地尔硫[艹卓]在器官移植和小儿肾病综合征患者中对他克莫司血药浓度的影响规律研究进展  

Research progress on the effect of Diltiazem on tacrolimus concentration in organ transplant population and children with nephrotic syndrome

作　　者：耿魁魁 张圣雨 兰雷 史天陆 GENG Kuikui;ZHANG Shengyu;LAN Lei;SHI Tianlu(Department of Pharmacy,The First Affiliated Hospital of USTC,Division of Life Sciences and Medicine,University of Science and Technology of China,Anhui Hefei 230001,China;Nephrology,The First Affiliated Hospital of USTC,Division of Life Sciences and Medicine,University of Science and Technology of China,Anhui Hefei 230001,China)

机构地区：[1]中国科学技术大学附属第一医院/安徽省立医院,药学部,安徽合肥230001 [2]中国科学技术大学附属第一医院/安徽省立医院,肾脏内科,安徽合肥230001

出　　处：《中国医院药学杂志》2023年第12期1406-1411,共6页Chinese Journal of Hospital Pharmacy

基　　金：中国科学技术大学附属第一医院药剂科药学科研探索基金(编号:YJKJJ04)。

摘　　要：他克莫司是钙调磷酸酶抑制剂型免疫抑制剂,在临床上有着广泛的应用,但它在体内血药浓度易受多种因素影响,部分患者常规剂量达不到有效治疗浓度。地尔硫[艹卓]是非二氢吡啶类钙离子拮抗剂,通过抑制CYP3A代谢酶和P-糖蛋白活性,使他克莫司代谢和排出减少,从而导致血药浓度上升,临床常作为他克莫司保留剂以提高他克莫司治疗效果,减少患者药物治疗费用。该文综述了地尔硫[艹卓]对他克莫司血药浓度的作用机制和在不同疾病状态下对患者血药浓度的影响规律,以期为临床使用地尔硫[艹卓]作为他克莫司保留剂提供参考和借鉴。Tacrolimus was a calcineurin inhibitor-type immunosuppressant,which had a wide range of clinical applications,but its blood concentration in vivo was susceptible to many factors,and some patients with conventional dose can not reach the effective therapeutic concentration.Diltiazem was a non-dihydropyridine calcium antagonist,which reduced the metabolism and excretion of tacrolimus by inhibiting the activity of CYP3A metabolic enzyme and p-glycoprotein,resulting in an increase in blood drug concentration.It was often used as a tacrolimus retentionist in clinical practice to improve the therapeutic effect of tacrolimus and reduce the cost of drug treatment for patients.This article reviewed the mechanism of action of diltiazem on tacrolimus concentration and the rule of influence on blood concentration of patients in different disease states,in order to provide reference for clinical use of diltiazem as tacrolimus retentant.

关 键 词：地尔硫[艹卓] 他克莫司 血药浓度 器官移植 肾病综合征 

分 类 号：R96[医药卫生—药理学]