Montelair, Chewable tablets 4mg, 14pcs

Composition

Active ingredient:

montelukast sodium 4 mg;

Auxiliary substances:  

mannitol — 155.92/194.9 mg;

MKC — 52,8/66 mg;

croscarmellose sodium — 12/15 mg;

of hyprolose type EXF — 7,2/9 mg;

flavor cherry* — 1,92/2,4 mg;

aspartame — 0,96/1.2 mg;

cherry flavoring — 0,48/0.6 mg;

dye iron (III) oxide red — 0,36/0.45 mg;

magnesium stearate — 4,2/5,25 mg

Pharmacological action

Montelair is a bronchodilator.

Pharmacodynamics

Blocker of cysteinyl leukotriene receptors of the airway epithelium CysLT1 (LT C4, D4 and E4 are mediators of chronic persistent inflammation that supports bronchial hyperreactivity in bronchial asthma). Prevents excessive secretion in the bronchi, swelling of the mucous membrane of the respiratory tract. Reduces the severity of bronchial asthma and the frequency of asthmatic attacks. Highly effective when taken orally.

The bronchodilator effect develops within 1 day and persists for a long time.

Pharmacokinetics

Suction. Montelukast is rapidly and almost completely absorbed after ingestion of the gastrointestinal tract. Bioavailability for 5 mg tablets when taken orally is 73%; for film-coated tablets,10 mg-64%. After taking chewable tablets 4 and 5 mgT_max — 2 hours, for film — coated tablets,10 mg-3 hours.

Distribution and metabolism. Montelukast binds to plasma proteins by more than 99%. The average V_d of montelukast averages 8-11 liters.

Montelukast is actively metabolized in the liver. When using therapeutic doses, the concentration of montelukast metabolites in the blood plasma at steady state in adults and children is not determined.

It is assumed that cytochrome P 450 isoenzymes (3A4 and 2C9) are involved in the metabolism of montelukast, while at therapeutic concentrations montelukast does not inhibit the CYP isoenzymes: 3A4,2C9,1A2,2A6,2C19 and 2D6.

Output. Plasma clearance — 45 ml/min. After oral use, montelukast is almost completely excreted through the intestine (about 86%) and less than 0.2% — by the kidneys.

T_1/2 of montelukast in young healthy adults is from 2.7 to 5.5 h

. Pharmacokinetics in special cases

, the pharmacokinetics of montelukast in women and men are similar.

There is no need to adjust the dosage regimen for elderly patients and patients with mild to moderate hepatic insufficiency.

Since montelukast and its metabolites are eliminated from the body through the intestines, there is no need to adjust the dose for patients with renal insufficiency.

Indications

• Prophylaxis and chronic treatment of asthma, including the prevention of daytime and nighttime symptoms (for children from 2 years and adults);
• the treatment of asthma in patients with hypersensitivity to acetylsalicylic acid (for children from 6 years and older and adults);
• the prevention of bronchospasm caused by exercise (for children from 2 years and adults);
• relief of symptoms of seasonal and perennial allergic rhinitis in children aged 2 years and adults.

Use during pregnancy and lactation

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

Contraindications

• Hypersensitivity to any of the components of the drug;
• children under 2 years of age (for a dosage of 4 mg) and up to 6 years (for a dosage of 5 mg);
• phenylketonuria.

Side effects

From the central nervous system:  often — headache.

From the gastrointestinal tract:  often-abdominal pain.

Post-marketing observations

Infectious and parasitic diseases:  very often — upper respiratory tract infections.

From the side of hemostasis:  increased tendency to bleed, including nosebleeds, bruising.

From the immune system:  infrequently-hypersensitivity reactions, including anaphylaxis; rarely-angioedema; very rarely – eosinophilic liver infiltration.

Skin and subcutaneous tissue disorders:  often-rash; infrequently – tendency to form hematomas, urticaria, pruritus; very rarely-erythema nodosum, erythema multiforme.

