metopimazine

Metopimazine is a phenothiazine derivative and small molecule antiemetic used primarily for the prevention and treatment of nausea and vomiting. It acts as a highly potent and selective antagonist of dopamine D2 and D3 receptors, with its antiemetic effects attributed to antagonism at D2 receptors in the chemoreceptor trigger zone (area postrema) as well as in the gut, leading to increased gastrointestinal motility. Unlike some other agents in its class, metopimazine does not readily cross the blood–brain barrier, resulting in peripheral selectivity and reduced central nervous system side effects. It also exhibits antihistamine (H1 receptor antagonism), anticholinergic activity, alpha-adrenoceptor blocking properties, but does not interact with serotonin 5HT3 or 5HT4 receptors nor inhibit hERG channels—suggesting a favorable cardiovascular safety profile compared to similar drugs like domperidone or metoclopramide. Metopimazine has been marketed for many years in Europe for acute nausea/vomiting; it is under development in the United States for gastroparesis[1][6][8].

Brand names

VogalenVogaleneNorzelan

Other names

MetopimazinaMetopimazinum