Montelar, 14 pcs., 10 mg, film-coated tablets
Montelukast can be prescribed together with other drugs traditionally used for the prevention and long-term treatment of bronchial asthma, such as bronchodilators and inhaled corticosteroids. The recommended therapeutic dose of montelukast did not have a clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethisterone 35/1), terfenadine, digoxin and warfarin.
The AUC value decreases in individuals concomitantly receiving phenobarbital (by approximately 40%), however, no adjustment of the montelukast dosage regimen is required in such patients. in vitro studies
It has been shown that montelukast is a potential inhibitor of the CYP2C8 isoenzyme of the cytochrome P450 system, however, data from clinical studies of drug-drug interactions, including montelukast and rosiglitazone (a preliminary substrate of a representative of medications primarily metabolized by the CYP2C8 isoenzyme) showed that doses of montelukast do not inhibit the CYP2C8 isoenzyme
in vivo
. Therefore, montelukast does not have a significant effect on the metabolism of medications metabolized by this enzyme (for example, paclitaxel, rosiglitazone and repaglinide).
In vitro studies
showed that montelukast is a substrate of CYP2C8, CYP2C9 and CYP3A4. Data from a clinical drug interaction study regarding montelukast and gemfibrozil (an inhibitor of both CYP2C8 and CYP2C9) demonstrate that gemfibrozil increases the effect of systemic exposure to montelukast by 4.4 times.
Co-administration of intraconazole, a strong CYP3A4 inhibitor, with gemfibrozil and montelukast did not result in an additional increase in the effect of systemic exposure to montelukast. The effect of gemfibrozil on the systemic exposure of montelukast may not be considered clinically significant based on safety data when used at doses higher than the approved dose of 10 mg in adults (e.g., 200 mg/day for adults for 22 weeks and up to 900 mg/day - no clinically significant adverse effects were observed for patients taking the drug for approximately one week).
Therefore, no dosage adjustment of montelukast is required when coadministered with gemfibrozil.
Based on in vitro
There are no clinically significant drug interactions expected with other known CYP2C8 inhibitors (for example, trimethoprim). In addition, coadministration of montelukast with intraconazole alone did not significantly increase the effect of systemic exposure to montelukast.
Combination treatment with bronchodilators
Montelar® is a reasonable addition to monotherapy with bronchodilators if the latter do not provide adequate control of bronchial asthma. Once a therapeutic effect has been achieved (usually after the first dose) from treatment with Montelar®, a gradual reduction in the dose of bronchodilators can begin.
Combined treatment with inhaled corticosteroids
Treatment with Montelar® provides an additional therapeutic effect to patients using inhaled corticosteroids. Once the condition has stabilized, you can begin to gradually reduce the dose of GCS under the supervision of a physician. In some cases, complete abolition of inhaled corticosteroids is acceptable, but abrupt replacement of inhaled corticosteroids with Montelar® is not recommended.
Since montelukast is metabolized by the CYP3A4 isoenzyme, caution should be exercised, especially in children over 15 years of age, if montelukast is co-administered with drugs that induce the CYP3A4 isoenzyme, such as phenytoin, phenobarbital and rifampicin.
Montelar film-coated tablets 10 mg 14 pcs. in Moscow
Montelukast can be prescribed together with other drugs traditionally used for the prevention and long-term treatment of bronchial asthma, such as bronchodilators and inhaled corticosteroids. The recommended therapeutic dose of montelukast did not have a clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethinsterone 35/1), terfenadine, digoxin and warfarin.
The AUC value decreases in individuals concomitantly receiving phenobarbital (by approximately 40%), however, no adjustment of the montelukast dosage regimen is required in such patients. in vitro studies
It has been shown that montelukast is a potential inhibitor of the CYP2C8 isoenzyme of the cytochrome P450 system, however, data from clinical studies of drug-drug interactions, including montelukast and rosiglitazone (a preliminary substrate of a representative of medications primarily metabolized by the CYP2C8 isoenzyme) showed that doses of montelukast do not inhibit the CYP2C8 isoenzyme
in vivo
. Therefore, montelukast does not have a significant effect on the metabolism of medications metabolized by this enzyme (for example, paclitaxel, rosiglitazone and repaglinide).
