Chirality of reduced haloperidol in humans

Eur Neuropsychopharmacol. 1998 May;8(2):127-9. doi: 10.1016/s0924-977x(97)00049-7.

Abstract

In vitro, cytosolic human ketone reductases catalyse the stereospecific (i.e. >99%) formation of S(-) reduced haloperidol (RHP) from haloperidol (HP). Whether this situation is reflected in patients taking the drug is unknown. In this study in nine patients taking HP, only 73.2+/-18.2% of the RHP excreted in urine was the S(-) enantiomer. Thus, enzymes other than cytosolic ketone reductases must be responsible for the formation of the minor enantiomer.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Antipsychotic Agents / chemistry*
  • Antipsychotic Agents / pharmacokinetics
  • Antipsychotic Agents / urine
  • Chromatography, High Pressure Liquid
  • Haloperidol / analogs & derivatives*
  • Haloperidol / chemistry
  • Haloperidol / pharmacokinetics
  • Haloperidol / urine
  • Humans
  • Male
  • Middle Aged
  • Oxidation-Reduction
  • Stereoisomerism

Substances

  • Antipsychotic Agents
  • 4-(4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-1-butanol
  • Haloperidol