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Direct-Acting Oral Anticoagulants and Their Reversal Agents—An Update

机译:直接作用的口服抗凝药及其逆转剂—最新进展

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摘要

Over the last ten years, a new class of drugs, known as the direct-acting oral anticoagulants (DOACs), have emerged at the forefront of anticoagulation therapy. Like the older generation anticoagulants, DOACs require specific reversal agents in cases of life-threatening bleeding or the need for high-risk surgery. Published literature was searched, and information extracted to provide an update on DOACS and their reversal agents. The DOACs include the direct thrombin inhibitor—dabigatran, and the factor Xa inhibitors—rivaroxaban, apixaban, edoxaban, and betrixaban. These DOACs all have a rapid onset of action and each has a predictable therapeutic response requiring no monitoring, unlike the older anticoagulants, such as warfarin. Two reversal agents have been approved within the last five years: idarucizumab for the reversal of dabigatran, and andexanet alfa for the reversal of rivaroxaban and apixaban. Additionally, ciraparantag, a potential “universal” reversal agent, is currently under clinical development. A new generation of anticoagulants, the DOACs, and their reversal agents, are gaining prominence in clinical practice, having demonstrated superior efficacy and safety profiles. They are poised to replace traditional anticoagulants including warfarin.
机译:在过去的十年中,一类称为直接作用口服抗凝剂(DOAC)的新型药物出现在抗凝治疗的前沿。与上一代抗凝剂一样,DOAC在威胁生命的出血或需要高风险手术的情况下也需要特定的逆转剂。搜索出版的文献,提取信息以提供DOACS及其逆转代理的最新信息。 DOAC包括直接凝血酶抑制剂达比加群和因子Xa抑制剂利伐沙班,阿哌沙班,依多沙班和贝曲沙班。与较早的抗凝剂(如华法林)不同,这些DOAC均起效迅速,并且每种药物均具有可预测的治疗反应,无需监测。在过去的五年中,已经批准了两种逆转剂:依达昔单抗用于逆转达比加群,和安达沙坦阿尔法用于逆转利伐沙班和阿哌沙班。此外,西拉帕那坦(一种潜在的“通用”逆转剂)目前正在临床开发中。新一代的抗凝剂,DOAC及其逆转剂在临床实践中正变得越来越重要,已显示出卓越的功效和安全性。它们有望替代包括华法林在内的传统抗凝剂。

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