Department of Pharmacy, Montefiore Medical Center, Bronx, NY 10461, USA.
Cardiol Rev. 2011 May-Jun;19(3):154-61. doi: 10.1097/CRD.0b013e3182137758.
For more than 5 decades, warfarin has been the mainstay of therapy when oral anticoagulation is required. It has been shown to be effective in the prevention as well as treatment of various thromboembolic disorders. However, drawbacks of warfarin, such as time-consuming requirements for frequent international normalized ratio monitoring, as well as drug and food interactions, have encouraged the development of alternative oral agents. One such agent, dabigatran, has risen up to the challenge. Due to its predictable anticoagulation response, dabigatran does not require routine anticoagulation monitoring. Another advantage dabigatran has over warfarin is its more favorable drug and food interaction profiles. Dabigatran was shown to be noninferior to warfarin in studies evaluating the prevention of stroke and systemic embolism in patients with atrial fibrillation, thus leading to the US Food and Drug Administration approval for this indication. Dabigatran has also demonstrated efficacy in the prevention of venous thromboembolism in patients undergoing total hip or knee replacement surgery as well as the prevention of recurrent venous thromboembolism, although these are not current Food and Drug Administration-approved indications. The safety profile appears to be similar to warfarin with regards to overall bleeding risk, though the risk for gastrointestinal bleeds was higher in patients on dabigatran 150 mg twice daily. Disadvantages of dabigatran may include a higher frequency of dyspepsia compared with warfarin, lack of dosing information in severe renal impairment, possible missed opportunities for periodic health examinations and interventions due to elimination of regular physician's visit for international normalized ratio monitoring, and drug costs. This article provides an overview of the clinical studies, pharmacokinetic profile, adverse effects, drug interactions as well as advantages and disadvantages associated with dabigatran.
50 多年来，华法林一直是需要口服抗凝治疗时的主要治疗方法。它已被证明在预防和治疗各种血栓栓塞性疾病方面有效。然而，华法林的缺点，如需要频繁进行国际标准化比值监测，以及药物和食物相互作用，促使人们开发替代的口服药物。达比加群就是其中一种。由于其抗凝反应可预测，达比加群不需要常规抗凝监测。达比加群相对于华法林的另一个优势是其更好的药物和食物相互作用谱。研究表明，在评估房颤患者预防中风和全身性栓塞的研究中，达比加群与华法林等效，从而导致美国食品和药物管理局批准了这一适应证。达比加群还在髋关节或膝关节置换手术患者的静脉血栓栓塞预防以及复发性静脉血栓栓塞预防中显示出疗效，尽管这些并非当前食品和药物管理局批准的适应证。在总体出血风险方面，其安全性与华法林相似，尽管每日两次服用 150mg 达比加群的患者胃肠道出血风险更高。达比加群的缺点可能包括与华法林相比消化不良的发生率更高，在严重肾功能损害患者中缺乏剂量信息，由于消除了定期进行国际标准化比值监测的医生就诊，可能会错过定期健康检查和干预的机会，以及药物费用较高。本文概述了达比加群的临床研究、药代动力学特征、不良反应、药物相互作用以及其优缺点。