From the central nervous system:  infrequently — headache, dizziness, drowsiness, paresthesia/hypesthesia, convulsions, hyperkinesia.

Mental disorders:  infrequently — sleep disturbances (including nightmares), somnambulism, insomnia, irritability, restlessness, agitation (including aggressive behavior or hostility), depression; rarely — tremor; very rarely — hallucinations, disorientation, suicidal thoughts and behavior.

From the CCC side:  rarely-palpitation of the heart.

Blood and lymphatic system disorders:  rarely — increased tendency to bleeding.

From the gastrointestinal tract:  often — abdominal pain, diarrhea, nausea, vomiting, pancreatitis; infrequently — dry mouth, dyspepsia.

Liver and biliary tract disorders:  often-increased activity of hepatic transaminases (ALT, ACT); very rarely — cholestatic hepatitis, damage to hepatocytes, most often against the background of concomitant drug therapy or existing liver pathology (various forms of hepatitis).

Musculoskeletal and connective tissue disorders:  infrequently-arthralgia, myalgia, including muscle spasms.

Respiratory system disorders:  infrequently-nosebleeds; very rarely-Charga-Strauss syndrome.

From the side of the senses:  otitis media (including moderate).

Other services:  infrequently-asthenia/fatigue, malaise, edema, hyperthermia, thirst, flu-like syndrome, pyrexia.

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 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 value of the AUC indicator decreases in individuals receiving phenobarbital at the same time (by approximately 40%), but such patients do not need to adjust the dosage regimen of montelukast.

In vitro studies showed that montelukast is a potential inhibitor of the isoenzyme CYP2 8 of cytochrome P-450, but data from clinical studies of interaction “drug — drug” involving montelukast and rosiglitazon (preliminary substrate representative of medicinal drugs primarily metabolized by the isoenzyme CYP2 8) showed that doses of montelukast do not inhibit the isoenzyme CYP2 8 in vivo.

Consequently, montelukast does not significantly affect the metabolism of medicinal products that are metabolized by this enzyme (for example, paclitaxel, rosiglitazone and repaglinide).

In vitro studies have shown that montelukast is a substrate of CYP2C8, CYP2C9 and CYP3A4. Data from a clinical drug interaction study with montelukast and gemfibrozil (an inhibitor of both CYP2C8 and CYP2C9) show that gemfibrozil increases the effect of systemic exposure to montelukast by 4.4 times.

Concomitant use of intraconazole, a strong CYP3A4 inhibitor, 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 effects of montelukast cannot be considered clinically significant based on safety data when used at 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 patients taking the drug for about one week, no clinically significant adverse effects were observed).

Thus, when co-administered with gemfibrozil, no dose adjustment of montelukast is required.

According to the results of in vitro studies, no clinically significant drug interactions are expected with other known CYP2C8 inhibitors (for example, trimethoprim). In addition, co-use of montelukast with intraconazole alone did not significantly increase the effect of systemic exposure to montelukast.

Combined treatment with bronchodilators

Montelair® is a reasonable adjunct to monotherapy with bronchodilators, if the latter do not provide adequate control of bronchial asthma. When the therapeutic effect is achieved (usually after the first dose) from treatment with Montelair®, you can start gradually reducing the dose of bronchodilators.

Combined treatment with inhaled corticosteroids

Treatment with Montelair ® provides an additional therapeutic effect for patients using inhaled corticosteroids. When the condition is stabilized, you can start gradually reducing the dose of corticosteroids under the supervision of a doctor.In some cases, complete withdrawal of inhaled corticosteroids is acceptable, but abrupt replacement of inhaled corticosteroids with Montelair® 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.

How to take, course of use and dosage

Inside,1 time a day, before going to bed.

If the drug is taken in combination with food, montelukast should be taken 1 hour before or 2 hours after a meal.

The drug is prescribed to children under adult supervision.

