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QuickView for Ketotifen (compound)


PubChem
Name: Ketotifen
PubChem Compound ID: 3827
Description: A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.
Molecular formula: C19H19NOS
Molecular weight: 309.426 g/mol
Synonyms:
NINDS_000111; 10H-Benzo[4,5]cyclohepta[1,2-b]thiophen-10-one, 4,9-dihydro-4-(1-methyl-4-piperidinylidene)-; HC 20-511; AIDS-033084; NCGC00015580-02; Spectrum2_001198; NCGC00015580-01; SPBio_001275; Ketotifen; KBio1_000111.
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DrugBank
Identification
Name: Ketotifen
Name (isomeric): DB00920
Drug Type: small molecule
Description: A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.
Synonyms:
Ketotifenum [INN-Latin]; Ketotifene fumarate; Ketotifene [INN-French]; Ketotifeno [INN-Spanish]; Ketotifen Fumarate
Brand: Ketotifen, Zaditor
Category: Histamine H1 Antagonists, Antipruritics, Anti-Allergic Agents
CAS number: 34580-14-8
Pharmacology
Indication: Indicated as an add-on or prophylactic oral medication in the chronic treatment of mild atopic asthmatic children. Also used as self-medication for the temporary relief of itching of the eye due to allergic conjunctivitis (ophthalmic).
Pharmacology: Ketotifen is a fast acting non-competitive histamine antagonist. It inhibits the release of mediators from mast cells. It is a non-bronchodilator antiasthmatic drug (when taken orally).
Mechanism of Action:
Ketotifen is a relatively selective, non-competitive histamine antagonist (H1-receptor) and mast cell stabilizer. Ketotifen inhibits the release of mediators from mast cells involved in hypersensitivity reactions. Decreased chemotaxis and activation of eosinophils have also been demonstrated. Ketotifen also inhibits cAMP phosphodiesterase. Properti...
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Absorption: Following oral administration absorption is at least 60%
Protein binding: 75%
Biotransformation: Primarily hepatic. The main metabolite found in both plasma and urine is the inactive ketotifen-N-glucuronide. Nor-ketotifen, the N-demethylated metabolite, and the 10-alpha-hydroxyl derivative are the only other metabolites detectable in human urine.
Half Life: 21 hours (for elimination)
Toxicity: Adverse reactions include headaches, conjunctival injection and rhinitis.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take without regard to meals.
Drug interaction:
TrimethobenzamideTrimethobenzamide and Ketotifen, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
TriprolidineTriprolidine and Ketotifen, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
TrospiumTrospium and Ketotifen, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
TacrineThe therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Ketotifen, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.

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