Active substanceMontelukastMontelukast
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  • Dosage form: & nbsptchewing abhea
    Composition:

    1 chewable tablet contains:

    Active substance: Montelukast sodium 4.2 mg and 5.2 mg (equivalent to 4 mg and 5 mg montelukast respectively).

    Excipients: Mannitol - 124,440 / 154,068 mg, croscarmellose sodium - 7,350 / 9,100 mg, microcrystalline cellulose - 4,200 / 5,200 mg, magnesium stearate - 2,940 / 3,640 mg, low-substituted giprolose - 3,000 / 3,714 mg, aspartame - 0,600 / 0,743 mg, cherry flavoring - 0,150 / 0.186 mg, iron oxide red - 0.120 / 0.149 mg.

    Description:

    Round, flat pills of pink color, with a bevel.

    Pharmacotherapeutic group:Anti-inflammatory anti-bronchoconstrictive agent - leukotriene receptor blocker
    ATX: & nbsp

    R.03.D.C.03   Montelukast

    Pharmacodynamics:

    Montelukast selectively inhibits CysLT1receptors for cysteinyl leukotrienes (LTC4, LTD4, LTE4) epithelium of the respiratory tract, thus possessing the ability to prevent bronchial asthma in patients with bronchial asthma caused by the inhalation of cysteinyl leukotriene LTD4. Doses 5 mg is enough to stop the bronchospasm, provoked LTD4. Use of montelukast in doses exceeding 10 mg per day in a single dose regimen does not increase the therapeutic efficacy of the drug. Montelukast causes bronchodilation within 2 hours after ingestion and may supplement the bronchodilation caused by β2-adrenomimetics. Montelukast Suppresses both early and late stages of bronchospasm caused by the action of antigens. Montelukast reduces the number of eosinophils in the peripheral blood, on average 9-15%, and also significantly reduces the number of eosinophils in the airways.

    Pharmacokinetics:

    Suction

    Montelukast quickly and almost completely absorbed after ingestion. The intake of normal food does not affect the bioavailability and maximum concentration in the plasma (Cmax) of chewable tablets. In adults CmOh when taking fasting tablets chewing 5 mg is achieved after 2 hours. Bioavailability is 73% and decreases to 63% when eating. In children aged 2 to 6 years, CmOh is achieved 2 hours after taking 4 mg of chewing tablets on an empty stomach.

    Distribution

    Montelukast almost completely (more than 99%) binds to blood plasma proteins.The volume distribution of Montelukast averages 8-11 liters.

    Metabolism

    Montelukast is actively metabolized in the liver. When using therapeutic doses, metabolites of montelukast in plasma in an equilibrium state in adults and children are not determined.

    It is assumed that the metabolism of montelukast involves cytochrome P450 isoenzymes CYP (3A4 and 2C9), while in therapeutic concentrations montelukast Does not inhibit cytochrome P450 isoenzymes CYP: 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6.

    Excretion

    The clearance of montelukast in healthy adults is an average of 45 ml / min. After ingestion of montelukast 86% of the total is excreted with feces for 5 days and less than 0.2% - with urine, which confirms the excretion of montelukast and its metabolites by excretion into bile.

    The half-life of montelukast in healthy adults ranges from 2.7 to 5.5 hours. The pharmacokinetics of montelukast retains a practically linear character when administered in doses over 50 mg. When taking montelukast in the morning and evening hours, there is no difference in pharmacokinetics.

    Peculiarities of pharmacokinetics in different patient groups

    Floor

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

    Liver failure

    In patients with hepatic insufficiency of mild and moderate severity and clinical manifestations of cirrhosis, a decrease in montelukast metabolism was noted, accompanied by an increase in the area under the pharmacokinetic curve "concentration-time" (AUC) by approximately 41% after a single dose of 10 mg. The recovery period of montelukast in patients with hepatic insufficiency is slightly increased in comparison with healthy volunteers (mean half-life is 7.4 hours). Correction of the dose of montelukast in patients with hepatic insufficiency of mild and moderate severity is not required. There is no data on the character of the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (more than 9 on the Child-Pugh scale).

    Renal insufficiency

    Because the montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast in patients with renal insufficiency has not been evaluated. Correction of the dose of the drug in this group of patients is not required.

    Race

    Clinically significant differences in pharmacokinetic parameters in patients of different racial-ethnic groups were not detected.

    Indications:

    - Prolonged treatment and prevention of bronchial asthma (including prevention of day and night symptoms of the disease) in children, starting from the age of 2 years; treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid and the prevention of bronchospasm caused by physical exertion.

