Montelukast sodium 5.2 mg, which corresponds to the content of montelukast 5 mg. Auxiliary substances: mannitol - 201.2 mg, microcrystalline cellulose - 66 mg, hyprolose - 9 mg, croscarmellose sodium - 9 mg, dye Pigment Blend PB-24880 (lactose monohydrate - 4.5 mg, iron dye red oxide - 0.5 mg) - 5 mg, magnesium stearate - 3 mg, aspartame - 1.5 mg, cherry flavoring (Silarom Cherry Flavor 1219813182) - 0.1 mg.
Antagonist of leukotriene receptors. Cysteine leukotrienes (LTC4, LTD4, LTE4) are strong pro-inflammatory eicosanoids that are released from various cells, including mast cells and eosinophils. These important prostatic mediators bind to cysteinyl-leukotriene receptors (CysLT) present in the human respiratory tract and are responsible for bronchospasm reaction, sputum production, vascular permeability and an increase in the number of eosinophils. Montelukast is an orally active compound that has a high affinity and selectivity CysLT1 receptors. Montelukast in a dose of less than 5 mg suppresses bronchospasm induced by inhalation LTD4. Bronchodilating effect is observed within 2 hours after oral administration. The bronchodilatory effect of beta2-adrenomimetikov is enhanced when taking montelukast. Montelukast suppresses both the early and late stages of bronchospasm caused by exposure to antigens. Montelukast reduces the number of eosinophils in peripheral blood in adults and children, and also significantly reduces the number of eosinophils in the airways. In patients with hypersensitivity to acetylsalicylic acid, receiving inhaled and / or oral GCS, adding to the therapy of montelukast provides better control of the disease.
AbsorptionAfter taking oral montelukast quickly and almost completely absorbed. In adult patients after taking chewable pills at a dose of 5 mg on an empty stomach, Cmax in plasma is reached after 2 hours. The average bioavailability value is 73%, this value is reduced to 63% when taking montelukast with food. After taking chewable pills in a dose of 4 mg on an empty stomach in patients aged 2 to 5 years, Cmax is reached in 2 hours. The average Cmax value for this group of patients is 66% higher, and the average Cmin value is lower than in adults when taking pills covered film cover, in a dose of 10 mg.In adult patients after taking fasting film-coated pills at a dose of 10 mg, the average Cmax in the blood plasma is reached after 3 hours. The average bioavailability value is 64%; when taken orally with food, the values of bioavailability and Cmax are not violated. DistributionThe binding of montelukast to plasma proteins is more than 99%. Vd in equilibrium is on average 8-11 liters. Preclinical studies have revealed a minimal penetration of Montelukast through the BBB. 24 h after administration, the concentration of montelukast is minimal in other tissues. MetabolismMontelukast is actively metabolized in the liver. When used in therapeutic doses, Css metabolites of montelukast in plasma are not detected in adults and children. In vitro studies have shown that cytochrome P450 isoenzymes (3A4, 2A6 and 2C9) are involved in the montelukast metabolism process, while in therapeutic concentrations montelukast does not inhibit cytochromes. P450: 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6. The metabolites have an insignificant therapeutic effect of montelukast. Introduction of T1 / 2 montelukast in young healthy adult volunteers ranges from 2.7 to 5.5 hours. The plasma clearance of montelukast in healthy adult volunteers averages 45 ml / min. After oral administration of montelukast, 86% of the total amount is eliminated through the intestine within 5 days and less than 0.2% by the kidneys, which, along with data on its bioavailability, confirms the elimination of montelukast and its metabolites mainly with bile. The pharmacokinetics in particular clinical cases of montelukast pharmacokinetics in women and men are the same In elderly patients or patients with mild to moderate hepatic insufficiency, no correction of the montelukast dosing regimen is required. The pharmacokinetics of montelukast in patients with renal insufficiency has not been assessed. Since montelukast and its metabolites are not excreted by the kidneys, dose adjustment is not required in this category of patients. There are no data on the nature of pharmacokinetics of montelukast in patients with severely impaired liver function (more than 9 points on the Child-Pugh scale). When receiving montelukast in high doses (20 and 60 times higher than the recommended doses for adults), a decrease in theophylline concentration in plasma is observed.When taking montelukast at recommended doses (10 mg 1 time / day), this effect is not observed.
