Pharmacokinetic Study of Rilmazafone Hydrochloride in patients with Chronic Renal Failure

Shinichi KOBAYASHI, Eiji UCHIDA, Katsuji OGUCHI, Hajime YASUHARA, Shouzou KOSHIKAWA, Tadao AKIZAWA, Kimihiro TAKAYAMA, Tetsushi NAGAI, Takayoshi OGUMA, Kenji SHIMAMURA, Hiromi KAWAMOTO, Gorou KOMINAMI
1992 Rinsho yakuri/Japanese Journal of Clinical Pharmacology and Therapeutics  
8: Co., Ltd. Rilmazafone Hydrochloriode (RZ), a prodrug of benzodiazepine derivatives, is used clinically as a sleep inducer. The pharmacokinetics of RZ in patients were studied to determine the clinical dose for patients with chronic renal failure. 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
more » ... or 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 RUC'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.
doi:10.3999/jscpt.23.573 fatcat:5nfrh6e2ijc5lnofjepzmpw54m