Department of Medicine, McMaster University and Thrombosis and Atherosclerosis Research Institute, Hamilton, Ontario, Canada.
Drug Saf. 2011 Jun 1;34(6):449-63. doi: 10.2165/11587290-000000000-00000.
Dabigatran etexilate is a novel orally administered anticoagulant that exerts its action through reversible direct thrombin inhibition. This anticoagulant has been approved for prophylaxis against venous thromboembolism (VTE) after hip or knee arthroplasty, and in a few countries also for atrial fibrillation. This article reviews the efficacy and safety of dabigatran for the prophylaxis of VTE-indication compared with data on the most common current regimen with low-molecular-weight heparin (LMWH), specifically enoxaparin. Alternative prophylactic agents are also discussed. The results regarding efficacy and safety are very similar for dabigatran and LMWH. Bleeding and gastrointestinal reactions are the most frequently reported adverse events with a comparable incidence on LMWH and are probably the result of surgery and anaesthaesia. No adverse event that is specific for dabigatran has been observed in these studies, although dyspepsia has been reported as significantly more frequent than warfarin in long-term studies on other indications. The fact that dabigatran has no antidote has so far not been a problem in patients undergoing orthopaedic surgery. The use of the lower dose of dabigatran (150 mg) appears beneficial to reduce the risk of bleeding in patients over 75 years of age and in those with moderate renal impairment to avoid drug accumulation. The convenience of oral administration is an advantage for dabigatran over LMWH, particularly for extended prophylaxis up to 1 month after surgery. In conclusion, the benefit-risk profile of dabigatran is favourable for use as prophylaxis against VTE after major orthopaedic surgery with its convenient oral administration without need for laboratory monitoring and a low risk of bleeding or other adverse events.
达比加群酯是一种新型的口服抗凝药物,通过可逆性直接抑制凝血酶发挥作用。这种抗凝药物已被批准用于预防髋关节或膝关节置换术后的静脉血栓栓塞症(VTE),在一些国家也用于治疗心房颤动。本文回顾了达比加群预防 VTE 的疗效和安全性,并与最常用的低分子肝素(LMWH),特别是依诺肝素的数据进行了比较。还讨论了其他替代预防药物。达比加群和 LMWH 的疗效和安全性结果非常相似。出血和胃肠道反应是最常报告的不良事件,其发生率与 LMWH 相当,可能是手术和麻醉的结果。在这些研究中,没有观察到与达比加群特异性相关的不良事件,尽管在其他适应证的长期研究中,与华法林相比,消化不良的报告更为频繁。在接受骨科手术的患者中,达比加群没有解毒剂到目前为止还不是一个问题。达比加群较低剂量(150mg)的使用似乎有助于降低 75 岁以上患者和中度肾功能不全患者出血风险,避免药物蓄积。与 LMWH 相比,达比加群的口服给药方便,是其优势之一,特别是在手术后长达 1 个月的延长预防中。总之,达比加群预防骨科大手术后 VTE 的获益风险比是有利的,其口服给药方便,无需实验室监测,出血或其他不良事件的风险较低。