Singlon - instructions for use, doses, side effects, contraindications

Composition:1 tablet contains:
Active substance: Montelukast sodium 5.20 mg (equivalent to 5 mg montelukast).
Excipients: mannitol 201.675 mg, microcrystalline cellulose 101-66.00 mg, giprolose 9.00 mg, croscarmellose sodium 9.00 mg, cherry flavoring, powder 4.50 mg, aspartame 1.50 mg, iron oxide yellow (E 172) 0.125 mg, magnesium stearate 3.00 mg.

Description:Round, biconvex tablets of pale yellow color, with a pronounced cherry smell, are allowed blotches of a darker color. On one side is the engraving R14 (figure 14 is located under the letter R).
The determination is performed organoleptically.

Pharmacotherapeutic group:Anti-inflammatory anti-bronchoconstrictive means - leukotriene receptor blocker.

ATX: & nbsp

R.03.D.C.03 Montelukast

Pharmacodynamics:Montelukast has a high degree of affinity and selectivity of binding to receptors of cysteinyl leukotrienes.The use of montelukast inhibits the early and late phases of bronchospasm. Montelukast reduces bronchospasm even in very low doses (5 mg). Bronchodilation continues for 2 hours after ingestion. The effect of bronchodilation, caused by beta-adrenomimetic, increases the effect caused by Montelukast. Montelukast reduces the number of eosinophils in the peripheral blood and respiratory tract (in sputum) of children and adults and improves control over the clinical course of bronchial asthma.
In adult patients montelukast significantly improves the morning volume of forced expiration (FEV1) for 1 second. Montelukast increases the clinical effect of inhaled glucocorticosteroids. Montelukast reduces the severity of daytime (including coughing, wheezing, shortness of breath and restriction of activity) and nocturnal symptoms of bronchial asthma. Montelukast reduces the need for beta-adrenomimetics and glucocorticosteroids, used when necessary (with deterioration). In patients receiving montelukast, there is a longer remission than patients who did not take it.The therapeutic effect is noted after the first dose. In children aged 2 years with bronchial asthma of mild severity and episodic exacerbations montelukast significantly reduces the incidence of episodes of exacerbations of bronchial asthma and improves respiratory function. Weakened bronchospasm, which occurs against the background of physical exertion. In patients with bronchial asthma, sensitive to acetylsalicylic acid and taking concomitant therapy with inhaled and / or oral glucocorticosteroids, treatment with montelukast leads to a significant improvement in the management of symptoms of asthma.

Pharmacokinetics:Absorption
The maximum concentration of the substance in the blood plasma (C max) was achieved in children aged 2 to 5 years 2 hours after taking an empty stomach at a dose of 4 mg. The mean Cmax was 66% higher, while the mean Cmin was lower than in adults after receiving a dose of 10 mg.
In adult patients with fasting at a dose of 5 mg C max is achieved 2 hours after admission. The average bioavailability is 73%; it decreases to 63% when taking the drug after a normal meal.
Distribution
Montelukast is more than 99% bound to plasma proteins. The volume distribution of Montelukast in the equilibrium state averages 8-11 liters. Poorly penetrates the blood-brain barrier.
Metabolism
Montelukast undergoes active metabolism in the liver. In the equilibrium state after administration at therapeutic doses, the concentrations of montelukast metabolites in plasma in children and adults are not determined.
Isozymes of cytochrome ZA4, 2A6 and 2C9 are involved in the metabolism of montelukast, but in therapeutic concentrations montelukast does not inhibit cytochrome isoenzymes ZA4, 2C9, 1A2, 2A6, 2C19 and 2D6. Metabolites of Montelukast have little pharmacological activity.
Excretion
The clearance of Montelukast from plasma in healthy adults is an average of 45 ml / min. After ingestion of labeled Montelukast, 86% of the drug was excreted within 5 days through the intestine and less than 0.2% by the kidneys. This indicates that the drug and its metabolites are excreted primarily with bile. The half-life (T_1/2) montelukast in young patients is from 2.7 to 5.5 h. The pharmacokinetics of montelukast retains a practically linear character when ingested doses above 50 mg.
Special patient groups
Studies in patients with renal insufficiency have not been conducted. Because the montelukast and its metabolites are excreted in bile, dose adjustment in patients with renal insufficiency is not required.
Data on the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (score> 9 on the Child-Pugh scale) are not available.

Indications:The drug is shown to children 6-14 years old for:
- long-term treatment and prevention of bronchial asthma (including the prevention of day and night symptoms of the disease);
- treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid and prevention of bronchospasm of physical effort.

Contraindications:- Hypersensitivity to the active ingredient or to any of the excipients.
- Children under 6 years.
- Phenylketonuria (the drug contains aspartame).
- Severe liver dysfunction.

Carefully:Simultaneous application with CYP inductors ЗА4.

Dosing and Administration:Dose for children aged 6-14 years: one tablet chewing 5 mg daily in the evening. The drug Singlon® should be taken 1 hour before or 2 hours after eating.Dose adjustments within this age group are not required. General recommendations:
The therapeutic effect of the drug Singlon® develops within one day. The patient should continue taking Singlon ® as during periods of controlled course of bronchial asthma, and during periods of worsening of the course of the disease.
In patients with renal insufficiency, mild or moderate degree of hepatic insufficiency, dose adjustment is not required. Data for patients with severe hepatic impairment are not available.
The dose of the drug does not depend on the sex of the patient.
Therapy with Singlon ® in combination with other medications to treat bronchial asthma.
If the drug Singlon® is prescribed against the background of inhalation glucocorticosteroids, then you should not suddenly replace inhaled glucocorticosteroids with Singlon®.

