Singlon, pills 10mg, 28pcs

Composition

1 film-coated tablet contains:

Active ingredient:

montelukast sodium, which corresponds to the content of montelukast 10 mg,

Auxiliary substances:

lactose monohydrate,

microcrystalline cellulose 101,

hyprolose,

croscarmellose sodium,

magnesium stearate.

Shell composition:

opadray yellow 20B32427

Pharmacological action

Montelukast is a specific oral leukotriene receptor antagonist. Montelukast has the ability to inhibit bronchospasm caused by inhaling LTD4 in very low doses (5 mg). Bronchodilation is observed within 2 hours after ingestion of the drug. The effect of bronchodilation caused by the beta-adrenomimetic is supplemented by the action of montelukast.

Montelukast inhibits the early and late phases of bronchospasm caused by antigen use. Montelukast reduces the number of eosinophils in the peripheral blood, in the respiratory tract (sputum) of adult patients and children and improves the control of the course of bronchial asthma.

Montelukast significantly improves morning FEV (forced expiratory volume) in 1 s, MOSV (maximum volume expiratory velocity) and significantly reduces the need for beta-adrenomimetics.

Montelukast enhances the effect of inhaled glucocorticosteroids. Montelukast significantly weakens bronchospasm that occurs during exercise. In patients with asthma who are sensitive to acetylsalicylic acid and are taking concomitant inhaled and/or oral glucocorticosteroids, treatment with montelukast leads to a significant improvement in the control of asthma symptoms

PHARMACOKINETICS

Absorption. Montelukast is rapidly absorbed after oral use. In adults, when taking 10 mg of montelukast on an empty stomach_{, cmax} in plasma is reached in 3 hours. On average, bioavailability after oral use is 64%. Food intake does not affect the bioavailability and_cmaxof montelukast.

Distribution. Montelukast binds more than 99% to plasma proteins. The V_d of montelukast at steady state averages 8-11 liters. The drug does not penetrate well through the blood-brain barrier. Montelukast concentrations were minimal in all body tissues 24 hours after use of the drug.

Biotransformation. Montelukast undergoes intensive metabolism. 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 P450 isoenzymes 3A4,2A6, and 2C9 are involved in the metabolism of montelukast, while at therapeutic concentrations montelukast does not inhibit cytochrome P450 isoenzymes 4A,2C9,1A2,2A6,2C19, and 2D6. The contribution of metabolites to the therapeutic effect of montelukast is minimal.

Output. Plasma clearance of montelukast in healthy adults averages 45 ml/min. After oral use of montelukast,86% of the drug is excreted through the intestines and less than 0.2% – by the kidneys. The drug and its metabolites are mainly excreted in the bile.

Pharmacokinetics in different groups of patients

For the elderly, patients with mild or moderate hepatic insufficiency, no dose adjustment is required. No studies have been conducted in patients with renal insufficiency. Since montelukast and its metabolites are excreted in the bile, no dose adjustment is required for patients with renal insufficiency. Data on the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (score >9 on the Child-Pugh scale) are not available.

Indications

Long-term treatment and prevention of bronchial asthma (including prevention of day and night symptoms of the disease); treatment of “aspirin” asthma and prevention of bronchospasm of physical effort.

Use during pregnancy and lactation

Singlon can be used during pregnancy and lactation if the expected benefit to the mother exceeds the potential risk to the fetus and child.

Contraindications

• hypersensitivity to the Active ingredient or to any of the excipients;
• children under 15 years of age;
• lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

With caution: pregnancy and lactation.

Side effects

Blood and lymphatic system disorders: increased tendency to bleed.

Immune system disorders: hypersensitivity reactions, including anaphylaxis; eosinophilic liver infiltrates.

Mental disorders: sleep disorders, including nightmares, hallucinations, insomnia; irritability, anxiety, agitation, including aggressive behavior, tremor, depression, suicidal thoughts and suicidal behavior (suicidality).

Nervous system disorders: headache, dizziness, drowsiness, paresthesia/hypesthesia, seizures.

Disorders of the heart: rapid heartbeat.

Gastrointestinal disorders: abdominal pain, diarrhea, dry mouth, dyspepsia, nausea, vomiting.

Disorders of the hepatobiliary system: increased activity of transaminases in the blood serum (alanine aminotransferase, aspartate aminotransferase), cholestatic hepatitis.

Skin and subcutaneous tissue disorders: angioedema, ecchymosis, urticaria, pruritus, rash, erythema nodosum.

Musculoskeletal and connective tissue disorders: arthralgia, myalgia, including muscle spasms.

