Drug intelligence / Profile preview

domperidone

Development stage
Phase 4
Lead developer
Janssen Pharmaceutica
Modality
Small Molecules
Administration
Oral, Rectal
01

Overview

Domperidone is a peripherally selective dopamine D2 and D3 receptor antagonist used primarily as an antiemetic (to treat nausea and vomiting) and as a prokinetic agent to enhance gastrointestinal motility. It works by blocking dopamine receptors in the gut and the chemoreceptor trigger zone (CTZ) of the brain located outside the blood-brain barrier. This action increases esophageal and gastric peristalsis—helping food move more quickly through the digestive tract—and reduces symptoms of nausea. Unlike some other dopamine antagonists such as metoclopramide, domperidone does not significantly cross the blood-brain barrier, minimizing central nervous system side effects[1][5][6][7]. Additionally, it can increase prolactin release from the anterior pituitary gland by blocking D2 receptors on lactotrophs; this effect is sometimes used off-label to stimulate breast milk production[1][7]. Domperidone was first introduced in the late 1970s and is approved for use in many countries but not in the United States due to concerns about cardiac adverse events[1][3].

Brand names
MotiliumNauzelinDomstalEucitonMoperidonaVometaZilium
Other names
domperidonDomperidonumDomperidona
02

Targets

DRD3 (Dopamine receptor D3)DRD2 (Dopamine D2 Receptor)

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