Montelar - instructions for use, doses, side effects, contraindications

Composition:For 1 tablet:
core tablet: active substance: montelukast sodium - 10,40 mg (corresponds to montelukastu - 10,00 mg); auxiliary substances: lactose monohydrate 89.10 mg, giprolose, type EF 4.00 mg, microcrystalline cellulose, 89.00 mg, croscarmellose sodium 6.00 mg,
magnesium stearate 1.50 mg; Sheath tablet: beige ointment * 5,00 mg.
* The composition of a decadent beige: hypromellose 3.13 mg, titanium dioxide 1.52 mg, macrogol-400 0.31 mg, iron (III) oxide, yellow 0.04 mg, iron (III) oxide red 3 μg.

Description:Rectangular shape with rounded, sides, biconvex tablets covered with a beige film cover, p. marking "10" on one side.
View of the fracture: a homogeneous mass of white color.

Pharmacotherapeutic group:Anti-inflammatory anti-bronchoconstrictive means - leukotriene receptor blocker.

ATX: & nbsp

R.03.D.C.03 Montelukast

Pharmacodynamics:The blocker of cysteinyl leukotriene receptors of the respiratory tract epithelium CysLTl (leukotrienes C4, D4 and E4 - mediators of chronic persistent inflammation, supporting bronchial hyperreactivity in bronchial asthma). Prevents excessive formation of secretions in the bronchi, swelling of the mucous membrane of the respiratory tract. Reduces the severity of the course of bronchial asthma and the frequency of asthmatic attacks. Highly effective at ingestion.
Bronchodilator effect develops within 1 day and persists for a long time.

Pharmacokinetics:Suction
Montelukast quickly and almost completely absorbed after ingestion from the gastrointestinal tract (GIT). Bioavailability for tablets 5 mg when taken orally is 73%. After taking chewable tablets 4 and 5 mg, the time to reach the maximum concentration (TCmax) -2 hours.
Distribution and Metabolism
Montelukast binds to plasma proteins more than 99%. The average volume distribution of Montelukast averages 8-11 liters.
Montelukast is actively metabolized in the liver. When using therapeutic doses, the concentration of metabolites of montelukast in plasma in equilibrium in adults and children is not determined.It is assumed that the isoenzymes of cytochrome P450 (ZA4 and 2C9) are involved in the metabolism of montelukast, while in therapeutic concentrations montelukast does not inhibit CYP isoenzymes: 3 A4, 2C9, 1A2, 2A6, 2C19 and 2D6.
Excretion
Plasma clearance - 45 ml / min. After oral administration montelukast almost completely eliminated through the intestine (about 86%) and less than 0.2% - by the kidneys.
The half-life of montelukast (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.
There is no need to adjust the dosage regimen for elderly patients and for patients with mild to moderate hepatic impairment.
Because the montelukast and its metabolites are excreted from the body through the intestine, for patients with renal insufficiency there is no need for dose adjustment.

Indications:Prophylaxis and long-term treatment of bronchial asthma, including:
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;
-Ease of symptoms of seasonal and all-year-round allergic rhinitis.

Contraindications:- Hypersensitivity to any of the components of the drug;
- rare hereditary diseases, such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption.
- Children under 15 years of age (for this dosage form).

Pregnancy and lactation:The use of the drug Montelar® during pregnancy and lactation is possible only if the intended benefit to the mother exceeds the potential risk to the fetus or child.

Dosing and Administration:The drug Montelar® is taken orally 1 time / day, regardless of food intake, before bedtime.
For the treatment of bronchial asthma, alleviating the symptoms of allergic rhinitis in children aged 15 and adults: 1 tablet 10 mg once a day, before bedtime.
The therapeutic effect of montelukast on the indicators reflecting the course of bronchial asthma develops during the first day. The patient should continue to take montelukast as in the period of achieving control of symptoms of bronchial asthma,and during the exacerbation of the disease.
For prophylaxis in children aged 15 and adults suffering from bronchospasm caused by physical exertion: 1 tablet 10 mg once a day, before going to bed for 2-4 weeks, in the absence of a satisfactory effect, additional or alternative therapy should be prescribed.
For elderly patients, patients with renal insufficiency, patients with mild or moderate liver function disorders, and also, depending on gender, a special dose selection is not required. Montelukast It is not recommended as a monotherapy for patients with bronchial asthma of moderate severity of constant flow.

