Mezhdunarodnoye the unlicensed
name Montelukast Dosage Form
chewable tablets of 4 mg, 5 mg
One tablet contains
active agent – sodium montelukast (it is equivalent to montelukast) 4.16 (4.0) mg and 5.2 (5.0) mg
excipients: Mannitolum, cellulose microcrystalline, gipromelloza, sodium of a kroskarmelloz, aspartame, magnesium stearate, fragrance crimson, gland (III) oxide red E 172.
of the Tablet of round shape, with a biconvex surface, pink color, with impregnations (for a dosage of 4 mg)
Tablets of round shape, with biconvex a surface, pink color, with impregnations, with risky on the one hand (for a dosage of 5 mg)
Other drugs for treatment of bronchial asthma for system use. Antagonists of leukotriene receptors.
ATC R03D C03 code
Pharmacokinetics Montelukast properties is quickly and almost completely soaked up after intake. At reception on an empty stomach the maximum concentration in blood plasma at children at the age of 2 – 5 years and adults is reached in 2 hours after reception. The bioavailability is 73%, and decreases to 63% after intake of standard food.
More than 99% of montelukast contact proteins of blood plasma. The volume of distribution of montelukast averages 8-11 liters.
Montelukast is actively metabolized in a liver.
Isoenzymes of CYP (3A4, 2A6 and 2C9) P450 cytochrome are involved in process of metabolism of montelukast, at the same time in therapeutic concentration montelukast is not inhibited by isoenzymes of CYP P450 cytochrome: 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6.
Montelukast discharge on average makes 45 ml/min. of blood plasma. After oral administration of montelukast, 86% of its quantity are removed with a stake within 5 days and less than 0.2% – with urine that confirms that montelukast and its metabolites are excreted almost only with bile.
Elimination half-life of montelukast makes from 2.7 to 5.5 hours.
Montelukast specifically inhibits CysLT1-receptors of tsisteinilovy leukotrienes (LTS4, LTD4 and LTE4) – mediators of the chronic persistent inflammation maintaining hyperreactivity of bronchial tubes in bronchial asthma. Reduces expressiveness of a spasm of smooth muscles of bronchioles and vessels, hypostasis, migration of eosinophils and macrophages, reduces secretion of slime and improves mukotsiliarny transport. Montelukast causes a bronkhodilatation within 2 hours after intake, and shows synergism with ß2 – adrenomimetikam.
In clinical trials montelukast showed the efficiency at inhibition of the bronkhokonstriktion caused by inhalation LTD4 in low dosages, such as 5 mg. Bronkhodilatation was observed within 2 hours after oral introduction. The effect of a bronkhodilatation caused β by adrenomimetika supplemented that, arising under the influence of montelukast. Treatment by montelukast inhibited both an early, and late phase of a bronkhokonstriktion, owing to effect of antigen. Montelukast in comparison with placebo reduced quantity of eosinophils in peripheral blood at adult persons and children. In a separate research the treatment by montelukast significantly reduced quantity of eosinophils in airways (on phlegm researches) and in peripheral blood at improvement of clinical control. At adult persons and children at the age of 2-14 years montelukast in comparison with placebo reduced quantity of eosinophils in peripheral blood at improvement of clinical control of asthma.
– prevention and long-term treatment of bronchial asthma at adults and children since 2 years, including prevention of day and night symptoms of a disease, prevention of the bronchospasm caused by physical activity
– prevention and treatment of persistent asthma easy and moderately severe as additional therapy, at treatment by inhalation corticosteroids, short-range β-agonists
– as an alternative to low dosed inhalation corticosteroids in slight persistent asthma which in the anamnesis have no recently postponed serious attacks of asthma and also at treatment of patients who cannot apply inhalation corticosteroids
the Route of administration and doses
In 1 times a day, daily in the evening in 1 hour prior to or in 2 hours after a meal.
For children at the age of 2–5 years – chewable tablets in a dose of 4 mg.
For children at the age of 6–14 years – chewable tablets in a dose of 5 mg.
There is no need of dose adjustment for these age groups.
