Expiration date: 10/2025
Release form and composition:
Chewable tablets pink, oval, lenticular, with the embossed inscription SINGULAIR on one side and MSD 711 on the other.
1 tablet contains:
montelukast 4 mg
Auxiliary substances: mannitol, cellulose microcrystalline, hyprolose, iron oxide red, croscarmellose sodium, cherry flavour, aspartame and magnesium stearate.
7 PCs. - blisters (1) - packs of cardboard.
7 PCs. - blisters (2) - packs of cardboard.
7 PCs. - blisters (4) - packs of cardboard.
Chewable tablets pink, round, lenticular, with the embossed inscription MSD 275 on one side and SINGULAIR on the other.
1 tablet contains:
montelukast 5 mg
Auxiliary substances: mannitol, cellulose microcrystalline, hyprolose, dye iron oxide red, croscarmellose sodium, cherry flavour, aspartame and magnesium stearate.
7 PCs. - blisters (1) - packs of cardboard.
7 PCs. - blisters (2) - packs of cardboard.
7 PCs. - blisters (4) - packs of cardboard.
Tablets, film-coated light cream color, square, with rounded edges, engraved MSD 117 on one side and SINGULAIR on the other.
1 tablet contains:
montelukast 10 mg
Excipients: cellulose microcrystalline, lactose, croscarmellose sodium, hyprolose, magnesium stearate.
The composition of the shell: hyprolose, hypromellose, titanium dioxide, dyes iron oxide red and iron oxide yellow, Carnauba wax.
7 PCs. - blisters (1) - packs of cardboard.
7 PCs. - blisters (2) - packs of cardboard.
7 PCs. - blisters (4) - packs of cardboard.
Pharmacological action:
Antagonist of leukotriene receptors. Cysteinyl montelukast inhibits leukotriene receptors in the airway epithelium, at the same time showing the ability to inhibit bronchoconstriction due to inhalation cysteinyl-of leukotriene LTD4 in patients with bronchial asthma. The dose of 5 mg is sufficient for relief of bronchoconstriction induced by LTD4. The use of montelukast in doses exceeding 10 mg/day 1 time/day does not increase efficacy of the drug.
Montelukast causes bronchodilatation within 2 h after ingestion, and can complement bronchodilatation caused by beta2-agonists.
Pharmacokinetics:
Suction
After ingestion of montelukast rapidly and almost completely absorbed from the gastrointestinal tract. The intake of normal food does not affect Cmax in plasma and bioavailability of coated tablets and chewable tablets. In adults in the fasting of coated tablets, at a dose of 10 mg Cmax in plasma achieved through 3 h. the oral Bioavailability is 64%.
After ingestion on an empty stomach the drug in the form of chewable tablets at a dose of 5 mg in adults Cmax is achieved in 2 h. Bioavailability is 73%.
Distribution
The binding of montelukast with proteins of blood plasma is more than 99%. Vd is on average 8-11 L.
In single dose of the drug in the form of coated tablets, at a dose of 10 mg 1 times/day has a moderate (about 14%) of accumulation of active substance in plasma.
Metabolism
Montelukast is actively metabolized in the liver. When used in therapeutic doses, concentrations of metabolites of montelukast in plasma at steady state in adults and children is not determined.
It is assumed that the metabolism of montelukast involves cytochrome P450 isoenzymes (3A4 and 2C9), while in therapeutic concentrations of montelukast do not inhibit cytochrome P450 isoenzymes: 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6.
Excretion
T1/2 of montelukast in young healthy adults is 2.7 to 5.5 h. the clearance of montelukast in healthy adults is in average 45 ml/min After oral administration of montelukast 86% is excreted in feces within 5 days and less than 0.2% - with urine, which confirms that montelukast and its metabolites are excreted almost exclusively in the bile.
Pharmacokinetics in special clinical cases
The pharmacokinetics of montelukast remains almost linear when administered more than 50 mg.
When taking montelukast in the morning and evening differences in pharmacokinetics not observed.
The pharmacokinetics of montelukast in women and men has a similar character.
