Source: Health Products Regulatory Authority (IE) Revision Year: 2017 Publisher: Pharma Stulln GmbH, Werksstrasse 3, 92551 Stulln, Germany
Pharmacotherapeutic group: Ophthalmologicals, other antiallergics
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 ketotifen-containing 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 a practically inactive ketotifen-N-glucuronide.
Non-clinical data reveal no special hazard which is considered relevant in connection with use of ketotifen-containing 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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