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Ketotifen, sold under the brand name Zaditor among others, is a second-generation noncompetitive H₁–antihistamine and mast cell stabilizer. It is most commonly sold as a salt with fumaric acid, ketotifen fumarate, and is available in two forms. In its ophthalmic form, it is used to treat allergic conjunctivitis.^[1] In its oral form, it is used to prevent asthma attacks or anaphylaxis, as well as various mast cell, allergic-type disorders.^{[2][3][4][5][6]}

It was patented in 1970 and came into medical use in 1976.^[7]

Medical uses[edit]

Ketotifen relieves and prevents eye itchiness and/or irritation associated with most seasonal allergies. It starts working within minutes after administering the drops. The drug has not been studied in children under three.^[1] The mean elimination half life is 12 hours.^[8] Besides its anti-histaminic activity, it is also a functional leukotriene antagonist^[9] and a phosphodiesterase inhibitor.^[10]

“[O]ral ketotifen has been used in patients with asthma, allergic rhinitis, allergic conjunctivitis, atopic dermatitis, chronic urticaria, cold-induced urticaria, cholinergic urticaria, exercise-induced urticaria, [systemic mast cell disease including mastocytosis, MCAS, allergic and nonallergic anaphylaxis, angioedema], and food allergy in Canada, Europe, and Mexico.” Now available via prescription at US compounding pharmacies: “For adults and older children with asthma or allergic disease, the recommended dose of ketotifen is 1 mg twice daily.” “FDA staff did recommend more extensive evaluations for management of urticaria.”^[4][5]

The drug may also help relieve irritable bowel syndrome.^[11]

Side effects[edit]

Side effects include drowsiness, weight gain (11-12lbs), dry mouth, irritability, and increased nosebleeds.^[12]

Pharmacology[edit]

Ketotifen is a selective antihistamine