Inhibitory Effect of Azole Antifungal Agents on the Glucuronidation of Lorazepam Using Rabbit Liver Microsomes in Vitro
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概要
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Azole antifungal agents (azoles) have inhibitory effects on the cytochrome P450. However, the effect of azoles on conjugative metabolism has not been given much attention. Lorazepam (LZP), a benzodiazepine sedative agent, is known to be metabolized by uridine 5'-diphosphate (UDP)-glucuronyltransferase. Herein we report investigation of the effect of azoles on the enzyme-kinetics of glucuronidation of lorazepam using rabbit liver microsomes in vitro. The K_m and V_<max> for LZP glucuronidation were determined to be 0.26±0.08 mM and 1.25±0.21 nmol/min/mg protein, respectively, when evaluated in the presence of a detergent 3-[(3-cholamidopropyl)-dimethylammonio]-1-prooanesulfonate (CHAPS) (0.8 mg/mg protein). Azoles fluconazole, miconazole, and ketoconazole competitively inhibited the glucuronidation of LZP, with K_i values of 7.17±4.78 mM, 0.17±0.08 mM, and 0.092±0.026 mM, respectively. These results are comparable to the previously reported K_i values of azoles with zidovudine (AZT) glucuronidation (1.4,0.18,and 0.08 mM for fluconazole, miconazole, and ketoconazole, respectively) [Sampol et al., Br. J. Clin. Pharmacol., 40,83-86,1995]. Therefore, in order to avoid possible side effects of LZP, the concomitant administration of LZP and azles should be carefully evaluated.
- 2000-05-01
著者
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SATO Hitoshi
Department of Clinical and Molecular Pharmacokinetics/Pharmacodynamics, School of Pharmaceutical Sci
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KAWAKAMI Junichi
Department of Pharmacy, The University of Tokyo Hospital, Faculty of Medicine, University of Tokyo
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SAWAMURA Ryoko
Department of Pharmacy, University of Tokyo Hospital, Faculty of Medicine, University of Tokyo
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IGA Tatsuji
Department of Pharmacy, University of Tokyo Hospital, Faculty of Medicine, University of Tokyo
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Sato Hitoshi
Department Of Cardiovascular Medicine Tohoku University Graduate School Of Medicine
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Iga Tatsuji
Department Of Biopharmaceutics Faculty Of Pharmaceutical Sciences Nagoya City University:department
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Iga Tatsuji
Department Of Pharmacy University Of Tokyo Hospital Faculty Of Medicine University Of Tokyo
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Kawakami Junichi
Department Of Hospital Pharmacy Hamamatsu University School Of Medicine
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Kawakami Junichi
Department Of Hospital Pharmacy Toyama Medical And Pharmaceutical University
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Sawamura Ryoko
Department Of Pharmacy University Of Tokyo Hospital Faculty Of Medicine University Of Tokyo
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Sato Hitoshi
Department Of Pharmacy University Of Tokyo Hospital Faculty Of Medicine University Of Tokyo
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Sato Hitoshi
Department Of Cardiology Juntendo University School Of Medicine
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SATO Hitoshi
Department of Animal Science, Faculty of Agriculture, Tohoku University
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