Prevention and long-term treatment of asthma, including: - Prevention of day and night symptoms of the disease in children aged 2 years and older (for chewable 4 mg and 5 mg pills) and in adults and adolescents from 15 years old (for film-coated pills , 10 mg); - treatment of bronchial asthma in children aged 6 years and older (for chewable pills 4 mg and 5 mg) and in adults and adolescents from 15 years old (for film-coated pills, 10 mg) with hypersensitivity to acetylsalicylic acid; - prevention of bronchospasm a, caused by physical exertion, in children aged 2 years and older (for chewable pills 4 mg and 5 mg) and in adults and adolescents from 15 years old (for film-coated pills, 10 mg). Relief of seasonal and year-round symptoms allergic rhinitis in children aged 2 years and older (for chewable pills 4 mg and 5 mg) and in adults and adolescents from 15 years old (for film-coated pills, 10 mg).
- hypersensitivity to the active substance or any auxiliary component of the drug; - children's age up to 2 years (for 4 mg chewable pills); - children up to 6 years old (for 5 mg chewable pills); - children up to 15 years (for pills. 10 mg); - rare hereditary diseases, such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption; - phenylketonuria (for chewable pills), because pills contain aspartame.
During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
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. Decision on the elimination of breastfeeding for the period of use of the drug Almont is made on the basis of an assessment of the estimated benefit to the mother and the potential risk to the baby.
Dosage and administration
The drug is taken orally. Chewable pills are taken 1 hour before or 2 hours after a meal; the pill should be chewed. Film-coated pills are taken orally, regardless of the meal, without chewing, with a sufficient amount of liquid. Adults and adolescents from 15 years old are prescribed 10 mg (1 film-coated tablet) 1 time / day. For bronchial for asthma or bronchial asthma and allergic rhinitis, children aged 2 to 6 years old are prescribed 1 chewable tablet 4 mg 1 time per day in the evening; children aged 6 to 14 years old - 1 chewable tablet 5 mg 1 time / day in the evening. For allergic rhinitis, children aged 2 to 6 years old are prescribed 1 chewable tablet 4 mg 1 time / day, children aged 6 to 14 years - on 1 chewable tablet 5 mg 1 time / day in an individual mode depending on the time of the most acute exacerbation of symptoms. It is not necessary to adjust the dose within these age groups. Children take the drug under adult supervision. The therapeutic effect of the drug Almont allows you to control asthma symptoms , before TIGA within days after administration. The patient is advised to continue taking the drug, both during periods of controlled bronchial asthma, and during the exacerbation of bronchial asthma. Patients with renal insufficiency and patients with mild and moderate hepatic insufficiency do not need a special dose selection. There is no data on the use of montelukast in patients with severely impaired liver function. Elderly patients do not need dose adjustment. Do not require dose adjustment depending on the patient's gender.
Infectious and parasitic diseases: upper respiratory tract infections. On the part of the blood system and lymphatic system: increased tendency to bleeding, thrombocytopenia. On the part of the immune system: hypersensitivity reactions, incl.anaphylaxis, eosinophilic liver infiltration. On the mental side: pathological dreams (including nightmares), hallucinations, insomnia, somnambulism, irritability, anxiety, anxiety, agitation (including aggressive behavior or hostility), tremor, depression, disorientation, suicidal thoughts and behavior suicidality). From the nervous system: headache, dizziness, drowsiness, paresthesia / hypesthesia, convulsions. From the cardiovascular system: feeling of heartbeat. From the respiratory system: n wasp bleeding. From the gastrointestinal tract: diarrhea, dry mouth, dyspepsia, nausea, vomiting, abdominal pain, pancreatitis. From the side of the liver and biliary tract: increased ALT and AST, hepatitis (including cholestatic, hepatocellular and mixed liver damage). On the part of the skin and subcutaneous tissues: angioedema, tendency to hematomas, urticaria, pruritus, rash, erythema nodosum, erythema multiforme. From the musculoskeletal system: arthralgia, myalgia, including muscle cramps. power, swelling, pyrexia, thirst; in very rare cases during treatment with montelukast, the development of Churg-Strauss syndrome has been reported.
Symptoms of drug overdose in patients with chronic bronchial asthma when used at a dose of more than 200 mg / day for 22 weeks and at a dose of 900 mg / day for 1 week have not been identified. There are reports of an acute overdose of montelukast (when taken 1 g / day) in the post-marketing period and in clinical studies in adults and children. Clinical and laboratory data testify to the compliance of the safety profile of the drug in children, adults and elderly patients. The most frequent symptoms were feeling of thirst, drowsiness, vomiting, psychomotor agitation, headache and abdominal pain. Treatment: conducting symptomatic therapy. Data on the possibility of removal of montelukast by peritoneal dialysis or hemodialysis are not available.
