Sulpiride

• IUPAC: (RS)- N-[( 1-ethyl pyrrolidin-2- yl ) methyl] -2 - methoxy-5 - sulfamoylbenzamid
• Latin: Sulpiridum

• N05AL01
• N05AL07

White to off- white crystalline powder

Neuroleptics, atypical neuroleptics

Blockade of D2 receptors

9.12

Practically insoluble in water ( 2280 mg · l-1 at 25 ° C), slightly soluble in methanol, sparingly soluble in dichloromethane and ethanol 96 %

170 mg · kg -1 ( LD50, mouse, ip)

Template: Infobox chemical / molecular formula search available

Sulpiride is a drug which is mainly used in psychiatry. It is one of the atypical antipsychotics ( but is handled in some texts as a typical antipsychotic ), but also has a certain anti -depressant effect. The chemical structure is a substituted benzamide. Sulpiride was brought to market in 1972.

Action profile

Sulpiride has a strong affinity for the D2 and D3 receptors in the brain. Other neurotransmitter systems are hardly affected.

The antipsychotic effect will occur from doses above 600 mg / day. The reason for this probably is the low cross barriers of sulpiride, which can act as a highly potent neuroleptic actually the fabric only at higher doses. The higher permeability of the blood -brain barrier in the area of ​​tubero - infundibular system means that even relatively low doses of sulpiride may cause increased prolactin secretion.

With low doses of sulpiride affects mood enhancing and activating.

Indication

Sulpiride is approved to treat depression when other antidepressants have failed or could not be applied. In higher doses it can be used for the treatment of schizophrenia.

Sulpiride is also licensed for the symptomatic treatment of vertigo ( Meniere's disease ). The application for this indication is controversial.

Adverse effects

The main side effect of sulpiride is the increase in prolactin secretion, which can lead to feminization and gynecomastia in women, for example, to cycle disorders in men. The activating effect of sulpiride may sometimes be perceived as very annoying and cause sleep disturbances.

Especially in high doses sulpiride may cause extrapyramidal disorders ( extrapyramidal syndrome ).

Dosage forms

Sulpiride is in various dosage forms for oral ingestion before (tablets, capsules, juice, etc. ) and as a solution for injection.

The daily dose depends on the particular field of application, due to the activating effect of sulpiride should be taken in the morning, or the last single dose should be given at the latest until 16:00 clock. The dosage should - especially at higher target dose - be changed on or gradually.

Production

A multi-step synthesis for sulpiride is described in the literature.