Domilium Mechanism of Action





Full Prescribing Info
Pharmacologic classification: Propulsive.
Pharmacology: Domperidone is a dopamine antagonist with anti-emetic properties. It does not readily cross the blood-brain barrier. In domperidone users, especially in adults, extrapyramidal side effects are very rare, but domperidone promotes the release of prolactin from the pituitary. Its anti-emetic effect may be due to a combination of peripheral (gastrokinetic) effects and antagonism of dopamine receptors in the chemoreceptor trigger zone, which lies outside the blood-brain barrier in the area postrema.
Pharmacokinetics: The systemic bioavailability of domperidone is only about 15% in fasting subjects given a dose by mouth, although this is increased when domperidone is given after food. The low bioavailability is thought to be due to first-pass hepatic and intestinal metabolism.
Domperidone is more than 90% bound to plasma proteins, and has a terminal elimination half-life of about 7.5 hours. It is chiefly cleared from the blood by extensive metabolism. About 30% of an oral dose is excreted in faeces over several days, about 10% as unchanged drug. It does not readily cross the blood-brain barrier.
Small amounts of domperidone are distributed into breast milk, reaching concentrations about one-quarter of those in maternal serum.
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