a Institute of Cardiovascular Sciences , University of Birmingham , Birmingham , UK.
b Liverpool Centre for Cardiovascular Science , University of Liverpool and Liverpool Heart & Chest Hospital , Liverpool , UK.
Expert Opin Pharmacother. 2018 Dec;19(18):1999-2009. doi: 10.1080/14656566.2018.1537368. Epub 2018 Oct 25.
: Atrial fibrillation (AF) is associated with high morbidity and mortality rates due to thromboembolic complications, and anticoagulation is central to the management of this common arrhythmia to prevent acute thromboembolic events. The traditional anticoagulants: heparin, fondaparinux, and vitamin K antagonists (VKA, e.g. warfarin, acenocoumarol or phenprocoumin) have long served as pharmacotherapy for ischemic stroke prophylaxis. : In this review article, the authors provide an overview on current and emerging pharmacotherapy for ischemic stroke prevention. Furthermore, they review the data from novel therapeutic targets in the coagulation cascade, and investigational anticoagulant drugs currently assessed in preclinical and clinical studies. : The introduction of nonvitamin K antagonist oral anticoagulants (NOACs) was an important milestone, as these drugs show relative efficacy, safety, and convenience compared to the VKAs. Nevertheless, their clinical use still has some limitations with, for example, patients with severe renal impairment and those with mechanical heart valves, high bleeding risks, lack of standard laboratory monitoring and (some) reversal agents. To overcome some of these limitations, various attempts are now underway to discover new strategies and targets via the hemostatic pathway in order to develop new coagulation inhibiting drugs.
心房颤动(AF)与血栓栓塞并发症相关的高发病率和死亡率有关,抗凝治疗是管理这种常见心律失常以预防急性血栓栓塞事件的核心。传统的抗凝剂:肝素、磺达肝素和维生素 K 拮抗剂(VKA,如华法林、醋硝香豆素或苯丙香豆素)长期以来一直是预防缺血性中风的药物治疗方法。在这篇综述文章中,作者提供了当前和新兴的缺血性中风预防药物治疗的概述。此外,他们还回顾了凝血级联中的新治疗靶点的数据,以及目前正在临床前和临床研究中评估的新型抗凝药物。非维生素 K 拮抗剂口服抗凝剂(NOACs)的引入是一个重要的里程碑,因为与 VKA 相比,这些药物具有相对的疗效、安全性和便利性。然而,它们的临床应用仍然存在一些局限性,例如严重肾功能不全的患者、机械心脏瓣膜的患者、高出血风险、缺乏标准的实验室监测和(一些)逆转剂。为了克服其中的一些局限性,目前正在通过止血途径进行各种尝试,以发现新的策略和靶点,从而开发新的抗凝药物。