General disorders and disorders at the injection site: thirst, asthenia/increased fatigue, discomfort, edema.

Cases of Charga-Strauss syndrome (systemic eosinophilic vasculitis)have been reported in patients suffering from bronchial asthma, while taking montelukast.

Interaction

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

The plasma AUC of montelukast decreased by approximately 40% in patients taking montelukast and phenobarbital. Since CYP3A4 is involved in the metabolism of montelukast, caution should be exercised, especially in children, when using montelukast with CYP3A4 inducers such as phenytoin, phenobarbital and rifampicin.

In vitro studies have established that montelukast is a potent inhibitor of CYP2C8. However, the results of a clinical interaction study of montelukast and rosiglitazone (an example of marker substrates for drugs whose main metabolism is carried out by the CYP2C8 enzyme) did not reveal an inhibitory effect of montelukast on CYP2C8 invivo.

Therefore, it is expected that montelukast will not significantly alter the conversion of drugs that are metabolized with this enzyme (for example, paclitaxel, rosiglitazone and repaglinide).

When taking high doses of montelukast (with a 20-and 60-fold excess of the recommended dose for adults), a decrease in the concentration of theophylline in plasma is observed. This effect is not observed when taking the drug in the recommended doses of 10 mg / day.

How to take, course of use and dosage

Inside.

Adults and adolescents aged 15 years and older for the treatment of bronchial asthma, take one tablet of Singlon 10 mg daily in the evening, regardless of food intake.

General recommendations:

The therapeutic effect of Singlon on the symptoms associated with bronchial asthma is manifested within one day. The patient is recommended to continue taking Singlon both during periods of controlled course of bronchial asthma, and during periods of worsening of the course of the disease.

The drug Singlon should not be taken together with other drugs containing the same Active ingredient – montelukast.

In elderly patients with mild or moderate renal insufficiency, hepatic insufficiency, no dose adjustment is required. There are no data available for patients with severe hepatic insufficiency.

The dose of the drug is the same for female and male patients.

The drug Singlon can be included in existing treatment regimens for bronchial asthma.

Inhaled glucocorticosteroids: Singlon is prescribed for the treatment of bronchial asthma as an adjunct therapy for patients whose inhaled glucocorticosteroids and short-acting beta-adrenomimetics used as needed do not provide the necessary clinical control of the disease. Montelukast should not replace inhaled corticosteroids.

For children aged 6 to 14 years, chewable tablets of 5 mg are used.

Overdose

There is no specific information on the treatment of overdose with Singlon. There are no data on overdose symptoms when taking the drug in adult 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 have been cases of acute overdose of montelukast in adults and children at a dose higher than 1000 mg (approximately 61 mg / kg for a child aged 42 months).

The obtained clinical and laboratory results were consistent with the safety profile for adults and children.

The most common adverse events were consistent with the safety profile of montelukast and included abdominal pain, drowsiness, mydriasis, thirst, headache, vomiting, and psychomotor hyperactivity.

There are no data on the possibility of elimination of montelukast during peritoneal dialysis or hemodialysis.

Special instructions

Singlon should not replace inhaled or oral glucocorticosteroids.

There are no data indicating the possibility of reducing the dose of oral glucocorticosteroids with concomitant use of Singlon.

In rare cases, patients taking medications for the treatment of bronchial asthma, including Singlon, may experience systemic eosinophilia, sometimes accompanied by clinical manifestations of vasculitis and Charg-Strauss syndrome; this condition is usually treated with systemic glucocorticosteroids. Such cases are usually, but not always, associated with dose reduction or discontinuation of oral glucocorticosteroids. It is impossible to exclude or confirm the possibility that the use of leukotriene receptor antagonists may be associated with the occurrence of Charg-Strauss syndrome. Doctors should be aware of the potential for patients to develop eosinophilia, vasculitis, increased pulmonary symptoms, cardiac complications, and / or neuropathy. Patients who experience the above symptoms should be re-evaluated, and their treatment regimen should be reviewed.

Taking Singlon does not affect the use of acetylsalicylic acid and other non-steroidal anti-inflammatory drugs in patients with bronchial asthma with hypersensitivity to acetylsalicylic acid.

The drug contains lactose, so it should not be taken in patients with rare hereditary diseases such as lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Effect of the drug on the ability to drive vehicles and mechanisms

It is assumed that the drug Singlon does not affect the ability to drive a car or other mechanisms. However, in very rare cases, patients experienced drowsiness.

Form of production

Film-coated tablets

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Montelukast

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children over 15 years of age, Adults as prescribed by a doctor, Children as prescribed by a doctor

Indications

Bronchial Asthma, Bronchospasm