Department of Clinical Pharmacy Practice, College of Pharmacy and Health Sciences, St. John's University, Queens, NY 11439, USA.
Cardiol Rev. 2013 Jul-Aug;21(4):207-12. doi: 10.1097/CRD.0b013e318293d6e6.
Atrial fibrillation (AF) is an independent risk factor for ischemic stroke occurrence, severity, recurrence, and mortality. Anticoagulation therapy for the prevention of thromboembolism is critical in patients with AF who are at risk of stroke. Warfarin has been an efficacious anticoagulant for this purpose, but its use has been limited by frequent laboratory monitoring, drug interactions, unpredictable individual response, delayed onset of action, and bleeding. Apixaban is the second oral direct selective factor Xa inhibitor approved for the prevention of stroke/systemic embolism in patients with nonvalvular AF. It was significantly better than aspirin in reducing stroke (ischemic or hemorrhagic) or systemic embolism without increasing the risk of major bleeding in patients with AF who were at increased risk of stroke and for whom warfarin was unsuitable. In a randomized, double-blind trial that was originally designed to test for noninferiority, apixaban was superior to warfarin (target international normalized ratio 2-3) in preventing stroke or systemic embolism, caused less bleeding, and resulted in lower mortality in patients with AF. Apixaban has a half-life of about 12 hours, and the normal dosage is 5 mg orally twice daily. However, it may be reduced to 2.5 mg twice daily based on individual factors of the patient (age, renal function, and body weight) and the concomitant use of potent dual inhibitors of cytochrome P450 3A4 and P-glycoprotein. Similar to other novel oral anticoagulants (dabigatran and rivaroxaban), apixaban has no reversal agent for its anticoagulant effect. Overall, apixaban is a safe and efficacious alternative for stroke prophylaxis in high-risk patients who have AF and who are unable to achieve therapeutic goals with warfarin therapy.
心房颤动(AF)是缺血性卒中发生、严重程度、复发和死亡的独立危险因素。对于有卒中风险的 AF 患者,抗凝治疗预防血栓栓塞至关重要。华法林一直是一种有效的抗凝药物,但由于需要频繁的实验室监测、药物相互作用、不可预测的个体反应、起效延迟和出血风险,其应用受到限制。阿哌沙班是第二种获批用于预防非瓣膜性心房颤动患者卒中/全身性栓塞的口服直接选择性 Xa 因子抑制剂。与阿司匹林相比,它在降低卒中(缺血性或出血性)或全身性栓塞风险方面更优,且不增加大出血风险,适用于有卒中高风险且不适合使用华法林的 AF 患者。在一项最初设计用于检验非劣效性的随机、双盲试验中,阿哌沙班在预防卒中或全身性栓塞方面优于华法林(目标国际标准化比值 2-3),导致更少的出血,且降低了 AF 患者的死亡率。阿哌沙班的半衰期约为 12 小时,常规剂量为每日口服 5 mg,2 次。然而,根据患者的个体因素(年龄、肾功能和体重)和同时使用强效细胞色素 P450 3A4 和 P-糖蛋白双重抑制剂,其剂量可能会减少至每日 2.5 mg,2 次。与其他新型口服抗凝剂(达比加群和利伐沙班)类似,阿哌沙班没有逆转其抗凝作用的逆转剂。总体而言,阿哌沙班是一种安全有效的替代华法林治疗的选择,适用于有 AF 且无法通过华法林治疗达到治疗目标的高危患者。