Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, USA.
Br J Clin Pharmacol. 2011 Oct;72(4):581-92. doi: 10.1111/j.1365-2125.2011.03916.x.
Heparins and vitamin K antagonists have been the primary agents used for anticoagulation in certain cardiovascular and thromboembolic diseases for over 50 years. However, they can be difficult to administer and are fraught with limitations. In response to the need for new anticoagulants, direct thrombin inhibitors (DTIs) have been developed and investigated for their utility in prophylaxis and treatment of venous thromboembolism (VTE), heparin-induced thrombocytopenia (HIT), acute coronary syndromes (ACS), secondary prevention of coronary events after ACS, and nonvalvular atrial fibrillation. Currently, four parenteral direct inhibitors of thrombin activity are FDA-approved in North America: lepirudin, desirudin, bivalirudin and argatroban. Of the new oral DTIs, dabigatran etexilate is the most studied and promising of these agents. This review discusses the clinical indications and efficacy of these direct thrombin inhibitors as well as future directions in anticoagulant therapy.
肝素和维生素 K 拮抗剂在过去 50 多年中一直是某些心血管和血栓栓塞性疾病中抗凝的主要药物。然而，它们的给药较为困难，并且存在许多限制。为了满足对新型抗凝剂的需求，已经开发并研究了直接凝血酶抑制剂（DTIs），以将其用于预防和治疗静脉血栓栓塞症（VTE）、肝素诱导的血小板减少症（HIT）、急性冠状动脉综合征（ACS）、ACS 后冠状动脉事件的二级预防和非瓣膜性心房颤动。目前，有四种肠外直接凝血酶活性抑制剂获得了北美 FDA 的批准：来匹卢定、地西卢定、比伐卢定和阿加曲班。在新型口服 DTIs 中，达比加群酯是研究最多且最有前途的药物。本文综述了这些直接凝血酶抑制剂的临床适应证和疗效，以及抗凝治疗的未来方向。