The ingestion of coated tablets, at a dose of 10 mg 1 times/day pharmacokinetic profile and bioavailability are similar in elderly patients and young age.
In patients with liver failure mild and moderate severity and clinical manifestations of cirrhosis of the liver marked by the slow metabolism of montelukast, accompanied by an increase in AUC of approximately 41% after a single dose of the drug at a dose of 10 mg. Excretion of montelukast in these patients increases slightly compared to healthy subjects (T1/2 on average 7.4 h). Change the dose of montelukast for patients with liver failure mild and moderate severity is not required. Data on the nature of the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (more 9 points on a scale child-Pugh) no.
Because montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast in patients with renal insufficiency has not been assessed. Dose adjustment in this category of patients is not required.
There were no differences in clinically important pharmacokinetic effects in patients, depending on race.
Indications:
Prophylaxis and chronic treatment of asthma in adults and children 2 years and older, including:
— preventing daytime and nighttime symptoms
— treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid
— prevention of bronchospasm caused by physical load.
Relief of daytime and nighttime symptoms of seasonal allergic rhinitis (in adults and children 2 years and older) and persistent allergic rhinitis (in adults and children 2 years and older).
Dosing regimen:
The drug is taken orally 1 times/day regardless of the meal. For the treatment of asthma Singulair® should be taken in the evening. In the treatment of allergic rhinitis, the drug can be taken any time of the day. When combined pathology (bronchial asthma and allergic rhinitis) medication should be taken in the evening.
Adults and adolescents aged 15 years and older drug appointed dose of 10 mg (1 tab., coated)/day.
Children aged 6 to 14 years administered in a dose of 5 mg (1 tab. chewing)/d. Dose selection for this age group is not required.
Children aged 2 to 5 years for the treatment of asthma and/or allergic rhinitis, the drug appointed dose of 4 mg (1 tab. chewing)/d.
The therapeutic effect of Singular on the indicators of the bronchial asthma, develops during the first day. The patient should continue to take Singulair® as in the period of achieving control of symptoms of asthma, and in the period of exacerbation.
For elderly patients, patients with renal insufficiency, patients with mild or moderate liver dysfunction, as well as depending on the sex special dose adjustment is not required.
Singulair® can be added to treatment with bronchodilators and inhaled corticosteroids.
Side effects:
Allergic reactions: anaphylaxis, angioedema, rash, itching, hives rarely - eosinophilic infiltration of the liver.
CNS: unusual vivid dreams, hallucinations, drowsiness, irritability, agitation including aggressive behavior, fatigue, suicidal thoughts and suicidal behaviour (CitiDirect), insomnia, paraesthesia/hypoesthesia, headache, very rarely - convulsive seizures.
From the digestive system: nausea, vomiting, diarrhea, abdominal pain, rarely - cholestatic hepatitis, damage to hepatocytes, most often on the background of concomitant drug therapy or liver disease (alcoholic and other forms of hepatitis).
From the side of musculoskeletal system: arthralgia, myalgia including muscle cramps.
Dermatological reactions: erythema nodosum, a tendency to the formation of subcutaneous hemorrhage (hematoma).
Other: the tendency to increase bleeding, palpitations, swelling, in children aged 2 to 5 years - thirst.
In General, Singulair® is well tolerated. Side effects are generally mild and usually does not require discontinuation of the treatment. The overall frequency of side effects reported with the use of the Singular, is comparable to placebo.
Contraindications:
— children up to age 2 years
— hypersensitivity to the drug.
Pregnancy and lactation:
Singulair® should be used during pregnancy and lactation only in cases where the expected benefit to the mother outweighs the potential risk to the fetus or child.
Special instructions:
Singulair® is not recommended for the treatment of acute asthma attacks. In acute period of bronchial asthma patients should appoint drug therapy, acute and preventive attacks of the disease.
Patients with asthma are advised to always carry emergency medications (inhaled short-range agonists beta-adrenergic receptors).
For the relief of acute attack of asthma after exercise drug used for the relief of attack, i.e. short-range inhalation agonists beta-adrenergic receptors. Treatment of the Singular does not guarantee the absolute prevention of exacerbations.
