increased when sulpiride is combined with other drugs, but this is not related to substrates, inducers and inhibitors of CYPs. Pharmacology Pharmacodynamics Sulpiride is a selective antagonist at dopamine D2, D3 and 5-HT1A receptors. Antagonism at 5-HT1A dominates in doses exceeding 600 mg daily. In doses of 600 to 1,600 mg sulpiride shows mild sedating and antipsychotic activity. Its antipsychotic potency compared to chlorpromazine is only 0.2 (1/5). In low doses (in particular 50 to 200 mg daily) its prominent feature is antagonism of presynaptic inhibitory dopamine and serotonin receptors, accounting for some antidepressant activity and a stimulating effect. Additionally, it alleviates vertigo. The benzamide neuroleptics (including sulpiride, amisulpride, and sultopride) have been shown to activate the endogenous gamma-hydroxybutyrate receptor in vivo at therapeutic concentrations. Sulpiride was found in one study in rats to upregulate GHB receptors. GHB has neuroleptic properties and it is believed binding to this receptor may contribute to the effects of these neuroleptics. Sulpiride, along with clozapine, and valproate has been found to activate DNA demethylation in the brain. History Sulpiride was discovered in 1966 as a result of a research program by Justin-Besançon and C. Laville at Laboratoires Delagrange who were working to improve the anti-dysrhythmic properties of procainamide; the program led first to metoclopramide and later to sulpiride. Laboratoires Delagrange was acquired by Synthelabo in 1991 which eventually became part of Sanofi. Society and culture Brand names Sulpiride is marketed under the brand names Dogmatil (DE, HK, SG, PH), Dolmatil (IE, UK), Eglonyl (RU, ZA, HR, SI), Espiride (ZA), Modal (IL), Prometar (UY), Equilid (BR) and Sulpor (UK), among many others. Medicinal forms These include tablet and oral solution Patient Aversions Some individuals from the Caribbean region may have an aversion to taking the medication due to the association with the brand name of Dogmatil. Dogmatil has been associated with dog medication. Research Sulpiride has been studied for use as a hormonal contraceptive in women in whom conventional oral contraceptives are contraindicated and to potentiate progestogen-only contraceptives. The contraceptive effects of sulpiride are due to its prolactin-releasing and antigonadotropic effects and the hyperprolactinemia–amenorrhea state that it induces. Since the use of psychotropic drugs is efficient in treating irritable bowel syndrome (IBS), sulpiride is studied as potential sole maintenance therapy in the treatment of IBS. References External links Atypical antipsychotics Antigonadotropins Benzamides Galactagogues GHB receptor ligands Hormonal contraception Phenol ethers Prolactin releasers Pyrrolidines Sulfonamides