[The neurotoxicity of pyridinium metabolites of haloperidol]

Postepy Hig Med Dosw (Online). 2015 Oct 19:69:1169-75. doi: 10.5604/17322693.1175009.
[Article in Polish]

Abstract

Haloperydol is a butyrophenone, typical neuroleptic agent characterized as a high antipsychotics effects in the treatment of schizophrenia and in palliative care to alleviation many syndromes, such as naursea, vomiting and delirium. Clinical problems occurs during and after administration of the drug are side effects, particularly extrapyrramidal symptoms (EPS). The neurotoxicity of haloperydol may be initiated by the cationic metabolites of haloperydol, HPP+, RHPP+, formed by oxidation and reduction pathways. These metabolites are transported by human organic cation transporters (hOCT) to several brain structures for exapmle, in substantia nigra, striatum, caudate nucleus, hippocampus. After reaching the dopaminergic neurons inhibits mitochondrial complex I, evidence for free radical involvement, thus leading to neurodegeneration.

Publication types

  • Review

MeSH terms

  • Antipsychotic Agents / pharmacology*
  • Biotransformation*
  • Brain / drug effects*
  • Delirium / drug therapy
  • Haloperidol / adverse effects*
  • Haloperidol / metabolism
  • Haloperidol / pharmacology
  • Humans
  • Nausea / drug therapy
  • Neurodegenerative Diseases / chemically induced*
  • Neurotoxicity Syndromes*
  • Schizophrenia / drug therapy

Substances

  • Antipsychotic Agents
  • Haloperidol