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Azoles and allylamines: the clinical implications of interaction with cytochrome P-450 enzymes

 

作者: BackDj,   TijaJf,  

 

期刊: Journal of Dermatological Treatment  (Taylor Available online 1990)
卷期: Volume 1, issue sup2  

页码: 11-13

 

ISSN:0954-6634

 

年代: 1990

 

DOI:10.3109/09546639009089023

 

出版商: Taylor&Francis

 

数据来源: Taylor

 

摘要:

Two antimycotic agents, the azole ketoconazole and the allylamine terbinafine (Lamisil), have been examined for their effects on the metabolism of tolbutamide, ethinyloestradiol and cyclosporin by human liver microsomes (n = 4) in vitro. Ketoconazole caused marked inhibition of all enzyme activities with mean IC50values (concentration producing 50% inhibition) of 17.9μM (tolbutamide hydroxylase), 1.9μM (ethinyloestradiol 2–hydroxylase), 2.0μM (cyclosporineN-demethylase) and 2.1μM (cyclosporine hydroxylase). At 50μM terbinafine concentration, inhibition was less than 5% for tolbutamide, approximately 12% for both cyclosporin pathways and 30% for ethinyloestradiol. Terbinafine does not have the same inhibitory potential for cytochrome P-450 isozymes as ketoconazole.

 

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