Pharmacokinetics of haloperidol and reduced haloperidol in chinese schizophrenic patients after intravenous and oral administration of haloperidol

Wen Ho Chang, Y. W. Francis Lam, Michael W. Jann, Hong Chen

Research output: Contribution to journalArticle

20 Scopus citations

Abstract

The pharmacokinetics of haloperidol were studied in eight Chinese schizophrenic patients after intravenous administration and in six of the patients who also received oral haloperidol. After intravenous dosing, haloperidol disposition was best characterized by a three compartment model. The mean elimination half-life of 54.8 h determined by model dependent analysis was similar to the mean elimination half-life of 59.9 h determined by model independent analysis. The mean plasma clearance was 21.7 l/h and the mean volume of distribution during the distribution phase was 1754.3 l. After oral dosing, bioavailability of haloperidol was 35±8%, suggesting extensive first pass metabolism. Determination of reduced haloperidol concentration confirmed a previous finding of significant variability in haloperidol reductive capacity in individual patients. Comparison of area under the plasma concentration-time curve of reduced haloperidol after intravenous and oral administration of haloperidol suggests that reduction of haloperidol may only account for a small portion of first pass metabolism of haloperidol. However, conversion of reduced haloperidol back to haloperidol necessitates the monitoring of both haloperidol and reduced haloperidol concentrations in clinical practice.

Original languageEnglish (US)
Pages (from-to)517-522
Number of pages6
JournalPsychopharmacology
Volume106
Issue number4
DOIs
StatePublished - Apr 1 1992

Keywords

  • Chinese schizophrenics
  • Haloperidol
  • Pharmacokinetics
  • Reduced haloperidol

ASJC Scopus subject areas

  • Pharmacology

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