Active substanceMontelukastMontelukast
Similar drugsTo uncover
  • Almonte
    pills inwards 
  • Almonte
    pills inwards 
  • Glemont
    pills inwards 
  • Monax®
    pills inwards 
  • Monax®
    pills inwards 
  • Moncasta®
    pills inwards 
    KRKA-RUS, LLC     Russia
  • Moncasta®
    pills inwards 
    KRKA-RUS, LLC     Russia
  • Montler®
    pills inwards 
  • Montler®
    pills inwards 
  • Montelar
    pills inwards 
    Sandoz d.     Slovenia
  • Montelar
    pills inwards 
    Sandoz d.     Slovenia
  • Montelukast
    pills inwards 
    VERTEKS, AO     Russia
  • Montelukast
    pills inwards 
    VERTEKS, AO     Russia
  • Montelukast
    pills inwards 
  • Montelukast
    pills inwards 
  • Montelukast
    pills inwards 
  • Singlon®
    pills inwards 
    GEDEON RICHTER, OJSC     Hungary
  • Singlon®
    pills inwards 
    GEDEON RICHTER, OJSC     Hungary
  • Singlon®
    pills inwards 
    GEDEON RICHTER, OJSC     Hungary
  • Singular®
    pills inwards 
    Merck Sharp and Doum B.V.     Netherlands
  • Singular®
    pills inwards 
    Merck Sharp and Doum B.V.     Netherlands
  • Singular®
    pills inwards 
    Merck Sharp and Doum B.V.     Netherlands
  • Ektalust®
    pills inwards 
  • Ektalust®
    pills inwards 
  • Dosage form: & nbspfilm-coated tablets
    Composition:One tablet, film-coated, contains:
    active substance: montelukast sodium - 10,4000 mg (in terms of montelukast -10,0000 mg);
    Excipients: lactose monohydrate - 115,0000 mg; cellulose microcrystalline - 65,0000 mg; croscarmellose sodium - 8,0000 mg; magnesium stearate -1.6000 mg;
    film sheath: [hypromellose - 3.0000 mg. giprolose (hydroxypropyl cellulose) -1,1640 mg. talc - 1,1556 mg, titanium dioxide - 0,6522 mg, iron oxide yellow (iron oxide) - 0,0282 mg] or [dry film-coating mixture containing hypromellose (50%), giprolose (hydroxypropylcellulose) (19, 4%), talc (19.26%), titanium dioxide (10.87%), iron oxide yellow (iron oxide) (0.47%)] - 6.0000 mg.
    Description:Round biconvex tablets, covered with a film coating of yellow color. On the cross section, the nucleus is white or almost white in color.
    Pharmacotherapeutic group:Anti-inflammatory anti-bronchoconstrictive means - leukotriene peer reviewers.
    ATX: & nbsp

    R.03.D.C.03   Montelukast

    Pharmacodynamics:

    Cysteinyl-leukotrienes (LTC4, LTD4, LTE4) are strong mediators of inflammation-isikoanoidami, which are distinguished by different cells, including mast cells and eosinophils. These important proastmatic neurotransmitters are associated with cystandNile leukotriene receptors. Cysteinyl leukotriene type 1 receptors (CysLT1receptors) are present in the human respiratory tract (including bronchial smooth muscle cells, macrophages) and other pro-inflammatory cells (including eosinophils and some myeloid stem cells). Cysteinyl-leukotrienes correlate with the pathophysiology of bronchial asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include bronchospasm, increased mucus secretion, increased vascular permeability, and an increase in the number of eosinophils. In case of allergic rhinitis after exposure to the allergen, cysteinyl leukotrienes are released from the proinflammatory cells of the nasal mucosa during the early and late phases of the allergic reaction, which is manifested by the symptoms of allergic rhinitis.With an intranasal test with cysteinyl leukotrienes, an increase in the resistance of the airways and the symptoms of nasal obstruction was demonstrated.

    Montelukast - highly active when administered a drug that significantly improves the rates of inflammation in bronchial asthma. According to biochemical and pharmacological analysis, the drug with high selectivity and chemical affinity binds to CysLT1receptors and (in place of other pharmacologically important respiratory tract receptors, such as prostaglandin, cholinergic or β-adrenergic receptors). Montelukast inhibits the physiological action of LTC cysteinyl leukotrienes4, LTD4, LTE4 by binding to CysLT1receptors, without exerting a stimulating effect on these receptors.

    Montelukast inhibits CysLT1-receptors of the epithelium of the respiratory tract, due to this reduces the bronchospasm caused by the inhalation of cysteinyl-leukotriene LTD4) in patients with bronchial asthma. Doses of 5 mg are sufficient for arresting bronchospasm, induced LTD4.