For children from 2 to 5 years — one chewable tablet at a dose of 4 mg once a day, before bedtime (the use of 4 mg montelukast chewable tablets is not recommended under the age of 2 years); from 6 to 14 years-one chewable tablet at a dose of 5 mg once a day, before bedtime (the use of 5 mg Montelair chewable tablets is not recommended under the age of 6 years). The therapeutic effect of montelukast develops during the 1st day of taking the drug. The patient should continue to take montelukast both during the period of achieving control of symptoms of bronchial asthma, and during periods of exacerbation of bronchial asthma.

For prevention in children suffering from exercise-induced bronchospasm: from 2 to 5 years — 1 chewable tablet at a dose of 4 mg once a day, before going to bed for 2-4 weeks; from 6 to 14 years — 1 chewable tablet at a dose of 5 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 the treatment of patients older than 15 years and adults, it is recommended to use other dosage forms of montelukast (for example, film-coated tablets,10 mg).

For patients with renal insufficiency, mild or moderate hepatic impairment, as well as depending on gender, special dose selection is not required.

Overdose

Symptoms: the most common symptoms are thirst, drowsiness, vomiting, mydriasis, hyperkinesis, psychomotor agitation, headache and abdominal pain.

Treatment: conducting symptomatic therapy. There are no data on the possibility of removing montelukast by peritoneal dialysis or hemodialysis.

Special instructions

It is recommended to continue taking montelukast after achieving a significant improvement. Montelukast is not recommended for the treatment of acute asthma attacks. In the acute course of bronchial asthma, patients should use emergency medications to stop seizures (short-acting inhaled beta_-2-adrenomimetics).

Reducing the systemic dose of corticosteroids in patients receiving anti-asthmatic agents, including leukotriene receptor antagonists, was accompanied in rare cases by the development of Charg-Strauss syndrome (systemic eosinophilic vasculitis), manifested in the form of eosinophilia, vascular rash, increased severity of pulmonary symptoms and, if not properly treated, cardiac complications and/or neuropathy. Although the causal relationship of these adverse events with leukotriene receptor antagonist therapy has not been established, caution should be exercised and appropriate clinical monitoring should be carried out when reducing the systemic dose of corticosteroids in patients taking montelukast.

The dose of corticosteroids used together with montelukast should be reduced gradually, under the supervision of a doctor. Abrupt replacement of therapy with inhaled or oral corticosteroids with montelukast is not recommended. Patients with confirmed allergies to acetylsalicylic acid and other NSAIDs should avoid contact with these drugs during treatment with montelukast, since montelukast, while improving respiratory function in patients with allergic bronchial asthma, nevertheless does not prevent bronchoconstriction due to the action of NSAIDs.

When reducing the systemic dose of corticosteroids in patients taking montelukast, caution should be exercised and appropriate clinical monitoring should be carried out. There were no age-related differences in the efficacy and safety profiles of montelukast. Patients with phenylketonuria should be informed that 1 4 mg chewable tablet contains at least 0.96 mg of aspartame, and 1 5 mg chewable tablet contains at least 1.2 mg of aspartame.

Chewable tablets contain the dye red “Charming” (Allura red), which can cause allergic reactions.

Special precautions when disposing of an unused medicinal product. There is no need for special precautions when disposing of unused Montelair®.

Influence on the ability to drive vehicles and engage in other activities that require concentration of attention and speed of psychomotor reactions. There is no evidence that taking Montelukast affects the ability to drive a car or use moving machinery. However, drowsiness and dizziness have been reported, so when these signs appear, patients are not recommended to drive vehicles or engage in other activities that require concentration and speed of psychomotor reactions.

Form of production

chewable tablets

Storage conditions

In a place protected from light and moisture, at a temperature not exceeding 30 °C.

Shelf life

2 years

Active ingredient

Montelukast

Conditions of release from pharmacies

By prescription

Dosage form

tablets for resorption

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor, Children over 2 years of age

Indications

Bronchospasm, Allergic rhinitis