达比加群及其逆转剂在心血管疾病中的研究进展

Dabigatran and Its Reversal Agent in Cardiovascular Diseases

新型口服抗凝药通过抑制凝血酶促反应中特定凝血因子的途径预防和治疗血栓,包括凝血酶抑制剂(达比加群)和凝血因子Ⅹa抑制剂(利伐沙班、阿哌沙班、依杜沙班等),主要用于非瓣膜性心房颤动、肺栓塞和关节置换术后深静脉血栓的预防和治疗等。达比加群可产生有效、可预测、稳定的抗凝效果,且较少与药物食物发生相互作用,无需常规进行凝血功能监测及剂量调整,临床应用更加方便。随着依达赛珠单抗的获批,达比加群成为第一种拥有特异性逆转剂的新型口服抗凝药,标志着抗凝治疗进入了一个新阶段。现将达比加群酯的药物作用机制、药物相互作用、在心血管疾病中的研究进展及其逆转剂做一简要综述。

New oral anticoagulants inhibit blood coagulation pathways in particular of the clotting factors,for example thrombin inhibitors(dabigatran etexilate)and blood coagulation factor Xa inhibitors(rivaroxaban,apixaban,edoxaban,etc.).It is mainly used for the prevention and treatment of non-valvular atrial fibrillation,pulmonary embolism and deep venous thrombosis after joint replacement.Dabigatran can produce effective,predictable and stable anticoagulant effect,and has less interaction with drug and food.No routine monitoring of coagulation function and dose adjustment are required,and it is more convenient for clinical application.With the approval of idarucizumab,dabigatran became the first new oral anticoagulants with a specific reversal agent,marking a new stage in anticoagulant therapy.The drug mechanism of action of dabigatran etexilate,drug interactions,its application in cardiovascular diseases and its reversal agents are now briefly reviewed.