    Montelukast causes bronchodilation within two hours after ingestion and may supplement the bronchodilation induced by β2-adrenomimetics.

    The use of montelukast in doses exceeding 10 mg per day, taken once, the effectiveness of the drug does not increase.

    Pharmacokinetics:

    Suction

    Montelukast quickly and almost completely absorbed after ingestion. In adults, when taking fasting tablets coated with a film coat, 10 mg maximum concentration in the blood plasma (Cmax) is achieved in 3 hours. The average bioavailability with oral administration is 64%. Food intake does not affect Cmax in blood plasma and the bioavailability of the drug.

    Distribution

    Montelukast binds to plasma proteins more than 99%. The volume distribution of Montelukast in a state of equilibrium concentration averages 8-11 liters. Studies performed on rats with radiolabeled Montelukast indicate a minimal penetration through the blood-brain barrier. In addition, the concentration of labeled Montelukast 24 hours after administration was minimal in all other tissues.

    Metabolism

    Montelukast is actively metabolized. When studying therapeutic doses in a state of equilibrium concentration in blood plasma in adults and children, the concentration of metabolites of montelukast is not determined.

    Research in vitro using human liver microsomes showed that cytochrome P450 isoenzymes CYP: ZA4, 2A6, 2C8 and 2C9 are involved in the metabolism of montelukast. According to further research conducted by in vitro in microsomes of human liver, the therapeutic concentration of montelukast in blood plasma does not inhibit cytochrome P450 isoenzymes CYP: ZA4, 2C9, 1A2, 2A6, 2C19 and 2D6. Excretion

    Plasma clearance of montelukast in healthy adults is an average of 45 ml / min. After ingestion of radioactively labeled montelukast, 86% of its quantity is excreted through the intestine within 5 days and less than 0.2% by the kidneys, which confirms that montelukast and its metabolites are excreted almost exclusively with bile. The half-life of montelukast in young 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. When receiving 10 mg of montelukast, a moderate (about 14%) cumulation of the active substance in the blood plasma is observed once a day.

    Peculiarities of pharmacokinetics in different patient groups

    Floor

    The pharmacokinetics of montelukast in women and men is similar.

    Elderly patients

    With a single oral administration of 10 mg montelukast, the pharmacokinetic profile and bioavailability are similar in elderly patients and young patients. The half-life of montelukast from blood plasma is somewhat greater in elderly patients. Correction of the dose of the drug in elderly patients is not required.

    Race

    There were no differences in clinically significant pharmacokinetic effects in patients of different races.

    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) approximately 41% after a single dose of 10 mg. The half-life of montelukast in these patients is slightly increased (mean half-life is 7.4 hours). Changes in the dose of montelukast for patients with mild to moderate hepatic insufficiency are 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 through the kidneys, pharmacokinetics of montelukast in patients with renal insufficiency has not been evaluated. A dose adjustment for this group of patients is not required.

