mepyramine

Mepyramine is a first-generation antihistamine used for the symptomatic treatment of allergy, hypersensitivity reactions, and pruritic skin disorders. Also known as pyrilamine or as its salt form pyrilamine maleate, it acts as a histamine H1 receptor inverse agonist. Mepyramine binds to the G protein-coupled form of the H1 receptor and promotes an inactive state that interferes with Gq/11-mediated signaling. This results in suppression of histaminic edema (swelling), flare (redness), and pruritus (itching). Due to its ability to rapidly cross the blood-brain barrier and act at subcortical levels in the CNS, it often causes drowsiness as a side effect. Mepyramine has been included in over-the-counter combination products for colds and menstrual symptoms but is considered unapproved for some uses in certain countries[1][2][5].

Brand names

Midol CompleteMidol Cramps & BodyachesPamprin Multi-symptomPremsyn PmsVanacof-8Vanacof8Vanacof 8

Other names

pyrilamine maleatemepyraminummépyraminemepiraminapyranisaminepyrilaminmepyramon