Carmoxirole is able to reduce amisulpride-induced hyperprolactinemia without affecting its central effect

Eur J Pharmacol. 2002 Jun 28;447(1):109-14. doi: 10.1016/s0014-2999(02)01896-4.

Abstract

Prolactin blood level and apomorphine-induced yawning were studied in rats treated with the substituted benzamide amisulpride in association with bromocriptine or carmoxirole; two dopamine D(2) receptor agonists with high or low propensity to cross the brain-blood barrier, respectively. Administration of amisulpride produced a maximum increase in rat serum prolactin level (315+/-18%) vs. vehicle-treated animals (ED(50)=0.25+/-0.017 mg/kg, s.c.). The concurrent administration of carmoxirole or bromocriptine completely reversed the hyperprolactinemia induced by amisulpride (0.5 mg/kg, s.c.) (ID(50)=14.9+/-0.8 mg/kg and 0.81+/-0.03 mg/kg, respectively). Carmoxirole (15 mg/kg, i.p.) did not affect yawning induced by apomorphine (0.08 mg/kg, s.c.) nor amisulpride (0.5 mg/kg, s.c.) blockade of apomorphine-induced yawning. Conversely, a significant increase in the number of yawns was observed when bromocriptine (0.8 mg/kg, i.p.) was associated with apomorphine in the absence or presence of amisulpride. These results suggested that a peripheral dopamine D(2) receptor agonists could be a useful tool in alleviating amisulpride-induced hyperprolactinemia without possibly affecting its central effect.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amisulpride
  • Animals
  • Antipsychotic Agents / adverse effects
  • Antipsychotic Agents / pharmacology*
  • Binding, Competitive
  • Bromocriptine / pharmacology
  • Dopamine Agonists / pharmacology*
  • Hyperprolactinemia / chemically induced
  • Hyperprolactinemia / drug therapy*
  • In Vitro Techniques
  • Indoles / pharmacology*
  • Male
  • Pituitary Gland / metabolism
  • Pituitary Gland / ultrastructure
  • Prolactin / blood
  • Pyridines / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Dopamine D2 / drug effects
  • Sulpiride / adverse effects
  • Sulpiride / analogs & derivatives*
  • Sulpiride / pharmacology*
  • Synaptosomes / metabolism
  • Yawning / drug effects

Substances

  • Antipsychotic Agents
  • Dopamine Agonists
  • Indoles
  • Pyridines
  • Receptors, Dopamine D2
  • Bromocriptine
  • Sulpiride
  • Amisulpride
  • Prolactin
  • carmoxirole