Uchiyama Shinichiro
Department of Neurology, Tokyo Women's Medical University, Shinjuku-ku, Tokyo, Japan.
Brain Nerve. 2011 Apr;63(4):411-5.
Warfarin is underused because it has many disadvantages for clinical use despite it has been used more than a half century as an only oral anticoagulant. Dabigatran is a direct thrombin inhibitor, which is not metabolized by cytochrome P450, and thus does not require blood coagulation monitoring or vitamin K intake limitation, or produce drug interaction. RE-LY was a randomized controlled trial to prove non-inferiority of dabigatran to warfarin in 18,113 high risk patients with non-valvular atrial fibrillation. The results showed that stroke or systemic embolism was less frequent in patients on 150 mg dabigatran, major hemorrhage was less frequent in patients on 110 mg dabigatran, and hemorrhagic stroke was less frequent in patients on both 110 mg and 150 mg dabigatran than in patients on warfarin. Dabigatran is expected to be approved as a more effective and safer oral anticoagulant than warfarin for stroke prevention in patients with atrial fibrillation. Randomized controlled trials of many factor Xa inhibitors in comparison with warfarin are also ongoing in patients with atrial fibrillation.
华法林的使用未得到充分利用，因为尽管它作为唯一的口服抗凝剂已使用了半个多世纪，但在临床应用中有许多缺点。达比加群是一种直接凝血酶抑制剂，它不通过细胞色素P450代谢，因此不需要进行凝血监测或限制维生素K摄入，也不会产生药物相互作用。RE-LY是一项随机对照试验，旨在证明在18113例非瓣膜性房颤高危患者中，达比加群不劣于华法林。结果显示，服用150mg达比加群的患者中风或全身性栓塞的发生率较低，服用110mg达比加群的患者大出血的发生率较低，服用110mg和150mg达比加群的患者出血性中风的发生率均低于服用华法林的患者。预计达比加群将被批准为一种比华法林更有效、更安全的口服抗凝剂，用于预防房颤患者的中风。许多Xa因子抑制剂与华法林比较的随机对照试验也正在房颤患者中进行。
