Pharmacokinetic Study of Rilmazafone Hydrochloride in patients with Chronic Renal Failure.
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- KOBAYASHI Shinichi
- Department of Pharmacology, School of Medicine, Showa University
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- UCHIDA Eiji
- Department of Pharmacology, School of Medicine, Showa University
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- OGUCHI Katsuji
- Department of Pharmacology, School of Medicine, Showa University
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- YASUHARA Hajime
- Department of Pharmacology, School of Medicine, Showa University
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- KOSHIKAWA Shouzou
- Department of Nephrology, Showa University, Fujigaoka Hospital
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- AKIZAWA Tadao
- Department of Nephrology, Showa University, Fujigaoka Hospital
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- TAKAYAMA Kimihiro
- Department of Nephrology, Showa University, Fujigaoka Hospital
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- NAGAI Tetsushi
- Department of Nephrology, Showa University, Fujigaoka Hospital
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- OGUMA Takayoshi
- Shionogi Research Laboratories, Shionogi & Co., Ltd.
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- SHIMAMURA Kenji
- Shionogi Research Laboratories, Shionogi & Co., Ltd.
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- KAWAMOTO Hiromi
- Shionogi Research Laboratories, Shionogi & Co., Ltd.
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- KOMINAMI Gorou
- Shionogi Research Laboratories, Shionogi & Co., Ltd.
Bibliographic Information
- Other Title
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- 塩酸リルマザホンの腎不全患者における薬物速度論的研究
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Abstract
Rilmazafone Hydrochloriode (RZ), a prodrug of benzodiazepine derivatives, is used clinically as a sleep inducer.<br>The pharmacokinetics of RZ in patients were studied to determine the clinical dose for patients with chronic renal failure.<br>Five patients (2 male, 3 female, aged 44-62yr) who participated in this study were undergoing hemodialysis. They were given RZ (1mg, p. o.) one time on the day of dialysis, and 5-7 days later on the day of non-dialysis. Blood samples were collected for 48hr after each administration to determine the concentrations of metabolites of RZ (M1, M2, MA, M3, M4). Pharmacokinetic profiles of RZ in these patients were compared with those in healthy volunteers (2mg, p. o.). Despite the dose difference and body weight difference (patients, 53kg (mean), volunteers, 60kg), Cmax's of M1 and M4 in patients were double and AUC's were five times those in healthy volunteers. T1/2's of M1, M2, M4 in patients were two to four times longer than those in healthy volunteers. The pharmacokinetic profiles of total active metabolites in patients were not significantly different. However, plasma concentration-time curves of potent active metabolites (M1, M2) in patients would probably be higher than those in healthy volunteers, if both were given the same dose of RZ.<br>These results may indicate that dosage of RZ in patients with chronic renal failure should be started from 1mg, because of the reduction of hepatic metabolism and renal excretion of RZ in these patients.
Journal
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- Rinsho yakuri/Japanese Journal of Clinical Pharmacology and Therapeutics
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Rinsho yakuri/Japanese Journal of Clinical Pharmacology and Therapeutics 23 (3), 573-580, 1992
The Japanese Society of Clinical Pharmacology and Therapeutics
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Details 詳細情報について
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- CRID
- 1390001205340643968
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- NII Article ID
- 130002045686
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- COI
- 1:CAS:528:DyaK3sXjt1CltA%3D%3D
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- ISSN
- 18828272
- 03881601
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- Text Lang
- ja
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- Data Source
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- JaLC
- Crossref
- CiNii Articles
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- Abstract License Flag
- Disallowed