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Isothipendyl is a first-generation antihistamine of the azaphenothiazine class, primarily used as an antipruritic agent. It acts as a selective antagonist at the histamine H1 receptor, competitively inhibiting the effects of endogenous histamine and thereby providing relief from symptoms such as itching (pruritus) associated with allergic reactions and insect bites. In addition to its antihistaminic activity, isothipendyl exhibits anticholinergic and antiserotoninergic properties, which can contribute to sedative side effects like somnolence. Due to these side effects, its use has declined in favor of newer agents but it remains available for topical application in dermatological conditions[1][4][5][6].
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