ISSN:
1432-2072
Keywords:
Neuroleptic
;
Benperidol
;
Reduced benperidol
;
Pharmacokinetics
;
Bioavailability
;
Schizophrenics
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Abstract Pharmacokinetics and bioavailability of benperidol were determined in 13 schizophrenic patients after acute administration of 6 mg benperidol as an intravenous (i.v.) bolus injection, orally as liquid, and orally as tablets using a partially randomized cross-over design. Drug plasma levels were determined by high performance liquid chromatography with electrochemical detection and subjected to model independent pharmacokinetic analyses. After i.v. dosing the geometric means (mean-g) were 3.2 min for the distribution half-life, 5.80 h for the elimination half-life (t 1/2β), 4.21 l/kg for the distribution volume, 7.50 h for the mean residence time (MRT), and 0.50 l/(h*kg) for the clearance. After oral administration as liquid and as tablet mean-g data for the time lag until the first appearance of measurable plasma concentrations were 0.33 and 1.1 h, mean-g t 1/2β values were 5.5 and 4.7 h, respectively, mean-g t max data were 1.0 h and 2.7 h, mean-g MRT values were 8.44 and 8.84 h, and mean-g C max maxvalues were 10.2 and 7.3 ng/ml. Differences between liquid and tablet administration were statistically significant for time lag,t max, andC max. Mean-g absolute bioavailabilities were computed as 48.6% after liquid and 40.2% after tablet administration respectively. All parameters studied exhibited large intersubject variation. The plasma concentrations of the presumed metabolite “reduced benperidol” were found to be very low.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF02247478
