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Mode of action - antiallergic, antihistamine, membrane, antiasthmatic.
Ketotifen (Ketotiphenum,Ketotipheni) mast cell stabilizer, has a moderate activity N1- gistaminoblokiruyuschey inhibits the release of histamine, leukotrienes from basophils and neutrophils, reduces the accumulation of eosinophils in the airway response to histamine and suppress early and late asthmatic responses to allergen. It prevents the development of bronchospasm, has no bronchodilatory effect. Inhibits phosphodiesterase, thereby increasing cAMP in adipose tissue cells.
The therapeutic effect is fully manifested in 1.5-2 months after initiation of therapy.
Inhibits the release of histamine and other mediators (slow reacting substance of anaphylaxis, and other lymphokines.) From mast cells and basophils. Noncompetitively blocks H1-histamine receptor inhibits phosphodiesterase, increases the level of cAMP in cells. Suppresses sensitization eosinophil recombinant human cytokines and their accumulation in the airways. It prevents the development of airway hyperresponsiveness symptoms caused by platelet activating factor or exposure to allergens. It prevents the development of bronchospasm (bronchodilator has no action). The clinical effect develops within 6-8 weeks. CNS depressants.
Once inside it absorbed almost completely. The bioavailability is approximately 50%, due to the effect of "first pass" through the liver. Time to achieve Cmax in plasma - 2-4 hours, binding to plasma proteins - 75%. It passes through the BBB and enters the breast milk. It is metabolized in the liver; major metabolite (ketotifen-N-glucuronide) is practically inactive. Excretion takes place in two phases: a T1 / 2 3-5 h and 21 h, respectively. Within 48 hours, urine output main part of the dose: 1% - unchanged, and 60-70% - in the form of metabolites.
From the nervous system and sensory organs: sedative effect, slowing the rate of reaction, confusion, fatigue, mild dizziness, headache, drowsiness, rare - anxiety, insomnia, nervousness (especially in children).
From the digestive tract: dry mouth, increased appetite, nausea, vomiting, gastralgia, constipation.
Other: thrombocytopenia, dysuria, cystitis, weight gain, allergic skin reactions.
Inside (during the meal), adults - 1 mg 2 times a day (morning and evening). If necessary, the daily dose was increased to 4 mg (2 mg 2 times a day). For patients in whom there is a significant sedative effect slow increase recommended dose for the first week, starting with 0.5 mg in the evening before going to bed, to achieve a therapeutic dose gradually.
Children older than 3 years - on 1 tab. (1 mg) or 5 ml syrup two times a day (morning and evening); from 6 months to 3 years of age - 2.5 ml syrup (0.5 mg), 2 times a day, morning and evening.
Therapy is prolonged, the effect is achieved after a few weeks of therapy. Treatment should be carried out for at least 2-3 months, especially in patients who have no effect was observed in the first week. Ketotifen Termination treatment should gradually, within 2-4 weeks.
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