The general recommendations
Therapeutic action of Asmenol on the indicators reflecting a course of bronchial asthma develops during the first day. Patients should
continue to accept Asmenol, both at improvement of a course of the disease, and during the deterioration period.
To patients of advanced age, and also or with a renal failure the dose adjustment is not required to patients with an abnormal liver function of easy and moderate degree.
When treatment by Asmenol is combined with therapy to inhalation corticosteroids, it is not necessary to cancel montelukast sharply.
– a headache
– an abdominal pain
– the increased tendency to bleedings
– reactions of hypersensitivity, including an anaphylaxis, eosinophilic
infiltration of a liver
– a sleep disorder, including nightmares, hallucinations, psychomotor
hyperactivity (including irritability, concern, excitement,
including agressive behavior and a tremor), a depression and insomnia
– dizzinesses, drowsiness, paresthesias/hypesthesias, spasms
– diarrhea, dryness in a mouth, dyspepsia, nausea, vomiting
– increase in levels of serumal transaminases (ALT, nuclear heating plant),
– a Quincke’s disease, bruises, urticaria, an itching, rash
– an arthralgia, myalgia, including muscular spasms
– asthenia/fatigue, an indisposition, hypostasis
– the Cherga-Strauss’s syndrome (CSS)
of the Contraindication
– hypersensitivity to any of drug components
– children’s age up to 2 years (safety and efficiency of chewable
tablets are not established)
– pregnancy and the period of a lactation.
Asmenol can be accepted with other medicines used for prevention and long-term treatment of bronchial asthma. In researches of medicinal interactions the recommended Asmenol’s dose had no clinically significant impact on pharmacokinetics of the following drugs: theophylline, Prednisonum, Prednisolonum, oral contraceptives (ethinylestradiol/norethindrone 35/1), terfenadin, digoxin and warfarin.
The area under a concentration curve in blood plasma (AUC) decreased approximately at 40% of patients at joint administration of phenobarbital, however correction of the mode of dosing Asmenola is not required to such patients.
As montelukast is metabolized by means of CYP A4, it is necessary to be careful, especially at children when Asmenol is applied together with inductors CYP 3A4, such as Phenytoinum, phenobarbital and rifampicin.
Treatment by bronchodilators: Asmenol it is possible to add to treatment of patients at whom bronchial asthma is not controlled by use of some bronchodilators. At achievement of therapeutic effect (usually after the first dose) against the background of therapy by Asmenol, the dose of bronchodilators can be reduced gradually.
Inhalation glucocorticosteroids: Treatment by Asmenol provides additional therapeutic effect to the patients receiving treatment by inhalation glucocorticosteroids. At achievement of stabilization of a condition of the patient the dose decline of glucocorticosteroids is possible. The dose of glucocorticosteroids needs to be reduced gradually, under observation of the doctor. At some patients the reception of inhalation glucocorticosteroids can be completely cancelled. Sharp replacement of therapy with inhalation glucocorticosteroids with Asmenol’s appointment is not recommended.
it is not necessary to use montelukast orally for treatment of bad attacks of asthma and to continue intake of usual acceptable and available drugs for emergency aid. At emergence of a bad attack it is necessary to apply short-range inhalation β-adrenomimetik.
Asmenol it is not necessary to replace with inhalation or oral corticosteroids sharply.
Patients with phenylketonuria need to observe extra care at montelukast use as Asmenol contains aspartame, a phenylalanine source.
Features of influence of medicine on ability to run motor transport or potentially dangerous mechanisms
Considering a possibility of development of side effects against the background of the Asmenol drug treatment, it is necessary to show extra care at control of vehicles and work with potentially dangerous mechanisms.
Symptoms: abdominal pain, drowsiness, thirst, headache, vomiting, psychomotor hyperactivity.
A release form at packing
On 14 tablets in blister strip packaging from OOPS / aluminum foil / aluminum PVC / foil.
On 2 planimetric packs together with the instruction for medical use in the state and Russian languages put in a pack from cardboard.
To Store storage conditions at a temperature not above 25 °C.
To store out of children’s reach!
A period of storage
not to use drug after expiry date.
According to the prescription
the Pharmaceutical plant of Polfarm
of JSC Razvernut