Домперидон

Химические свойства

White or almost white powder.

Использование

A novel peripheral dopamine receptor antagonist that does not cross the blood-brain barrier; anti-emetic. Domperidone(Motilium) is a dopamine blocker and an antidopaminergic reagent.

Определение

ChEBI: 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used s an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet reparations.

Всемирная организация здравоохранения(ВОЗ)

Domperidone, a peripheral dopaminergic antagonist, was introduced in 1979 for the symptomatic relief of acute nausea and vomiting. The major manufacturer became aware that the injectable formulation was being used in some countries in much higher doses than those recommended to combat nausea and vomiting in cancer patients treated with cytostatic agents. Such use - which was not in conformity with the approved indications - was associated with cardiotoxicity, which in some cases was fatal, and the manufacturer decided to withdraw the injectable dosage form from the market worldwide in January 1985. Suppositories, tablets and a suspension remain available and the manufacturer continues to supply the injection for the treatment of a named patient at the written request of a doctor on the understanding that the appropriate dosage recommendations will be followed.

Биологическая активность

Peripheral dopamine D 2 -like receptor antagonist that does not readily cross the blood brain barrier. Displays gastroprokinetic and antiemetic properties; increases the frequency and duration of antral and duodenal contractions and protects from apomorphine-induced emesis (ED 50 values are 0.003 and 0.03 mg/kg for i.v. and oral administration respectively).