    Indications:- prevention and long-term treatment of bronchial asthma, including the prevention of day and night symptoms of the disease;
    - treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid;
    - prevention of bronchospasm caused by physical exertion;
    - relief of day and night symptoms of seasonal allergic rhinitis and persistent allergic rhinitis.
    Contraindications:- hypersensitivity to any of the components of the drug;
    - age up to 15 years (for a given dosage of the drug);
    - Lactase deficiency, lactose intolerance and pokozo-galactose malabsorption.
    Pregnancy and lactation:Clinical studies of montelukast with the participation of pregnant women have not been conducted. A drug Montelukast should be used during pregnancy and during lactation, only if the expected benefit for the mother exceeds the potential risk to the fetus or child.During the post-marketing application of montelukast, the development of birth defects in the limbs of newborns whose mothers were taken montelukast during pregnancy. Most of these women also took other medications to treat bronchial asthma during pregnancy. The causal relationship between the administration of montelukast and the development of birth defects of the limbs has not been established.
    It is not known whether montelukast with breast milk. Since many drugs are excreted in breast milk, it is necessary to take this into account when appointing the drug Montelukas breast-feeding women.
    Dosing and Administration:A drug Montelukast take inside once a day, regardless of food intake. For treatment of bronchial asthma, the drug should be taken in the evening.
    In the treatment of allergic rhinitis, the drug can be taken at any time of the day. Patients with bronchial asthma and allergic rhinitis should take one tablet once a day in the evening.
    Adults and teens from age 15
    One tablet, covered with a film membrane (10 mg), once a day.
    General recommendations
    Therapeutic effect of the drug Montelukast on the symptoms that reflect the course of bronchial asthma, manifests itself during the first day. The patient should continue to take the drug Montelukast as in the period of reaching the control of symptoms of bronchial asthma, and during the exacerbation of the disease.
    Special patient groups
    For elderly patients, patients with renal insufficiency, patients with impaired liver function of mild or moderate severity, correction of the dose is required. The dose of the drug is the same for both female and male patients. Application of the drug Montelukast simultaneously with other types of treatment of bronchial asthma
    A drug Montelukast can be added to the treatment of the patient with bronchodilators and inhaled glucocorticosteroids (GCS).
    Side effects:Side effects are usually mild and, as a rule, do not require withdrawal of the drug.
    Impaired nervous system: headache, dizziness, drowsiness, paresthesia / hypesthesia, convulsions.
    Heart Disease: cardiopalmus.
    Disturbances from the respiratory system, chest and mediastinal organs: nosebleeds, pulmonary eosinophilia.
    Disorders of the psyche: agitation, including aggressive behavior or hostility, anxiety, depression, disorientation, attention impairment, pathological dreams, hallucinations, insomnia, memory disorders, psychomotor activity (including irritability, anxiety and tremor), somnambulism, suicidal ideation and behavior.
    Disorders from the gastrointestinal tract: diarrhea, dyspepsia, nausea, vomiting, pancreatitis, abdominal pain, thirst.
    Disorders from the liver and bile ducts: increased activity of alanine aminotransferase (ALT) and aspartate aminotransferase (ACT), hepatitis (including cholestatic, hepatocellular and mixed liver damage).
    Disturbances from the musculoskeletal and connective tissue: arralgia, myalgia, muscle cramps.
    Violations from the blood and lymphatic system: increased tendency to bleeding, thrombocytopenia.
    Disturbances from the skin and subcutaneous tissues: tendency to form hematomas, erythema nodosum, erythema multiforme, itching, rashes, hives, angioedema.
    Immune system disorders: hypersensitivity reactions, including anaphylaxis, eosinophilic liver infiltration.
    Infectious and parasitic diseases: infections of the upper respiratory tract. General disorders and disorders at the site of administration: asthenia (weakness) / fatigue, swelling, pyrexia.
    Overdose:Symptoms
    Data on symptoms of an overdose with montelukast receiving patients with bronchial asthma at a dose exceeding 200 mg per day for 22 weeks and at a dose of 900 mg per day for one week was not revealed.
    There have been cases of acute overdose of montelukast (intake of at least 1000 mg per day) during the post-registration period and during clinical trials in adults and children. Clinical and laboratory data indicated the comparability of the safety profiles of Montelukast in children, adults and elderly patients.
    The most common side effects were thirst, drowsiness, vomiting, psychomotor agitation, headache, mydriasis, abdominal pain. These side effects are consistent with the Montelukast safety profile.
    Treatment
    Treatment for acute overdose is symptomatic.There is no information on the specific treatment of the overdose of montelukast. There is no data on the effectiveness of peritoneal dialysis or hemodialysis.
    Interaction:Montelukast can be prescribed together with other drugs that are commonly used for the prevention and long-term treatment of bronchial asthma and / or the treatment of allergic rhinitis. The recommended therapeutic dose of montelukast no clinically significant effect on the pharmacokinetics of the following drugs: theophylline, nrednizona, prednisolone, oral contraceptives (etnnilestradiol / norethisterone 35/1), terfenadine, digoxin and warfarip.
    The value of AUC of montelukast decreases with simultaneous administration of phenobarbital by about 40%, but this does not require a change in the dosage regimen of the drug Montelukast.
    In vitro studies found that montelukast inhibits the CYP 2C8 isoenzyme of the cytochrome P450 system. However the investigation of drug interactions in vivo montelukast and rosiglitazone (metabolized involving CYP isoenzyme cytochrome 2S8) is not received confirmation montelukast isoenzyme inhibition CYP 2S8.Therefore, in clinical practice, the effect of montelukast on CYP 2C8-mediated metabolism of a number of drugs, including paclitaxel, rosiglitazone, repaglinide, etc., is not expected to be influenced by clinical practice.
