Culento is a selective competitor to leukotriene D4 receptors (cystenyl leukotriene CysLT1) - the most potent mediator of chronic persistent inflammation, maintaining bronchial hyperactivity with bronchial asthma.
Cystenylleukotrienes (LTC4, LTD4, LTE4) - metabolic products of arachidonic acid - are secreted by mast cells and eosinophils. These eicosanoids bind to cystenylleucotriene receptors. Bronchodilator effect is associated with blockade of leukotriene D4 receptors in the respiratory tract and reduction of the effect of leukotrienes, which play an important role in the regulation of bronchial reactivity, advanced bronchoconstriction, swelling of the bronchial mucosa, bronchial hypersecretion.
The drug blocks the action of LTD4 leukotrienes at the level of CysLT1 receptors without agonistic effect.
The therapeutic effect of Culento begins to manifest itself on the first day of taking the drug.
PHARMACOKINETICS
Montelukast sodium is rapidly absorbed after oral administration. Maximum plasma concentrations are reached 2-4 hours after taking the drug. When taken orally, the bioavailability of montelukast is 64%.
More than 99% of montelukast sodium is bound to blood plasma proteins. The plasma half-life in healthy adults is 3 to 5,5 hours. The pharmacokinetics of montelukast remain linear when taken orally in doses greater than 50 mg. There are no differences in pharmacokinetics when taking Montelukast in the morning and evening.
Montelukast sodium is actively metabolized in the liver by the P3 cytochrome system via the CYP4A2, CYP6A2 and CYP9C450 isoenzymes. Therapeutic plasma concentrations of montelukast do not inhibit isoenzymes ZA4, 2C9, 1A2, 2A6, 2C19, or 2D6. In healthy adults, the plasma clearance of montelukast is approximately 45 ml / min. Montelukast sodium is excreted in feces and bile.
Children, elderly patients, and patients with renal insufficiency have the same pharmacokinetic parameters as healthy adults.
In patients with moderate hepatic insufficiency and clinical manifestations of liver cirrhosis, the metabolism of montelukast slows and the half-life is prolonged, the area under the concentration-time curve (AUC) increases by 10% after a dose of 41 mg.
Long-term use of montelukast in children aged 6 to 11 months and variability in plasma concentrations were higher than in adults. In a study of pharmacokinetics in children aged 6 to 23 months, the safety and acceptable single dose of montelukast sodium were similar in patients 2 years and older.
INSTRUCTIONS FOR USE
- Asthma treatment as an adjunctive therapy in patients aged 6 months to 5 years with mild to moderate chronic asthma, inadequate control of inhaled corticosteroids, and short-term effects if necessary qiluvchi-on agonists provide incorrect clinical treatment of asthma. .
- An alternative to low-dose inhaled corticosteroids in patients with mild chronic asthma aged 2–5 years who do not have severe asthma attacks requiring oral corticosteroids and who are unable to use inhaled corticosteroids method of treatment.
- For the prevention of asthma in patients aged two years and older, the main cause of which is bronchospasm caused by exercise.
DOSAGE AND USE
Children should take this drug only under adult supervision. The pellets are mixed with a small portion of soft food (about a tablespoon) cooled to room temperature. The package should be opened immediately before use. Once the package is opened, the full dose of the drug should be consumed within 15 minutes. Do not store drug residues with food for reuse, they should be discarded. The granules should not be dissolved in the liquid, but the liquid can be taken after taking the drug. The drug can be taken with or without food.
Asthma treatment
Dosage
For children from 6 months to 5 years, one packet of the drug is taken every evening. No dose adjustment is required for this age.
Data from clinical studies on the efficacy of the drug in children aged 6 months to 2 years with persistent asthma are limited. After 2–4 weeks, patients should be screened to verify response to treatment with montelukast. If there is no reaction, treatment with the drug should be discontinued.
Culento 4 mg is not recommended for patients under 6 months.
The therapeutic effect of Culento on asthma symptom control parameters is manifested within a day. Patients should take the drug for a long time, both in the period of disease exacerbation and in remission.
No dose adjustment is required for patients with impaired renal function or mild to moderate hepatic impairment. There are no data on patients with liver failure.
Dosage
the same for male and female patients.
As an alternative treatment for mild persistent asthma instead of low-dose inhaler corticosteroids
Montelukast is not recommended as monotherapy in patients with moderate to severe chronic asthma. The use of montelukast as an alternative to oral corticosteroids in children 2 to 5 years of age with mild persistent asthma is possible only in patients who have not recently experienced an asthma attack requiring oral corticosteroids. corticosteroids.korticosteroids. Mild persistent asthma more than once a week, but with symptoms less than once a day, nocturnal symptoms more than twice a month, but less than 1 time per week, as asthma with normal lung function between attacks described. If a satisfactory follow-up result is not achieved (usually within a month), additional or other anti-inflammatory treatment based on a phased asthma management system may be needed. Patients should be monitored periodically to control respiration.
As for the prevention of asthma, its main cause is bronchospasm caused by exercise in patients aged 2 to 5 years. 2 to 5 years old
In patients with persistent asthma may occur due to bronchospasm caused by exercise, in which case treatment with inhaled corticosteroids. necessary. Patients should be screened 2–4 weeks after treatment with montelukast. If a satisfactory result is not achieved, additional or other treatment should be prescribed.
Concomitant treatment of asthma with Culento and other drugs
If Culento inhaler is used as an adjunct to corticosteroids, inhaled corticosteroids should not be replaced with Culento at once.
COMPOUNDS
- Hypersensitivity to montelukast sodium or other components of the drug;
- acute attack of bronchial asthma, including asthmatic status.
