montelukast | Almont chewable tablets 4 mg 98 pcs.

Pharmacological action of

Pharmacotherapeutic group: Anti-inflammatory anti-bronchoconstrictor agent - leukotriene receptor

ATX blocker:

R.03.DC03 Montelukast

different pharmacodynamics: Cysteenyl-4 cells, strong 4 LTE4 cells, strong 4-LTE4 cells mast cells and eosinophils. These important pro-asthmatic mediators bind to cysteinyl-leukotriene receptors (CysLT), which are present in the human airways and are responsible for the reaction of bronchospasm, sputum production, vascular permeability and an increase in the number of eosinophils.

Montelukast is an orally active compound that has great affinity and selectivity for CysLT1 receptors. Montelukast in a dose of less than 5 mg relieves bronchospasm, inhalation induced LTD4. The bronchodilating effect is observed within 2 hours after oral administration. The bronchodilating effect of beta2-adrenergic agonists is enhanced when taking montelukast. Montelukast inhibits both the early and late stages of bronchospasm caused by exposure to antigens. Montelukast reduces the number of eosinophils in the peripheral blood in adults and children, and also significantly reduces the number of eosinophils in the respiratory tract. In patients with hypersensitivity to acetylsalicylic acid receiving inhaled and / or oral glucocorticosteroids (GCS), the addition of montelukast to therapy provides better disease control.

Pharmacokinetics: Absorption

After oral administration, montelukast is rapidly and almost completely absorbed. In adult patients, after taking chewable tablets at a dose of 5 mg on an empty stomach, the maximum plasma concentration (Cmax) is reached after 2 hours. The average bioavailability is 73%, this value decreases to 63% when taking Montelukast with food. After taking chewable tablets at a dose of 4 mg on an empty stomach in patients aged 2 to 5 years, Cmax is achieved after 2 hours. The average Cmax value in this group of patients is 66% higher, and the average Cmax value is lower than that in adults when taking film-coated tablets at a dose of 10 mg.

Distribution of

The binding of montelukast to plasma proteins is more than 99%. The distribution volume at equilibrium is on average 8-11 liters. Preclinical studies have revealed minimal penetration of montelukast across the blood-brain barrier. 24 hours after administration, the concentration of montelukast is minimal in other tissues.

Metabolism

Montelukast is extensively metabolized in the liver. When used in therapeutic doses, the concentration of montelukast metabolites in plasma in equilibrium in adults and children is not determined.

In vitro studies have shown that P450 cytochrome isoenzymes (3A4, 2A6 and 2C9) are involved in the montelukast metabolism, while montelukast does not inhibit cytochrome P450 isoenzymes at therapeutic concentrations: 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6. Metabolites have a minor therapeutic effect of montelukast.

Excretion

The half-life of montelukast in young healthy adult volunteers is from 2.7 to 5.5 hours. Montelukast plasma clearance in healthy adult volunteers averages 45 ml / min. After oral administration of montelukast, 86% of the total amount is excreted through the intestines within 5 days and less than 0.2% through the kidneys, which, along with data on its bioavailability, confirms the excretion of montelukast and its metabolites mainly with bile.

Pharmacokinetics in special cases

The pharmacokinetics of montelukast in women and men is the same.

In elderly patients or patients with mild to moderate hepatic insufficiency, dosage adjustment of montelukast is not required.

The pharmacokinetics of montelukast in patients with renal failure have not been evaluated. Since montelukast and its metabolites are not excreted by the kidneys, dose adjustment in this category of patients is not required.

There is no data on the nature of the pharmacokinetics of montelukast in patients with severe hepatic impairment (more than 9 points on the Child-Pugh scale).

When taking high doses of montelukast (20 and 60 times the recommended dose for adults), a decrease in theophylline concentration in blood plasma is observed. When taking montelukast in recommended doses of 10 mg once a day, this effect is not observed.

Indications

Prevention and long-term treatment of bronchial asthma in children, including:

prevention of day and night symptoms of the disease (for children 2 years of age and older)

treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid (for children from 6 years or older)

warning of bronchospasm, caused by physical activity (for children from 2 years of age and older).

Relief of symptoms of seasonal and perennial allergic rhinitis in children from 2 years.

Contraindications

Hypersensitivity to the active or any auxiliary substance of the drug

children under 2 years of age (for a dosage of 4 mg) and up to 6 years of age (for a dosage of 5 mg)

patients with rare hereditary diseases: galactose intolerance, lactase deficiency or glucose-galactose malabsorption

phenylketonuria (contains aspartame).

Special instructions

The drug Almont is not recommended for the treatment of acute attacks of bronchial asthma. Patients with asthma are advised to always have emergency medications with them. When an acute attack occurs, short-acting inhaled betag-adrenomimetics should be used. Patients should consult their doctor as soon as possible, if they need more short-acting beta-adrenergic agonist inhalations than usual.

Do not abruptly replace Almonotherapy with inhaled or oral corticosteroids. There is no evidence proving the possibility of reducing the dose of oral corticosteroids while taking montelukast.

