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Ketotifen

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From Pharmacopedia
Ketotifen
Zaditor, Alaway (ophthalmic, OTC); Zaditen (systemic, outside US)

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Summary
Common uses
Allergic conjunctivitis (ophthalmic)0
Pharmacy
Starting dose
Ophthalmic 1 drop in each eye every 8-12 hours
Preparations
0.025%, 0.035% ophthalmic solutions
US FDA Max
1 drop per eye q8-12h
Pharmacology
Routes
Topical ophthalmic
Onset
Within minutes
Duration
8-12 hours
Half-life
Not meaningfully described for ophthalmic use[1]
Bioavailability
Topical with minimal systemic absorption[1]
Pregnancy
Generally considered safe (minimal systemic exposure).[citation needed]
Legal status
OTC in US
Purported mechanism
Ketotifen is a dual-acting agent like olopatadine: selective H1 receptor antagonism provides immediate symptom relief, while mast cell membrane stabilization prevents further degranulation.0 Systemic oral ketotifen (available outside US) has historical use for asthma adjunct therapy via the same dual mechanism, but oral use produces sedation and weight gain — the topical ophthalmic application largely avoids both[1].

References

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  1. 1.0 1.1 1.2 FDA Prescribing Information, Zaditor (ketotifen fumarate), Novartis Consumer Health (now OTC), current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021066s019lbl.pdf