氨甲环酸未能逆转口服直接因子 Xa 抑制剂依度沙班的抗凝作用和出血。
Tranexamic Acid Failed to Reverse the Anticoagulant Effect and Bleeding by an Oral Direct Factor Xa Inhibitor Edoxaban.
机构信息
Rare Disease and LCM Laboratories, Tokyo, Japan.
Department of Medical Science, Tokyo, Japan.
出版信息
Pharmacology. 2018;101(1-2):92-95. doi: 10.1159/000484172. Epub 2017 Nov 3.
BACKGROUND/AIMS: Agents to reverse the anticoagulant effect of edoxaban, an oral direct factor Xa inhibitor, would be desirable in emergency situations. The aim of this study is to determine the effect of tranexamic acid, an antifibrinolytic agent, on the anticoagulant activity and bleeding by edoxaban in rats.
METHODS
A supratherapeutic dose of edoxaban (3 mg/kg) was intravenously administered to rats. Three minutes after dosing, tranexamic acid (100 mg/kg) was given intravenously. Bleeding was induced by making an incision with a blade on the planta 8 min after edoxaban injection and bleeding time was measured. Prothrombin time (PT) and clot lysis were examined.
RESULTS
A supratherapeutic dose of edoxaban significantly prolonged PT and bleeding time. Tranexamic acid did not affect PT or bleeding time prolonged by edoxaban, although tranexamic acid significantly inhibited clot lysis in rat plasma.
CONCLUSION
An antifibrinolytic agent tranexamic acid failed to reverse the anticoagulant effect and bleeding by edoxaban in rats.
背景/目的：在紧急情况下，需要一种能逆转依度沙班（一种口服直接 Xa 因子抑制剂）抗凝作用的药物。本研究旨在确定氨甲环酸（一种抗纤维蛋白溶解剂）对依度沙班在大鼠体内抗凝活性和出血的影响。
方法
给大鼠静脉注射超治疗剂量的依度沙班（3mg/kg）。给药 3 分钟后，静脉给予氨甲环酸（100mg/kg）。依度沙班注射 8 分钟后，用刀片在足底做切口诱导出血，并测量出血时间。检测凝血酶原时间（PT）和血栓溶解情况。
结果
超治疗剂量的依度沙班显著延长了 PT 和出血时间。氨甲环酸对依度沙班延长的 PT 或出血时间没有影响，尽管氨甲环酸显著抑制了大鼠血浆中的血栓溶解。
结论
抗纤维蛋白溶解剂氨甲环酸未能逆转依度沙班在大鼠体内的抗凝作用和出血。
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