Analysis of Pharmacological Effects of Drugs Used for Treatment of Urinary Disturbance Based on Anticholinergic and Smooth Muscle-Relaxing Effects(Biopharmacy)

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概要

• 論文の詳細を見る

• Propiverine hydrochloride, oxybutynin hydrochloride and terodiline hydrochloride have both anticholinergic and antispasmodic effects, and are used for the management of urinary frequency and incontinence. The average standard therapeutic doses of these drugs differ greatly. We retrospectively analyzed their pharmacological effects with consideration given to muscarinic acetylcholine receptor binding affinities, anticholinergic activities, and inhibitory effects on KCl-induced contraction. Muscarinic acetylcholine receptor occupancies and the inhibitory ratios of the drugs for both acetylcholine-induced and KCl-induced contraction in a steady state after oral administration of standard doses were calculated based on pharmacokinetics and the receptor occupancy theory. The average muscarinic acetylcholine receptor occupancy and inhibitory ratio of acetylcholine-induced contraction were estimated to be 12.6±1.06% and 3.27±0.74%, respectively, with no significant differences found between the drugs for those parameters. A significant linear relationship was found between muscarinic acetylcholine receptor occupancy and the maximum ratio of increase in bladder urinary capacity. On the other hand, the inhibitory ratios of KCl-induced contraction varied from 0.01 to 0.48%. The present results suggest that muscarinic acetylcholine receptor occupancy is a principal determinant of the therapeutic effect of a drug used for treatment of urinary disturbance.

• 公益社団法人日本薬学会の論文
• 2007-07-01

著者

• YAMADA Yasuhiko

  Department of Mathematics, Faculty of Science, Kobe University

• Yokoyama Haruko

  Department Of Cardiology Hiroshima City Asa Hospital

• Yokoyama Haruko

  東京薬科大学 薬学部臨床薬効解析学

• Yokoyama Haruko

  Department Of Clinical Evaluation Of Drug Efficacy School Of Pharmacy Tokyo University Of Pharmacy A

• Yokoyama Haruko

  Department Of Biomaterials Institute For Frontier Medical Sciences Kyoto University

• OZEKI Takeshi

  Department of Clinical Evaluation of Drug Efficacy, School of Pharmacy, Tokyo University of Pharmacy

• TAKAYANAGI Risa

  Department of Clinical Evaluation of Drug Efficacy, School of Pharmacy, Tokyo University of Pharmacy

• Ozeki Takeshi

  Department Of Clinical Evaluation Of Drug Efficacy School Of Pharmacy Tokyo University Of Pharmacy A

• Takayanagi Risa

  Department Of Clinical Evaluation Of Drug Efficacy School Of Pharmacy Tokyo University Of Pharmacy A

• IGA Tatsuji

  International University of Health and Welfare

• MIZUSHIMA Haruhi

  Department of Clinical Evaluation of Drug Efficacy, School of Pharmacy, Tokyo University of Pharmacy

• Yamada Yasuhiko

  Department Of Clinical Evaluation Of Drug Efficacy School Of Pharmacy Tokyo University Of Pharmacy A

• Yamada Yasuhiko

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

• Iga Tatsuji

  Department Of Biopharmaceutics Faculty Of Pharmaceutical Sciences Nagoya City University:department

• Iga T

  Department Of Biopharmaceutics Faculty Of Pharmaceutical Sciences Nagoya City University:department

• Yamada Yasuhiko

  Department Of Clinical Evaluation Of Drug Efficacy School Of Pharmacy Tokyo University Of Pharmacy A

• Mizushima Haruhi

  Department Of Clinical Evaluation Of Drug Efficacy School Of Pharmacy Tokyo University Of Pharmacy A

• Yamada Yasuhiko

  Department Of Clinical Evaluation Of Drug Efficacy School Of Pharmacy Tokyo University Of Pharmacy A

• Ozeki Takeshi

  Department Of Clinical Evaluation Of Drug Efficacy School Of Pharmacy Tokyo University Of Pharmacy A

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