Ketotifenum

General characteristics. Structure:

Active ingredient: 1 mg of Ketotifenum.

Pharmacological properties:

Pharmacodynamics. Ketotifenum concerns to group of stabilizers of membranes of mast cells. Slows down release of a histamine and other mediators (including leukotrienes, cytokines) from mast cells, interferes with eosinophilic infiltration in places of an allergic inflammation. Has the blocking effect on (H1) histamine receptors, inhibits phosphodiesterase, blocks calcium channels of cells, is a functional antagonist of leukotrienes.

Ketotifenum — effective peroral remedy for prevention of bronchial asthma. Possesses the expressed anti-anaphylactic and antiallergenic action. At independent use does not stop asthma attacks, and leads to reduction of number, duration and intensity of these attacks. Total disappearance of attacks of bronchial asthma is in certain cases noted. Drug favorably influences an ekspektoration, reduces an eosinophilia, reduces need for use of bronchodilators, corticosteroids, etc.

Pharmacokinetics. After intake drug is soaked up almost completely. Bioavailability makes about 50% that is explained by effect of "the first passing" through a liver. Time of achievement of the maximum concentration in plasma — 2 — 4 hours, linkng with proteins of plasma — 75%. The main metabolite is the Ketotifenum-N-glucuronide. Removal from an organism proceeds in two phases: shorter is characterized by an elimination half-life of 3 — 5 hours, longer makes 21 hour. Within 48 hours with urine the main part of the accepted dose is removed: 1% — in not changed look and 60 — 70% — in the form of metabolites.

Indications to use:

Long prevention of allergic bronchial asthma and the mixed forms, allergic bronchitis, asthmatic complications at hay fever, allergic rhinitis, an allergic dermatosis, migraine.

Route of administration and doses:

Drug is accepted inside. Appoint the adult — twice a day (in the morning and in the evening) on 1 tablet (1 mg) during food. If necessary it is possible to increase a daily dose to 4 mg (to divide into 2 receptions).

To children 3 years of a tablet of Ketotifenum are more senior appoint as follows: at body weight to 25 kg — twice a day (in the morning and in the evening) on 1/2 tablets; more than 25 kg — twice a day on 1 tablet. At insufficient therapeutic effect after 4 weeks treatment of children with body weight a dose it is possible to increase less than 25 kg to 1 tablet 2 times a day.

Features of use:

In the first days of treatment delay of motor and coordination reactions is possible. It is necessary to warn patients about need to abstain from the activity demanding the increased concentration of attention and good motor coordination, including driving of vehicles.

Side effects:

In the first days of reception drowsiness, dryness in a mouth, weak dizziness, fatigue which usually pass spontaneously are possible. In such cases the dose the adult is reduced to 1 mg a day.

Thrombocytopenia, increase in body weight, allergic skin reactions are in rare instances possible.

Interaction with other medicines:

It is desirable to avoid the combined use of Ketotifenum with oral anti-diabetic means because of possible reversible thrombocytopenia. Perhaps also potentiation of effect of sedative drugs, narcotic medicines and alcohol in view of what similar combinations should be avoided.

Contraindications:

Pregnancy, lactation (to suspend breastfeeding), the increased individual sensitivity to Ketotifenum, children's age — up to 3 years.

Overdose:

The phenomena of overdose are observed at concentration of Ketotifenum in a blood plasma of 5 — 122 ng/ml (therapeutic concentration of 1 — 4 ng/ml).

Symptoms: weakness, a disorientation, confusion, диспноэ, tachycardia or bradycardia, spasms, the expressed hypotension.

Treatment: symptomatic therapy. The specific antidote does not exist.

Issue conditions:

According to the recipe

Packaging:

Tablets of 1 mg in a blister strip packaging No. 10х3.