Prescrire Int. 2012 Sep;21(130):201-2, 204.
The standard anticoagulant for prevention of venous thromboembolism in patients undergoing hip or knee replacement surgery is a low-molecular-weight heparin (LMWH) such as subcutaneous enoxaparin. Apixaban is the second oral factor Xa inhibitor, after rivaroxaban, to be approved in the European Union for use in these two situations. Three double-blind randomised trials versus enoxaparin in a total of nearly 12 000 patients failed to show that apixaban was more effective in terms of relevant endpoints: mortality, and the incidence of pulmonary embolism and symptomatic deep vein thrombosis. The incidence of bleeding did not differ between the apixaban and enoxaparin groups under the conditions of these trials. Apixaban is mainly metabolised by cytochrome P450 isoenzymes CYP 3A4 and 3A5 and also binds to P-glycoprotein, resulting in a high potential for pharmacokinetic interactions. Renal failure is a risk factor for overdose. Pharmacodynamic interactions are also likely. There is no known antidote for apixaban. In practice, LMWH remains the standard treatment.
在接受髋关节或膝关节置换手术的患者中,预防静脉血栓栓塞的标准抗凝剂是低分子量肝素(LMWH),如皮下注射依诺肝素。阿哌沙班是继利伐沙班之后,第二种在欧盟获批用于这两种情况的口服Xa因子抑制剂。三项针对近12000名患者的双盲随机试验,比较了阿哌沙班与依诺肝素,结果未能表明阿哌沙班在相关终点(死亡率、肺栓塞和有症状的深静脉血栓形成的发生率)方面更有效。在这些试验条件下,阿哌沙班组和依诺肝素组的出血发生率没有差异。阿哌沙班主要通过细胞色素P450同工酶CYP 3A4和3A5代谢,并且还与P-糖蛋白结合,导致药代动力学相互作用的可能性很高。肾衰竭是过量用药的一个危险因素。药效学相互作用也很可能发生。目前尚无已知的阿哌沙班解毒剂。在实际应用中,低分子量肝素仍然是标准治疗方法。