Stereoselective Pharmacokinetics and Pharmacodynamics of Verapamil and Norverapamil in Rabbits

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概要

• 論文の詳細を見る

• We have estimated the pharmacokinetic and pharmacodynamic interactions of verapamil(VP)enantiomers and also the interaction between VP and its metabolite, norverapamil(NVP). ECGs of conscious rabbits were studied to determine the pharmacokinetics of VP enantiomers and racemic NVP in relation to their prolongation effect on PR intervals, which were used as an index of VP's antiarrhythmic effect. Plasma free fractions of VP enantiomers showed constant values at concentrations ranging from 0.022 to 1.10μ_M. There were no interactions between enantiomers or between VP and NVP. The pharmacological effect of the S-enantiomer(S-VP), which was determined by linear regression analysis, showed it was about 20 times more potent than that of the R-enantiomer(R-VP). The effect of racemic VP was the simple sum of those elicited by both enantiomers. These relationships were not significantly different between intravenous infusion and bolus injection. Simultaneous intravenous infusion of NVP had no influence on the PR intervals. In conclusion, we demonstrated that the relationship between plasma unbound concentration of VP enantiomers and their pharmacological effect was the simple sum of two enantiomers.

• 公益社団法人日本薬学会の論文
• 2001-07-01

著者

• Hanada Kazuhiko

  Department of Biopharmaceutics, Meiji Pharmaceutical University

• Ogata Hiroyasu

  Department of Biopharmaceutics, Meiji Pharmaceutical University

• Ogata Hiroyasu

  Deparment Of Biopharmaceutice Meiji Pharmaceutical University

• Ogata Hiroyasu

  Dep. Of Biopharmaceutics Meiji Pharmaceutical Univ.

• HANADA Kazuhiko

  明治薬科大学大学院臨床薬学薬剤学

• OGATA Hiroyasu

  明治薬科大学大学院臨床薬学薬剤学

• Mori Yuko

  Department Of Biopharmaceutics Meiji Pharmaceutical University

• Ogata H

  Meiji Pharmaceutical Univ. Tokyo Jpn

• HASHIGUCHI Masayuki

  Department of Medication Use Analysis and Clinical Research, Meiji Pharmaceutical University

• Hayashi Masamiti

  Department Of Cardiology Tokyo Women's Medical University

• MORI Tatsuya

  Department of Biopharmaceutics, Meiji Pharmaceutical University

• TSUKAHARA Yoko

  Department of Biopharmaceutics, Meiji Pharmaceutical University

• Hanada Kazuhiko

  Dep. Of Biopharmaceutics Meiji Pharmaceutical Univ.

• Hanada Kazuhiko

  Department Of Biopharmaceutics Meiji College Of Pharmacy

• Tsukahara Y

  Department Of Biopharmaceutics Meiji Pharmaceutical University

• Mori T

  Department Of Biopharmaceutics Meiji Pharmaceutical University

• Hashiguchi Masayuki

  Department Of Medication Use Analysis And Clinical Research Meiji Pharmaceutical University

• Mori Tatsuya

  Department Of Advanced Bioscience Faculty Of Agriculture Kinki University

• HASHIGUCHI Masayuki

  Division for Evaluation and Analysis of Drug Information, Faculty of Pharmacy, Keio University

• Hashiguchi Masayuki

  Division For Evaluation And Analysis Of Drug Information Faculty Of Pharmacy Keio University

• Hanada Kazuhiko

  Department of Biopharmaceutics & Clinical Pharmacokinetics, Meiji Pharmaceutical University

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