Expiration date: 08/2025
Dosage form
Round biconvex tablets, film-coated yellow color. In cross section, the kernel white, or almost white
Composition
One tablet, film-coated, contains:
active substance: montelukast sodium 10.4 mg (in terms of montelukast -10 mg);
excipients: lactose monohydrate -115 mg; microcrystalline cellulose - 65 mg; croscarmellose sodium 8 mg; magnesium stearate -1.6 mg;
film cover: [polymer - 3 mg. of hyprolose (hydroxypropyl cellulose) -1.164 mg, talc - 1,1556 mg, titanium dioxide - 0,6522 mg, iron oxide yellow (iron oxide) - 0.0282 mg] or [dry mix for film coating containing hypromellose (50%), hyprolose (hydroxypropyl cellulose) (19,4%), talc (of 19.26%), titanium dioxide (with 10.87 %), iron oxide yellow (iron oxide) (0,47 %)] - 6,0000 mg
Pharmacological action
Cysteinyl-leukotrienes (LTC4, LTD4, LTE4) are strong inflammatory mediators - eicosanoids, which are allocated to different cells, including mast cells and eosinophils. These important mediators prostrations contact cysteinyl leukotriene receptors. Cysteinyl leukotriene receptor type 1 (CysLTi-receptors) are present in the respiratory tract of a person (including, in the cells of bronchial smooth muscle, macrophages) and other cells prosopalgia (including eosinophils and certain myeloid stem cells). Cysteinyl-leukotrienes correlated with the pathophysiology of asthma and allergic rhinitis. Asthma leukotriene-mediated effects include bronchoconstriction, increased mucus secretion, increased vascular permeability and an increased number of eosinophils. In allergic rhinitis after exposure to the allergen is the release of cysteinyl-leukotrienes from inflammatory cells of the mucosa of the nasal cavity during early and late phases of the allergic reaction that is manifested by symptoms of allergic rhinitis. When intranasal sample with cysteinyl-leukotriene demonstrated the increased resistance of Airways and symptoms of nasal obstruction.
Montelukast is a highly active when administered a drug that significantly improves parameters of inflammation in bronchial asthma. According to biochemical and pharmacological analysis of drug with high selectivity and chemical affinity binds to CysLT]-receptors (instead of other pharmacologically important airway receptors, such as prostaglandin, or cholinergic, P-adrenergic receptors). Montelukast inhibits physiological action tsistinovyh leukotrienes LTC4, LTD4, LTE4 by binding to CysLTi-receptors without exerting a stimulatory effect on these receptors.
Montelukast inhibits CysLT-receptors of the airway epithelium, thereby simultaneously possessing the ability to inhibit bronchoconstriction due to inhalation cysteinyl-of leukotriene LTD4 in patients with bronchial asthma. Montelukast dose is 5 mg, sufficient for relief of bronchoconstriction induced by LTD4.
Montelukast causes bronchodilatation within two hours after ingestion and can add to the broncho dilation caused by (ZG-agonists.
The use of montelukast in doses greater than 10 mg per day taken as a single dose, efficacy does not increase.
Elderly patients
After a single ingestion of 10 mg of montelukast pharmacokinetic profile and bioavailability are similar in elderly patients and young patients. The half-life of montelukast from blood plasma, several more elderly patients. Dose adjustment 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 liver failure mild and moderate severity and clinical manifestations of cirrhosis of the liver marked by the slow metabolism of montelukast, accompanied by an increase in the area under the curve "concentration - time" (AUC) of approximately 41% after a single dose of the drug at a dose of 10 mg. the half-life of montelukast in these patients is somewhat longer (average half-life of 7.4 hours). Dosage of montelukast for patients with liver failure mild and moderate severity is not required. Data on the nature of the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (more 9 points on a scale child-Pugh) no. Renal failure
Because montelukast and its metabolites are excreted through the kidneys, the pharmacokinetics of montelukast in patients with renal insufficiency has not been assessed. Adjustment of the dose for this group of patients is not required.
Side effects
Side effects are generally mild and usually does not require discontinuation of the drug.
From the nervous system: headache, dizziness, drowsiness,
paresthesia/hypoesthesia, seizures.
From the side of cardiovascular system: heart palpitations.
