Ketotifenum of Sofarm of the tab. of 1 mg No. 30

Structure and form of release

Active ingredient: Ketotifenum hydrofumarating.

Structure

• 1 tablet contains Ketotifenum of the hydrofumarat 1.38 mg that is equivalent to Ketotifenum of 1 mg;
• other components: calcium hydrophosphate waterless, cellulose microcrystalline, starch wheat, magnesium stearate.

a release Form

Round flat tablets with a facet, with distributive line on the one hand, with a diameter of 7 mm, from white to white with a gray shade of color; flavourless.

Pharmacological properties

Pharmacodynamics. Ketotifenum belongs to group of cycloheptathiophenons and has the expressed antihistaminic effect. it belongs to group of nebronkhodilatiruyushchy antiasthmatic means. The mechanism of its action is connected with slowing down of release of a histamine and other mediators from mast cells, blocking of histamine n1-receptors and oppression of enzyme fde therefore level tsamf in mast cells increases. suppresses effects of a platelet activating factor. At independent application does not stop attacks of bronchial asthma, and prevents their emergence and leads to decrease in their duration and intensity, and in certain cases they completely disappear.

Pharmacokinetics. Resorption: it is characterized by almost full resorption in a GIT. The C _max in blood plasma is reached in 2–4 h. The equilibrium state is reached after reception of the minimum daily dose making 2 mg.

Distribution: contacts proteins of blood plasma approximately for 75%. Distribution volume — 2.7 l/kg of body weight.

Metabolism: about 60% of the accepted dose are metabolized in a liver in three ways: demethylation, N-oxidation, N-glyukurokonjyugation, to such metabolites: Ketotifenum-N-glyukuronid (pharmacological inactive), holes Ketotifenums (having the pharmacological activity similar to activity of not changed Ketotifenum), N-oxide Ketotifenum and 10 hydroxies Ketotifenum (the pharmacological activity is unknown).

Excretion: the T _½ (3–5 h) and longer — is removed bifazno, with short 21 h. About 1% of substance is removed in not changed view with urine within 48 h, and 60–70% — in the form of metabolites.

Indication

Preventive treatment oh, mainly atopic form.

At symptomatic treatment of allergic states, including allergic rhinitis and conjunctivitis.

Use

Pill is taken inside during meal, washing down with water.

Adult: on 1 tablet (1 mg) 2 times a day in the morning and in the evening during meal. For patients at whom the expressed sedation is observed the slow increase in a dose for the 1st week, since 0.5 mg 2 times a day before gradual achievement of a therapeutic dose is recommended. If necessary it is possible to raise a daily dose to 4 mg (4 tablets) 2 times a day. At use of medicine in higher dose it is possible to expect faster approach of therapeutic effect.

Children are aged more senior than 3 years: on 1 tablet (1 mg) 2 times a day in the morning and in the evening during meal.

treatment Duration. Treatment is long, and the therapeutic effect is reached after several weeks of therapy. Treatment has to last not less than 2-3 months, especially at patients at whom improvement of health in the first weeks of therapy was not observed. The accompanying bronkhodilatiruyushchy therapy: use of Ketotifenum along with bronchodilators can reduce the frequency of use of bronchodilators.

therapy Termination. It is necessary to stop treatment by Ketotifenum gradually, for 2–4 weeks, in order to avoid risk of a recurrence of asthmatic symptoms.

Patients of advanced age.

special requirements for elderly people do not exist.

Contraindication

Hypersensitivity to acting or to excipients of medicine.

feeding Period breast.

Side effects

Infection and an invasion

Infrequently — cystitis.

from the immune system

It is very rare — heavy skin reactions, a multiformny erythema, Stephens's syndrome — Johnson.

Disturbance of metabolism and food.

it is rare — increase in body weight owing to increase in appetite.

Mental violations

it is frequent — psychomotor excitement, irritability, insomnia, concern, nervousness.

from central nervous system

Infrequently — dizziness, is rare — sedation, is very rare — spasms.

from a GIT

Infrequently — dryness in a mouth.

