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Antidotes for reversal of direct oral anticoagulants

机译:用于直接口服抗凝剂的逆转的解毒剂

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摘要

The main advantage of the direct oral anticoagulants over vitamin K antagonists is reduced rates of major bleeding, especially intracranial hemorrhage. While use of different clotting factor supplements have been used in patients with direct oral anticoagulant induced major bleeding or when there is need for urgent surgery, the lack of preclinical and clinical data are concerning. Idarucizumab is a specific antibody developed with a 350-fold greater affinity for dabigatran than its pharmacologic target thrombin. Andexanet is a modified factor Xa molecule that binds the direct and indirect Xa inhibitors without being enzymatically active. Ciraparantag, has potential to reverse the anticoagulant activity of multiple agents. The pharmacology, preclinical, and clinical data that have developed these specific antidotes are reviewed in this manuscript. (C) 2019 Elsevier Inc. All rights reserved.
机译:直接口服抗凝血剂对维生素K拮抗剂的主要优点降低了重大出血,特别是颅内出血的速率。 虽然使用不同的凝血因子补充剂,用于直接口服抗凝剂诱导的重大出血或需要紧急手术时,缺乏临床前和临床数据。 idarucizumab是一种特异性抗体,其具有比其药理学靶凝血酶更高的350倍更大的亲和力。 Andexanet是一种修饰的因子XA分子,其结合直接和间接XA抑制剂而不被酶促活性。 ciraparantag,有可能反转多个代理人的抗凝血活动。 在本手稿中审查了开发这些特异性解毒剂的药理,临床前和临床数据。 (c)2019 Elsevier Inc.保留所有权利。

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