Effect of Nilvadipine, a Dihydropyridine Calcium Antagonist, on Cytochrome P450 Activities in Human Hepatic Microsomes (Biochemistry/Molecular Biology)
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概要
- 論文の詳細を見る
The effects of nilvadipine, a dihydropyridine calcium antagonist, on cytochrome P450 (CYP) activities in human hepatic microsomes were investigated. Nilvadipine competitively inhibited CYP1A2-mediated 7-ethoxyresorufin O-deethylase, CYP2A6-mediated coumarin 7-hydroxylase, CYP2C8/9-mediated tolbutamide methylhydroxylase, CYP2C19-mediated S-mephenytoin 4'-hydroxylase, and CYP3A4-mediated nifedipine oxidase activities, and the inhibition constant (K_i) values were 13.0, 35.8, 5.02, 24.5 and 44.3 μM, respectively. On the other hand, no inhibition of CYP2B6-mediated 7-benzyloxyresorufin O-debenzylation, CYP2D6-mediated bufuralol 1'-hydroxylation, or CYP2E1-mediated chlorzoxazone 6-hydroxylation by nilvadipine at 40μM concentration was observed. The free fractions of nilvadipine in the incubation mixture estimated by ultracentrifugation were 18.9-27.4%. These results suggest that nilvadipine would not cause clinically significant interactions with other drugs, which are metabolized by CYPs, via the inhibition of metabolism.
- 公益社団法人日本薬学会の論文
- 2004-03-01
著者
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Kawamura A
Pharmacokinetic Research Laboratories Fujisawa Pharmaceutical Co. Ltd.:(present Address)analysis And
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Hashimoto T
Faculty Of Pharmaceutical Sciences Hokuriku University
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橋本 忠
北陸大・薬
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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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橋本 忠
北陸大学薬学部
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Niwa T
近畿大学 薬学部
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NIWA Toshiro
Biopharmaceutical and Pharmacokinetic Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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SHIRAGA Toshifumi
Biopharmaceutical and Pharmacokinetic Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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KAGAYAMA Akira
Biopharmaceutical and Pharmacokinetic Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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HASHIMOTO Tomoko
Biopharmaceutical and Pharmacokinetic Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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Hashimoto Tadashi
Faculty Of Pharmaceutical Sciences Hokuriku University
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Niwa T
Post-marketing Development Research Center Fujisawa Pharmaceutical Co. Ltd.
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Hashimoto T
Hokuriku Univ. Kanazawa Jpn
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Kagayama Akira
Biopharmaceutical And Pharmacokinetic Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Shiraga Toshifumi
Biopharmaceutical And Pharmacokinetic Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Hashimoto Toshihiro
Fac. Of Pharmaceutical Sciences Tokushima Bunri Univ.
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Niwa Toshiro
Post Marketing Product Development Astellas Pharma Inc.
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Kawamura Akio
Department Of Surgery Sapporo Hokuyu Hospital Research Institute For Artificial Organs Transplantati
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Hashimoto Tadashi
Drug Metabolism Laboratories Drug Development Division Yamanouchi Pharmaceutical Co. Ltd.
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