Inhibitory Effects of Nicardipine to Cytochrome P450 (CYP) in Human Liver Microsomes(Biopharmacy)

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概要

• 論文の詳細を見る

• To anticipate drug-drug interactions by nicardipine in vivo, cytochrome P450 (CYP) forms responsible for the metabolism of nicardipine and inhibition of CYP-dependent drug metabolism by nicardipine were investigated. Microsomes of human B-lymphoblastoid cells expressing each human CYP form were used for the metabolism of nicardipine. Inhibitory effects of nicardipine on drug metabolism were studied using human liver microsomes. CYP2C8, CYP2D6 and CYP3A4 were identified as major CYP forms for the metabolism of nicardipine in human liver microsomes. Nicardipine strongly inhibited two-pathways of triazolam hydroxylation both catalyzed by CYP3A4. Comparison of three Ca^<2+> antagonists, nicardipine, nifedipine, and diltiazem revealed that only nicardipine showed such a strong inhibitory potency on the typical CYP2D6-catalyzed drug metabolism. Furthermore, nicardipine inhibited other reactions catalyzed by CYP1A, CYP2A6, CYP2C8, CYP2C9 and CYP2C19 with K_i values ranging from 1.1 to 29.4μm. In conclusion, nicardipine was a relatively potent inhibitor of human CYP2D6, CYP3A4 and CYP2C (especially for CYP2C8 and CYP2C19) in vitro, suggesting that drug-drug interactions between nicardipine and other drugs metabolized mainly by these CYP forms appear to occur in vivo.

• 社団法人日本薬学会の論文
• 2005-05-01

著者

• YAMAMOTO Koujirou

  Department of Pharmacy, The University of Tokyo Hospital, Faculty of Medicine, University of Tokyo

• Yokoi T

  Department Of Medicine And Clinical Science Gunma University Graduate School Of Medicine

• Yokoi Tsuyoshi

  北海道大学 薬研究 代謝分析

• HORIUCHI RYUYA

  Department of Clinical Pharmacology, Gunma University Graduate School of Medicine

• KAMATAKI Tetsuya

  Laboratory of Drug Metabolism, Graduate School of Pharmaceutical Sciences, Hokkaido University

• Horiuchi Ryuya

  Department Of Pharmacy The Gunma University Hospital Gunma University School Of Medicine:department

• NAKAMURA Katsunori

  Laboratory of Drug Metabolism, Hokkaido University Graduate School of Pharmaceutical Sciences

• ARIYOSHI Noritaka

  Laboratory of Drug Metabolism, Hokkaido University Graduate School of Pharmaceutical Sciences

• IWATSUBO Takafumi

  Yamanouchi Pharmaceutical Co., Ltd., Drug Metabolism Laboratories

• FUKUNAGA Yasuhisa

  Yamanouchi Pharmaceutical Co., Ltd., Drug Metabolism Laboratories

• HIGUCHI Saburou

  Yamanouchi Pharmaceutical Co., Ltd., Drug Metabolism Laboratories

• ITOH Kunio

  Daiichi Pure Chemicals Co., Ltd., Tokai Research Laboratories

• SHIMADA Noriaki

  Daiichi Pure Chemicals Co., Ltd., Tokai Research Laboratories

• NAGASHIMA Kazuo

  Molecular and Cellular Pathology, Hokkaido University Graduate School of Medicine

• YOKOI Tsuyoshi

  Laboratory of Drug Metabolism, Hokkaido University Graduate School of Pharmaceutical Sciences

• Yamamoto Keiko

  Department Of Pharmaceutics

• NAKAMURA Katsunori

  Department of Clinical Pharmacology, Graduate School of Medicine, Gunma University

• Kamataki T

  Hokkaido Univ. Sapporo Jpn

• Nakayama K

  Laboratory Of Drug Metabolism Graduate School Of Pharmaceutical Sciences Hokkaido University

• Horiuchi Ryuya

  Department Of Clinical Pharmacology Gunma University Graduate School Of Medicine

• Yamamoto Koujirou

  Department Of Pharmacy The University Of Tokyo Hospital Faculty Of Medicine The University Of Tokyo

• Yamamoto Koujirou

  Department Of Pharmacy The Gunma University Hospital Gunma University School Of Medicine:department

• Yamamoto Koujirou

  Department Of Clinical Pharmacology Gunma University School Of Medicine

• Yamamoto Koujirou

  Department Of Clinical Pharmacology Gunma University Graduate School Of Medicine

• Kamataki Tetsuya

  Lab.drug Metab. Grad.sch.pharm.sci. Hokkaido Univ.

• Itoh Kunio

  北海道大学 薬 代謝分析

• Tsumita Yuki

  Department Of Medicine And Clinical Science Gunma University Graduate School Of Medicine

• Yokoi Tsuyoshi

  Division Of Drug Metabolism And Toxicology Faculty Of Pharmaceutical Sciences Kanazawa University

• Yokoi Tsuyoshi

  Laboratory Of Drug Metabolism Division Of Pharmacobio-dynamics Graduate School Of Pharmaceutical Sci

• Nakayama Kazuo

  Laboratory Of Drug Metabolism Division Of Pharmacobio-dynamics Graduate School Of Pharmaceutical Sci

• Yokoi T

  Laboratory Of Drug Metabolism Graduate School Of Pharmaceutical Sciences Hokkaido University

• Yokoi Tsuyoshi

  Fac.pharm. Sci. Hokkaido Univ.

• Nakayama Katsuo

  Department Of Clinical Pharmacology Graduate School Of Medicine Gunma University

• Higuchi Saburou

  Yamanouchi Pharmaceutical Co. Ltd. Drug Metabolism Laboratories

• Ariyoshi Noritaka

  Laboratory Of Drug Metabolism Division Of Pharmacobiodynamics Graduate School Of Pharmaceutical Scie

• Horiuchi Ryuya

  Department Of Clinical Pharmacology And Department Of Pharmacy Gunma University School Of Medicine

• Nakamura Katsunori

  Department Of Clinical Pharmacology Graduate School Of Medicine Gunma University

• Kamataki Tetsuya

  Laboratory Of Drug Metabolism Division Of Pharmacobio-dynamics Graduate School Of Pharmaceutical Sci

• Shimada Noriaki

  Daiichi Pure Chemicals Co. Ltd.

• Shimada Noriaki

  Daiichi Pure Chemicals Co. Ltd. Tokai Research Laboratories

• Yokoi Tsuyoshi

  Div.drug Metab. Fac.of Pharm.sic. Hokkaido Univ.

• Kamataki Tetsuya

  Div.drug Metab. Fac.of Pharm.sic. Hokkaido Univ.

• Kamataki Tetsuya

  Lab. Drug Metab. Fac. Pharm. Sci. Hokkaido University

• Fukunaga Yasuhisa

  Yamanouchi Pharmaceutical Co. Ltd. Drug Metabolism Laboratories

• Iwatsubo Takafumi

  Yamanouchi Pharmaceutical Co. Ltd. Drug Metabolism Laboratories

• Ariyoshi Noritaka

  Dev.drug Metab. Faculty Of Pharm.sci. Hokkaido Univ.

• Yamano Katsuhiro

  Biopharmaceutical And Pharmacokinetic Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• Nagashima Kazuo

  Molecular & Cellular Pathology Hokkaido University School Of Medicine

• Kamataki Tetsuya

  Laboratory of Drug Metabolism, Hokkaido University Graduate School of Pharmaceutical Sciences

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