Quantitative Prediction of in Vivo Drug Interactions between Nevirapine and Antifungal Agents from in Vitro Data in Rats

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概要

• 論文の詳細を見る

• We investigated the effects of ketoconazole (KCZ) and fluconazole (FCZ) on rat liver microsomal nevirapine (NVP) metabolism in vitro and on NVP plasma profiles in vivo in order to determine whether the in vivo drug interactions could predicted quantitatively from the in vitro data. The K_i values of KCZ and FCZ for NVP 12-hydroxylation were 1.59 μM and 11.5 μM, respectively, indicating that KCZ inhibited this activity more strongly than FCZ in vitro. In contrast, FCZ orally pre-administered at 20 mg/kg to rats increased the area under the plasma concentration-time curve (AUC) of NVP 7.4-fold, whereas KCZ increased it 2.1-fold, compared to the vehicle. We next investigated the inhibitory potency and unbound concentrations of KCZ and FCZ in microsomal mixtures with or without rat albumin. In the presence of albumin, the inhibition by KCZ was greatly decreased. Further, the unbound fraction of KCZ was decreased dramatically to around 3%, whereas more than 90% of FCZ remained in unbound form. When the increase in the AUC for NVP was calculated based on the concentrations of unbound inhibitors in the portal vein, good agreement with the observed in vivo values was obtained.

• 公益社団法人日本薬学会の論文
• 2000-09-01

著者

• Igarashi Takashi

  Department Of Drug Metabolism And Pharmacokinetics Kawanishi Pharma Research Institute Nippon Boehri

• Ishiguro Naoki

  Department Of Drug Metabolism And Pharmacokinetics Kawanishi Pharma Research Institute Nippon Boehri

• Ishiguro Naoki

  Department Of Biotechnology Graduate School Of Engineering Osaka University

• KISHIMOTO Wataru

  Department of Chemical Biology, Osaka City University

• Sakai Kenji

  Department Of Environmental Chemistry And Engineering Faculty Of Engineering Oita University

• Kishimoto W

  Osaka City Univ. Osaka Jpn

• Kishimoto Wataru

  Department Of Chemical Biology Osaka City University

• Takano Jun-ichi

  Department Of Chemistry Graduate School Of Science Tokyo Metropolitan University

• TAKANO Juni-ichi

  Department of Drug Metabolism and Pharmacokinetics, Kawanishi Pharma Research Institute, Nippon Boeh

• SENDA Chiaki

  Department of Drug Metabolism and Pharmacokinetics, Kawanishi Pharma Research Institute, Nippon Boeh

• Senda Chiaki

  Department Of Drug Metabolism And Pharmacokinetics Kawanishi Pharma Research Institute Nippon Boehri

• Takano Juni-ichi

  Department Of Drug Metabolism And Pharmacokinetics Kawanishi Pharma Research Institute Nippon Boehri

• Igarashi Takashi

  Department Of Anesthesia Mitsui Memorial Hospital

• Sakai Kenji

  Department Of Applied Chemistry Faculty Of Engineering Oita University

• Sakai Kenji

  Department Of Drug Metabolism And Pharmacokinetics Kawanishi Pharma Research Institute Nippon Boehri

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