Ketotifenum

General characteristics. Structure:

International and chemical names: Ketotifen; 4 (1-methylpiperidine-4-илиден) - 4,9-dihydro-10 N-benzo-[4,5] - tsiklogepta-[1,2-b] - thiophene - 10 - it fumarates; main physical and chemical properties: colourless or slightly yellowish transparent viscous liquid, with a specific smell; structure: 5 ml of syrup contain 1 mg of Ketotifenum; excipients: Natrium benzoicum, мальтитол liquid, saccharin of sodium, dinatrium phosphate dodecahydrate, citric acid monohydrate, fumaric acid, glycerin, hydroxyethylcellulose, fragrance food banana, the water purified.

Pharmacological properties:

Pharmacodynamics. Ketotifenum has membrane stabilizing, antiallergic, antihistaminic effect. The mechanism of action of Ketotifenum is caused by suppression of release of biologically active agents mast cells and basophiles (a histamine, leukotrienes and so forth), suppression of a sensitization of eosinophilic granulocytes cytokines, blocking their migration in the inflammation centers. Drug constrains development of the hyperreactivity of respiratory tracts caused by activation of thrombocytes under the influence of the factor of activation of thrombocytes (FAT) or allergens. Drug inhibits phosphodiesterase, increases the tsAMF level in cells. Ketotifenum causes non-competitive blockade of H1-histamine receptors. Effectively the bronchospasm warns, reduces the need for use of corticosteroids, bronkhodilyatator. Does not possess broncholitic action. The therapeutic effect after administration of drug develops slowly, within 1-2 months.

Pharmacokinetics. At intake Ketotifenum is soaked up almost completely. The main metabolite of Ketotifenum of N-gluronid is almost non-toxical. The maximum concentration in a blood plasma is reached in 2–4 hours. Linkng with proteins makes about 75%. Removal of Ketotifenum from an organism has two-phase character: the first elimination half-life makes 3-5 hours, the second - is excreted by kidneys and 30-20% 21 hour of 60-70% of drug – to cookies in the form of metabolites, 10% of drug are removed in not changed look. Within 48 hours with urine the main part of the accepted single dose of drug is removed. The nature of metabolism at children same, as at adults, however clearance higher. Therefore to children 3 years are more senior the same daily dose, as well as the adult is required.

Indications to use:

Prevention of attacks of bronchial asthma, allergic bronchitis, asthmatic complications at hay fever, an allergic dermatosis, allergic rhinitis and conjunctivitis, a small tortoiseshell.

Route of administration and doses:

Drug is appointed to adults and children 14 years on 1 – 2 mg of Ketotifenum 2 times a day are more senior. To children from 6 months to 3 years drug is appointed by 2 times a day on 0,0125 mg of Ketotifenum to 1 kg of body weight. To children drug is more senior than 3 years appoint 2 times a day on 0,025 mg of Ketotifenum to 1 kg of body weight. A necessary dose measure by means of the portioning device with scale interval 0,1 ml.

Features of use:

The patients accepting Ketotifenum have to abstain from potentially dangerous types of activity connected with need of the increased concentration of attention; during treatment by drug it is necessary to refuse control of vehicles. In an initiation of treatment Ketotifenum it is not necessary to cancel sharply antiasthmatic drugs, especially system glucocorticosteroids (GKS), in connection with possible development of insufficiency of bark of adrenal glands. During treatment by Ketotifenum it is necessary to avoid alcohol intake.

Side effects:

At administration of drug there can be a drowsiness, dryness in a mouth, slight dizziness, delay of mental reactions, usually disappearing after several days of reception. The increase in body weight caused by increase in appetite is occasionally observed; dispeptic frustration, thrombocytopenia, dysuria, cystitis.

Interaction with other medicines:

Ketotifenum can strengthen action sedative, hypnotic drugs, antihistamines and alcohol. At reception of Ketotifenum the need for glucocorticosteroids and bronchial spasmolytics at patients with bronchial asthma can decrease. The concomitant use of Ketotifenum with peroral antidiabetic means causes development of thrombocytopenia.

Contraindications:

Hypersensitivity to drug, pregnancy, a lactation, children up to 6 months.

Overdose:

It is characterized by drowsiness, confusion of consciousness, orientation disturbance, tachycardia, arterial hypotension, a hyperexcitability, spasms (especially at children), coma. At overdose purpose of vomitives, a gastric lavage, purpose of absorbent carbon, salt laxatives is recommended; in case of need carry out a symptomatic treatment and control of a condition of cardiovascular system, at excitement or spasms appoint barbiturates of short action or benzodiazepines.

Storage conditions:

To store in the dry, protected from light place at a temperature from 15 °C to 25 °C. A period of validity – 3 years.

Issue conditions:

According to the recipe

Packaging:

On 100 ml in bottles or banks, or on 50 ml in bottles together with the portioning device in a pack.