Montelar tab p / 10 mg of the film 14 pc

Description

Composition
Active substance:
1 tablet comprises montelukast sodium – 10.40 mg (corresponding montelukast – 10.00 mg).
Excipients:
Lactose monohydrate 89.10 mg, giproloza type EF 4,00 mg Microcrystalline cellulose 89.00 mg Croscarmellose sodium 6.00 mg Magnesium stearate 1.50 mg; coating of the tablets: Opadry Beige * 5.00 mg. * Opadry Beige composition: 3.13 mg of hypromellose, 1.52 mg of titanium dioxide, Macrogol 400 0.31 mg, dye iron (III) oxide yellow 0.04 mg, dye iron (III) oxide red 3 micrograms.
Description:
Rectangular shape with rounded sides, biconcave tablets, film-coated beige with marking “10” on one side.
View of the fracture: a homogeneous mass of white.
Product form:
Tablets, film-coated 10mg.
At 7, 10 or 14 tablets were placed in Al / Al blister.
1, 2, 3, 4, 8, 10 or 14 blister packs 7 tablets were placed in a cardboard box, together with instructions for medical use.
1, 2, 3, 4, 5 or 7 blister 10 tablets were placed in a cardboard box, together with instructions for medical use.
1, 2, 3, 4, 5 or 7 blister of 14 tablets were placed in a cardboard box, together with instructions for medical use.
Contraindications
Hypersensitivity to any component of the drug; rare inherited disease, such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption; Children up to age 15 years (for a given dosage form).
Dosage
10 mg
Indications
Prevention and long-term treatment of asthma, including prevention of daytime and nighttime symptoms; treatment of asthma in patients with hypersensitivity to acetylsalicylic acid; Warning bronchoconstriction induced by exercise; relief of symptoms of seasonal and perennial allergic rhinitis.
Interaction with other drugs
Montelukast can be administered together with other drugs conventionally used for the prevention and long term treatment of asthma, such as bronchodilators and inhaled glucocorticosteroids. The recommended therapeutic dose of montelukast no clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinylestradiol / noretinsteron 35/1), terfenadine, and warfarin digoxin. The index value is the area under the curve “concentration-time» (AUC) decreasing in individuals concurrently receiving phenobarbital (approximately 40%), but the correction of Montelukast dosing regimen for such patients is not required. In studies in vitro demonstrated that montelukast is a potent inhibitor of isozyme CYP 2S8 cytochrome P450, but clinical data interaction “drug-drug” comprising montelukast and rosiglitazone (provisional substrate Representative medicines, primarily metabolized isoenzyme CYP 2S8) showed that doses montelukast not inhibit CYP 2S8 isozyme in vivo. Therefore, montelukast has no appreciable effect on the metabolism of medicines metabolized by this enzyme (e.g., paclitaxel, rosiglitazone and repaglinide).
In vitro studies have shown that montelukast is a substrate of CYP 2C8, 2C9 and 3A4. These clinical studies of drug interactions in relation montelukast and gemfibrozil (an inhibitor of both CYP 2C8, and 2C9) demonstrated that gemfibrozil effect increases the systemic exposure of Montelukast 4.4 times. Co-administration of itraconazole, a potent inhibitor of CYP 3A4, with gemfibrozil and montelukast did not lead to an additional increase in the effect of the systemic exposure of montelukast. Effect of gemfibrozil on systemic exposure of Montelukast can not be considered clinically significant on grounds of safety when used at doses higher than the approved dose of 10 mg for adult patients (e.g., 200 mg / day for adult patients for 22 weeks, and up to 900 mg / day for patients taking the drug for approximately one week, no clinically meaningful adverse effects). Therefore, when co-administered with gemfibrozil montelukast dose adjustment is required. By in vitro studies results not expected clinically significant drug interactions with other known inhibitors of CYP 2C8 (e.g., trimethoprim). In addition, co-administration of montelukast with itraconazole alone did not lead to a significant increase in the effect of the systemic exposure of montelukast.
Combined treatment with bronchodilators.
The drug is justified Montelar® addition to bronchodilators alone, if they do not provide adequate control of asthma. Upon reaching therapeutic effect (usually after first dose) of the drug treatment can begin Montelar® gradual reduction in the dose of bronchodilators.
The combined treatment with inhaled corticosteroids.
Treatment with Montelar® provide additional therapeutic benefit to patients applying inhaled glucocorticosteroids. Upon reaching stabilization can start a gradual reduction of the dose of glucocorticosteroid under the supervision of a physician. In some cases a complete abolition of inhaled glucocorticosteroids, but a sharp substitution of inhaled glucocorticosteroids on Montelar® drug is not recommended.
Since montelukast is metabolized by isoenzyme CYP 3A4, caution should be exercised, particularly in children, when montelukast is appointed simultaneously with drugs that induce isoenzyme CYP 3A4, such as phenytoin, phenobarbital and rifampicin.
Overdose
Data on overdose symptoms while taking montelukast patients with asthma in a dose exceeding 200 mg a day for 22 weeks and at a dose of 900 mg a day for 1 week, were found.
There have been reports of acute overdose of montelukast in children (intake of at least 1000 mg per day). Clinical and laboratory data at the same time demonstrate compliance safety profile of montelukast in children safety profile in adults and elderly patients.
The most common symptoms are thirst, drowsiness, vomiting, mydriasis, hyperkinesia, agitation, headache, and abdominal pain.
Treatment: symptomatic therapy.
elimination of the possibility of data montelukast by peritoneal dialysis or hemodialysis is not.
pharmachologic effect
Pharmacological group:
The anti-inflammatory agent antibronhokonstriktornoe – leukotriene receptor blocker.
