五酯胶囊对心脏移植受者全血他克莫司浓度的影响

摘要

目的 探讨心脏移植术后五酯胶囊对他克莫司血浓度的影响,为临床他克莫司个体化剂量调整提供依据.方法 回顾性收集心脏移植术后联合使用五酯胶囊受者40例,比较用药前后他克莫司血浓度变化,同时分析受者CYP3A4* 1G和CYP3A5*3基因多态性,阐明五酯胶囊发挥作用是否与基因型相关.结果 心脏移植受者服用五酯胶囊后他克莫司剂量校正浓度显著增加至2.02倍(P＜0.01),其作用结果与CYP3A4* 1G和CYP3A5*3基因型无直接相关性.五酯胶囊与他克莫司联用可显著降低总胆红素(P＜0.01),对其他肝、肾指标无影响.结论 五酯胶囊能明显升高心脏移植受者全血他克莫司浓度,不增加他克莫司的肝肾毒性,是一种安全、有效的升高他克莫司血浓度的辅助用药.%Objective To investigate the effects of Wuzhi capsules on tacrolimus concentration in heart transplant recipients and provide evidence for individualized dose optimization of tacrolimus.Methods Forty heart transplant recipients receiving Wuzhi capsules were enrolled in this study.Tacrolimus trough concentration was compared before and after coadminstration of Wuzhicapsules.Furthermore,polymorphisms of CYP3A4 * 1G and CYP3A5 * 3 were also detected to clarify correlations between genotypes and effects of Wuzhi capsule.Results Dose-normalized concentration of tacrolimus after coadministartion with Wuzhi capsules was 2.02-fold higher than before,the results of which was not associated with CYP3A4 * 1G and CYP3A5 * 3 genotypes.Wuzhi capsule could significantly decrease the total bilimbin (T-BiL),but not other hepatic and renal function.Conclusion Dose-normalized concentration of tacrolimus in heart transplant recipients is remarkably increased by Wuzhi capsule.The elevated trough levels rarely result in hepatic and renal toxicity.Wuzhi capsule is a safe,effective,and stable drug to increase the trough concentration of tacrolimus.