The respiratory system, chest and mediastinum disorders: epistaxis, pulmonary eosinophilia.
Disorders psychiatric disorders: agitation including aggressive behavior or hostility, anxiety, depression, disorientation, impaired attention, abnormal dreams, hallucinations, insomnia, memory impairment, psychomotor activity (including irritability, anxiety and tremor), somnambulism, suicidal thinking and behavior (suicidality).
From gastrointestinal tract: diarrhea, dyspepsia, nausea, vomiting, pancreatitis, abdominal pain.
Violations of the liver and biliary tract: increased activity of alanine aminotransferase (ALT) and aspartate aminotransferase (ACT), hepatitis (including cholestatic, hepatocellular and mixed liver injury).
From the side of musculoskeletal system: arthralgia, myalgia, muscle cramps.
The blood and lymphatic system: increased tendency to bleeding, thrombocytopenia.
The skin and subcutaneous tissues: a tendency to form hematomas, erythema nodosum, erythema multiforme, pruritus, rash, urticaria, angioedema. The immune system: hypersensitivity reactions, including anaphylaxis, eosinophilic infiltration of the liver.
Infectious and parasitic diseases: infections of the upper respiratory tract. Other: asthenia (weakness)/fatigue, edema, pyrexia.
Special conditions
The efficacy of montelukast for oral administration in the treatment of acute attacks of bronchial asthma is not established. Therefore, the drug is Montelukast tablets are not recommended for the treatment of acute asthma attacks. Patients should be instructed to always carry emergency medications for relief of asthma attacks (inhaled (P-agonist short action).
You should not stop taking the drug Montelukast in acute asthma. Be aware of the need for the use of drugs emergency cupping (agonists inhaled short-acting).
Patients with demonstrated Allergy to acetylsalicylic acid and other nonsteroidal anti-inflammatory drugs (NSAIDs) should not take these drugs during treatment with the drug Montelukast, as montelukast, improving respiratory function in patients with allergic asthma, however, cannot completely prevent them caused by non-steroidal anti-inflammatory drug bronchoconstriction.
Dose of glucocorticoids for inhalation or ingestion, taken to the treatment with montelukast, can be gradually reduced under medical supervision. However, the abrupt replacement of corticosteroids drug Montelukast possible.
In patients who received montelukast, was described neuropsychiatric disorders (see section "Side effects"). Given that these symptoms could be caused by other factors, it is unknown whether they are associated with receiving montelukast. The doctor should discuss the undesirable with patients and/or their parents/guardians. Patients and/or their parents/guardians need to explain that in the event of such symptoms should inform your doctor.
In rare cases, patients receiving asthma medications, including leukotriene receptor antagonists, have experienced one or more adverse events of the following: eosinophilia, rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy sometimes diagnosed as the syndrome Charge-Strauss, a systemic eosinophilic vasculitis. These cases sometimes have been associated with a reduction in dose or termination of therapy with corticosteroids for oral administration. Although a causal relationship of these adverse events with treatment with leukotriene receptor antagonists has not been established, in patients taking montelukast, be careful and conduct a proper clinical observation.
The drug Montelukast chewable tablets 5 mg contains aspartame a source of phenylalanine. Patients with phenylketonuria should be aware that each chewable tablet contains aspartame in the amount equivalent 0,842 mg of phenylalanine, and the preparation of Montelukast chewable tablets 5 mg should not be taken by patients with phenylketonuria.
Effects on ability to drive vehicles and mechanisms
Evidence suggesting that intake of montelukast affects the ability to drive a car or moving machinery, is not revealed. However, in applying the drug may experience side effects such as dizziness and drowsiness. Therefore, use caution when driving and performing actions that require speed of psychomotor reactions.
Method of application
The drug Montelukast is taken orally 1 time a day with or without food. The tablet can be swallowed whole or chewed before swallowing. For the treatment of asthma the drug should be taken in the evening. In the treatment of allergic rhinitis, the drug can be taken any time of the day. Patients with bronchial asthma and allergic rhinitis should take one tablet once a day in the evening. Children aged 6 to 14 years, One chewable tablet 5 mg once a day. Dose selection for this age group is not required. Children above 15 years adults Dose for adults and children over 15 years of age is 10 mg of montelukast per day. Therapeutic effect of Montelukast drug on the indicators of the bronchial asthma, develops during the first day. The patient should continue to take the drug between achieving control of symptoms of asthma, and in the period of exacerbation. For elderly patients, patients with renal insufficiency, patients with mild or moderate impaired hepatic function a special dose adjustment is not required. Montelukast can be added to treatment with bronchodilators and inhaled glucocorticosteroids (GCS).
