Singulair, Chewable tablets 5mg, 14pcs

Composition

1 chewable tablet contains: Active ingredient: Montelukast – 5 mg. Auxiliary substances: Mannitol; Microcrystalline cellulose; Hyprolose; Red iron oxide dye; Croscarmellose sodium; Cherry flavor;Aspartame; Magnesium stearate.

Pharmacological action

Pharmacodynamics

Montelukast inhibits cysteinyl leukotriene receptors in the airway epithelium, thereby simultaneously being able to inhibit bronchospasm caused by inhalation of cysteinyl leukotriene LTD4 in patients with bronchial asthma. A dose of 5 mg is sufficient to relieve LTD4-induced bronchospasm. The use of montelukast in doses exceeding 10 mg per day, taken once, does not increase the effectiveness of the drug.

Montelukast causes bronchodilation within 2 hours after oral use; and may supplement bronchodilation caused by beta-2-adrenomimetics.

Pharmacokinetics

Absorption: Telukast is rapidly and almost completely absorbed after oral use. Regular food intake does not affect the bioavailability and maximum plasma concentration (Cmax) of coated tablets and chewable tablets. In adults, when taking 10 mg coated tablets on an empty stomach, Cmax is reached after 3 hours. Oral bioavailability is 64%. When taking 5 mg chewable tablets on an empty stomach, Cmax in adults is reached after 2 hours. Bioavailability is 73%.

Distribution

Montelukast binds to plasma proteins by more than 99%. The volume of distribution of montelukast is on average 8-11 liters.

Metabolism

Montelukast is actively metabolized in the liver. When using therapeutic doses, the concentration of montelukast metabolites in plasma at steady state in adults and children is not determined. It is assumed that cytochrome P 450 CYP isoenzymes (3 A 4 and 2 C 9) are involved in the metabolism of montelukast, while at therapeutic concentrations montelukast does not inhibit cytochrome P 450 CYP isoenzymes: 3 A 4,2 C 9,1 A 2,2 A 6,2 C 19 and 2D6.

Deduction

The clearance of montelukast is on average 45 ml/min in healthy adults. After oral use of montelukast,86% of its amount is excreted in the faeces within 5 days and less than 0.2% in the urine, which confirms that montelukast and its metabolites are excreted almost exclusively in the bile.

The elimination half-life of montelukast in young healthy adults is 2.7 to 5.5 hours. The pharmacokinetics of montelukast remain almost linear when taking oral doses of more than 50 mg. When taking montelukast in the morning and evening hours, there are no differences in pharmacokinetics. When taking 10 mg coated tablets once a day, moderate (about 14%) accumulation of the Active ingredient in plasma is observed.

Features of pharmacokinetics in different groups of patients

The

pharmacokinetics of montelukast in women and men are similar.

Elderly patients When taking 10 mg film-coated tablets orally once a day, the pharmacokinetic profile and bioavailability are similar in the elderly and young patients.

Hepatic insufficiency Patients with mild to moderate hepatic insufficiency and clinical manifestations of cirrhosis of the liver showed a slowdown in the metabolism of montelukast, accompanied by an increase in the area under the pharmacokinetic curve “concentration-time” (AUC) by approximately 41% after a single dose of the drug in a dose of 10 mg.

The elimination of montelukast in these patients is slightly increased compared to healthy subjects (the average elimination half-life is 7.4 hours). No dose adjustment of montelukast is required for patients with mild to moderate hepatic insufficiency. There are no data on the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (more than 9 points on the Child-Pugh scale).

There were no differences in clinically significant pharmacokinetic effects in patients with different races.

Renal insufficiency Since montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast in patients with renal insufficiency have not been evaluated. No dose adjustment is required for this group of patients.

Indications

• Prevention and long-term treatment of bronchial asthma in adults and children starting from 6 years of age, including prevention of day and night symptoms of the disease, treatment of aspirin-sensitive patients with bronchial asthma, and prevention of exercise-induced bronchospasm.

• Relief of day and night symptoms of seasonal allergic rhinitis (in adults and children from 6 years) and permanent allergic rhinitis (in adults and children from 6 years).

Use during pregnancy and lactation

Singulair should be used during pregnancy and lactation only if the expected benefit to the mother exceeds the potential risk to the fetus or child.

Contraindications

Hypersensitivity to any of the components of the drug Singulair, children under 6 years of age.

Side effects

In general, Singulair is well tolerated. Side effects are usually mild and usually do not require discontinuation of treatment.

The overall incidence of side effects reported with Singulair is comparable to that of placebo:  

• Hypersensitivity reactions (including anaphylaxis, angioedema, rash, pruritus, urticaria and very rarely eosinophilic liver infiltrates);

• Erythema nodosum, unusual vivid dreams;

• Hallucinations; drowsiness;

• Irritability.