Gepatobiliarny violations

It is very rare — increase in level of liver enzymes, hepatitis.

In an initiation of treatment can appear dryness in a mouth and dizziness, but they usually pass spontaneously in the therapy course. Symptoms of stimulation of central nervous system, such as excitement, irritability, insomnia and concern, especially at children are in rare instances observed.

Drug is inefficient

at treatment of acute allergic reaction and attacks of suffocation at oh.

Maximum therapeutic effect of medicine occurs after several weeks of systematic reception.

function Normalization the hypophysis - an adrenal system can last till 1 year. Therefore in the first weeks of use of Ketotifenum the previous treatment is recommended to continue and cancel it gradually for a long time.

at the beginning of long therapy by Ketotifenum cannot stop sharply treatment by other antiasthmatic medicines, especially GKS. At patients with steroid dependence the development of adrenocortical insufficiency is possible.

needs to carry out by

in case of an intercurrent infection specific antibacterial therapy.

to

during use of medicine needs observation of the doctor, considering possibility of spasms.

should appoint Ketotifenum by

with care to patients with epilepsy in the anamnesis because of a possibility of decrease in a convulsive threshold at medicament treatment.

during therapy by Ketotifenum should not take alcohol because it enhances depressive effect of Ketotifenum on central nervous system.

Should stop administration of medicament in 10–14 days prior to implementation of skin tests for definition of an allergy.

If needs to stop treatment by Ketotifenum, the dose is gradually reduced during 2–4 weeks to avoid repeated emergence of symptoms OH.

Should be careful at use of Ketotifenum to patients with abnormal liver functions. In view of that simultaneous application with oral hypoglycemic medicines can cause thrombocytopenia, it is necessary to avoid such combination or attentively to control the level of platelets if such treatment is recommended.

Wheat starch as a part of a tablet may contain only traces of gluten and it is considered safe for patients with a Gee's disease.

Use during pregnancy or feeding by a breast. During the researches on animals it is not established embriotoksichny and teratogenic effect of Ketotifenum. Controlled clinical trials with participation of pregnant women were not conducted. During pregnancy it is necessary to appoint Ketotifenum only after strict assessment of existence of direct instructions, in cases when the expected advantage of treatment exceeds potential risk for a fruit.

Ketotifenum gets into breast milk. Therefore for treatment it is necessary to stop feeding by a breast.

Children. Clinical observations confirm pharmacokinetic features and show that higher dose (in mg/kg), than the adult, can be necessary for children for obtaining optimum results. Higher doses are transferred also well, as well as lower.

Ability to influence speed of response at control of vehicles or work with other mechanisms. In an initiation of treatment the medicine Sofarm Ketotifenum can slow down the speed of reactions that demands from the patient of the increased care during control of vehicles and work with the automated mechanisms.

Interaction

At simultaneous use of Ketotifenum and oral antidiabetic means the risk of developing reversible thrombocytopenia exists. at patients it is necessary to control quantity of platelets.

At the combined use of atropine, means with atropinopodobny action and Ketotifenum the risk of emergence of side reactions, such as ischuria, lock, dryness in a mouth increases.

Ketotifenum can exponentiate effects of other medicines (sedative, somnolent) oppressing central nervous system.

to mutual potentiation of their effects.

Overdose

Symptoms: considerable violations of psychomotor reaction, drowsiness to the expressed sedation, a headache, a disorientation, tachycardia, decrease hell, a coma (especially at children), symptoms of excitement of central nervous system, including a spasm are possible.

Also note bradycardia, arrhythmia, oppression of function of a respiratory center, a nystagmus.

in case of the above-stated symptoms of the patient needs to be surveyed carefully.

Treatment: general actions for removal of nerezorbirovanny amount of medicine from a GIT: to wash out a stomach, to artificially cause vomiting. Intake of activated carbon can have positive action. If necessary symptomatic treatment and monitoring of cardiovascular and respiratory systems is recommended. At conditions of excitement it is possible to apply barbiturates of short action or benzodiazepines.

Storage conditions

B the dry, protected from light place at a temperature not above 25 °C.