    - Relief of day and night symptoms of allergic rhinitis (seasonal and year-round) in children from 2 years of age.

    Contraindications:

    - Hypersensitivity to any of the components of the drug.

    - Phenylketonuria.

    - Children under 2 years.

    Pregnancy and lactation:

    The drug can be used during pregnancy only if the expected benefit for the mother exceeds the potential risk to the fetus.

    For the period of application of the drug, breastfeeding should be discontinued.

    Dosing and Administration:

    Inside, once a day in the evening, 1 hour before meals or 2 hours after eating.

    Children aged 2 to 6 years with bronchial asthma and / or allergic rhinitis:

    1 chewable tablet 4 mg. Dosing for this age group is not required.

    Children aged 6 to 14 years with bronchial asthma and / or allergic rhinitis:

    1 chewable tablet 5 mg. Dosing for this age group is not required.

    Children over 15 years and adults it is recommended that montelukast tablets, film-coated 10 mg.

    General recommendations

    The therapeutic effect of the drug on the indices of the course of bronchial asthma develops throughout the day. The patient should continue to take the drug as during the control of the symptoms of bronchial asthma, and during periods of exacerbation of the disease.

    Older patients, patients with renal insufficiency and patients with impaired liver function of mild and moderate severity selection of a dose is not required. Data on the use of montelukast in patients with severe hepatic insufficiency are absent.

    Montelukast may be added to the treatment of the patient by bronchodilators, for example, β2-adrenomimetics and inhaled glucocorticosteroids (see section "Interaction with other drugs").

    Side effects:

    In general, the drug is well tolerated. Side effects are usually mild and, as a rule, do not require withdrawal of the drug. The overall incidence of side effects with drug treatment is comparable to that of placebo.

    Infectious and parasitic diseases: infections of the upper respiratory tract.

    On the part of the blood and lymphatic system: increased tendency to bleeding, thrombocytopenia.

    From the immune system: hypersensitivity reactions, including anaphylaxis, eosinophilic liver infiltration.

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

    Disorders of the psyche: pathological dreams, nightmares, hallucinations, insomnia, somnambulism, irritability, anxiety, anxiety, depression, attention and memory disturbances, agitation, including aggressive behavior or hostility, tremor, disorientation, suicidal thoughts and behavior (suicidal).

    From the cardiovascular system: cardiopalmus.

    On the part of the respiratory system, the organs of the thorax and the mediastinum: nose bleed.

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

    From the liver and biliary tract: increased activity alanine aminotransferase (ALT) and aspartate aminotransferase (ACT), Hepatitis (including cholestatic, hepatocellular and mixed liver damage).

    From the skin and subcutaneous tissues: angioneuroticesky edema, propensity to form hematomas, erythema nodosum, erythema multiforme, itching, urticaria, rashes.

    On the part of the organs of the musculoskeletal system and connective tissue: arthralgia, myalgia, including muscle cramps.

    General and local disorders: asthenia (weakness) / increased fatigue, swelling, pyrexia, thirst.

    Other: In rare cases, patients with bronchial asthma had a development of the Chard-Strauss syndrome (see section "Special instructions").

    Overdose:

    After a long (during 22 weeks) treatment of patients with bronchial asthma with a drug at a dose of 200 mg per day and after a short (during the first week) treatment of patients at a dose of 900 mg per day, symptoms of overdose were not observed.

    There are cases of acute overdose with montelukast (intake of at least 1000 mg per day) in the postmarketing period and in clinical studies in adults and children.

    Clinical and laboratory data indicated the comparability of drug safety profiles in children, adults and elderly patients.

    Symptoms: the most frequent are thirst, drowsiness, vomiting, headache, mydriasis, psychomotor agitation and abdominal pain.

    Treatment in case of acute overdose symptomatic. Data on the effectiveness of peritoneal dialysis or hemodialysis Montelukast no.

    Interaction:

    Montelukast can be used in conjunction with other medicinal products for the prevention and treatment of bronchial asthma and / or allergic rhinitis.

    The recommended therapeutic dose of montelukast does not have a clinically significant effect on the pharmacokinetics of such drugs as theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol / norethisterone 35/1), terfenadine, digoxin and warfarin.

    Area under the pharmacokinetic curve "concentration-time" (AUC) montelukast with simultaneous administration with phenobarbital is reduced by about 40%, which does not require changes in the dosage regimen of Montelukast.

    Because the montelukast metabolized by enzyme CYP 3A4, caution should be used, especially in children, with concomitant administration with inhibitors CYP 3A4, such as, phenytoin, phenobarbital and rifampicin. However, no change in the dose of montelukast is required.

