环孢素、硝苯地平等5种肾移植受者常用药物对人体红细胞硫瞟岭甲基转移酶活性的影响

中国临床药理学与治疗学 ›› 2007, Vol. 12 ›› Issue (12): 1411-1414.

环孢素、硝苯地平等5种肾移植受者常用药物对人体红细胞硫瞟岭甲基转移酶活性的影响

熊晖^1,2, 熊磊¹, 苏丹¹, 辛华雯¹, 吴笑春¹, 李罄¹, 李高²

¹广州军区武汉总医院临床药理科,武汉 430070,湖北;
²华中科技大学同济医学院药学院,武汉 430070,湖北

收稿日期:2007-09-22 修回日期:2007-11-19 发布日期:2020-11-10
通讯作者: 辛华雯,女,主任医师,研究方向:临床药理学。Tel:027-68878688 E-mail:huawernxin@163.com
作者简介:熊晖,女,在读硕士研究生,研究方向:临床药理学。E-mail:aring918@yahoo.com.cn
基金资助:
全军科学技术研究“十一五”计划课题资助(06MA131)

Effects of five drugs including ciclosporin and nifedipine which were usually used in patients with kidney transplantation on erythrocyte thiopurinemethyltransferase activity

XIONG Hui^1,2, XIONG Lei¹, SU Dan¹, XIN Hua-wen², WU Xiao-chun¹, LI Qing¹, LI Gao²

¹Department of Clinical Pharmcology Wuhan General Hopial of Gungzhou Command, Wuhan 43007, Hubei, China;
²Tongji Pharmaceutical College, Huazhong University of Science and Technology Wuhan 43007, Hubei, China

Received:2007-09-22 Revised:2007-11-19 Published:2020-11-10

摘要/Abstract

摘要： 目的: 研究肾移植受者中常与硫唑嘌呤(AZA)同时服用的药物如环孢素、泼尼松的活性代谢物氢化可的松、硝苯地平、卡托普利以及别嘌呤醇对硫嘌呤甲基转移酶(TPMT)活性的影响。方法: 应用高效液相色谱法(HPLC)测定健康受试者红细胞TPMT活性,其中中等活性和正常活性受试者各8例,计算药物各浓度对应的平均TPMT活性抑制率及有抑制作用药物的平均IC₅₀值。结果: 环孢素、氢化可的松、卡托普利以及别嘌呤醇对TPMT活性抑制作用较弱。硝苯地平能明显抑制TPMT的活性,中等活性组的平均IC₅₀值为(24±17)μg/mL, 正常活性组的平均IC₅₀值为(12±10)μg/mL结论:硝苯地平能明显抑制TPMT活性,当硝苯地平与嘌呤类药物同时服用时,应警惕可能发生不良相互作用。

关键词: 硫嘌呤甲基转移酶, 硫唑嘌呤, 环孢素, 氢化可的松, 硝苯地平, 卡托普利, 别嘌呤醇

Abstract: AIM: To investigate the effects of five dugs which were usually used simultaneously with azathioprine (AZA) in patients with kidney transplantation: ciclosporin, hydrocortisone, nifedipine, captopriland al-lopurinol on erythrocyte tliopuriner methyltransferase(TPMT) activity. METHODS: The erythrocyte TPMT activity of healthy volunteers was measured by high-per-formance liquid chromatography (HPLC). Sixteen volunteers were chosen, in which 8 cases with intermediate TPMT activity and others with normal TPMT activity. Themean inhibition ratio of each drug concentration and the mean IC values of the inhibitors were determined. RESULTS: Ciclosporin, hydrocortisone, captopril and allo-purinol had nearly no impacts on TPMT activity. Nifedip-lnehighly inhibited TPMT activity in vitro, the meanI IC₅₀ value in intermediate TPMT activity groupwas (24±17) μg/mL and in normal TPMT activity group was (12±10) μg/mL. CONCLUSION: The co-administration of nifedipine and thiopurines may lead to drug interactions.

Key words: thiopurine methyltransferase, azathio-prine, ciclosporin, hydrocortisone, nifedipine, captopril, allopurinol

中图分类号:

R969

熊晖, 熊磊, 苏丹, 辛华雯, 吴笑春, 李罄, 李高. 环孢素、硝苯地平等5种肾移植受者常用药物对人体红细胞硫瞟岭甲基转移酶活性的影响[J]. 中国临床药理学与治疗学, 2007, 12(12): 1411-1414.

XIONG Hui, XIONG Lei, SU Dan, XIN Hua-wen, WU Xiao-chun, LI Qing, LI Gao. Effects of five drugs including ciclosporin and nifedipine which were usually used in patients with kidney transplantation on erythrocyte thiopurinemethyltransferase activity[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2007, 12(12): 1411-1414.

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