Almont chewable tablets 4 mg 28 pcs. (montelukast)

Release form

Tablets

Packaging

In the package 28pcs. 4mg each

Pharmacological action of

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

ATX blocker:

R.03.DC03 Montelukast

Pharmacodynamics: Cysterinyl-4, Lake 4, LTE 4, Lake 4 LTE4) are strong pro-inflammatory eicosanoids that are released from various cells, including 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 stops the bronchospasm induced by inhalation 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 suppresses both 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. Plasma clearance of montelukast in healthy adult volunteers is an average of 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.

Data on the nature of the pharmacokinetics of montelukast in a patient

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.

Data on the nature of the pharmacokinetics of montelukast in a patient

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.

Data on the nature of the pharmacokinetics of montelukast in a patient Since montelukast and its metabolites are not excreted by the kidneys, dose adjustment in this category of patients is not required.

Data on the nature of the pharmacokinetics of montelukast in a patient Since montelukast and its metabolites are not excreted by the kidneys, dose adjustment in this category of patients is not required.

Data on the nature of the pharmacokinetics of montelukast in a patientThere are no patients with severely impaired liver function (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 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 and older)

prevention of bronchospasm caused by physical exertion (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 le (For a 5 mg dosage)

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

phenylketonuria (containing aspartame).

Use during pregnancy and lactation

Use of the drug Almont during pregnancy is possible if the intended benefit to the mother outweighs the potential risk to the fetus.

The decision to cancel breastfeeding for the period of use of the Almont drug is made on the basis of an assessment of the expected benefits to the mother and the potential risk to the baby.

Special instructions

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 inhalation of short-acting beta-adrenomimetics than usual.

Do not abruptly replace Almont 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, in patients who receive anti-asthma drugs, including montelukast, can 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 tablet chewable 4 mg contains: active substance: montelukast 4.00 mg (as mo telukasta sodium 4.16 mg)

Excipients: Mannitol 160.96 mg Cellulose microcrystalline 52.80 mg, giproloza 7.20 mg, 7.20 mg of croscarmellose sodium, 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 the supervision of adults. Montelast 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 individually depending on the time of the greatest exacerbation of symptoms. No dose adjustment is required within these age groups. General recommendations The therapeutic effect of the drug, which allows controlling asthma symptoms, is achieved within a day after administration. The patient is recommended to continue taking the drug, both during periods of controlled course of bronchial asthma, and during an 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.

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).

Drug Interactions

In patients simultaneously receiving phenobarbital, the area under the pharmacokinetic concentration-time curve of montelukast decreased by about 40%, however, correction of the dosage regimen in such patients is not required. Since montelukast is metabolized by the isoenzyme CYP3A4, caution should be exercised, especially in children, if montelukast is used simultaneously with inducers of the isoenzyme CYP3A4, such as phenytoin, phenobarbital and rifampicin.

Montelukast can be prescribed along with other drugs traditionally used for the prevention and long-term treatment of bronchial asthma and / or allergic rhinitis.

Montelukast in the recommended therapeutic dose did not have a clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol / norethinodrel 35/1), terfenadine, digoxin and warfarin.

In vitro studies have found that montelukast is a potent inhibitor of the CYP2C8 isoenzyme. However, when studying the drug interaction in vivo of montelukast and rosiglitazone (a marker substrate, a representative of drugs that are primarily metabolized by the CYP2C8 isoenzyme), there is no confirmation of the inhibition of CYP2C8 isoenzyme by montelukast. Thus, in clinical practice, the effect of montelukast on SUR2C8-mediated metabolism of a number of drugs, including paclitaxel, rosiglitazone, repaglinide.

In vitro studies have shown that montelukast is a substrate of the CYP2C8 isoenzyme, and to a lesser extent the CYP2C9 and 3A4 isoenzymes. Data from a clinical study of drug interactions in relation to montelukast and gemfibrozil (an inhibitor like CYP2C8, and 2C9) demonstrate that gemfibrozil increases the effect of systemic exposure to montelukast by 4.4 times. The combined administration of itraconazole, a potent inhibitor of the CYP3A4 isoenzyme, together with gemfibrozil and montelukast did not lead to an additional increase in the effect of systemic exposure to montelukast. The effect of gemfibrozil on the systemic effects of montelukast cannot be considered clinically significant based on safety data when used in doses exceeding the approved dose of 10 mg for adult patients (for example, 200 mg / day for adult patients for 22 weeks and up to 900 mg / day for patients taking the drug for about one week did not show clinically significant negative effects). Thus, when combined with gemfibrozil, dose adjustment of montelukast is not required. According to the results of in vitro studies, clinically significant drug interactions with other known inhibitors of the CYP2C8 isoenzyme (for example, with trimethoprim) are not expected. In addition, the combined administration of montelukast with itraconazole alone did not lead to a significant increase in the effect of systemic exposure to montelukast.

Combined treatment with bronchodilators

ALMONT is a reasonable supplement to monotherapy with bronchodilators, if the latter do not provide adequate control of bronchial asthma. Upon reaching the therapeutic effect of treatment with ALMONT, a gradual reduction in the dose of bronchodilators can begin.

Combined treatment with inhaled GCS

Treatment with ALMONT provides an additional therapeutic effect to patients using inhaled GCS. Upon reaching stabilization, a gradual decrease in the dose of corticosteroids can be started under the supervision of a physician. In some cases, the complete cancellation of inhaled GCS is acceptable, however, a sharp replacement of inhaled GCS with ALMONT is not recommended.

Overdose

Symptoms of drug overdose in patients with chronic bronchial asthma when administered at a dose greater than 200 mg per day for 22 weeks and at 900 mg per day for 1 week have not been detected. There are reports of an acute overdose of montelukast (with at least 1 g per day) in the post-marketing period and in clinical studies in adults and children. Clinical and laboratory data thus 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: carrying out symptomatic therapy.

Storage conditions

The product should be stored out of the reach of children, in a dry, dark place at a temperature not exceeding 30 ° C.

Shelf life

Shelf life 3 years.

Deystvuyushtee substance

Montelukast

Prescription conditions from

pharmacies Prescription

dosage form

lozenges

Prescribing

Prescribing

Children prescribed by a doctor, Adults prescribed by a doctor, Children older than 1 year old srdlp18 prd prd prd For children prescribed by a doctor, Adults prescribed by a doctor, Children over 2 years old

Actavis Ltd, Iceland



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