, mainly the low molecular weight heparins, fondaparinux and direct thrombin inhibitors. The need to develop new drugs has led to major efforts by the pharmaceutical industry and many promising anticoagulant oral agents are being tested. Ximelgatran has been withdrawn from the market after several cases of hepatotoxicity have been observed. Two oral agents, dabigatran and rivaroxaban, have recently been approved in Europe. Dabigatran inhibits thrombin, while rivaroxaban is factor X inhibitor. Other drugs include apixaban, idraparinux and are in Phase III studies.
抗凝治疗基于两种已使用超过60年的老牌药物:肝素和华法林。由于这些药物的局限性,新型胃肠外抗凝剂已被引入,主要是低分子量肝素、磺达肝癸钠和直接凝血酶抑制剂。开发新药的需求促使制药行业做出了巨大努力,许多有前景的口服抗凝剂正在进行试验。在观察到几例肝毒性病例后,希美加群已退出市场。两种口服药物,达比加群和利伐沙班,最近在欧洲获得批准。达比加群抑制凝血酶,而利伐沙班是X因子抑制剂。其他药物包括阿哌沙班、依达肝素,正处于III期研究阶段。