SIDE EFFECTS
The frequency parameters of the side effects used are defined as follows: frequent (≥ 1/100 to <1/10), rare (≥ 1/1000 to <1/100), infrequently in rare cases (≥ 1/10000 to <<1/1000), very rare (<1/10000).
Infections are very rare - infections of the upper respiratory tract.
In rare cases, the blood and lymphatic system - the tendency to bleed increases.
By the immune system, in rare cases - hypersensitivity reactions, including anaphylaxis; very rarely - eosinophilic infiltration in the parenchyma.
In rare cases, mental illness - nightmares, insomnia, insomnia, nervousness, anxiety, worry, agitation, including aggressive behavior or hostility, depression; in rare cases - tremor; very rarely - hallucinations, suicidal thoughts and suicidal tendencies.
By the nervous system, in rare cases - dizziness, drowsiness, paresthesia / hypoaesthesia.
By the cardiovascular system, in rare cases - palpitations.
Rarely from the respiratory system, chest and mediastinal organs - bleeding from the nose; very rarely - Churg-Strauss syndrome.
From the gastrointestinal tract, often - diarrhea, nausea, vomiting; in rare cases - dry mouth, dyspepsia.
Hepatobiliary diseases are often - high levels of serum transaminases (alanine aminotransferase, aspartate aminotransferase); in very rare cases - hepatitis (including a mixed picture of cholestatic, hepatocellular and liver damage).
Most often on the skin and subcutaneous tissue - rash; in rare cases - urticaria, itching; in rare cases - angioedema; very rarely - erythema nodosum.
Rarely by the musculoskeletal system and connective tissue - arthralgia, myalgia, muscle spasms.
Common disorders are often pyrexia; in rare cases - asthenia / fatigue, discomfort, edema.
special instructions
The treatment regimen should be strictly adhered to.
Should not be used to relieve acute asthma attacks (does not replace inhaled bronchodilators); when a therapeutic effect occurs (usually after the first dose), it is possible to reduce the inhalation of bronchodilators during the day.
Inhaled or oral corticosteroids should not be replaced with Culento at once. However, the dose of inhaled corticosteroid may be gradually reduced under medical supervision.
Decreased doses of systemic corticosteroids (prednisolone, dexamethasone, betamethasone, triamcinolone) in patients receiving asthma medications, including leukotriene receptor antagonists, have rarely been associated with the occurrence of one or more of the listed eosofinocular events. rash, exacerbation of symptoms and complications from the respiratory system and / or neuropathy, sometimes diagnosed as Churg-Strauss syndrome - systemic eosinophilic vasculitis. Although no causal association of these adverse events with treatment with leukotriene receptor antagonists has been established, caution should be exercised in reducing the systemic dose of corticosteroids in patients receiving Culento and appropriate clinical follow-up.
The drug should not be used as monotherapy for the treatment and control of exercise-induced asthma.
Patients with post-exercise asthma should continue to use inhaler b-agonists as usual for prophylaxis and should have an inhaler with them when needed.
Culento does not block the bronchospastic response to aspirin or other nonsteroidal anti-inflammatory drugs (NSAIDs) in asthmatic patients who are sensitive to aspirin. Such patients should not take aspirin and other NSAIDs. Caution should be exercised when using Culento concomitantly with bronchodilator therapy. If the clinical response is clear, bronchodilator therapy should be reduced.
Caution should be exercised when prescribing to patients with liver disease.
EFFECTS ON ENGINE DRIVING AND CONTROL MECHANISMS
The drug is intended for use in pediatric practice.
Use during pregnancy and lactation
Studies on the use of the drug Culento in pregnant women have not been performed because the drug is indicated for use in children.
APPLICATION IN PEDIATRY
The drug is not recommended for use in children under 6 months.
OTHER
MEDICINE OF THE UZBEKISTAN ECONOMY Culento can be prescribed in combination with other drugs traditionally used for the prevention and long-term treatment of bronchial asthma.
Treatment with Culento bronchodilators can be added to the treatment of patients with asthma who are not controlled by the use of bronchodilators only. When a therapeutic effect is achieved during therapy with Culento (usually after the first dose), the dose of bronchodilators can be gradually reduced.
Treatment with inhaled glucocorticosteroids with Culento has an additional therapeutic effect in patients treated with inhaled glucocorticosteroids. When stabilization of the patient's condition is achieved, the dose of glucocorticosteroids can be reduced. The dose of glucocorticosteroids should be reduced gradually, under the supervision of a physician. In some patients, inhaler glucocorticosteroids may be completely discontinued. Inhaled or oral corticosteroids should not be replaced with Culento at once.
The recommended clinical dose of montelukast did not have a clinically significant effect on the pharmacokinetics of the following theophylline, prednisolone, oral contraceptives (ethinylestradiol / noretindrone 35/1), terfenadine, digoxin, and warfarin.
In patients receiving phenobarbital concomitantly, the AUC of montelukast was reduced by approximately 40%. Because montelukast is metabolized by CYP3A4, 2C8, and 2C9, caution should be exercised when using montelukast in combination with inducers of CYP3A4, 2C8, and 2C9, such as phenytoin, phenobarbital, and rifampicin.
Dosage
overdose No overdose has been reported.
Symptoms may suggest that an overdose of the drug may exacerbate side effects such as abdominal pain, vomiting, drowsiness, headache, thirst, or psychomotor hyperactivity.
Treatment is symptomatic. There are no data on the possibility of removal of montelukast by peritoneal dialysis or hemodialysis.
Release
form granules for oral administration, 0,5 g in packets.
In a cardboard box with 28 packet sheets.
STORAGE CONDITIONS
Store in a place protected from moisture and light, at a temperature not exceeding 25 ° C.
