Interindividual variabilities in haloperidol interconversion and the reduced haloperidol/haloperidol ratio

Y. W.F. Lam, W. H. Chang, Michael Wong Jann, H. Chen

Research output: Contribution to journalArticle

7 Scopus citations

Abstract

Metabolism of haloperidol in humans includes N-dealkylation to inactive metabolites and reduction to reduced haloperidol; reduced haloperidol is also oxidized back to haloperidol. A single 0.5 mg/kg (0.00133 mmol/kg) oral dose of haloperidol and reduced haloperidol was administered to seven Chinese schizophrenics in a randomized crossover manner separated by a 2-week interval. The clearance values for the different metabolic pathways of haloperidol and reduced haloperidol were determined. There were differences up to 10-fold in both oxidation and reduction capacities. There were also interindividual variabilities in the elimination of reduced haloperidol (0.37 ± 0.20 L/hr/kg) and the N-dealkylation pathway (0.74 ± 0.36 L/hr/kg). Four weeks after the single-oral dose study, the same patients also received haloperidol (10 mg) twice daily for 4 weeks. The reduced haloperidol to haloperidol concentration ratio (0.40 ± 0.16) after the 4-week therapy is related to individual variabilities in the interconversion process and the N-dealkylation pathway of haloperidol.

Original languageEnglish
Pages (from-to)33-39
Number of pages7
JournalNeuropsychopharmacology
Volume7
Issue number1
StatePublished - 1 Jan 1992

Keywords

  • Biotransformation
  • Haloperidol
  • Interconversion
  • Metabolic clearance rate
  • Metabolic detoxication
  • Reduced haloperidol

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