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Direct thrombin inhibitors

机译:直接凝血酶抑制剂

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摘要

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.
机译:肝素和维生素K拮抗剂已成为某些心血管疾病和血栓栓塞性疾病抗凝的主要药物,已有50多年的历史了。然而,它们可能难以管理并且充满局限性。为响应对新型抗凝剂的需求,已开发并研究了直接凝血酶抑制剂(DTI)在预防和治疗静脉血栓栓塞(VTE),肝素诱导的血小板减少症(HIT),急性冠脉综合征(ACS),继发性凝血酶抑制剂方面的作用。预防ACS后的冠状动脉事件以及非瓣膜性房颤。目前,在北美,四种凝血酶活性的肠胃外直接抑制剂已获得FDA的批准:阿哌丁素,地西鲁丁,比伐卢定和阿加曲班。在新的口服DTI中,达比加群酯是这些药物中研究最多和最有前途的药物。这篇综述讨论了这些直接凝血酶抑制剂的临床适应症和功效以及抗凝治疗的未来方向。

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