Effect of Antifungal Drugs on Cytochrome P450 (CYP) 1A2, CYP2D6, and CYP2E1 Activities in Human Liver Microsomes(Biopharmacy)
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概要
- 論文の詳細を見る
The effects of five antifungal drugs, fluconazole, itraconazole, micafungin, miconazole, and voriconazole, on cytochrome P450 (CYP) 1A2-mediated 7-ethoxyresorufin O-deethylation, CYP2D6-mediated debrisoquine 4-hydroxylation, and CYP2E1-mediated chlorzoxazone 6-hydroxylation activities in human liver microsomes were compared. In addition, the effect of preincubation was estimated in order to investigate the mechanism-based inhibition. IC_<50> values of miconazole against CYP1A2 and CYP2D6 activities were 2.90 and 6.46μM, respectively, and miconazole at 10μM concentration slightly inhibited CYP2E1 activity. On the other hand, other antifungal drugs neither inhibited nor stimulated all of the metabolic activities. The stimulation of the inhibition of the metabolic activities mediated by CYP1A2, CYP2D6, or CYP2E1 by 15-min preincubation was not observed for any of the antifungal drugs, suggesting that these antifungal drugs are not mechanism-based inhibitors. These results suggest that miconazole is the strongest inhibitor against CYP1A2, CYP2D6, and CYP2E1 among the antifungal drugs investigated.
- 公益社団法人日本薬学会の論文
- 2005-09-01
著者
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Shirage Toshifumi
Departmnet Of Pharmacolinetics And Drug Metabolism Pharma Ceutical And Pharmacolinetic Research Labo
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Shiraga T
Biopharmaceutical And Pharmacokinetic Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Niwa T
近畿大学 薬学部
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Takagi Akira
Post Marketing Product Development Astellas Pharma Inc.
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NIWA Toshiro
Post Marketing Product Development, Astellas Pharma Inc.
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YAMAMOTO Sachiko
Astellas Research Services Co., Ltd.
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SHIRAGA Toshifumi
Drug Metabolism Research Laboratories, Astellas Pharma Inc.
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Tokunaga Akira
Post-marketing Development Research Center Fujisawa Pharmaceutical Co. Ltd.
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Niwa T
Post-marketing Development Research Center Fujisawa Pharmaceutical Co. Ltd.
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Tokunaga Akira
First Department Of Surgery Nippon Medical School
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Niwa Toshiro
Post Marketing Product Development Astellas Pharma Inc.
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Yamamoto Sachiko
Astellas Research Services Co. Ltd.
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Inoue-Yamamoto Sachiko
Astellas Research Services Co., Ltd.
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