Posted by ed_uk on May 3, 2006, at 13:09:59
Sulpiride (Dolmatil) and amisulpride (Solian) are antipsychotics which are used in the treatment of schizophrenia. Although these drugs cause less EPS than typical APs, hyperprolactinemia is still a common problem, leading to numerous unpleasant side effects eg. sexual dysfunction, lactation etc.
Carmoxirole is a peripherally-acting dopamine agonist, it does not cross the blood brain barrier in significant quantities. In theory, carmoxirole could reverse amisulpride-induced hyperprolactinemia without affecting antipsychotic efficacy.
Eur J Pharmacol. 2002 Jun 28;447(1):109-14.
Carmoxirole is able to reduce amisulpride-induced hyperprolactinemia without affecting its central effect.Marchese G, Ruiu S, Casti P, Bartholini F, Saba P, Gessa GL, Pani L.
Neuroscienze S.c.a.r.l., Cagliari, Italy.
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.
.........................................unfortunately, carmoxirole is not available as a medication.
Ed
poster:ed_uk
thread:639622
URL: http://www.dr-bob.org/babble/20060429/msgs/639622.html