epinastine

Epinastine is a small molecule, topically active antihistamine used primarily as an ophthalmic solution to prevent itching of the eyes caused by allergic conjunctivitis. It acts as a direct antagonist at the histamine H1 receptor and also inhibits histamine release from mast cells, thereby stabilizing them. Epinastine has additional affinity for the histamine H2 receptor, α1- and α2-adrenergic receptors, and 5-HT2 serotonin receptors. Its mechanism involves blocking histamine binding to both H1 and H2 receptors, stabilizing mast cells to prevent degranulation, and inhibiting the release of proinflammatory mediators from blood vessels. Epinastine does not significantly penetrate the blood-brain barrier, reducing central nervous system side effects. The drug is indicated for prevention of ocular itching associated with allergic conjunctivitis[1][3][6].

Brand names

Elestat

Other names

epinastine hydrochloride