In the period of exacerbation of asthma and need for cupping drugs emergency assistance (short-inhalation agonists beta-adrenergic receptors) to stop taking the drug Singulair® should not be.
The dose applied simultaneously with a Singular inhaled corticosteroids can be gradually reduced under medical supervision. Should not be abruptly replaced by a Singular therapy of inhaled or oral corticosteroids.
Patients with demonstrated Allergy to acetylsalicylic acid and other NSAIDs should be for the period of treatment of the Singular to avoid contact with these drugs as Singulair®, improving respiratory function in patients with allergic asthma, however, do not prevent bronchoconstriction due to the action of NSAIDs.
Reduce systemic doses of corticosteroids in patients receiving anti-asthmatic remedies, including antagonists of leukotriene receptors, accompanied in rare cases by the occurrence of one or more of the following phenomena: eosinophilia, hemorrhagic rash, worsening of symptoms from the lungs, cardiac complications and/or neuropathy sometimes diagnosed as a syndrome, Churg-Strauss systemic eosinophilic vasculitis. Although a causal relationship of these adverse events with treatment with leukotriene receptor antagonists has not been established, while reducing systemic doses of corticosteroids in patients receiving Singulair®, you must exercise caution and provide appropriate clinical supervision.
Age-related differences in the efficacy profile and the safety of the Singular is not revealed.
Patients with phenylketonuria should be informed that in 1 tablet chewable contains not less than 1.2 mg aspartame.
Effects on ability to drive vehicles and working with machinery
Evidence that the admission of Singular affects the ability to drive or moving mechanisms have not been identified.
Overdose:
Overdose symptoms of Singular. in patients with chronic asthma when used in a dose exceeding 200 mg/day, for 22 weeks in a dose of 900 mg/day within 1 week not detected.
There are reports of acute overdose, montelukast in children (in doses less than 150 mg/day). Clinical and laboratory data indicate that the safety profile of Singular in children the safety profile in adults and elderly patients. The most common adverse events were thirst, somnolence, mydriasis, hyperkinesias, and abdominal pain.
Treatment: symptomatic therapy.
Data on the possible excretion of montelukast by peritoneal dialysis or hemodialysis do not exist.
Drug interactions:
Singulair® can be used together with other medications, traditionally used for prevention and long-term treatment of asthma. Montelukast in the recommended clinical dose had no clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethindrone 35/1), terfenadine, digoxin and warfarin.
In patients simultaneously treated with phenobarbital, the AUC of montelukast decreased approximately 40%. Dose selection of the Singular for this category of patients is not required.
The ineffectiveness of bronchodilators as a single agent asthma treatment you can add Singulair®. Upon reaching the therapeutic effect (usually after the first dose) on the background of therapy with Singular® the dose of bronchodilator can be gradually reduced.
Treatment Singular provides additional therapeutic effect in patients receiving inhaled corticosteroids. Upon reaching stabilization of the patient's condition may reduce the dose of corticosteroids. The dose of corticosteroids should be reduced gradually under medical supervision. Some patients receiving inhaled corticosteroids can be canceled completely. Not recommended sharp replacement therapy with inhaled corticosteroids in the appointment of the Singular.
In research in all vitr found that montelukast inhibits CYP2C8 isoenzyme. However, in the study of drug interaction in viv montelukast and rosiglitazone (metabolized with the participation of izofermenta CYP2C8) was not confirmed inhibition of the isoenzyme CYP2C8 montelukast. Thus, in clinical practice does not assume the effect of montelukast on CYP2C8-mediated metabolism of several drugs, including paclitaxel, rosiglitazone, Repaglinide.
Terms and conditions of storage:
List B. chewable Tablets 5 mg and tablets, film-coated, 10 mg should be stored away from moisture and light place at temperature not exceeding 30°C. the chewable Tablets of 4 mg should be stored away from moisture and light place at temperature from 15°C to 30°C. the shelf Life of chewing tablets - 2 years tablets, film-coated, is 3 years.
The drug should be stored out of the reach of children.