CYCLOSPORINE METABOLISM IN HUMAN LIVER-MICROSOMES AND ITS INHIBITION BY OTHER DRUGS

被引:28
作者
HENRICSSON, S
LINDHOLM, A
ARAVOGLOU, M
机构
[1] KAROLINSKA INST,HUDDINGE HOSP,DEPT CLIN PHARMACOL,S-14186 HUDDINGE,SWEDEN
[2] KAROLINSKA INST,HUDDINGE HOSP,DEPT TRANSPLANTAT SURG,S-14186 HUDDINGE,SWEDEN
来源
PHARMACOLOGY & TOXICOLOGY | 1990年 / 66卷 / 01期
关键词
D O I
10.1111/j.1600-0773.1990.tb00701.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The metabolism of cyclosporin was studied in human liver microsomes. There was no metabolism in the presence of cytochrome C or carbon monoxide or in the absence of cofactors, suggesting metabolism by cytochrome P‐450 enzymes. The metabolism was inhibited by ketoconazole and erythromycin, by the steroids methylprednisolone and oestradiol, and by the calcium antagonists diltiazem, nifedipine, prenylamine and verapamil. These in vitro findings correlate well with previously published clinical reports suggesting that these drugs may inhibit the metabolism of cyclosporin in vivo. Our observations suggest that metabolic interactions between cyclosporin and other drugs in vivo may be predicted in vitro under proper experimental conditions. 1990 Nordic Pharmacological Society
引用
收藏
页码:49 / 52
页数:4
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