Pharmacodynamics:
Blocker epithelium Cysteinyl leukotriene receptor airway CysLT1 (leukotrienes C4, D4 and E4 – mediators chronic persistent inflammation, bronchial hyperreactivity support bronchial asthma). Prevents excessive formation of secretions in the bronchi, airway edema, mucous membranes. It reduces the severity of asthma and frequency of asthmatic attacks. Highly effective when taken orally.
Bronchodilator effect develops within 1 day and long preserved.
Pharmacokinetics:
Suction
Montelukast is rapidly and almost completely absorbed after oral administration of the gastrointestinal tract (GIT). Bioavailability tablet 5 mg ingestion of 73%. After receiving tablets chewable 4 and 5 mg of the time to reach maximum concentration (TCmax) – 2 hours.
Distribution and metabolism
Montelukast binds to plasma proteins by more than 99%. The average volume of distribution of montelukast averages 8-11 liters. Montelukast is extensively metabolised in the liver. When using therapeutic doses the concentration of metabolites of montelukast in plasma at steady state in adults and children is not determined. It is assumed that in the metabolism of montelukast involved isozymes of cytochrome P450 (3A4 and 2C9) wherein at therapeutic concentrations montelukast does not inhibit isozymes CYP: 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6.
breeding
Plasma clearance – 45 ml / min. After oral administration of montelukast almost completely excreted via the intestine (about 86%) and less than 0.2% – kidneys. Montelukast half-life (T1 / 2) in young healthy adults ranges from 2.7 to 5.5 hours.
Pharmacokinetics in special cases
The pharmacokinetics of montelukast in women and men has a similar character. No need to adjust the dosage regimen for elderly patients and patients with hepatic mild to moderate impairment. Since montelukast and its metabolites are excreted through the intestines, for patients with renal insufficiency no need to adjust dosages.
Pregnancy and breast-feeding
Montelar® use of the drug during pregnancy and lactation is possible only if the expected benefit to the mother outweighs the potential risk to the fetus or child.
Conditions of supply of pharmacies
On prescription.
side effects
According to clinical studies (analyzed results of treatment of montelukast in the age dosages 5194 children under 15 years of age and 5195 adolescents> 15 years and adults) more frequently compared to placebo, were observed headache, abdominal pain, dry mouth (with a frequency of > 1/100 to
According to the World Health Organization (WHO), undesirable effects are classified according to their rate of development as follows: very common (> 1/10), common (by> 1/100 to
special instructions
It is recommended to continue taking montelukast and after achieving significant improvements. Montelukast is not recommended for the treatment of acute asthma attacks. In acute bronchial asthma patients should use emergency medication cupping (inhaled beta2-adrenoceptor agonists short-acting).
In patients receiving anti-asthma agents including leukotriene receptor antagonists, in rare cases can develop systemic eosinophilic vasculitis, which manifests itself in the form of eosinophilia, vascular rash, increased severity of pulmonary symptoms, cardiac complications and / or neuropathy. This syndrome (sometimes diagnosed as Churg-Strauss syndrome) is more common in the abolition or reduction of corticosteroids. Although the causation of these undesirable phenomena therapy with antagonists of leukotriene receptors has not been ascertained, while reducing systemic dose corticosteroids in patients taking montelukast, care should be taken to conduct an appropriate clinical observation.
Age differences efficacy and safety profile of montelukast is not revealed.
Dose corticosteroids used together with montelukast, should be reduced gradually under medical supervision. We do not recommend sharp replacement therapy with inhaled or oral corticosteroids use of montelukast. Patients with confirmed allergy to aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs) that the period of treatment montelukast avoid contact with these drugs as montelukast, improving pulmonary function in patients with allergic bronchial asthma, however, does not prevent the bronchoconstriction due to the action of NSAIDs .
By reducing the systemic dose corticosteroids in patients taking montelukast, care should be taken to conduct an appropriate clinical observation.
Patients with PKU have to be informed that a 1 to 4 mg chewing tablet contains at least 0.96 mg of aspartame, and 1 tablet of 5 mg chewing – not less than 1.20 mg of aspartame.
Chewable tablets contain red dye amazing (Allura red), which can cause allergic reactions.
There is no evidence that receiving montelukast affect the ability to drive a car or moving machinery, is not revealed. However, reports of drowsiness and dizziness, so the appearance of these symptoms is not recommended in patients as the management of vehicles, as well as engaging in other activities that require concentration and speed of psychomotor reactions.
Storage conditions
Keep protected from light and moisture at a temperature not higher than 30 C. Keep out of reach of children.
Dosing and Administration
The drug is taken orally Montelar® 1 time / day regardless of the meal before bedtime.
For the treatment of bronchial asthma, allergic rhinitis, relief of symptoms in children from 15 years and adults: 1 tablet of 10 mg once a day, at bedtime.
The therapeutic effect of montelukast on indicators reflecting for asthma, developed for the first day. The patient should continue taking montelukast in period to achieve control of asthma symptoms, and in the period of exacerbation.
For the prevention of children 15 years and adults suffering bronchospasm induced by exercise: 1 tablet of 10 mg once a day at bedtime for 2-4 weeks in the absence of a satisfactory effect it is necessary to assign additional or alternative therapy.
For older patients, patients with renal failure, patients with mild or moderate hepatic impairment, and also depending on the sex specific dose adjustment is required.
Montelukast is not recommended as a monotherapy in patients with bronchial asthma severity average DC current.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist