Ahmed Shameer, Levin Vadim, Malacoff Robert, Martinez Matthew W
Division of Cardiology, Lehigh Valley Health Network, Allentown, PA 18103, USA.
Cardiovasc Hematol Agents Med Chem. 2012 Jun;10(2):116-23. doi: 10.2174/187152512800388911.
For the last 60 years warfarin has been the cornerstone for chronic anticoagulation in prevention of ischemic strokes and systemic embolization. Warfarin therapy has several limitations including frequent monitoring and various food and significant drug interactions, which make it a less than ideal chronic oral anticoagulant. The continued search for safe, effective, medications with predictable pharmacokinetic profiles has led to newer alternatives. Dabigatran is a potent reversible, competitive direct thrombin inhibitor which is available as the prodrug, Dabigatran etexilate. It was first approved in Europe and recently in October 2010, the US food and drug administration (FDA) has approved the use of this novel oral anticoagulation for prevention of stroke in those with non valvular atrial fibrillation. This review will cover the chemical structure, mechanism of action, pharmacokinetic profile, clinical trials, dosage, clinical implication and adverse effects of dabigatran.
在过去60年里，华法林一直是预防缺血性中风和全身性栓塞的慢性抗凝治疗的基石。华法林治疗存在一些局限性，包括需要频繁监测、与多种食物及大量药物存在相互作用，这使其成为一种不太理想的慢性口服抗凝剂。对具有可预测药代动力学特征的安全、有效药物的持续探索催生了更新的替代药物。达比加群是一种强效、可逆、竞争性的直接凝血酶抑制剂，以其前体药物达比加群酯的形式存在。它首先在欧洲获批，最近在2010年10月，美国食品药品监督管理局（FDA）批准将这种新型口服抗凝剂用于预防非瓣膜性心房颤动患者的中风。本综述将涵盖达比加群的化学结构、作用机制、药代动力学特征、临床试验、剂量、临床意义及不良反应。
