Bounameaux H
Division of Angiology and Hemostasis, Department of Internal Medicine, University Hospitals of Geneva and Faculty of Medicine, Geneva, Switzerland.
Swiss Med Wkly. 2009 Feb 7;139(5-6):60-4. doi: 10.4414/smw.2009.12447.
During the past five decades, anticoagulant therapy has consisted of rapidly acting parenteral drugs (unfractionated heparin [UFH] low-molecular-weight heparins [LMWH]) for prevention of venous thromboembolism and initial treatment of arterial and venous thromboembolism, whereas vitamin K antagonists (VKA) are used for longer term oral treatment. These drugs act by indirectly inhibiting several activated plasma clotting factors (UFH, LMWH) or by blocking the synthesis of some of them (VKA). In recent years, compounds that specifically block activated coagulation factor X (FXa) or thrombin have been developed. Thus, fondaparinux, and its long-acting derivative idraparinux, are administered subcutaneously. These substances inhibit F Xa indirectly via antithrombin. Small molecules have also been developed that directly block FXa (rivaroxaban, apixaban) or thrombin (dabigatran etexilate) following oral administration. In the present review we discuss the currently available evidence supporting the use of these new anticoagulants, in particular rivaroxaban and dabigatran etexilate, in the setting of thromboprophylaxis following major orthopaedic surgery, and the broader perspectives that these new drugs may open up in the next few years.
在过去的五十年里，抗凝治疗包括使用起效迅速的肠外给药药物（普通肝素[UFH]、低分子肝素[LMWH]）来预防静脉血栓栓塞以及对动脉和静脉血栓栓塞进行初始治疗，而维生素K拮抗剂（VKA）则用于长期口服治疗。这些药物通过间接抑制几种活化的血浆凝血因子（UFH、LMWH）或通过阻断其中一些因子的合成（VKA）来发挥作用。近年来，已经开发出了特异性阻断活化凝血因子X（FXa）或凝血酶的化合物。因此，磺达肝癸钠及其长效衍生物依达肝素通过皮下给药。这些物质通过抗凝血酶间接抑制FXa。还开发出了一些小分子药物，口服后可直接阻断FXa（利伐沙班、阿哌沙班）或凝血酶（达比加群酯）。在本综述中，我们讨论了目前支持在大型骨科手术后的血栓预防中使用这些新型抗凝剂，特别是利伐沙班和达比加群酯的现有证据，以及这些新药在未来几年可能带来的更广阔前景。