In vitro studies
showed that montelukast is a substrate of CYP2C8, CYP2C9 and CYP3A4. Data from a clinical drug interaction study regarding montelukast and gemfibrozil (an inhibitor of both CYP2C8 and CYP2C9) demonstrate that gemfibrozil increases the effect of systemic exposure to montelukast by 4.4 times.
Co-administration of intraconazole, a strong CYP3A4 inhibitor, with gemfibrozil and montelukast did not result in an additional increase in the effect of systemic exposure to montelukast. The effect of gemfibrozil on the systemic exposure of montelukast may not be considered clinically significant based on safety data when used at doses higher than the approved dose of 10 mg in adults (e.g., 200 mg/day for adults for 22 weeks and up to 900 mg/day - no clinically significant adverse effects were observed for patients taking the drug for approximately one week).
Therefore, no dosage adjustment of montelukast is required when coadministered with gemfibrozil.
Based on in vitro
There are no clinically significant drug interactions expected with other known CYP2C8 inhibitors (for example, trimethoprim). In addition, coadministration of montelukast with intraconazole alone did not significantly increase the effect of systemic exposure to montelukast.
Combination treatment with bronchodilators
Montelar® is a reasonable addition to monotherapy with bronchodilators if the latter do not provide adequate control of bronchial asthma. Once a therapeutic effect has been achieved (usually after the first dose) from treatment with Montelar®, a gradual reduction in the dose of bronchodilators can begin.
Combined treatment with inhaled corticosteroids
Treatment with Montelar® provides an additional therapeutic effect to patients using inhaled corticosteroids. Once the condition has stabilized, you can begin to gradually reduce the dose of GCS under the supervision of a physician. In some cases, complete abolition of inhaled corticosteroids is acceptable, but abrupt replacement of inhaled corticosteroids with Montelar® is not recommended.
Since montelukast is metabolized by the CYP3A4 isoenzyme, caution should be exercised, especially in children over 15 years of age, if montelukast is co-administered with drugs that induce the CYP3A4 isoenzyme, such as phenytoin, phenobarbital and rifampicin.
Montelar chewable tablets 5 mg No. 28
A country
Turkey
The country of production may vary depending on the batch of goods. Please check with the operator for detailed information when confirming your order.
Compound
1 tablet contains: montelukast sodium 5.2 mg.
Excipients: mannitol - 194.9 mg, microcrystalline cellulose - 66 mg, croscarmellose sodium - 15 mg, hyprolose (EXF type) - 9 mg, cherry flavor - 2.4 mg (contains 0.07% Allura red AC (E129)), aspartame - 1.2 mg, cherry flavor - 0.6 mg, iron (III) oxide red dye - 0.45 mg, magnesium stearate - 5.25 mg. Chewable tablets are round, pink in color, with numerous darker inclusions, marked “5” on one side, with a cherry odor.
pharmachologic effect
Leukotriene receptor antagonist. Montelukast selectively inhibits CysLT1 receptors of cysteinyl leukotrienes (LTC4, LTD4, LTE4) of the respiratory tract epithelium, and also prevents bronchospasm in patients with bronchial asthma caused by inhalation of cysteinyl leukotriene LTD4. A dose of 5 mg is sufficient to relieve bronchospasm induced by LTD4. The use of montelukast in doses exceeding 10 mg 1 time / day does not increase the effectiveness of the drug. Montelukast causes bronchodilation within 2 hours after oral administration and may be additive to the bronchodilation caused by beta2-agonists.
Mode of application
The dose is set individually, depending on age, indications and the dosage form used. Take orally in a dose of 4-10 mg 1 time/day. The therapeutic effect of montelukast on indicators reflecting the course of bronchial asthma develops during the first day. You should continue taking montelukast both during the period of achieving control of bronchial asthma symptoms and during the period of exacerbation of the disease. Monteluxt can be added to treatment with bronchodilators and inhaled corticosteroids.
