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Ketotifen belongs to the group of mast cell membrane stabilizers. It inhibits the release of histamine and other mediators (including leukotrienes, cytokines) from mast cells, prevents eosinophilic infiltration in places of allergic inflammation. It has a blocking effect on (H1) histamine receptors, inhibits phosphodiesterase, blocks cell calcium channels, is a functional leukotriene antagonist.
Ketotifen is an effective oral medication for the prevention of bronchial asthma. It has a pronounced anti-anaphylactic and anti-allergic effect. When used alone, it does not stop asthma attacks, but leads to a decrease in the number, duration and intensity of these attacks. In some cases, there is a complete disappearance of attacks of bronchial asthma. The drug has a positive effect on the exposure, reduces eosinophilia, reduces the need for the use of bronchodilators, corticosteroids, etc.
Long-term prophylaxis of allergic bronchial asthma and mixed forms, allergic bronchitis, asthmatic complications of hay fever, allergic rhinitis, allergic dermatoses, migraine.
1 tablet contains 1 mg ketotifen fumarate.
Ketotifen is marketed under different brands and generic names, and comes in different dosage forms:
|Brand name||Manufacturer||Country||Dosage form|
|Ketotifen pills 0,001 g||Irbit HFZ||Russia||pills|
|Ketotifen pills 0,001 g||Sopharma||Bulgaria||pills|
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Dosage and Administration
Ketotifen drug is taken orally. Assign adults - twice a day (morning and evening), 1 tablet (1 mg) with meals. If necessary, the daily dose can be increased to 4 mg (divided into 2 doses).
Children over 3 years old are prescribed ketotifen pills as follows: with a body weight of up to 25 kg, twice a day (in the morning and in the evening) 1/2 tablet; more than 25 kg - twice a day, 1 tablet. With insufficient therapeutic effect after 4-week treatment of children weighing less than 25 kg, the dose can be increased to 1 tablet 2 times a day.
In the first days of administration, drowsiness, dry mouth, mild dizziness, and fatigue are possible, which usually pass spontaneously. In such cases, the dose to adults is reduced to 1 mg per day.
In rare cases, thrombocytopenia, weight gain, allergic skin reactions are possible.
Pregnancy, lactation (suspend breastfeeding), increased individual sensitivity to ketotifen, children's age - up to 3 years.
It is advisable to avoid the combined use of ketotifen with oral antidiabetic agents because of possible reversible thrombocytopenia. It is also possible to potentiate the effect of sedatives, narcotic drugs and alcohol, which is why such combinations should be avoided.
In the first days of treatment, motor coordination reactions may slow down. Patients should be warned about the need to refrain from activities requiring high concentration of attention and good motor coordination, including driving vehicles.
Overdose events are observed at plasma concentrations of ketotifen 5–122 ng / ml (therapeutic concentration 1–4 ng / ml). Symptoms: weakness, disorientation, confusion, dyspnea, tachycardia or bradycardia, convulsions, severe hypotension.
Treatment: symptomatic therapy. There is no specific antidote.
- Brand name: Ketotifen pills 0,001 g
- Active ingredient: Ketotifen
- Dosage form: Pills.
- Manufacturer: Irbit HFZ
- Country of Origin: Russia
Studies and clinical trials of Ketotifen (Click to expand)
- Direct Differential Pulse Polarographic and Adsorptive Stripping Voltammetric Assay of Ketotifen in Tablets
- Determination of ketotifen fumarate by capillary electrophoresis with tris(2,2′-bipyridyl) ruthenium(II) electrochemiluminescence detection
- Quantification of ketotifen and its metabolites in human plasma by gas chromatography mass spectrometry
- Deuterium-labelling and quantitative measurement of Ketotifen in human plasma by gas chromatography/negative ion chemical ionization mass spectrometry
- Further studies on the distinctive sleep-wakefulness profiles of antihistamines (astemizole, ketotifen, terfenadine) in dogs
- Ketotifen-loaded microspheres prepared by spray-drying poly(D,L-lactide) and poly(D,L-lactide-co-glycolide) polymers: Characterization and in vivo evaluation
- In vitro—in vivo correlation of a modified-release oral form of ketotifen: In vitro dissolution rate specification
- Effects of ketotifen, a benzocycloheptathiophene, on methacholine -and acetylcholine-induced contractions of canine respiratory smooth muscle
- Effects of ketotifen on the responsiveness of peripheral blood lymphocyte β-adrenergic receptors
- Effect of ketotifen on allergen-induced interleukin 2 (IL2) responsiveness in patients with atopic dermatitis and/or bronchial asthma
- Effect of ketotifen on antigen-induced interleukin 2 (IL-2) responsiveness in lymphocytes from patients with atopic dermatitis and/or bronchial asthma
- Determination of ketotifen by using calcein as chemiluminescence reagent
- The comparison of the efficacy and safety of cetirizine, oxatomide, ketotifen, and a placebo for the treatment of childhood perennial allergic rhinitis
- Enhanced affinity of ketotifen toward tamarind seed polysaccharide in comparison with hydroxyethylcellulose and hyaluronic acid: A nuclear magnetic resonance investigation
- Characterization and in vivo evaluation of ketotifen-loaded chitosan microspheres
- Determination of ketotifen in human plasma by LC–MS
- Prevention of mast-cell degranulation by ketotifen in patients with physical urticarais: Husto DP, Bressler RB, Kalne M et al Ann Intern Med 104:507–510 Apr 1986
- Gas chromatographic–mass spectrometric method for quantitative determination of ketotifen in human plasma after enzyme hydrolysis of conjugated ketotifen
- Dry powder inhalation of liposomal Ketotifen fumarate: formulation and characterization
- Adsorption of ketotifen onto some pharmaceutical excipients
- Estimation of action site of l-lactic acid-ethanol-isopropyl myristate mixed system for its enhancing effect on the skin permeation of ketotifen
- Inhibitory effects of ketotifen on eotaxin-dependent activation of eosinophils: consequences for allergic eye diseases
- A Comparison of the Effects of Olopatadine and Ketotifen on Model Membranes
- Comparative Study of Clinical Efficacy and Tolerance in Seasonal Allergic Conjunctivitis Management with 0.1% Olopatadine Hydrochloride versus 0.05% Ketotifen Fumarate