新型口服抗凝药物拮抗剂的研究进展

Progression of Specific Antidotes for New Oral Anticoagulants

华法林曾作为唯一的口服抗凝剂在临床应用上已逾60年。近年来,一批新型口服抗凝药物有取代华法林用于血栓栓塞性疾病和非瓣膜性心房颤动脑卒中预防和治疗的趋势,新型口服抗凝药物较华法林的优势在其药代动力学的可预测性,较少的食物与药物相互作用以及无需常规监测凝血指标等。虽然新型口服抗凝药物半衰期较短,多数情况下无需特异性拮抗剂,但在大出血或紧急手术时,缺乏拮抗剂使处理更为困难。目前,一些关于新型口服抗凝药物潜在特异性拮抗剂已在早期临床试验中表现出良好的疗效和安全性,现就其研究进展做简要综述。

Warfarin has been the only available oral anticoagulant for more than 60 years. During the past decade,several new oral anticoagulants（ NOACs） have been approved for the prophylaxis and treatment of thromboembolism and stroke prevention in patients with non-valvular atrial fibrillation,which will be treated as a substitute for warfarin. These new agents have several advantages over warfarin including; more predictable pharmacokinetics and pharmacodynamics,fewer food and drug interactions and a lack of need for routine coagulation monitoring. Specific antidotes for NOACs may not be needed in most situations due to their short half-life,yet the absence of antidotes for these agents may make the situation worse,especially in emergency situations such as life-threatening major bleeding or urgent surgery. Several potentially specific antidotes for NOACs have been developed and have shown promising in early clinical trials,evaluating their efficacy and safety. In this review,the progress made in developing specific antidotes for NOACs is summarized.