Department of Cardiology, Onze Lieve Vrouwe Gasthuis, 9 Oosterpark, Amsterdam, The Netherlands.
Fundam Clin Pharmacol. 2012 Feb;26(1):11-5. doi: 10.1111/j.1472-8206.2011.00979.x. Epub 2011 Aug 10.
Vitamin K antagonists have been used as oral anticoagulants (OACs) for over five decades, yet their use in real-world practice is problematic primarily because of their narrow therapeutic window, exacerbated by extensive food and drug interactions, necessitating regular coagulation monitoring and dose adjustment. Around half of patients receiving warfarin are within the therapeutic range, exposing them to the dangers of under-anticoagulation (i.e. thrombosis formation) or over-anticoagulation (i.e. bleeding). A new generation of OACs with improved pharmacology promises to revolutionize antithrombotic management. Rivaroxaban, apixaban (both oral direct Factor Xa inhibitors) and dabigatran (a direct thrombin inhibitor) all exhibit predictable anticoagulant responses and few drug-drug interactions and do not require routine coagulation monitoring.
维生素 K 拮抗剂作为口服抗凝剂(OACs)已经使用了五十多年,但它们在实际应用中存在问题,主要是因为它们的治疗窗狭窄,加上广泛的食物和药物相互作用,需要定期进行凝血监测和剂量调整。大约一半接受华法林治疗的患者处于治疗范围内,使他们面临抗凝不足(即血栓形成)或抗凝过度(即出血)的危险。新一代具有改善药理学特性的 OACs 有望彻底改变抗血栓治疗管理。利伐沙班、阿哌沙班(均为口服直接 Xa 因子抑制剂)和达比加群(直接凝血酶抑制剂)均表现出可预测的抗凝反应,且很少发生药物相互作用,无需常规凝血监测。