Duke Heart Center, Duke Clinical Research Institute, Duke University School of Medicine, Box 3943 DUMC, Durham, NC, 27710, USA.
J.W. Goethe University, Frankfurt, Germany.
J Thromb Thrombolysis. 2019 Apr;47(3):345-352. doi: 10.1007/s11239-019-01823-y.
Warfarin is dependent on multiple hepatic enzymes for metabolism while apixaban is a substrate for P-glycoprotein (P-gp) transport and hepatic CYP3A4 metabolism. The aim of this analysis was to assess the impact of interacting medication use on the treatment effects of apixaban versus warfarin. Outcomes were compared between apixaban and warfarin using Cox proportional hazards modeling according to the use of interacting medications at randomization in ARISTOTLE (n = 18,201). Interacting medications for apixaban were identified as combined P-gp and 3A4 inhibitors or inducers while interacting medications for warfarin were defined as those highly probable for warfarin potentiation or inhibition. At randomization, 5547 (30.5%) patients were on an interacting medication, including 2722 on apixaban and 2825 on warfarin. Patients using an interacting medication were more likely to be female, taking aspirin, and have a history of prior bleeding and were less likely to have a prior stroke or transient ischemic attack. No significant differences were observed on the treatment effect of apixaban compared with warfarin in patients on and off interacting medications for outcomes including the primary efficacy outcome of stroke or systemic embolism (P for interaction = 0.79) or the primary safety outcome of major bleeding (P for interaction = 0.75). Use of interacting medications with anticoagulants occurs often in patients with atrial fibrillation. Despite the potential for altered exposure, interacting medication use was not associated with a significant change in the efficacy or safety of apixaban compared with warfarin in the ARISTOTLE trial.Trial registration ClinicalTrials.gov, NCT00412984.
华法林的代谢依赖于多种肝酶,而阿哌沙班是 P-糖蛋白(P-gp)转运和肝 CYP3A4 代谢的底物。本分析旨在评估相互作用药物的使用对阿哌沙班与华法林治疗效果的影响。使用 Cox 比例风险模型根据 ARISTOTLE(n=18201)随机分组时相互作用药物的使用情况,比较阿哌沙班与华法林的结局。阿哌沙班的相互作用药物被确定为联合 P-gp 和 3A4 抑制剂或诱导剂,而华法林的相互作用药物则定义为那些极有可能增强或抑制华法林作用的药物。在随机分组时,5547 名(30.5%)患者正在使用相互作用药物,其中 2722 名患者使用阿哌沙班,2825 名患者使用华法林。使用相互作用药物的患者更可能为女性,服用阿司匹林,并有既往出血史,既往中风或短暂性脑缺血发作的可能性较小。对于包括中风或全身性栓塞(交互 P 值=0.79)在内的主要疗效结局或大出血(交互 P 值=0.75)在内的主要安全性结局,在使用相互作用药物的患者与未使用相互作用药物的患者中,阿哌沙班与华法林的治疗效果无显著差异。在接受抗凝治疗的心房颤动患者中,经常使用相互作用药物。尽管潜在的暴露情况可能发生变化,但与华法林相比,相互作用药物的使用与阿哌沙班的疗效或安全性无显著相关性,在 ARISTOTLE 试验中也是如此。试验注册ClinicalTrials.gov,NCT00412984。