    Research in vitro showed that montelukast inhibits isoenzyme CYP 2C8 of the cytochrome P450 system. However, in the study of drug interactions in vivo Montelukast and rosiglitazone (metabolized with the participation of isoenzyme CYP 2C8 of the cytochrome system), the inhibition of isoenzyme by montelukast CYP 2C8. Thus, the effect of Montelukast on CYP 2C8-mediated metabolism of drugs, including paclitaxel, rosiglitazone, repaglinide, etc.

    Gemfibrozil (inhibitor CYP 2C8 and 2C9) increases the effect of systemic action of Montelukast 4.4 times. However, the effect of gemfibrozil on the systemic effect of montelukast can not be considered clinically significant on the basis of safety data for the use of montelukast in doses exceeding the approved dose of 10 mg. Therefore, when co-administered with gemfibrozilom correction dosage of Montelukast is not required.

    Joint use of itraconazole, a potent inhibitor CYP 3A4, together with gemfibrozil and montelukast did not lead to an additional increase in the effect of systemic effects of montelukast. The simultaneous administration of montelukast with itraconazole alone did not lead to an additional increase in the effect of systemic exposure to montelukast.

    Combined treatment with bronchodilators: montelukast is a justified addition to monotherapy with bronchodilator if the latter do not provide effective control of bronchial asthma. When the therapeutic effect (usually after the first dose) from treatment with Montelukast is achieved, a gradual decrease in the dose of bronchodilators can be started.

    Combined treatment with inhaled glucocorticosteroids: treatment montelukast provides an additional therapeutic effect to patients using inhaled glucocorticosteroids.

    Once stabilization is achieved, it is possible to begin gradually and under the supervision of a doctor to reduce doses of a glucocorticosteroid. In some cases, complete cancellation of inhaled glucocorticosteroids is permissible, but a sharp replacement of inhaled glucocorticosteroids by montelukast Not recommended.

    Special instructions:

    The effectiveness of the drug in relation to the treatment of acute attacks of bronchial asthma is not established, therefore the drug is not recommended for acute attacks of bronchial asthma.

    Patients should always have emergency medication to relieve asthma attacks (inhalation beta2agonists of short action).

    You should not stop taking montelukast during a period of exacerbation of asthma and the need to use emergency drugs to stop the attacks.

    Patients with a confirmed allergy to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (NSAIDs) should not take these drugs during treatment with montelukast, since montelukast, improving respiratory function in patients with allergic bronchial asthma, nevertheless, can not completely prevent the bronchoconstriction caused in them by NSAID.

    The dose of inhaled glucocorticosteroids used simultaneously with montelukast can be gradually reduced under the supervision of a physician, however, a sharp substitution of inhaled or oral glucocorticosteroids for montelukast Not recommended.

    Reduced doses of systemic corticosteroids in patients receiving anti-asthma drugs, including blockers of leukotriene receptors, rarely accompanied by the appearance of eosinophilia, rash, worsening pulmonary symptoms, cardiac complications and / or neuropathy, sometimes diagnosed as a Chardzhev-Strauss syndrome (eosinophilic systemic vasculitis). The causal relationship of these unwanted phenomena with the leukotriene receptor antagonist therapy has not been proven, nevertheless it is necessary to carry out careful and appropriate clinical observation at lower doses of systemic glucocorticoids in patients taking montelukast.

    The composition of the drug is aspartameThat is the source of phenylalanine, and the drug is not recommended for use in patients with phenylketonuria.

    Effect on the ability to drive transp. cf. and fur:

    Montelukast does not affect the ability to drive and other mechanisms, but very rarely, some patients were observed drowsiness and dizziness. Whenthe emergence of these signs of patients is not recommended to drive vehicles and engage in other activities that require concentration and speed of psychomotor reactions.

    Form release / dosage:

    Chewable tablets, 4 mg and 5 mg.

    Packaging:

    For 14 chewable tablets in a blister from Al / Al foil.

    One or two blisters together with instructions for use are placed in a cardboard box.

    Storage conditions:

    At a temperature of no higher than 25 ° C, in a place protected from light.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002761
    Date of registration:15.12.2014
    Expiration Date:15.12.2019
    The owner of the registration certificate:Beluga, medicines and cosmetics.Beluga, medicines and cosmetics. Croatia
    Manufacturer: & nbsp
    Representation: & nbspBeluga, medicines and cosmetics. Beluga, medicines and cosmetics. Croatia
    Information update date: & nbsp13.06.2018
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