Determination of clozapine in serum by radioreceptor assay versus high-performance liquid chromatography: possible detection of hydroxy-metabolites

J Clin Pharm Ther. 1996 Oct;21(5):337-42. doi: 10.1111/j.1365-2710.1996.tb00028.x.

Abstract

Clozapine is an antipsychotic drug with few extra-pyramidal motor side-effects, used to treat schizophrenia which is resistant to classical neuroleptic therapy. This report shows that norclozapine but not clozapine-N-oxide has the same D2 receptor affinity as clozapine. Assay results suggest a bimodal distribution which may be explained by CYP1A2 polymorphism. Extensive metabolizers could produce other active metabolites, probably other hydroxy-clozapine derivatives.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Antipsychotic Agents / blood*
  • Antipsychotic Agents / therapeutic use
  • Chromatography, High Pressure Liquid
  • Clozapine / analogs & derivatives
  • Clozapine / blood*
  • Clozapine / therapeutic use
  • Corpus Striatum / metabolism
  • Female
  • Humans
  • Hydroxylation
  • Male
  • Radioligand Assay
  • Rats
  • Receptors, Dopamine D2 / metabolism
  • Schizophrenia / blood*
  • Schizophrenia / drug therapy

Substances

  • Antipsychotic Agents
  • Receptors, Dopamine D2
  • norclozapine
  • Clozapine
  • clozapine N-oxide