Source: Health Products Regulatory Authority (IE) Revision Year: 2020 Publisher: Laboratoires Thea, 12, rue Louis Blériot, 63017 Clermont-Ferrand Cedex 2, France
Pharmacotherapeutic group: Ophthalmologicals, other anti-allergics
ATC code: S01GX08
Ketotifen is a histamine H1-receptor antagonist. In vivo animal studies and in vitro studies suggest the additional activities of mast cell stabilisation and inhibition of infiltration, activation and degranulation of eosinophils.
In a pharmacokinetic study conducted in 18 healthy volunteers with Zaditen eye drops, plasma levels of ketotifen after repeated ocular administration for 14 days were in most cases below the limit of quantitation (20 pg/ml).
After oral administration, ketotifen is eliminated biphasically with an initial half-life of 3 to 5 hours and a terminal half-life of 21 hours. About 1% of the substance is excreted unchanged in the urine within 48 hours and 60 to 70% as metabolites. The main metabolite is the practically inactive ketotifen-N-glucuronide.
Preclinical data reveal no special hazard which is considered relevant in connection with use of Zaditen eye drops in humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential and toxicity to reproduction.
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