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非维生素K口服抗凝剂用于心房颤动:我们目前处于什么阶段?

Non-vitamin K oral anticoagulants in atrial fibrillation: Where are we now?

作者信息

Dzeshka Mikhail S, Lip Gregory Y H

机构信息

Centre for Cardiovascular Sciences, University of Birmingham, City Hospital, Birmingham, UK; Grodno State Medical University, Grodno, Belarus.

Centre for Cardiovascular Sciences, University of Birmingham, City Hospital, Birmingham, UK; Thrombosis Research Unit, Department of Clinical Medicine, Aalborg University, Aalborg, Denmark.

出版信息

Trends Cardiovasc Med. 2015 May;25(4):315-36. doi: 10.1016/j.tcm.2014.10.017. Epub 2014 Oct 30.

DOI:10.1016/j.tcm.2014.10.017
PMID:25440108
Abstract

Atrial fibrillation (AF) confers increased risk of stroke and other thromboembolic events, and oral anticoagulation therefore is the essential part of AF management to reduce the risk of these complications. Until recently, the vitamin K antagonists (VKAs, e.g., warfarin) were the only oral anticoagulants available, acting by decreased synthesis of vitamin K-dependent coagulation factors (II, VI, IX, and X). The VKAs had many limitations: delayed onset and prolonged offset of action, variability of anticoagulant effect among patients, multiple food and drug interactions affecting pharmacological properties of warfarin, narrow therapeutic window, and obligatory regular laboratory control, which all made warfarin "inconvenient" both for patients and clinicians. The limitations of VKAs led to development of a new class of drugs collectively defined as non-VKA oral anticoagulants (NOACs), which included direct thrombin inhibitors (dabigatran) and factor Xa inhibitors (rivaroxaban, apixaban, and edoxaban). The NOACs avoid many of the VKA drawbacks. In this review, we will focus on the current evidence justifying the use of NOACs in non-valvular AF.

摘要

心房颤动(AF)会增加中风和其他血栓栓塞事件的风险,因此口服抗凝治疗是房颤管理的重要组成部分,以降低这些并发症的风险。直到最近,维生素K拮抗剂(VKAs,如华法林)还是唯一可用的口服抗凝剂,其作用机制是减少维生素K依赖的凝血因子(II、VII、IX和X)的合成。VKAs有许多局限性:起效延迟和作用消退时间延长、患者之间抗凝效果存在差异、多种食物和药物相互作用影响华法林的药理特性、治疗窗狭窄以及必须定期进行实验室检查,所有这些都使得华法林对患者和临床医生来说都“不方便”。VKAs的局限性促使了一类新药物的开发,统称为非维生素K拮抗剂口服抗凝剂(NOACs),其中包括直接凝血酶抑制剂(达比加群)和Xa因子抑制剂(利伐沙班、阿哌沙班和依度沙班)。NOACs避免了许多VKA的缺点。在本综述中,我们将聚焦于支持在非瓣膜性房颤中使用NOACs的当前证据。

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Adv Ther. 2021 Jul;38(7):3771-3788. doi: 10.1007/s12325-021-01746-2. Epub 2021 May 25.
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Pharmacogenomics of CYP2C9: Functional and Clinical Considerations.CYP2C9的药物基因组学:功能与临床考量
J Pers Med. 2017 Dec 28;8(1):1. doi: 10.3390/jpm8010001.
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Dabigatran Etexilate: A Review in Nonvalvular Atrial Fibrillation.
达比加群酯:非瓣膜性心房颤动的研究进展。
Drugs. 2017 Mar;77(3):331-344. doi: 10.1007/s40265-017-0699-z.
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Edoxaban in venous thromboembolism and stroke prevention: an appraisal.依度沙班用于静脉血栓栓塞症及预防卒中:一项评估
Vasc Health Risk Manag. 2016 Feb 29;12:45-51. doi: 10.2147/VHRM.S81569. eCollection 2016.