Side effects:Below are the adverse reactions in the system-organ classes according to the MedDRA classification, which often (> 1/100, <1/10) were observed in patients receiving montelukast:
Impaired nervous system: headache;
During the post-marketing research, the following adverse manifestations were identified:
Violations from the blood and lymphatic system: increased tendency to bleeding.
Immune system disorders: hypersensitivity reactions, including anaphylaxis; eosinophilic liver infiltrates.
Disorders of the psyche: sleep disturbances, including nightmares, hallucinations, psychomotor hyperactivity (including irritability, anxiety, agitation, including aggressive behavior, and tremors), depression and insomnia, suicidal thoughts and suicidal behavior.
Impaired nervous system: drowsiness, dizziness, paresthesia / hyperesthesia, convulsive seizures.
Disorders from the cardiovascular system: cardiopalmus.
Disorders from the gastrointestinal tract: diarrhea, dry mouth, indigestion, nausea and vomiting.
Disorders from the hepatobiliary system: increased activity of "hepatic" transaminases in the blood serum (alanine aminotransferase, aspartate aminotransferase), cholestatic hepatitis, pancreatitis.
Disturbances from the skin and subcutaneous tissue: angioedema, appearance of ecchymosis, urticaria, pruritus, rash, erythema nodosum, tendency to form bruises.
Disturbances from the musculoskeletal and connective tissue: arthralgia, myalgia, including muscle cramps.
General disorders and disorders at the site of administration: asthenia / fatigue, discomfort, swelling.
In very rare cases, against the background of taking montelukast in patients suffering from bronchial asthma, the syndrome of Charga-Strauss develops.

Overdose:There is no specific information on the treatment of overdose with the drug Singlon® In clinical studies, adult patients with bronchial asthma took the drug at doses up to 200 mg / day for 22 weeks, and in short-term studies at doses up to 900 mg / day for about a week, without clinically significant adverse events.
There have been cases of acute overdose of montelukast in adults and children with a dose of 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 adults and pediatric patients.Most reports on overdose did not contain indications of adverse manifestations. The most common adverse events corresponded to the safety profile of montelukast and included abdominal pain, drowsiness, thirst, headache, vomiting, psychomotor hyperactivity, mydriasis. There is no data on the possibility of removing montelukast for peritoneal dialysis or hemodialysis.

Interaction:The preparation Singlon® can be appointed together with other drugs traditionally prescribed for the prevention and long-term treatment of bronchial asthma. In the recommended doses, the drug 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 area under the concentration-time curve (AUC) of Montelukast in blood plasma decreased by approximately 40% in patients who took montelukast and phenobarbital. Since the metabolism of montelukast is attended by the isoenzyme CYP 3A4, caution should be exercised, especially in children,when using montelukast with such CYP inducers as 4 phenytoin, phenobarbital and rifampicin.
In vitro studies it was found that montelukast is a potent inhibitor of the CYP 2C8 isoenzyme. However, the results of a study of the clinical interaction of montelukast and rosiglitazone (an example of marker substrates for preparations whose basic metabolism is carried out by the CYP 2C8 isoenzyme) did not reveal the inhibitory effect of montelukast on the CYP 2C8 isoenzyme in vivo. Therefore, it is expected that montelukast will not significantly change the conversion of drugs that are metabolized with the participation of this enzyme (for example, paclitaxel, rosiglitazone and repaglinide). When taking high doses of montelukast (at a 20- and 60-fold excess of the recommended dose for adults), a decrease in the concentration of theophylline in the plasma is observed. This effect is not observed when taking the drug in the recommended doses.

Special instructions:Patients should not take chewable tablets Synngon ® for the relief of acute attacks of bronchial asthma. When an attack occurs, it is recommended to use inhaled beta-adrenomimetics.If the need for short-acting beta-adrenomimetics increases, patients should consult a doctor as soon as possible.
Do not abruptly replace inhaled or oral glucocorticosteroids with Singlon®.
There are no data indicating the possibility of reducing the dose of oral glucocorticosteroids with the concomitant use of the Singlon® preparation.
In rare cases, patients taking medications for the treatment of bronchial asthma, including montelukast, systemic eosinophilia may occur, sometimes accompanied by clinical manifestations of vasculitis and Charge-Strauss syndrome; this is an indication for the use of systemic glucocorticosteroids. Such cases are usually, but not always, associated with a decrease in dose or with the elimination of oral glucocorticosteroids. We can neither exclude nor confirm the possibility that the administration of leukotriene receptor antagonists may be associated with the onset of the Chang-Strauss syndrome. Doctors should be informed about the possibility of occurrence in their patients of eosinophilia, vasculitic rash, an increase in pulmonary symptoms, complications from the heart and / or neuropathy.Patients who have the above symptoms should be re-examined and treatment regimens reviewed.
Chewing tablets of Singlon® 5 mg contain aspartame - A source of phenylalanine. Patients with phenylketonuria should be aware that each 5 mg chewing tablet contains 1.5 mg of aspartame.

Effect on the ability to drive transp. cf. and fur:When taking Singlon®, dizziness and drowsiness may develop, which should be considered when driving or working with machinery.

Form release / dosage:Tablets are chewable, 5 mg.

Packaging:For 7 tablets in a blister of aluminum foil. For 2, 4 or 8 blisters are placed in a cardboard box together with instructions for use.

Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C.
Keep out of the reach of children!

Shelf life:2 years.
Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002100

Date of registration:13.06.2013 / 29.04.2014

Expiration Date:13.06.2018

The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary

Manufacturer: & nbsp

GEDEON RICHTER POLAND, Co. Ltd. Poland

Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary

Information update date: & nbsp2016-10-18

Illustrated instructions

Instructions

Singlon® (Singlon)