Lega Jean-Christophe, Bertoletti Laurent, Durupt Stéphane, Epinat Magali, Mismetti Patrick, Da Costa Antoine, Laporte Silvy
Centre hospitalier Lyon-Sud, hospices civils de Lyon, Université Claude-Bernard Lyon 1, service de médecine interne et médecine vasculaire, Lyon, France; Université Jean-Monnet, EA3065, groupe de recherche sur la thrombose, 42023 Saint-Étienne, France.
Presse Med. 2013 Sep;42(9 Pt 1):1225-31. doi: 10.1016/j.lpm.2013.06.004. Epub 2013 Aug 1.
Vitamin K antagonists (VKA) had several decades of proven efficacy in AF-related stroke prevention but the drug's numerous limitations make its implementation difficult for practitioners and patients. The drawbacks of VKA have prompted the development of new oral anticoagulants (NOAC) that are at least as efficacious and safe as warfarin in phase III trials. Dabigatran (220 and 300mg/day), rivaroxaban (20mg/day) and apixaban (10mg/day) were proved to be non-inferior compared with warfarin in the prevention of bleeding, stroke and systemic embolism. Dabigatran 300mg/day and apixaban were found to be statistically superior to warfarin in stroke reduction. All these drugs reduced the risk of intracranial bleeding compared to warfarin. Dabigatran 220mg/day and apixaban decreased the risk of major bleeding. The limitation of NOAC was an increase of gastrointestinal bleeding by dabigatran 300mg/j and rivaroxaban and myocardial infarction by dabigatran. Practitioners must also be aware of the disadvantages of these new drugs when choosing NOAC for their patients with unstable INR.
维生素K拮抗剂（VKA）在预防房颤相关卒中方面已有数十年经证实的疗效，但该药物存在诸多局限性，这使得从业者和患者在应用时面临困难。VKA的缺点促使新型口服抗凝药（NOAC）的研发，这些药物在III期试验中至少与华法林一样有效且安全。达比加群（每日220毫克和300毫克）、利伐沙班（每日20毫克）和阿哌沙班（每日10毫克）在预防出血、卒中和全身性栓塞方面被证明不劣于华法林。发现达比加群每日300毫克和阿哌沙班在减少卒中方面在统计学上优于华法林。与华法林相比，所有这些药物均降低了颅内出血风险。达比加群每日220毫克和阿哌沙班降低了大出血风险。NOAC的局限性在于，达比加群每日300毫克和利伐沙班导致胃肠道出血增加，达比加群导致心肌梗死增加。在为国际标准化比值（INR）不稳定的患者选择NOAC时，从业者还必须了解这些新药存在的缺点。
