Ketotifen - General Information:
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. [PubChem]Related offers from our Drug Store:
| Zaditor (Ketotifen) - for $45.79 Zaditor is used to treat itching of the eyes caused by allergy to dust, pollen, animals, or other allergens. |
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).Ketotifen for patients
To prevent contaminating the dropper tip and solution, care should be taken not to touch the eyelids or surrounding areas with the dropper tip of the bottle. Keep the bottle tightly closed when not in use. Patients should be advised not to wear a contact lens if their eye is red. ZADITOR™ should not be used to treat contact lens related irritation. The preservative in ZADITOR™, benzalkonium chloride, may be absorbed by soft contact lenses. Patients who wear soft contact lenses and whose eyes are not red, should be instructed to wait at least ten minutes after instilling ZADITOR™ before they insert their contact lenses.
Ketotifen Interactions
No information provided.
Ketotifen Contraindications
ZADITORTM is contraindicated in persons with a known hypersensitivity to any component of this product.
Additional information about Ketotifen
Ketotifen Indication: Indicated as an add-on or prophylactic oral medication in the chronic treatment of mild atopic asthmatic children. Also for the temporary prevention of itching of the eye due to allergic conjunctivitis (ophthalmic).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 has also been demonstrated. Ketotifen also inhibits cAMP phosphodiesterase. Properties of ketotifen which may contribute to its antiallergic activity and its ability to affect the underlying pathology of asthma include inhibition of the development of airway hyper-reactivity associated with activation of platelets by PAF (Platelet Activating Factor), inhibition of PAF-induced accumulation of eosinophils and platelets in the airways, suppression of the priming of eosinophils by human recombinant cytokines and antagonism of bronchoconstriction due to leukotrienes. Ketotifen inhibits of the release of allergic mediators such as histamine, leukotrienes C4 and D4(SRS-A) and PAF.
Drug Interactions: Not Available
Food Interactions: Take without regard to meals.
Generic Name: Ketotifen
Synonyms: Ketotifene [INN-French]; Ketotifeno [INN-Spanish]; Ketotifenum [INN-Latin]; Ketotifene fumarate; Ketotifen Fumarate
Drug Category: Anti-Allergic Agents; Antipruritics; Histamine H1 Antagonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Ketotifen: Ketotifen; Zaditor;
Absorption: Following oral administration absorption is at least 60%
Toxicity (Overdose): Adverse reactions include headaches, conjunctival injection and rhinitis.
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)
Dosage Forms of Ketotifen: Tablet Oral
Solution Ophthalmic
Liquid Ophthalmic
Syrup Oral
Chemical IUPAC Name: Not Available
Chemical Formula: C19H19NOS
Ketotifen on Wikipedia: http://en.wikipedia.org/wiki/Ketotifen
Organisms Affected: Humans and other mammals
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