Interaction with other drugs
In patients treated with phenobarbital, AUC of Montelukast decreased by approximately 40%, but correction of the dosage regimen in these patients is not required. Since Montelukast is metabolized by a CYP3A4 isoenzyme, caution should be exercised, especially in children, if phenytoin,phenobarbital and rifampicin. Montelukast can be prescribed together 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, prednisone, oral contraceptives (ethinyl estradiol / noretinodrel 35/1), terfenadine, digoxin and warfarin. In vitro studies have shown that montelukast is strong isoenzyme inhibitor of CYP2C8. However, in the study of drug interaction in vivo of montelukast and rosiglitazone (a marker substrate, a representative of drugs that are primarily metabolized by the isoenzyme CYP2C8), no confirmation of the inhibition by montelukast of the isoenzyme CYP2C8 was obtained. Thus, in clinical practice, Montelukast is not supposed to influence CYP2C8-mediated metabolism of a number of drugs, including paclitaxel, rosiglitazone, repaglinida. In vitro studies have shown that montelukast is a substrate of the CYP2C8 isoenzyme, and to a lesser extent the CYP2C9 and CYP3A4 isoenzymes. Data from a clinical study of drug interactions for montelukast and gemfibrozil (an inhibitor of both CYP2C8 and CYP2C9) demonstrate that gemfibrozil increases the effect of the systemic effect of montelukast 4.4 times. The combined use of itraconazole, a strong inhibitor of the CYP3A4 isoenzyme, together with gemfibrozil and montelukast did not lead to an additional increase in the effect of the systemic effect of montelukast. The effect of gemfibrozil on the systemic effect 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 no clinically significant adverse effects were observed in patients taking the drug for about 1 week. Thus, when combined with gemfibrozil, the dose adjustment of Montelukast is not required. According to the results of in vitro studies, no clinically significant drug interactions are expected with other known inhibitors of the CYP2C8 isoenzyme (for example, with trimethoprim).In addition, co-administration of montelukast with itraconazole alone did not lead to a significant increase in the effect of the systemic effect of montelukast. Combined treatment with bronchodilatorsPreparation Almont is a valid supplement to monotherapy with bronchodilators if the latter do not provide adequate control of asthma. Upon reaching the therapeutic effect of Almont treatment, a gradual reduction in the dose of bronchodilators can be started. Combined treatment with inhaled GCS. The treatment with Almont provides an additional therapeutic effect for patients using inhaled GCS. Upon reaching stabilization, you can begin a gradual reduction in the dose of corticosteroids under medical supervision. In some cases, the complete abolition of inhaled GCS is permissible, however, abrupt replacement of inhaled GCS with Almont is not recommended.
Almont is not recommended for treatment of acute attacks of asthma. Patients with bronchial asthma are advised to always carry emergency medications with them. In the event of an acute attack, inhaled short-acting beta2-adrenomimetics should be used. Patients should consult with their physician as soon as possible if they need more inhalations of short-acting beta2-adrenergic mimetics than usual. It is not necessary to sharply replace Almont with inhaled or oral GCS therapy. There is no data proving the possibility of reducing the dose of oral GCS while taking montelukast simultaneously. In rare cases, patients who receive anti-asthma drugs, including montelukast, can develop systemic eosinophilia, which is sometimes accompanied by clinical signs of vasculitis, the so-called Churge-Strauss syndrome, which is eliminated by the reception of systemic corticosteroids. These cases are usually associated with dose reduction or cancellation of therapy with oral corticosteroids. It is impossible to exclude or establish the likelihood that leukotriene receptor antagonists may be associated with the development of Churg-Strauss syndrome. Therefore, physicians should be warned about the possibility of eosinophilia, vascular rash, increased severity of pulmonary symptoms, cardiac complications and / or neuropathy in patients. Patients who have developed the aforementioned symptoms need to undergo a re-examination, and their treatment regimen should be reviewed.Treatment with Almont does not lead to the prevention of the development of bronchospasm in patients with hypersensitivity to acetylsalicylic acid when using acetylsalicylic acid and other NPVS. The Almont preparation in the form of chewable pills 4 mg and 5 mg contains aspartame - a source of phenylalanine. This drug can harm the health of patients with phenylketonuria. Almont contains lactose monohydrate, so patients should not take the drug with rare hereditary diseases such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption. Effect on ability to drive vehicles and control mechanisms As a rule, montelukast does not affect the ability to drive vehicles or work with other mechanisms, but very rarely in some patients Were drowsy and dizzy. With the appearance of these signs, patients are not recommended to drive vehicles and engage in other activities that require concentration of attention and speed of psychomotor reactions.