Bioavailability and Kinetics of Cibenzoline in Patients with Normal and Impaired Renal Function
作者:
George Aronoff,
Michael Brier,
Mary Lou Mayer,
Michael Barbalas,
Keiko Aogaichi,
Rebecca Sloan,
Romulus Brazzell,
Joseph Massarella,
期刊:
The Journal of Clinical Pharmacology
(WILEY Available online 1991)
卷期:
Volume 31,
issue 1
页码: 38-44
ISSN:0091-2700
年代: 1991
DOI:10.1002/j.1552-4604.1991.tb01884.x
出版商: Blackwell Publishing Ltd
数据来源: WILEY
摘要:
To test the hypothesis that renal failure alters the disposition of cibenzoline in humans, an absolute bioavailability and elimination kinetic study was performed. We used the simultaneous administration of a stable isotope variant (SASIV). Eight healthy volunteers and eight matched hemodialysis patients each received simultaneously an 80‐mg intravenous infusion of 15N‐2‐cibenzoline and a single 80‐mg cibenzoline capsule. Cibenzoline plasma concentrations were assayed by a gas chromatographic—mass spectrometric assay. A compartment‐independent kinetic analysis showed a plasma clearance of 707 mL/min and an elimination half‐life of 7.3 hours after the intravenous dose in healthy volunteers. In renal‐failure patients, cibenzoline clearance decreased to 224 mL/min and half‐life increased to 22.4 hours. Decreased plasma clearance was due to decreases in both renal and nonrenal clearance. Absolute bioavailability was 83% and 90% in healthy volunteers and renal‐failure patients, respectively. Hemodialysis accounted for only 13
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