Center for Pharmacoepidemiology Research and Training, Perelman School of Medicine at the University of Pennsylvania, Philadelphia, Pennsylvania, USA.
Center for Clinical Epidemiology and Biostatistics, Perelman School of Medicine at the University of Pennsylvania, Philadelphia, Pennsylvania, USA.
Clin Pharmacol Ther. 2020 Jun;107(6):1446-1456. doi: 10.1002/cpt.1819. Epub 2020 Mar 26.
Amiodarone inhibits warfarin metabolism and is associated with major bleeding during warfarin therapy. Managing this drug-drug interaction (DDI) is challenging because of substantial interpatient variability in DDI magnitude. Because renal dysfunction induces changes in drug metabolism and protein binding that could alter cytochrome P450 inhibition mechanisms, we hypothesized that renal dysfunction alters the impact of the warfarin-amiodarone DDI. We tested this question in a propensity-matched cohort study of hospitalized patients with atrial fibrillation. Patients were queried from an electronic health record database. Renal function was estimated with creatinine clearance (CrCl). Warfarin response was measured with the warfarin sensitivity index (WSI), a dose-normalized international normalized ratio (INR) measure, and was modeled with multilevel mixed-effects linear regression. Time to supratherapeutic INR (> 4) was modeled using Cox regression. Propensity score matching resulted in 4,518 patients administered amiodarone and 4,518 controls. Amiodarone's effect on warfarin response varied threefold across the renal function range, increasing WSI by 36% in patients with normal renal function (CrCl 115 mL/minute), but by only 11.8% in patients with severe renal dysfunction (CrCl 15 mL/minute). Similarly, amiodarone had a strong effect in patients with normal renal function (hazard ratio (HR) 1.80; 1.23, 2.64), but a negligible effect on supratherapeutic INR hazard in patients with severe renal dysfunction (HR 1.01; 0.75, 1.37). These results suggest that renal function is a novel factor that explains substantial variability in the warfarin-amiodarone DDI. This information could inform warfarin dosage adjustment and monitoring and may have implications for the selection of oral anticoagulation agents in patients treated with amiodarone.
胺碘酮抑制华法林代谢,与华法林治疗期间的大出血有关。由于药物相互作用(DDI)的幅度在患者间存在很大差异,因此管理这种药物相互作用具有挑战性。由于肾功能障碍会引起药物代谢和蛋白结合的变化,从而改变细胞色素 P450 抑制机制,我们假设肾功能障碍会改变华法林-胺碘酮 DDI 的影响。我们在一项因房颤住院的患者的倾向匹配队列研究中检验了这个问题。从电子病历数据库中查询了患者。用肌酐清除率(CrCl)来估计肾功能。用华法林敏感性指数(WSI)来衡量华法林的反应,WSI 是一种剂量标准化的国际标准化比值(INR)指标,并用多级混合效应线性回归进行建模。用 Cox 回归来建模达到高于治疗范围 INR(>4)的时间。通过倾向评分匹配,得出 4518 名接受胺碘酮治疗的患者和 4518 名对照者。胺碘酮对华法林反应的影响在肾功能范围内变化了三倍,在肾功能正常(CrCl 115 mL/min)的患者中增加了 36%的 WSI,但在肾功能严重障碍(CrCl 15 mL/min)的患者中仅增加了 11.8%。同样,胺碘酮在肾功能正常的患者中具有强烈的作用(危险比(HR)1.80;1.23,2.64),但对肾功能严重障碍患者的高于治疗范围 INR 危险几乎没有影响(HR 1.01;0.75,1.37)。这些结果表明,肾功能是解释华法林-胺碘酮 DDI 中大量变异性的一个新的因素。这些信息可以为华法林剂量调整和监测提供依据,并可能对接受胺碘酮治疗的患者选择口服抗凝剂产生影响。