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Fexofenadine is an antiallergic agent belonging to the second-generation antihistamines. It is approved for the symptomatic treatment of hay fever and chronic urticaria. Due to its long half-life, once-daily administration is sufficient. Fexofenadine causes drowsiness less frequently than first-generation antihistamines and has no anticholinergic activity. Unlike its predecessor terfenadine (Teldane®), it is not cardiotoxic and has a low interaction potential. Possible adverse effects include, among others, hypersensitivity reactions, headache, somnolence, and fatigue.
Fexofenadine (ATC R06AX26) has antihistaminic, antiallergic, anti-inflammatory, and mast cell-stabilizing properties. It does not cross the blood-brain barrier because it is hydrophilic and a substrate of P-glycoprotein. For this reason, it is less sedating than first-generation antihistamines.
Fexofenadine has no anticholinergic activity and is not cardiotoxic like its predecessor terfenadine. It is an inverse and selective antagonist at the H1 receptor, counteracting the effects of histamine and thereby relieving symptoms such as pruritus, sneezing, rhinorrhea, erythema, swelling, and lacrimation.
Mechanism of action of antihistamines, click to enlarge. Illustration © PharmaWiki