Testimony
prophylaxis and chronic treatment of asthma including prevention of daytime and nighttime symptoms;
treatment of asthma in patients with hypersensitivity to acetylsalicylic acid;
prevention of bronchospasm caused by physical load;
relief of daytime and nighttime symptoms of seasonal allergic rhinitis and persistent allergic rhinitis.
Contraindications
hypersensitivity to any component of the drug;
children up to age 6 years;
phenylketonuria.
Use during pregnancy and breastfeeding
Clinical studies of montelukast in pregnant women have not been conducted. The drug Montelukast should be used during pregnancy and lactation only if expected benefit for mother exceeds potential risk for fetus or child. During post-approval use of montelukast reported on the development of congenital limb defects in newborns whose mothers took montelukast during pregnancy. Most of these women also took other drugs for the treatment of asthma during pregnancy. A causal relationship between the use of montelukast and the development of congenital limb defects is not established.
Unknown, selects whether montelukast breast milk. Because many drugs are excreted in breast milk, you should consider it when prescribing the drug Montelukast lactating women.
Drug interactions
Montelukast can be administered together with other drugs that are typically used for the prevention and long-term treatment of asthma and/or treatment of allergic rhinitis. The recommended therapeutic dose montelukast had no 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 of montelukast reduced with concomitant administration of phenobarbital by about 40 %, but it does not require modification of the dosage regimen of the drug Montelukast.
In vitro studies established that montelukast inhibits the isoenzyme CYP 2C8 of cytochrome P450, however, in the study of drug interaction in vivo montelukast and rosiglitazona (metabolized with the participation of isoenzyme CYP 2C8 cytochrome) we have not received confirmation of inhibition of the isoenzyme CYP montelukast 2C8. Therefore, in clinical practice is not expected to impact on 2C8 montelukast CYP-mediated metabolism of several drugs, including paclitaxel, rosiglitazona, Repaglinide etc.
In vitro studies have shown that montelukast is a substrate of CYP isozymes 2C8, 2C9 and ZA4. Data from clinical studies of drug interactions in relation to montelukast and gemfibrozil (an inhibitor of CYP as 2C8 and 2C9) demonstrated that gemfibrozil increases the effect of systemic exposure of montelukast by 4.4 times. The co-administration of Itraconazole, a strong inhibitor of CYP isoenzyme ZA4, together with gemfibrozil and montelukast did not lead to further increase of the effect of systemic exposure of montelukast. The effect of gemfibrozil on the systemic exposure to montelukast can not be considered clinically significant based on safety data used in doses higher than approved dose of 10 mg for adult patients (for example, 200 mg/day to adult patients for 22 weeks and up to 900 mg/day for patients receiving the drug for approximately one week, there were no clinically significant adverse effects). Thus, when co-administered with gemfibrozil, the dose adjustment of montelukast is required. According to the results of in vitro studies is not expected clinically significant drug interactions with other known inhibitors of the isoenzyme CYP 2C8 (e.g. trimethoprim). In addition, the co-administration of montelukast with Itraconazole alone did not lead to a significant increase in the effect of systemic exposure of montelukast. Combined treatment with bronchodilators.
Montelukast is reasonable complement to monotherapy with bronchodilators, if the latter do not provide adequate control of asthma. Upon reaching the therapeutic effect of the therapy montelukast to begin a gradual reduction in the dose of bronchodilators.
Combined treatment with inhaled corticosteroids, Treatment with montelukast provides additional therapeutic effect in patients using inhaled glucocorticosteroids. Upon reaching stabilization of the patient's condition, you can start gradual reduction of the dose of the glucocorticosteroid under the supervision of a physician. In some cases, permissible total abolition of inhaled corticosteroids, but the abrupt replacement of inhaled corticosteroids on montelukast is not recommended.
