Emedastine difumarate, a potent H1-receptor antagonist, was launched in Japan for the
treatment of allergic rhinitis and urticaria. Emedastine exerts its antiallergic effect via
inhibition of substance P-induced histamine release. It has been demonstrated both in vitro
and in vivo that this effect is mediated by the inhibition of Ca2+release from extracellular
stores and of Ca2+ influx into mast cells. In a clinical trial with bronchial asthma, emedastine
improved asthmatic symptoms in 55.3% of patients.
ChEBI: The fumaric acid salt of emedastine containing two molecules of fumaric acid for each molecule of emedastine. A relatively selective histamine H1 antagonist, it is used for allergic rhinitis, urticaria, and pruritic skin disorders, and
in eyedrops for the symptomatic relief of allergic conjuntivitis.
