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IC_(50)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IC_(50)值为(24±17)μg/mL,正常活性组的平均,IC_(50)值为(12±10)μg/mL。结论:硝苯地平能明显抑制TPMT活性,当硝笨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。
AIM: To investigate the effects of five drugs which were usually used simultaneously with azathioprine (AZA) in patients with kidney transplantation: ciclosporin, hydrocortisone, nifedipine, captopril and allopurinol on erythrocyte thiopurine methyltransferase (TPMT) activity. METHODS: The erythrocyte TPMT activity of healthy volunteers was measured by high-performance liquid chromatography (HPLC). Sixteen volunteers were chosen, in which 8 cases with intermediate TPMT activity and others with normal TPMT activity. The mean inhibition ratio of each drug concentration and the mean IC50 values of the inhibitors were determined. RESULTS: Ciclosporin, hydrocortisone, captopril and allopurinol had nearly no impacts on TPMT activity. Nifedipine highly inhibited TPMT activity in vitro, the mean IC50 value in intermediate TPMT activity group was (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.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2007年第12期1411-1414,共4页
Chinese Journal of Clinical Pharmacology and Therapeutics
基金
全军科学技术研究"十一五"计划课题资助(06MA131)