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Psychopharmacology

, Volume 116, Issue 4, pp 457–463 | Cite as

Pharmacokinetics and bioavailability of benperidol in schizophrenic patients after intravenous and two different kinds of oral application

  • Walther Seiler
  • Hermann Wetzel
  • Andreas Hillert
  • Günter Schöllnhammer
  • Michael Langer
  • Uwe Barlage
  • Christoph Hiemke
Article

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 (t1/2β), 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-gt1/2β values were 5.5 and 4.7 h, respectively, mean-g tmax data were 1.0 h and 2.7 h, mean-g MRT values were 8.44 and 8.84 h, and mean-g Cmaxmaxvalues were 10.2 and 7.3 ng/ml. Differences between liquid and tablet administration were statistically significant for time lag,tmax, andCmax. 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.

Key words

Neuroleptic Benperidol Reduced benperidol Pharmacokinetics Bioavailability Schizophrenics 

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Copyright information

© Springer-Verlag 1994

Authors and Affiliations

  • Walther Seiler
    • 1
  • Hermann Wetzel
    • 1
  • Andreas Hillert
    • 1
  • Günter Schöllnhammer
    • 2
  • Michael Langer
    • 2
  • Uwe Barlage
    • 2
  • Christoph Hiemke
    • 1
  1. 1.Department of PsychiatryUniversity of MainzMainzGermany
  2. 2.Troponwerke, Department of Clinical ResearchKölnGermany

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