泮托拉唑对人肝脏药物代谢酶CYP1A2、NAT2和XO活性影响的研究  

Effect of pantoprazole on Cytochrome P4501A2,N-acetyltransferase2,and xanthine oxidase activity in human

作　　者：李军[1] 彭向前[2] 张鉴[1] 郭瑞臣[3] 徐济萍[1] 

机构地区：[1]山东省立医院临床药理中心 [2]山东大学药学院 [3]齐鲁医院药物监测中心

出　　处：《中国临床药理学与治疗学》2006年第3期296-299,共4页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：山东省自然科学基金项目(№Q99C05);山东省卫生厅科研项目(№1998CA1DBB5)

摘　　要：目的:探讨泮托拉唑对人肝脏药物代谢酶CYP1A2、NAT2和XO活性的影响,预测泮托拉唑与常用药物的相互作用,指导临床医师合理用药。方法:以咖啡因作为药物代谢酶CYP1A2、NAT2和XO的探针药物,以反相高效液相梯度洗脱法测定30名受试者服用泮托拉唑前后人尿液内咖啡因5种主要代谢产物的相对含量,采用代谢物的比率分别评价人肝脏药物代谢酶CYP1A2、NAT2和XO活性的变化。结果:受试者用药前CYP1A2、NAT2和XO平均活性为3.37±1.22、0.50±0.09、0.49±0.09;服用泮托拉唑7 d后CYP1A2、NAT2和XO平均活性为3.50±1.23、0.48±0.12、0.48±0.13;服药前后3种酶活性没有显著性差异(P>0.05)。结论:泮托拉唑对人肝脏药物代谢酶CYP1A2、NAT2和XO活性无明显影响,泮托拉唑可能不会影响与之合用的需经CYP1A2、NAT2和XO代谢的药物临床疗效。AIM： To investigate the effect of pantoprazole on Cytochrome P4501A2 （CYP1A2）, N-acetyltransferase2（NAT2）, and xanthine oxidase（XO） activity in human and to forecast the drug-drug interaction with it, so as to instruct clinician to prescribe rationally. METHODS：In thirty volunteers, use two-way cross design,caffeine was used as a metabolic probe for CYP1A2,NAT2, and XO, before and after pantoprazole administration, urine samples were collected. The contents of five major metabolites of caffeine in the urine were determined by RP-HPLC method and then evaluated the activity change of CYP1A2,NAT2,and XO by the ratio of metabolites of caffeine. RESUTS： It was found that the average activity of CYP1A2,NAT2, and XO were 3.37 ± 1.22,0.50 ± 0.09,0.49 ± 0.09 with before treatment, and 7 days after treatment, the average activity of CYP1A2, NAT2, and XO were 3.50±1.23,0.48 ± 0.12,0.48 ± 0.13. There were no statistical significance between before treatment and after treatmen（ P 〉 0.05）. CONCLUSIONS： Pantoprazole have no influence on CYP1A2, NAT2, and XO, so pantopmzole do not modify the efficacy of drugs which metabolized by CYP1A2,NAT2,and XO taken simuhaneously.

关 键 词：泮托拉唑 咖啡因代谢物 高效液相色谱 细胞色素P4501A2 N-乙酰基转移酶 黄嘌呤氧化酶 

分 类 号：R969.2[医药卫生—药理学]