Класт

General characteristics. Structure:

Active ingredient: 5,2 mg or 10,4 mg of sodium of montelukast that 5 mg or 10 mg of montelukast are equivalent.

Excipients: cellulose microcrystallic PH 102, lactoses monohydrate, sodium of a kroskarmelloz, SL hydroxypropyl cellulose, magnesium stearate.

Structure of a cover of Sepifilm LP 770: methylhydroxypropyl cellulose, cellulose microcrystallic, stearic acid, titanium dioxide (E171).

Pharmacological properties:

Pharmacodynamics. Montelukast - the selection antagonist of receptors of D4 leukotriene (tsistenit CysLT1 leukotriene) - the most powerful mediator of the chronic persistent inflammation maintaining hyperreactivity of bronchial tubes at bronchial asthma. Tsisteinil leukotrienes (LTC4, LTD4, LTE4) are the inflammatory eicosanoids emitted by mast cells and various other cells including eosinophils. These important pro-asthmatic mediators contact receptors tsisteinit leukotriene (CysLT1) in respiratory tracts and cause such phenomena as a bronkhokonstriktion, slime hypersecretion, increase in permeability of a vascular wall and accumulation of eosinophils. Tsisteinil leukotrienes play an important role in development of symptoms of allergic rhinitis.

On early and late phases of allergic reaction after influence of allergen in mucous a nose are released tsisteinit leukotrienes.

Their effect is shown in deterioration in passability of a nasal cavity and strengthening of a congestion of a nose. Montelukast, showing high affinity, selectively contacts CysLT1 receptors (instead of others pharmacological significant receptors of respiratory tracts, such as receptors of prostanoid, well-cared or β-adrenoceptors)))))))))) and, thus, inhibits physiological action of LTD4, causing bronkhodilatiruyushchy action.

Montelukast in small doses to 5 mg inhibited the bronkhokonstriktion caused by inhalation introduction of LTD4. Within 2 hours after intake the bronkhodilatation was observed, degree of manifestation of the allergic reaction of early and late phases caused by antigen influence decreased.

Pharmacokinetics. At oral administration montelukast is quickly soaked up from digestive tract. After intake on an empty stomach of 10 mg of drug by adult patients average peak concentration in plasma is reached within 3-4 hours.

Montelukast more than for 99% contacts proteins of plasma. The volume of distribution averages 8 – 11 l. Bioavailability at intake makes 64%.

Montelukast is actively metabolized in a liver with use of microsomal enzymes P450 3A4 and 2C9 cytochrome.

The elimination half-life makes 2,7–5,5 h. The montelukast pharmacokinetics in doses to 50 mg is almost linear. After reception of 10 mg of montelukast moderate cumulation is observed once a day (concentration of active agent in plasma made about 14%).

Clearance at adults about 45 ml/min. Montelukast and its metabolites are almost completely removed with bile.

The pharmacokinetics and bioavailability of a single peroral dose of 10 mg of montelukast at elderly and young are similar. The montelukast elimination half-life at elderly increases a little, however dose adjustment in this age group is not required.

At patients with a slight moderate liver failure and cirrhosis after reception of a single dose of montelukast of 10 mg average value of the area under a curve was 41% more, elimination was slightly longer, than at healthy volunteers (an average elimination half-life – 7,4 h). Correction of a dose from easy – a moderate liver failure is not required from patients. The montelukast pharmacokinetics at patients with a heavy liver failure or hepatitis was not investigated.

As montelukast and its metabolites are not removed with urine, the montelukast pharmacokinetics at patients with a renal failure was not investigated. Correction of a dose is not required from these patients.

Indications to use:

- treatment and prevention of bronchial asthma, including the prevention of day and night symptoms of a disease, including aspirinchuvstvitelny patients with bronchial asthma and the prevention of the bronchospasm caused by an exercise stress;

- treatment of seasonal allergic rhinitis.

Route of administration and doses:

For adults and teenagers 15 years are more senior it is appointed КЛАСТ® 10 once a day, and for children at the age of 6-14 KLAST® 5 once a day. Drug is accepted irrespective of meal.

At seasonal allergic rhinitis – reception time the patient defines at discretion.

For treatment of bronchial asthma drug should be accepted in the evening. The patients having at the same time asthma and seasonal allergic rhinitis have to accept drug once in the evening. Duration of a course of treatment is determined by the attending physician.

General recommendations. Therapeutic effect of drug on the indicators reflecting the course of bronchial asthma is shown during the first day.

The patient should continue to accept drug as during achievement of control of symptoms of bronchial asthma, and during the periods of an exacerbation of bronchial asthma.

For elderly patients with a renal or liver failure of easy, moderate degree, dose adjustment is not required.

Features of use:

КЛАСТ® it is not intended for stopping of a bronchospasm at bad attacks of asthma, and also for treatment of the asthmatic status.

At the acute course of bronchial asthma it is recommended to use the corresponding drugs for treatment of patients. In an acute phase of bronchial asthma treatment КЛАСТ® can be continued.

Even at a gradual controlled dose decline of an inhalation glucocorticosteroid it is not necessary to appoint КЛАСТ® instead of an inhalation corticosteroid at once.

