新型口服抗凝药达比加群酯特异性逆转剂idarucizumab

发布时间：2018-11-16 12:07

【摘要】：血栓栓塞性疾病的长期抗凝治疗一直是临床中的重要问题,新型口服抗凝药的问世,首次为房颤、深静脉血栓形成患者卒中和肺栓塞的预防提供了除华法林之外的选择。其中,达比加群酯为直接凝血酶抑制剂,多项研究已证实其疗效相较于华法林,具有起效快、相互作用少、无需定期监测等优势。但也存在一些劣势,如出现重大出血事件时缺乏相应的拮抗剂。idarucizumab是一种人源化单克隆抗体片段,可与达比加群特异性结合,从而逆转其抗凝效应,同时该抗体没有促凝作用。临床研究表明,静脉输注idarucizumab可在数分钟内逆转达比加群抗凝作用,主要不良反应包括头痛、低血钾、谵妄、便秘、发热和肺炎等。本文就idarucizumab的药理作用、药动学、临床研究及安全性作一阐述。
[Abstract]:Long-term anticoagulant therapy for thromboembolic diseases has been an important issue in clinical practice. The advent of new oral anticoagulants for the first time provides an alternative to warfarin for the prevention of stroke and pulmonary embolism in patients with atrial fibrillation and deep venous thrombosis. Among them, Darby plus group ester is a direct thrombin inhibitor. Many studies have proved that its efficacy compared with warfarin has the advantages of quick effect, less interaction and no need for regular monitoring. However, there are some disadvantages, such as the lack of corresponding antagonists in the event of major hemorrhage. Idarucizumab is a humanized monoclonal antibody fragment that can specifically bind to the Darbiga group, thus reversing its anticoagulant effect, while the antibody has no anticoagulant effect. Clinical studies have shown that intravenous infusion of idarucizumab can reverse the anticoagulant effect of Dac+ within a few minutes. The main adverse effects include headache hypokalemia delirium constipation fever and pneumonia. The pharmacological action, pharmacokinetics, clinical study and safety of idarucizumab are reviewed.
【作者单位】：中国医院科学院阜外医院药剂科;上海交通大学医学院附属仁济医院药剂科;
【基金】：上海医院药学科研项目(2014-YY-01-20)
【分类号】：R973.2

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