Metopimazine

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Metopimazine (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name, BANTooltip British Approved Name), sold under the brand names Vogalen and Vogalene, is an antiemetic of the phenothiazine group which is used to treat nausea and vomiting. It is marketed in Europe, Canada, and South America. As of August 2020, metopimazine has been repurposed and is additionally under development for use in the United States for the treatment of gastroparesis. Metopimazine has antidopaminergic, antihistamine, and anticholinergic activity. However, it has also been described as a highly potent and selective dopamine D2 and D3 receptor antagonist. The D2 receptor antagonism of metopimazine is thought to underlie its antiemetic and gastroprokinetic effects. It is said to not readily cross the blood–brain barrier and hence to have peripheral selectivity, in contrast to metoclopramide but similarly to domperidone. Unlike domperidone however, metopimazine shows no hERG inhibition and hence is expected to have a more favorable cardiovascular profile. In contrast to metoclopramide, metopimazine does not interact with serotonin 5-HT3 and 5-HT4 receptors. Metopimazine is an approved prescription drug in France under the brand name Vogalene® that has been used for the treatment of nausea and vomiting.