Domperidone

Domperidone (INN, USAN, BAN, JAN) (brand names Motilium, Motillium, Motinorm Costi, Nomit, Brulium, Molax) is a drug developed by Janssen Pharmaceutica that acts as a peripherally selective antagonist of the dopamine D₂ and D₃ receptors. It is administered orally, rectally, or intravenously. Domperidone is used to relieve nausea and vomiting; to increase the transit of food through the stomach (that is, as a prokinetic agent via increasing gastrointestinal peristalsis); and to promote lactation (breast milk production) by release of prolactin. It is also used in scientific research to study the biological function of dopamine, an important neurotransmitter and hormone, in the body.

Domperidone is available in the form of tablets, orally disintegrating tablets (based on Zydis technology),suspension and suppositories.

Mechanism of action

Domperidone is a peripheral dopamine D₂ and D₃ receptor antagonist. It provides relief from nausea by blocking receptors at the chemoreceptor trigger zone (a location in the nervous system that mediates nausea) at the floor of the fourth ventricle (a location near the brain). It increases motility in the upper gastrointestinal tract to a moderate degree and increaseslower esophageal sphincter pressure by blocking dopamine receptors in the gastric antrum and the duodenum. It blocks dopamine receptors in the anterior pituitary gland increasing release of prolactin which in turn increases lactation. Domperidone may be more useful in some patients and cause harm in others by way of the genetics of the person, such as polymorphisms in the drug transporter gene ABCB1 (which encodes P-glycoprotein), the voltage-gated potassium channel KCNH2 gene (hERG/K_v11.1), and the α_1D—adrenoceptor ADRA1D gene.