Side effects:According to clinical studies (the results of treatment with montelukast at age doses of 5194 children under 15 and 5195 teenagers ≥15 years and adults), headache, abdominal pain, dry mouth (at a frequency of ≥1 / 100 to <1/10).
According to the World Health Organization (WHO), unwanted effects are classified according to their frequency of development as follows: very often (≥1/10), often (from ≥1 / 100 to <1/10),infrequently (from ≥1 / 1,000 to <1/100), rarely (from ≥1 / 10,000 to <1 / 1,000), very rarely (<1 / 10,000); frequency is unknown - according to available data, it was not possible to establish the frequency of occurrence.
Infectious and parasitic diseases:
very often: infections of the upper respiratory tract.
From the immune system:
infrequently: hypersensitivity reactions, including anaphylaxis;
rarely: angioedema;
very rarely: eosinophilic liver infiltration.
From the skin and subcutaneous tissue:
often: rash;
infrequent: tendency to form hematomas, hives, itching;
very rarely: erythema nodosum, erythema multiforme.
From the central nervous system:
infrequently: headache, dizziness, drowsiness, paresthesia / hypoesthesia, convulsions.
Mental disorders:
infrequent sleep disorders (including nightmares), insomnia, somnambulism, irritability, anxiety, agitation (including aggressive behavior or hostility), psychomotor hyperactivity (including irritability, anxiety and tremor), depression;
rarely: violation of attention, memory impairment;
very rarely: hallucinations, disorientation, suicidal thoughts and suicidal behavior.
From the cardiovascular system:
rare: heartbeat.
From the side of the blood and lymphatic system:
rarely: increased tendency to bleeding.
From the gastrointestinal tract (GIT):
often: abdominal pain, diarrhea, nausea, vomiting, pancreatitis;
infrequently: indigestion, dryness of the oral mucosa.
From the liver and bile ducts:
often: increased activity of "hepatic" transaminases (alanine aminotransferase (ALT), aspartate aminotransferase, (ACT));
very rarely: hepatitis (including cholestatic, hepatocellular and mixed liver damage).
From the side of the musculoskeletal and connective tissue:
infrequently: arthralgia, myalgia (including muscle cramps).
From the respiratory system:
infrequently: nosebleeds;
very rarely: the Charge-Strauss syndrome, pulmonary eosinophilia.
Other:
often: hyperthermia;
infrequently: asthenia / fatigue, malaise, swelling.

Overdose:Data on the symptoms of an overdose when taking montelukast by 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 1 week have not been revealed. There are reports of acute overdose of montelukast in children (taking at least 1000 mg per day).Clinical and laboratory data indicate that the safety profile of Montelukast in children is consistent with the safety profile in adults and elderly patients.
The most common symptoms were thirst, drowsiness, vomiting, mydriasis, hyperkinesis, psychomotor agitation; headache and pain in the abdomen.
Treatment: symptomatic therapy.
There is no data on the possibility of removing montelukast by peritoneal dialysis or hemodialysis.