In rare cases, patients who receive anti-asthma drugs, including montelukast, may develop systemic eosinophilia, which is sometimes accompanied by clinical signs of vasculitis, the so-called Charge-Strauss syndrome, a condition that is eliminated by taking systemic corticosteroids. These cases are usually associated with dose reduction or discontinuation of oral corticosteroids therapy. It is impossible to exclude or establish the likelihood that antagonists of leukotriene receptors may be associated with the development of Charge-Strauss syndrome. Therefore, doctors need to be warned about the possibility of eosinophilia, a vascular rash, an increase in the severity of pulmonary symptoms, heart complications and / or neuropathy in patients. Patients who develop the above symptoms need to be re-examined and their treatment regimen reviewed. Treatment with Almont does not prevent the development of bronchospasm in patients with hypersensitivity to acetylsalicylic acid when using acetylsalicylic acid and other non-steroidal anti-inflammatory drugs.

Almont contains aspartame, a source of phenylalanine. This drug may be harmful to patients with phenylketonuria.

The drug contains lactose monohydrate and should not be taken by patients with rare hereditary diseases: galactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Influence on the ability to drive vehicles and mechanisms

As a rule, montelukast does not affect the ability to drive vehicles or work with other mechanisms, but very rarely drowsiness and dizziness were noted in some patients, when these signs appear, patients are not recommended to drive vehicles and engage in other activities that require concentration and speed of psychomotor reactions.

Composition

1 chewable tablet 4 mg contains: active substance: montelukast 4.00 mg (as montelukast sodium 4.16 mg) excipients: mannitol 160.96 mg, microcrystalline cellulose 52.80 mg, hyprolose 7.20 mg, krosk rmellose sodium 7.20 mg, Pigment Blend PB-24880 (lactose monohydrate 3.60 mg, iron oxide red 0.40 mg) 4.00 mg, magnesium stearate 2.40 mg, aspartame 1.20 mg, cherry flavor (Silarom Cherry Flavor 1219813182) 0 , 08 mg.

Dosage and administration

Inside, the tablet should be chewed.

Children take the drug under adult supervision.

ALMONT should be taken 1 hour before or 2 hours after a meal.

For bronchial asthma or bronchial asthma and allergic rhinitis: For children aged 2 to 6 years - 1 chewable tablet in a dose of 4 mg once a day in the evening.

For children aged 6 to 14 years - 1 chewable tablet in a dose of 5 mg once a day in the evening.

For allergic rhinitis: For children aged 2 to 6 years - 1 chewable tablet in a dose of 4 mg once a day and for children aged 6 to 14 years - 1 chewable tablet in a dose of 5 mg once a day in an individual mode depending on the time of the greatest exacerbation of symptoms.

Dose adjustment within these age groups is not required.

General recommendations

The therapeutic effect of ALMONT, which allows controlling asthma symptoms, is achieved within 24 hours after administration. The patient is recommended to continue taking the drug as during periods of controlled course of bronchial asthma, and during exacerbation of bronchial asthma.

Patients with renal failure and patients with hepatic insufficiency of mild to moderate severity do not need a special dose selection. No dose adjustment is required depending on the patient's gender.

There is no data on the use of montelukast in patients with severely impaired liver function.

For the treatment of patients of other age groups, a different dosage form and dose of the drug are available - film-coated tablets, 10 mg.

Side effects

Infectious and parasitic diseases: upper respiratory tract infections.

Disorders from the blood and lymphatic system: increased tendency to bleeding, thrombocytopenia.

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

Mental disorders: pathological dreams, including nightmares, hallucinations, insomnia, somnambulism, irritability, anxiety, anxiety, agitation, including aggressive behavior or hostility, tremors, depression, disorientation, suicidal thoughts and behavior (suicidality).

Disorders of the nervous system: headache, dizziness, drowsiness, paresthesia / hypesthesia, convulsions.

Disorders of the heart: palpitations.

Disorders of the respiratory system, chest and mediastinal organs: nosebleeds.

Disorders of the gastrointestinal tract: diarrhea, dry mouth, dyspepsia, nausea, vomiting, abdominal pain, pancreatitis.

Disorders of the liver and biliary tract: increased activity of alanine aminotransferase and aspartate aminotransferase, hepatitis (including cholestatic, hepatocellular and mixed liver lesions).

Disorders of the skin and subcutaneous tissues: angioedema, tendency to hematomas, urticaria, pruritus, rash, erythema nodosum, erythema multiforme.

Disorders of the musculoskeletal and connective tissue: arthralgia, myalgia, including muscle cramps.

General disorders and disorders at the injection site: asthenia / fatigue, malaise, swelling, pyrexia, thirst.

In very rare cases, during the treatment with montelukast, the development of Charge-Strauss syndrome has been reported (see section Special instructions).

Overdose

Symptoms of an overdose of the drug in patients with chronic bronchial asthma when used at a dose exceeding 200 mg per day for 22 weeks and at a dose of 900 mg per day for 1 week were not detected. There are reports of acute overdose of montelukast (when taking at least 1 g per day) in the post-marketing period and in clinical studies in adults and children. Clinical and laboratory data in this case indicate the compliance of the safety profile of the drug in children, adults and elderly patients. The most common symptoms were thirst, drowsiness, vomiting, psychomotor agitation, headache and abdominal pain. Treatment: symptomatic therapy.

Shelf life

3 years.

Terms and conditions

prescription

lekarstvennaja form

pills for resorption

Actavis Ltd, Iceland