Kees, Frieder and Faerber, L. and Bucher, M. and Mair, G. and Moerike, K. and Grobecker, H. (2001) Pharmacokinetics of therapeutic doses of tropisetron in healthy volunteers. BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 52 (6). pp. 705-707. ISSN 0306-5251
Full text not available from this repository. (Request a copy)Abstract
Aims To establish the bioavailability of tropisetron (5 mg) administered orally as capsule compared with 2 mg given intravenously. Methods Using a randomized crossover design, 18 healthy volunteers received a single oral dose of tropisetron (5 mg) and an intravenous bolus of tropisetron (2 mg) separated by a wash-out period of 1 week. Plasma concentrations of tropisetron were determined by h.p.l.c. and the pharmacokinetic parameters were estimated. Results The mean pharmacokinetic parameters for 5 mg tropisetron given orally were C-max 3.46 ng ml(-1), t(max) 2.6 h, t(1/2) 5.7 h and AUC(0,infinity) 32.9 ng ml(-1) h. After intravenous administration initial plasma concentration was 15.1 ng ml(-1) t(1/2) 5.6 h, AUC(0,infinity) 20.7 ng ml(-1) h, V 678 1 and CL 1800 ml min(-1). An inverse correlation was demonstrated between CYP2D6 activity, measured by the sparteine metabolic ratio, and the bioavailability (mean 0.60, range 0.27-0.99) of oral tropisetron. Conclusions Tropisetron exhibits a wide range of oral bioavailability at therapeutic doses, which is mainly determined by CYP2D6 activity.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | ; bioavailability; low doses; tropisetron; volunteers |
| Subjects: | 600 Technology > 610 Medical sciences Medicine 600 Technology > 615 Pharmacy |
| Divisions: | Medicine > Lehrstuhl für Anästhesiologie Chemistry and Pharmacy > Institute of Pharmacy > Pharmacology and Toxicology (Prof. Schlossmann, formerly Prof. Seifert) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 23 Nov 2021 10:50 |
| Last Modified: | 23 Nov 2021 10:50 |
| URI: | https://pred.uni-regensburg.de/id/eprint/40888 |
Actions (login required)
 |
View Item |
