Anticholinergic properties of antipsychotic drugs and their relation to extrapyramidal side-effects

Psychopharmacology (Berl). 1976 Dec 21;51(1):15-22. doi: 10.1007/BF00426315.

Abstract

The effects of haloperidol, alone and in combination with atropine, were compared with the effects of clozapine, alone and in combination with physostigmine, in a variety of tests commonly used to characterize neuroleptic compounds. It was found that clozapine in combination with physostigmine did not present the profile of activity of a classical neuroleptic agent; neither did haloperidol in combination with atropine present that of clozapine. In fact, some effects of haloperidol (catalepsy) were antagonized by atropine, while others (induction of striatal DA-receptor hypersensitivity) were enhanced. It is concluded that the interaction between dopaminergic and cholinergic systems in the striatum is highly complex, and that a neuroleptic possessing both potent DA-receptor blocking and muscarinic anticholinergic activity, while being less likely to cause parkinsonism in patients, would be more likely to induce tardive dyskinesias.

MeSH terms

  • Animals
  • Antipsychotic Agents / adverse effects
  • Antipsychotic Agents / pharmacology*
  • Atropine / pharmacology
  • Basal Ganglia Diseases / chemically induced*
  • Clozapine / pharmacology
  • Corpus Striatum / metabolism
  • Drug Interactions
  • Dyskinesia, Drug-Induced / etiology
  • Female
  • Haloperidol / pharmacology
  • Homovanillic Acid / metabolism
  • Male
  • Parasympathetic Nervous System / drug effects*
  • Physostigmine / pharmacology
  • Rats
  • Receptors, Dopamine / drug effects
  • Receptors, Muscarinic / drug effects

Substances

  • Antipsychotic Agents
  • Receptors, Dopamine
  • Receptors, Muscarinic
  • Atropine
  • Physostigmine
  • Clozapine
  • Haloperidol
  • Homovanillic Acid