Pharmacokinetics and Pharmacodynamics of Bisoprolol in Rats with Bilateral Ureter Ligation-induced Renal Failure
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- TAHARA Katsutoshi
- Graduate School of Pharmaceutical Sciences, University of Toyama
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- SAIGUSA Katsuya
- Graduate School of Pharmaceutical Sciences, University of Toyama
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- KAGAWA Yuka
- Graduate School of Pharmaceutical Sciences, University of Toyama
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- TAGUCHI Masato
- Graduate School of Pharmaceutical Sciences, University of Toyama
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- HASHIMOTO Yukiya
- Graduate School of Pharmaceutical Sciences, University of Toyama
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The effect of renal failure on the pharmacokinetics and pharmacodynamics of bisoprolol was investigated in bilateral ureter-ligated (BUL) rats. The blood bisoprolol concentrations following 30-min intravenous infusion at a rate of 60 μg/kg/min were higher in renal artery-occluded (RAO) rats than in control rats, and were higher in BUL rats than in RAO rats. Increased blood bisoprolol concentrations accompanied decreased mean systemic clearances: 50.7, 36.4, and 26.2 mL/min/kg in control, RAO, and BUL rats, respectively. The finding indicated that approximately 30% of administered bisoprolol was excreted via the kidney, and that not only the renal clearance but also non-renal clearance of bisoprolol was decreased in BUL rats. The β-blocking action of bisoprolol was assessed by the reduction in isoproterenol-induced increases in the heart rate. The relationship between blood concentration and the β-blocking action of bisoprolol in BUL rats was similar to that in control rats. These results suggested that renal excretion and hepatic metabolism of bisoprolol were significantly reduced in BUL rats, but that pharmacodynamics of bisoprolol was not altered by acute renal failure.<br>
収録刊行物
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- Drug Metabolism and Pharmacokinetics
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Drug Metabolism and Pharmacokinetics 21 (5), 389-394, 2006
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詳細情報 詳細情報について
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- CRID
- 1390001205179660544
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- NII論文ID
- 130004462980
- 10018307025
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- NII書誌ID
- AA1162652X
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- ISSN
- 18800920
- 13474367
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- Crossref
- CiNii Articles
- KAKEN
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- 使用不可