Interaction
When used concomitantly with phenobarbital, the AUC of montelukast decreased by approximately 40% (no adjustment of the montelukast regimen is required). In vitro studies have established that montelukast inhibits the CYP2C8 isoenzyme, however, an in vivo drug interaction study between montelukast and rosiglitazone (metabolized by the CYP2C8 isoenzyme) did not confirm that montelukast inhibits the CYP2C8 isoenzyme. Therefore, in clinical practice, the effect of montelukast on CYP2C8-mediated metabolism of a number of drugs, incl. paclitaxel, rosiglitazone, repaglinide. Montelukast is a reasonable addition to bronchodilator monotherapy if the latter do not provide adequate control of bronchial asthma. Once the therapeutic effect of montelukast treatment is achieved, a gradual reduction in the dose of bronchodilators can begin. The use of montelukast provides an additional therapeutic effect in patients receiving inhaled corticosteroids. Once the condition has stabilized, you can begin a gradual reduction in the dose of GCS under the supervision of a physician. In some cases, complete withdrawal of inhaled corticosteroids is acceptable, but abrupt replacement of inhaled corticosteroids with montelukast is not recommended.
Side effect
From the blood coagulation system: increased tendency to bleeding. From the immune system: - hypersensitivity reactions, incl. anaphylaxis; - very rarely (Mental: agitation (including aggressive behavior or hostility), anxiety, depression, disorientation, pathological dreams, hallucinations, insomnia, irritability, restlessness, somnambulism, suicidal thoughts and behavior (suicidality), tremor. From the nervous system: - dizziness, drowsiness, paresthesia/hypesthesia; - very rarely (from the cardiovascular system: tachycardia. From the respiratory system: nosebleeds, upper respiratory tract infections. From the digestive system: - diarrhea, dyspepsia, nausea, vomiting, pancreatitis, increased activity of ALT and AST in the blood; - very rare (from the skin and subcutaneous tissues: tendency to form hematomas, erythema nodosum, erythema multiforme, itching, rash. Allergic reactions: angioedema, urticaria. From the side musculoskeletal system: arthralgia, myalgia, including muscle cramps.From the body as a whole: asthenia (weakness)/fatigue, edema, pyrexia.
Contraindications
Children under 2 years of age, hypersensitivity to montelukast.
Use during pregnancy and breastfeeding Adequate and strictly controlled clinical studies of the safety of the use of montelukast during pregnancy and lactation (breastfeeding) have not been conducted. It is not known whether montelukast is excreted in breast milk. Montelukast should be used during pregnancy and breastfeeding only in cases where the expected benefit to the mother outweighs the potential risk to the fetus or child.
special instructions
The effectiveness of oral montelukast for the treatment of acute attacks of bronchial asthma has not been established. Therefore, oral montelukast is not recommended for the treatment of acute attacks of bronchial asthma. Patients should be instructed to always carry emergency medications to relieve asthma attacks (short-acting inhaled beta2-agonists). You should not stop taking montelukast during an exacerbation of asthma and the need to use emergency medications (short-acting inhaled beta2-agonists) to relieve attacks. Patients with a confirmed allergy to acetylsalicylic acid and other NSAIDs should not take these drugs during treatment with montelukast, since montelukast, while improving respiratory function in patients with allergic bronchial asthma, nevertheless cannot completely prevent bronchoconstriction caused by NSAIDs. The dose of inhaled corticosteroids used simultaneously with montelukast can be gradually reduced under the supervision of a physician, however, an abrupt replacement of inhaled or oral corticosteroids with montelukast cannot be carried out. Neuropsychiatric disorders have been described in patients taking montelukast. Given that these symptoms could be caused by other factors, it is unknown whether they are related to montelukast. Physicians should discuss these side effects with patients and/or their parents/guardians. Patients and/or their caregivers should be advised that if such symptoms occur, they should notify their physician. Reducing the dose of systemic corticosteroids in patients receiving anti-asthma drugs, including leukotriene receptor blockers, was accompanied in rare cases by the appearance of one or more of the following reactions: eosinophilia, rash, worsening of pulmonary symptoms, cardiac complications and/or neuropathy, sometimes diagnosed as Churg-Strauss syndrome, systemic eosinophilic vasculitis. Although a causal relationship between these adverse reactions and leukotriene receptor antagonist therapy has not been established, caution and appropriate clinical monitoring should be used when reducing the dose of systemic corticosteroids in patients receiving montelukast. Pediatric Use Montelukast should not be used in children under 2 years of age. In children over 2 years of age, montelukast should be used in the appropriate dosage form.
Dispensing conditions in pharmacies
On prescription