    In vitro studies have shown that montelukast is a substrate of isoenzymes CYP 2C8, 2C9 and 3A4. Data from the clinical study of drug interaction for montelukast and gemfibrozil (an inhibitor of both CYP 2C8 and 2C9) demonstrate that gemfibrozil increases the effect of systemic exposure to montelukast 4.4-fold. The simultaneous administration of itraconazole, a strong inhibitor of the CYP isoenzyme ZA4, 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 effect of montelukast can not be considered clinically significant on the basis of safety data when administered at doses exceeding the approved dose of 10 mg for adult patients (eg 200 mg / day for adult patients for 22 weeks and up to 900 mg / day for of patients taking the drug for about one week, there were no clinically significant adverse effects).Thus, with a co-administration with gemfibrozilom adjustment of the dose of montelukast is not required. According to the results of in vitro studies, clinically important drug interactions with other known inhibitors of the CYP 2C8 isoenzyme (for example, with trimethoprim) are not expected. In addition, the joint administration of montelukast with itraconazole alone did not result in a significant increase in the effect of systemic exposure to montelukast.
    Combined treatment with bronchodilators
    Montelukast is a well-founded addition to monotherapy with bronchodilators if the latter do not provide adequate control of bronchial asthma. When the therapeutic effect is achieved against the background of drug therapy Montelukast it is possible to begin a gradual decrease in the dose of bronchodilators.
    Combined treatment with inhaled glucocorticosteroids
    Treatment with Montelukast provides an additional therapeutic effect to patients who use inhaled glucocorticosteroids. When the patient's condition is stabilized, a gradual decrease in the glucocorticosteroid dose can be started under the supervision of the doctor.In some cases, complete cancellation of inhaled glucocorticosteroids is permissible, but a sharp substitution of inhaled glucocorticosteroids for the drug Montelukast Not recommended.
    Special instructions:The effectiveness of montelukast for oral administration in relation to the treatment of acute attacks of bronchial asthma has not been established. Therefore, the drug Montelukast in tablets it is not recommended to prescribe for the treatment of acute attacks of bronchial asthma. Patients should be instructed to always carry emergency medication to relieve asthma attacks (inhalation (β2agonists of short action).
    Do not stop taking the drug Montelukast in the period of exacerbation of bronchial asthma. It should be remembered the need for the use of emergency drugs to stop seizures (inhalation β2agonists of short action).
    Patients with a confirmed allergy to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (IPVP) should not take these drugs during the treatment with the drug Montelukast, because the montelukast, improving respiratory function in patients with allergic bronchial asthma, nevertheless, can not completely prevent bronchoconstriction caused by a nonsteroidal anti-inflammatory drug.
    The dose of glucocorticosteroids for inhalations or oral administration taken against the background of drug treatment Montelukast, you can gradually reduce under the supervision of a doctor. However, a sharp replacement of glucocorticosteroids with the drug Montelukast to conduct it is impossible.
    In patients who took montelukast, psychoneurological disturbances have been described (see the "Side effect" section). Given that these symptoms could be caused by other factors, it is not known whether they are associated with taking montelukast. The doctor should discuss this undesirable phenomenon with patients and / or their parents / guardians. Patients and / or their parents / guardians should explain that in case of such symptoms it is necessary to inform the attending physician about it.
    In rare cases, patients receiving antiasthmatic drugs, including leukotriene receptor antagonists, experienced one or more of the following adverse events: eosinophilia, rash,worsening of pulmonary symptoms, cardiac complications and / or neuropathy, sometimes diagnosed as Charge-Strauss syndrome (systemic eosinophilic vasculitis). These cases have sometimes been associated with a lower dose or withdrawal of oral corticosteroid therapy. Although the causal relationship of these adverse events with therapy with leukotriene receptor antagonists has not been established, in patients taking the drug Montelukast, care must be taken and clinical monitoring performed.
    A drug Montelukast tablets, film-coated, 10 mg contains lactose monohydrate. Patients with hereditary intolerance to galactose, congenital insufficiency of lactase or glucose-galactose malabsorption should not take the drug Montelukast.
    Effect on the ability to drive transp. cf. and fur:Data indicating that the administration of montelukast affects the ability to drive a car or moving machinery has not been identified. However, when the drug is used, side effects such as dizziness and drowsiness may occur.In view of this, care should be taken when driving vehicles and performing actions requiring quickness of psychomotor reactions.
    Form release / dosage:Tablets, film-coated, 10 mg.
    Packaging:10, 14, 15, 20, 28 or 30 tablets in a contoured cell pack made of a polyvinyl chloride light protective film and aluminum foil.
    10, 14 or 60 tablets in a can of high-density polyethylene.
    1, 3 or 6 contiguous cell packs of 10 tablets, 1 or 2 contour packs of 14 tablets, 1, 2 or 4 contiguous cell packs of 15 tablets, 1 circuit cell pack of 28 tablets, 3 contour packs but 20 tablets, 1 or 2 contourcell packs of 30 tablets or one bank together with instructions for use in a pack of cardboard.
    Storage conditions:Store in a dark place at a temperature of no higher than 25 ° C.
    Keep out of the reach of children.
    Shelf life:3 years.
    Do not use after expiry date.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-003249
    Date of registration:08.10.2015
    Expiration Date:08.10.2020
    The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp2016-10-28
    Illustrated instructions
      Instructions
      Up