Department of Pharmacy Practice, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, MC 886, Room 164, Chicago, IL 60612, USA.
Am J Health Syst Pharm. 2012 Jul 1;69(13):1113-26. doi: 10.2146/ajhp110418.
The pharmacology, pharmacokinetics, efficacy, and safety of apixaban are reviewed.
Apixaban is an oral, direct, selective factor Xa inhibitor with a rapid onset of action. It has a plasma elimination half-life of 12 hours and has been administered in a twice-daily dosing regimen in clinical trials without the need for anticoagulation monitoring or dosage adjustment. Apixaban has multiple elimination pathways, and its pharmacokinetics is not substantially altered by patient age, sex, race, or ethnicity. The results of three Phase III trials indicated that apixaban was similar to or more effective than enoxaparin for preventing venous thromboembolism (VTE) in patients undergoing total hip or knee replacement, with similar or lower rates of bleeding. Two Phase III trials found that apixaban was more effective for stroke prevention than either aspirin or warfarin in patients with atrial fibrillation (AF), with a similar (versus aspirin) or improved (versus warfarin) safety profile. A Phase III trial evaluating apixaban plus antiplatelet monotherapy or dual-antiplatelet therapy in patients with acute coronary syndrome ended early due to clear evidence of a clinically important increase in bleeding among patients randomized to apixaban without any meaningful reduction in ischemic events. The adverse-event profiles for apixaban and comparators have been similar in studies conducted to date.
Apixaban, a new anticoagulant, appears to offer an efficacy and safety profile comparable with that of enoxaparin for preventing VTE after orthopedic surgery, with the advantage of oral administration. In patients with AF, apixaban is more effective than either warfarin or aspirin for stroke prevention, with an acceptable safety profile.
综述阿哌沙班的药理学、药代动力学、疗效和安全性。
阿哌沙班是一种口服、直接、选择性的因子 Xa 抑制剂，起效迅速。其血浆消除半衰期为 12 小时，在临床试验中每日两次给药，无需抗凝监测或剂量调整。阿哌沙班有多种消除途径，其药代动力学不受患者年龄、性别、种族或民族的显著影响。三项 III 期临床试验的结果表明，阿哌沙班在预防全髋关节或全膝关节置换术后静脉血栓栓塞症（VTE）方面与依诺肝素相似或更有效，出血率相似或更低。两项 III 期临床试验发现，阿哌沙班在预防房颤（AF）患者中风方面比阿司匹林或华法林更有效，具有相似（与阿司匹林相比）或改善（与华法林相比）的安全性。一项评估阿哌沙班联合抗血小板单药或双联抗血小板治疗急性冠脉综合征患者的 III 期试验因阿哌沙班组患者出血明显增加而提前终止，而缺血事件无任何有意义减少，这表明有临床意义的增加。迄今为止进行的研究中，阿哌沙班和对照药物的不良事件谱相似。
新型抗凝剂阿哌沙班似乎在预防骨科手术后 VTE 方面具有与依诺肝素相当的疗效和安全性，且具有口服给药的优势。在 AF 患者中，阿哌沙班在预防中风方面比华法林或阿司匹林更有效，且安全性可接受。