• Agitation, including aggressive behavior.

• Fatigue;

• Suicidal thoughts and suicidal behavior (suicidality);

• Insomnia;

• Paresthesia/hypesthesia and very rarely convulsive seizures.

• Nausea, vomiting, diarrhea, abdominal pain;

• Headache;

• Arthralgia;

• Myalgia;

• Muscle cramps.

• Tendency to increase bleeding, formation of subcutaneous hemorrhages;

• Heartbeat.

• Edema.

Interaction

Singulair can be prescribed together with other medications traditionally used for the prevention and long-term treatment of bronchial asthma. The recommended clinical dose of montelukast did not have a clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethindrone 35/1), terfenadine, digoxin and warfarin.

AUC decreases in individuals receiving phenobarbital concomitantly (by approximately 40%), but adjustment of the dosage regimen of Singulair is not required in such patients.

Treatment with bronchodilators: Singulair can be added to the treatment of patients whose asthma is not controlled by the use of bronchodilators alone. When the therapeutic effect is achieved (usually after the first dose) against the background of Singulair therapy, the dose of bronchodilators can be gradually reduced.

Inhaled glucocorticosteroids: Treatment with Singulair provides an additional therapeutic effect for patients receiving treatment with inhaled glucocorticosteroids. When the patient’s condition stabilizes, it is possible to reduce the dose of glucocorticosteroids. The dose of glucocorticosteroids should be reduced gradually, under the supervision of a doctor. In some patients, inhaled glucocorticosteroids may be completely discontinued. Abrupt replacement of inhaled glucocorticosteroid therapy with Singulair is not recommended.

How to take, course of use and dosage

Inside 1 time a day, regardless of food intake. For the treatment of bronchial asthma, Singulair should be taken in the evening. In the treatment of allergic rhinitis, the dose can be taken at any time of the day at the request of the patient. Patients suffering from bronchial asthma and allergic rhinitis should take one tablet of Singulaira once a day in the evening. Adults aged 15 years and older The dosage for adults and children over 15 years is one 10 mg film-coated tablet per day. Children aged 6-14 years The dosage for children aged 6-14 years is one chewable tablet 5 mg per day. No dosage adjustment is required for this age group. General recommendationsthe therapeutic effect of Singulair on indicators reflecting the course of bronchial asthma develops during the first day. The patient should continue to take Singulair both during the period of achieving control of symptoms of bronchial asthma, and during periods of exacerbation of bronchial asthma. For elderly patients, patients with renal insufficiency, as well as patients with mild or moderate hepatic impairment, as well as depending on gender, special dose adjustment is not required. use of Singulaire concomitantly with other types of treatment for bronchial asthma, Singulair E can be added to the patient’s treatment with bronchodilators and inhaled glucocorticosteroids (See the section “Interaction with other drugs”).

Overdose

There are no data on overdose symptoms when taking Singulaire in patients with bronchial asthma at a dose exceeding 200 mg/day for 22 weeks and at a dose of 900 mg/day for 1 week.

There are reports of acute overdose of montelukast in children (taking at least 150 mg of the drug per day). Clinical and laboratory data indicate that the safety profile of Singulair in children corresponds to the safety profile in adults and elderly patients. The most common adverse events were thirst, drowsiness, mydriasis, hyperkinesis, and abdominal pain.

Treatment is symptomatic.

There are no data on the possibility of removing montelukast by peritoneal dialysis or hemodialysis.

Special instructions

Singulair tablets are not recommended for the treatment of acute attacks of bronchial asthma. In the acute course of bronchial asthma, patients should be prescribed medications to stop and prevent asthma attacks.

The dose of inhaled glucocorticosteroids used simultaneously with Singulair can be gradually reduced under the supervision of a doctor. Singulaire should not be abruptly substituted for inhaled or oral glucocorticosteroids.

Reducing the systemic dose of glucocorticosteroids in patients receiving anti-asthmatic agents, including leukotriene receptor blockers, was accompanied in rare cases by the appearance of one or more of the following phenomena: eosinophilia, vascular rash, worsening of pulmonary symptoms, cardiac complications and/or neuropathy, sometimes diagnosed as Charg-Strauss syndrome – systemic eosinophilic vasculitis.

Although the causal relationship of these adverse events with leukotriene receptor antagonist therapy has not been established, caution should be exercised and appropriate clinical monitoring should be carried out when reducing the systemic dose of glucocorticosteroids in patients taking Singulair.

Use in elderly patients

There were no age-related differences in the efficacy and safety profiles of Singulair.

Form of production

Chewable tablets.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 30 °C.

Shelf

life is 2 years.

Active ingredient

Montelukast

Conditions of release from pharmacies

By prescription

Dosage form

tablets for resorption

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor, Children over 2 years of age

Indications

Bronchial Asthma, Bronchospasm, Allergic Rhinitis