Reduction of a system dose or cancellation of glucocorticosteroids at the patients receiving antiasthmatic means including blockers of leukotriene receptors, was followed in rare instances by emergence of one or several of the following phenomena: eosinophilias, vascular rash, deterioration in pulmonary symptoms, cardiological complications and/or the neuropathy sometimes diagnosed as Charga-Stross's syndrome – a system eosinophilic vasculitis. Communication between treatment by antagonists of receptors of leukotriene and emergence of a syndrome of Charga-Stross cannot be excluded or confirmed. In case of such symptoms as an eosinophilia, rash, deterioration in pulmonary symptoms, cardiological complications and/or neuropathy, additional inspection and review of tactics of treatment is necessary.

At patients about aspirin - sensitive asthma treatment by montelukast does not influence need of use of aspirin or other non-steroidal anti-inflammatory drugs.

Features of influence of medicine on ability to manage motor transport or potentially dangerous mechanisms

КЛАСТ® can cause a headache, drowsiness, slackness, sluggishness. It should be considered in need of use of drug for persons whose activity is connected with driving, service of cars and mechanisms, with performance of work in unstable situation.

Side effects:

Often:

- fervescence, weakness;

- cough, nose congestion;

- abdominal pains, gastroenteritis, nausea, vomiting, dyspepsia, diarrhea;

- skin rash;

- hypersensitivity reactions, (anaphylaxis, Quincke's disease, itch, small tortoiseshell);

- headache, dizziness, abnormal dreams, noctambulation, disorientation, drowsiness, irritability, concern, hallucinations, agressive behavior, paresthesias/hypesthesias, fatigue;

- muscular spasms, mialgiya, arthralgia;

- bleeding, hematomas;

- hypostases;

Seldom:

- eosinophilic infiltration of a liver;

- a system eosinophilia, vasculitis symptoms (similar to Churg Strauss syndrome at treatment by system corticosteroids, is more often at reduction of a dose of peroral corticosteroids);

- suicide intentions and behavior (attempt of a suicide);

- cardiopalmus;

- upper respiratory tract infection (laryngitis, pharyngitis);

Very seldom:

- pancreatitis;

- increase in level (ALAT, ASAT) in blood;

- cholestatic hepatitis.

Interaction with other medicines:

КЛАСТ® it can be applied with other drugs to prevention and prolonged treatment of asthma without strengthening of side effects.

КЛАСТ® in the recommended dose did not cause clinically significant changes of pharmacokinetics of the following drugs: theophylline, Prednisonum, Prednisolonum, oral contraceptives (norethindrone of 1 mg / ethinylestradiol of 35 mkg), терфенадин, digoxin, warfarin.

The area under a concentration curve in a blood plasma (AUC) decreased approximately at 40% of patients at joint administration of phenobarbital, however correction of the mode of drug dosing КЛАСТ® is not required to such patients.

As montelukast is metabolized by means of CYP A4, it is necessary to be careful, especially at children when it КЛАСТ® is applied together with the inductors CYP 3A4, such as Phenytoinum, phenobarbital and rifampicin.

Treatment by bronchodilators: КЛАСТ® it is possible to add to treatment of patients at whom bronchial asthma is not controlled by use of one bronchodilators. At achievement of therapeutic effect (usually after the first dose) against the background of therapy by the drug KLAST®, the dose of bronchodilators can be reduced gradually.

Inhalation glucocorticosteroids: Treatment by the drug KLAST® provides additional therapeutic effect to the patients receiving treatment by inhalation glucocorticosteroids. At achievement of stabilization of a condition of the patient the dose decline of glucocorticosteroids is possible. The dose of glucocorticosteroids needs to be reduced gradually, under observation of the doctor. At some patients reception of inhalation glucocorticosteroids can be completely cancelled. Sharp replacement of therapy with inhalation glucocorticosteroids with appointment КЛАСТ® is not recommended.

The drugs containing the St. John's Wort which is made a hole can reduce montelukast level in a blood plasma.

Contraindications:

- hypersensitivity to montelukast or any other component of drug;

- fenilketonuriya;

- inborn insufficiency of lactase, glyukozo/galaktozny malabsorption, hereditary intolerance of fructose;

- pregnancy and period of a lactation;

- КЛАСТ®10 it is contraindicated to children up to 15 years;

- КЛАСТ®5 it is contraindicated to children up to 6 years.

Overdose:

Symptoms: dehydration, drowsiness, mydriasis, hyperkinesia, abdominal pain.

Treatment - drug withdrawal, a symptomatic treatment. There are no data on a possibility of removal of montelukast by peritoneal dialysis or a hemodialysis.

Storage conditions:

To store at a temperature not over 25 ºС, in the dry, protected from light place. To store in the place, unavailable to children! Period of storage 3 years. Not to apply after the storage expiration.

Issue conditions:

According to the recipe

Packaging:

On 14 tablets place in a blister strip packaging from a formatura of aluminum and printing aluminum foil.

On 1 or 2 planimetric packagings together with the instruction on a medical use in the state and Russian languages place in a pack cardboard with the hologram of firm – producer.