Siegal Deborah M, Cuker Adam
Division of Hematology and Thromboembolism, Department of Medicine, McMaster University, Hamilton, ON, Canada.
Department of Medicine, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA, USA; Department of Pathology and Laboratory Medicine, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA, USA.
Drug Discov Today. 2014 Sep;19(9):1465-70. doi: 10.1016/j.drudis.2014.05.013. Epub 2014 May 29.
Target-specific oral anticoagulants (TSOACs) provide safe and effective anticoagulation for the prevention and treatment of thrombosis in a variety of clinical settings by interfering with the activity of thrombin (dabigatran) or factor Xa (rivaroxaban, apixaban, edoxaban, betrixaban). Although TSOACs have practical advantages over vitamin K antagonists (VKAs), there are currently no antidotes to reverse their anticoagulant effect. Herein we summarize the available evidence for TSOAC reversal using nonspecific and specific reversal agents. We discuss important limitations of existing evidence, which is derived from studies in human volunteers, animal models and in vitro experiments. Studies evaluating the safety and efficacy of reversal agents on clinical outcomes such as bleeding and mortality in patients with TSOAC-associated bleeding are needed.
靶向特异性口服抗凝剂（TSOACs）通过干扰凝血酶（达比加群）或Xa因子（利伐沙班、阿哌沙班、依度沙班、贝曲沙班）的活性，在各种临床环境中为预防和治疗血栓形成提供安全有效的抗凝作用。尽管TSOACs相对于维生素K拮抗剂（VKAs）具有实际优势，但目前尚无逆转其抗凝作用的解毒剂。在此，我们总结了使用非特异性和特异性逆转剂进行TSOAC逆转的现有证据。我们讨论了现有证据的重要局限性，这些证据来自人体志愿者研究、动物模型和体外实验。需要开展评估逆转剂对TSOAC相关出血患者出血和死亡率等临床结局的安全性和有效性的研究。
