Icahn School of Medicine at Mount Sinai, One Gustave L. Levy Place, PO Box 1030, New York, NY 10029, USA.
Nat Rev Cardiol. 2014 Dec;11(12):693-703. doi: 10.1038/nrcardio.2014.170. Epub 2014 Nov 4.
Vitamin K antagonists (VKAs) have long been the standard of care for treatment of venous thromboembolism (VTE), and thromboprophylaxis in atrial fibrillation (AF). Despite their efficacy, their use requires frequent monitoring and is complicated by drug-drug interactions and the need to maintain a narrow therapeutic window. Since 2009, novel oral anticoagulants (NOACs), including the direct thrombin inhibitor dabigatran and the direct factor Xa inhibitors apixaban, edoxaban, and rivaroxaban, have become alternative options to VKAs owing to their predictable and safe pharmacological profiles. The overall clinical effect of these drugs, which is a balance between ischaemic benefit and bleeding harm, varies according to the clinical scenario. As adjunctive therapy to dual antiplatelet therapy in patients with acute coronary syndrome, NOACs are associated with incremental bleeding risks and modest benefits. For treatment of VTE, NOACs have a safer profile than VKAs and a similar efficacy. In thromboprophylaxis in AF, NOACs are associated with the greatest benefits by reducing both ischaemic events and haemorrhagic complications and might reduce mortality compared with VKAs. The role of NOACs continues to evolve as these drugs are evaluated in different patient populations, including those with renal impairment or with AF and undergoing percutaneous coronary intervention.
维生素 K 拮抗剂 (VKAs) 长期以来一直是静脉血栓栓塞症 (VTE) 和心房颤动 (AF) 血栓预防的标准治疗方法。尽管它们具有疗效，但它们的使用需要频繁监测，并受到药物相互作用和需要维持狭窄治疗窗的复杂性的影响。自 2009 年以来，新型口服抗凝剂 (NOACs)，包括直接凝血酶抑制剂达比加群和直接因子 Xa 抑制剂阿哌沙班、依度沙班和利伐沙班，已成为 VKA 的替代选择，因为它们具有可预测和安全的药理学特性。这些药物的总体临床效果是缺血益处与出血危害之间的平衡，根据临床情况而有所不同。作为急性冠状动脉综合征患者双联抗血小板治疗的辅助治疗，NOACs 与增加的出血风险和适度的益处相关。对于 VTE 的治疗，NOACs 的安全性优于 VKAs，且疗效相似。在 AF 血栓预防中，NOACs 通过减少缺血事件和出血并发症带来最大益处，与 VKAs 相比可能降低死亡率。随着这些药物在不同患者群体中的评估，包括肾功能不全或接受经皮冠状动脉介入治疗的患者，NOAC 的作用仍在不断发展。
