Singlon, 10 mg 28 pcs.

Montelukast is a specific oral leukotriene receptor antagonist. Montelukast has the ability to inhibit bronchospasm caused by inhaled LTD4 at very low doses (5 mg). Bronchodilation is observed within 2 h after oral administration. The bronchodilation effect caused by the beta-adrenomimetic is complemented by the effect of montelukast.

Montelukast inhibits the early and late phases of bronchospasm induced by antigen administration. Montelukast reduces the number of eosinophils in peripheral blood, in the airways (sputum) of adult patients and children and improves bronchial asthma control.

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

Montelukast enhances the effects of inhaled glucocorticosteroids. Montelukast significantly reduces bronchospasm that occurs against the background of physical activity. In patients with bronchial asthma sensitive to acetylsalicylic acid and taking concomitant inhaled and/or oral glucocorticosteroids, treatment with montelukast leads to a significant improvement in the control of bronchial asthma symptoms

PHARMACOKINETICS

Absorption. Montelukast is rapidly absorbed after oral administration. In adults, when 10 mg of montelukast is taken on an empty stomach, C_max in plasma is reached after 3 hours. On average, the bioavailability after oral administration is 64%. Food intake has no effect on the bioavailability and C_max of montelukast.

Distribution. Montelukast is more than 99% bound to plasma proteins. V_d montelukast in equilibrium averages 8-11 liters. The drug penetrates poorly through the blood-brain barrier. Concentrations of montelukast 24 h after administration of the drug were minimal in all body tissues.

Biotransformation. Montelukast is extensively metabolized. When using therapeutic doses, plasma concentrations of montelukast metabolites are not determined in equilibrium in adults and children. 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 WA4, 2C9, 1A2, 2A6, 2C19 and 2D6. The contribution of metabolites to the therapeutic effect of montelukast is minimal.

Elimination. Plasma clearance of montelukast in healthy adults is on average 45 ml/min. After oral administration of montelukast 86% of the drug is excreted through the intestine and less than 0.2% by the kidneys. The drug and its metabolites are excreted mainly with bile.

Pharmacokinetics in different groups of patients

Dose adjustment is not required in elderly patients and patients with mild to moderate hepatic impairment. No studies have been performed in patients with renal insufficiency. Because montelukast and its metabolites are excreted with bile, no dose adjustment is required for patients with renal insufficiency. There are no data on the pharmacokinetics of montelukast in patients with severe hepatic impairment (Child-Pugh score >9).

Indications

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

Active ingredient

Composition

1 film-coated tablet contains:

Active ingredient:

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

Associates:

Lactose monohydrate,

Microcrystalline cellulose 101,

How to take, the dosage

Ingestion.

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

General recommendations:

The therapeutic effect of Singlon on the symptoms associated with bronchial asthma is apparent within one day. The patient is advised to continue taking Singlon both during periods of controlled asthma and during periods of worsening asthma.

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

In elderly patients with mild to moderate renal impairment, hepatic impairment, dose adjustment is not required. There are no data for patients with severe hepatic impairment.

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

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

Inhaled glucocorticosteroids: Singlon is indicated for the treatment of bronchial asthma as adjunctive therapy for patients in whom inhaled glucocorticosteroids and short-acting beta-adrenomimetics used when appropriate do not provide adequate clinical control. Montelukast should not replace inhaled glucocorticosteroids.

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

Interaction

The drug Singlon may be administered together with other drugs traditionally prescribed for the prevention and long-term treatment of bronchial asthma. The drug in recommended doses had no clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinylestradiol/norethisterone 35/1), terfenadine, digoxin and warfarin.

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

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

Montelukast is therefore not expected to significantly alter the conversions of drugs that are metabolized with participation of this enzyme (e.g., paclitaxel, rosiglitazone and repaglinide).

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

Special Instructions

Singlon should not replace inhaled or oral glucocorticosteroids.

There is no evidence to suggest that the dose of oral glucocorticosteroids may decrease with concomitant use of Synglone.

In rare cases, patients taking bronchial asthma medications, including Singlon, may have systemic eosinophilia, sometimes accompanied by clinical manifestations of vasculitis and Churg-Strauss syndrome; this condition is usually treated with systemic glucocorticosteroids. Such cases are usually, but not always, associated with dose reduction or withdrawal of oral glucocorticosteroids. The possibility that administration of leukotriene receptor antagonists may be associated with the occurrence of Churg-Strauss syndrome cannot be excluded or confirmed. Physicians should be aware of the possibility of eosinophilia, vasculitic rash, increased pulmonary symptoms, cardiac and/or neuropathic complications in patients. Patients who develop the above symptoms should be reevaluated, and their treatment regimen should be reviewed.

The administration of Singlon does not affect the administration 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 by patients with such rare hereditary diseases as lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

The 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 vehicles or other mechanisms. However, in very rare cases, drowsiness has been noted in patients.

Contraindications

With caution: pregnancy and lactation.

Side effects

Blood and lymphatic system disorders: increased tendency to bleeding.

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

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

Nervous system disorders: headache, dizziness, somnolence, paresthesia/hypoesthesia, seizures.

Heart disorders: palpitations.

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

Hepatobiliary system disorders: increased transaminase activity in blood serum (alanine aminotransferase, aspartate aminotransferase), cholestatic hepatitis.

Skin and subcutaneous tissue disorders: angioedema, ecchymosis, urticaria, itching, rash, erythema nodosa.

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

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

The development of Churg-Strauss syndrome (systemic eosinophilic vasculitis) has been reported in patients with bronchial asthma while taking montelukast.

Overdose

There is no specific information on the treatment of overdose with Synglon. There are no data on overdose symptoms in adult patients with bronchial asthma at a dose greater than 200 mg/day for 22 weeks and at a dose of 900 mg/day for 1 week.

There have been observed cases of acute montelukast overdose in adults and children at doses above 1000 mg (approximately 61 mg/kg for a child aged 42 months).

The clinical and laboratory results obtained were consistent with the safety profile for adult and pediatric patients.

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

There are no data on the ability to excrete montelukast during peritoneal dialysis or hemodialysis.

Pregnancy use

Singlone may be used during pregnancy and lactation if the expected benefit to the mother outweighs the potential risk to the fetus and child.

Similarities