Francia Pietro, Adduci Carmen, Santini Daria, Musumeci Beatrice, Tocci Giuliano
Division of Cardiology, Department of Clinical and Molecular Medicine, University of Rome Sapienza, Sant'Andrea Hospital, Via di Grottarossa 1035, 00189 Rome, Italy.
High Blood Press Cardiovasc Prev. 2013 Jun;20(2):53-60. doi: 10.1007/s40292-013-0011-6. Epub 2013 May 8.
Atrial fibrillation (AF) is associated with an increased risk of embolic stroke. Dose-adjusted vitamin K antagonists (VKAs) to a target international normalized ratio (INR) range of 2.0-3.0 reduce the risk of ischemic stroke and are currently recommended in all patients with AF at moderate-high risk for stroke or systemic embolism. However, VKAs have several drawbacks, including unpredictable anticoagulant response, food and drug interactions, need for regular laboratory monitoring and dose adjustment. These limitations prompted the introduction of new oral anticoagulants (NOA) that target thrombin and factor Xa, key-enzymes in the coagulation pathway. NOA have predictable pharmacodynamics, allowing fixed dosing without the need of laboratory monitoring, and have few drug and food interactions. The present review focuses on pharmacological properties, safety, and appropriate clinical use of dabigatran, rivaroxaban and apixaban.
心房颤动(AF)与栓塞性中风风险增加相关。剂量调整后的维生素K拮抗剂(VKA)使国际标准化比值(INR)达到2.0 - 3.0的目标范围可降低缺血性中风风险,目前推荐用于所有中度至高度中风或全身性栓塞风险的房颤患者。然而,VKA有几个缺点,包括抗凝反应不可预测、食物和药物相互作用、需要定期实验室监测和剂量调整。这些局限性促使了新型口服抗凝药(NOA)的引入,其作用靶点为凝血酶和Xa因子,这两种是凝血途径中的关键酶。NOA具有可预测的药效学特性,允许固定剂量给药而无需实验室监测,并且药物和食物相互作用较少。本综述重点关注达比加群、利伐沙班和阿哌沙班的药理学特性、安全性及适当的临床应用。