Interaction: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 glucocorticosteroids. The recommended therapeutic dose of montelukast had no clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol / norethiston 35/1), terfenadine, digoxin and warfarin. The value of the area under the concentration-time curve (AUC) decreases in persons who simultaneously receive phenobarbital (approximately 40%), however, correction of the dosage regimen of montelukast to such patients is not required.
In vitro studies have shown that montelukast is a potential inhibitor of the CYP 2C8 isoenzyme of the cytochrome P450 system, however, clinical trials of drug-drug interactions, including montelukast and rosiglitazone (a preliminary substrate of a representative of medicinal preparations primarily metabolized by the CYP 2C8 isoenzyme) showed that the doses of montelukast did not inhibit the CYP 2C8 isoenzyme in vivo. Consequently, montelukast does not have a significant effect on the metabolism of medical drugs metabolized by this enzyme (for example, paclitaxel, rosiglitazone and repaglinide). In vitro studies have shown that montelukast is a substrate of CYP 2C8, 2C9 and 3A4. Data from the clinical study of the drug interaction with respect to montelukast and gemfibrozil (an inhibitor of both SUR 2S8 and 2C9) demonstrate that gemfibrozil increases the effect of systemic exposure to montelukast 4.4 times. The simultaneous administration of intraconazole, a strong CYP inhibitor of 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 patients taking the drug for about one week did not have clinically significant adverse effects). Thus, with co-administration with gemfibrozilom adjustment dose montelukast is not required. According to the results of in vitro studies, clinically significant drug interactions with other known inhibitors of CYP 2C8 (for example, with trimethoprim) are not expected. In addition, the simultaneous administration of montelukast with single-dose intraconazole did not result in a significant increase in the effect of systemic exposure to montelukast.
Combined treatment with bronchodilator.
The drug Montelar® is a justified addition to monotherapy with bronchodilators if the latter do not provide adequate control of bronchial asthma. Upon reaching a therapeutic effect (usually after the first dose) from treatment with Montelar® it is possible to begin a gradual decrease in the dose of bronchodilators.
Combined treatment with inhaled glucocorticosteroids.
Treatment with Montelar® provides an additional therapeutic effect to patients using inhaled glucocorticosteroids. Once the stabilization of the condition is achieved, a gradual decrease in the dose of the glucocorticosteroid can be started under the supervision of the physician. In some cases, complete cancellation of inhaled glucocorticosteroids is permissible, but a sharp replacement of inhaled glucocorticosteroids by the Montelar preparation® Not recommended. Because the montelukast is metabolized by the CYP isoenzyme ZA4, caution should be used, especially in children, if montelukast concomitantly administered with drugs inducing the CYP isoenzyme ZA4, such as phenytoin, phenobarbideadzrifampin.

Special instructions:It is recommended to continue receiving montelukast and after achieving a significant improvement. Montelukast It is not recommended to use for treatment of acute attacks of bronchial asthma. In the acute course of bronchial asthma, patients should use emergency drugs to stop seizures (short-acting inhaled beta2-adrenomimetics).
In rare cases, systemic eosinophilic vasculitis, manifested as eosinophilia, vascular rash, exacerbation of pulmonary symptoms, cardiac complications and / or neuropathy, may develop in patients receiving antiasthmatics, including leukotriene receptor antagonists. This syndrome (sometimes diagnosed as a Charge-Strauss syndrome) is more common when the SCS is abolished or decreased. Although the causal relationship of these adverse events with therapy of leukotriene receptor antagonists has not been established, with a reduction in the systemic dose of GCS in patients taking montelukast, care must be taken and clinical monitoring performed.
The dose of GCS used together with montelukast should be reduced gradually, under the supervision of a doctor. It is not recommended to sharply replace therapy with inhaled or oral GCS with montelukast. Patients with a confirmed allergy to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (NSAIDs) should avoid contact with these preparations for the period of treatment with montelukast, since montelukast, improving respiratory function in patients with allergic bronchial asthma, nevertheless, does not prevent bronchoconstriction due to the action of NSAIDs.
With a decrease in the systemic dose of GCS in patients taking montelukast, care must be taken and clinical monitoring performed.
Age differences in the profile of efficacy and safety of montelukast were not identified.
Patients with phenylketonuria should be informed that in 1 chewable tablet 4 mg contains not less than 0.96 mg aspartame, and in 1 tablet chewing 5 mg - not less than 1.20 mg aspartame.
Chewable tablets contain red dye (Allura red), which can cause allergic reactions.

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, it has been reported drowsiness and dizziness, so when these signs appear, patients are not recommended as driving vehicles, or engaging in other activities requiring concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets, film-coated 10 mg.

Packaging:For 7, 10 or 14 tablets are placed in A1 / A1 blister.
1, 2, 3, 4, 8, 10 or 14 blisters of 7 tablets are placed in a cardboard box together with instructions for medical use.
For 1, 2, 3, 4, 5 or 7 blisters of 10 tablets are placed in a cardboard box together with instructions for medical use.
For 1,2, 3, 4, 5 or 7 blisters of 14 tablets are placed in a cardboard box together with instructions for medical use.

Storage conditions:In a place protected from light and moisture at a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:2 years.
Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001546

Date of registration:29.02.2012 / 01.03.2013

Expiration Date:28.02.2017

The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia

Manufacturer: & nbsp

SANDOZ ILAC SANAYI VE TICARET, A.S. Turkey

Representation: & nbspSANDOZ SANDOZ Switzerland

Information update date: & nbsp2016-08-20

Illustrated instructions

Instructions

Montelar (Montelar)