Montelar, 5 mg 14 pcs

Montelar is a bronchodilator.

Pharmacodynamics

Blocker of cysteinyl leukotriene receptors of airway epithelium CysLT1 (LT C4, D4 and E4 – mediators of chronic persistent inflammation that maintain bronchial hyperresponsiveness in bronchial asthma). Prevents excessive formation of secretion in the bronchi, edema of the airway mucosa. Reduces the severity of bronchial asthma and the frequency of asthmatic attacks. It is highly effective when taken orally.

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

Pharmacokinetics

Absorption. Montelukast is rapidly and almost completely absorbed after oral administration from the GI tract. Bioavailability for oral tablets 5 mg is 73%; for film-coated tablets 10 mg – 64%. After taking chewable 4 and 5 mg tablets, T_max is 2 hours; for film-coated 10 mg tablets, 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. With therapeutic doses, plasma concentrations of montelukast metabolites are not detected in equilibrium in adults and children.

It is assumed that cytochrome P450 isoenzymes (3A4 and 2C9) are involved in the metabolism of montelukast, and at therapeutic concentrations montelukast does not inhibit CYP isoenzymes: 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6.

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

The T_1/2 of montelukast in young healthy adults is 2.7 to 5.5 hours.

Pharmacokinetics in special cases

The pharmacokinetics of montelukast in women and men is similar.

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

Because montelukast and its metabolites are excreted from the body through the intestine, no dose adjustment is necessary for patients with renal impairment.

Indications

– prevention and long-term treatment of bronchial asthma, including prevention of daytime and nighttime symptoms of the disease (for children over 2 years of age and adults);
– treatment of bronchial asthma in patients with hypersensitivity to acetylsalicylic acid (for children aged 6 years and older and adults);
– prevention of bronchospasm caused by physical activity (for children over 2 years old and adults);
– relief of symptoms of seasonal and year-round allergic rhinitis in children aged 2 years and adults.

Pharmacological effect

Montelar is a bronchodilator.

Pharmacodynamics

Blocker of cysteinyl leukotriene receptors of the respiratory tract epithelium CysLT1 (LT C4, D4 and E4 – mediators of chronic persistent inflammation that supports 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 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 oral administration from 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 mg Tmax – 2 hours, for film-coated tablets 10 mg – 3 hours.

Distribution and metabolism. Montelukast is more than 99% bound to plasma proteins. The average Vd of montelukast averages 8–11 L.

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 P450 isoenzymes (3A4 and 2C9) are involved in the metabolism of montelukast, while at therapeutic concentrations montelukast does not inhibit CYP isoenzymes: 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6.

Excretion. Plasma clearance – 45 ml/min. After oral administration, montelukast is almost completely eliminated through the intestines (about 86%) and less than 0.2% by the kidneys.

T1/2 of montelukast in young healthy adults ranges from 2.7 to 5.5 hours.

Pharmacokinetics in special cases

The pharmacokinetics of montelukast in women and men is similar.

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

Since montelukast and its metabolites are eliminated from the body through the intestines, no dose adjustment is necessary for patients with renal failure.

Special instructions

It is recommended to continue taking montelukast after achieving significant improvement. Montelukast is not recommended for the treatment of acute attacks of bronchial asthma. In acute cases of bronchial asthma, patients should use emergency medications to relieve attacks (short-acting inhaled β2-adrenergic agonists).

Reducing the systemic dose of GCS in patients receiving anti-asthma drugs, including leukotriene receptor antagonists, was accompanied in rare cases by the development of Churg-Strauss syndrome (systemic eosinophilic vasculitis), manifested in the form of eosinophilia, vascular rash, increased severity of pulmonary symptoms and, in the absence of proper treatment, cardiac complications and/or neuropathy. Although a causal relationship between these adverse events and leukotriene receptor antagonist therapy has not been established, caution and appropriate clinical monitoring should be used when reducing the systemic dose of GCS in patients taking montelukast.

The dose of corticosteroids used together with montelukast should be reduced gradually, under the supervision of a physician. Abrupt replacement of therapy with inhaled or oral corticosteroids with montelukast is not recommended. Patients with a confirmed allergy 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 caused by the action of NSAIDs.

When reducing the systemic dose of GCS 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 profile of montelukast. Patients with phenylketonuria should be informed that 1 chewable tablet of 4 mg contains at least 0.96 mg of aspartame, and 1 chewable tablet of 5 mg contains at least 1.2 mg of aspartame.

Chewable tablets contain Allura red dye, which can cause allergic reactions.

Special precautions when disposing of unused medicinal products. There is no need for special precautions when disposing of unused Montelar®.

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

Active ingredient

Montelukast

Composition

1 tablet contains:

Active substance:

montelukast sodium 5.2 mg (equivalent to montelukast 5 mg, respectively);

Excipients:

mannitol – 194.9 mg,

microcrystalline cellulose – 66 mg,

croscarmellose sodium – 15 mg,

hyprolose (type EXF) – 9 mg,

cherry flavor – 2.4 mg (contains 0.07% Allura red AC (E129)),

aspartame – 1.2 mg,

cherry flavor – 0.6 mg,

iron (III) oxide red dye – 0.45 mg,

magnesium stearate – 5.25 mg.

Pregnancy

The use of Montelar® during pregnancy and lactation is possible only if the expected benefit to the mother outweighs the potential risk to the fetus or child.

Contraindications

– hypersensitivity to any of the components of the drug Montelar (for all dosage forms);
– phenylketonuria (for chewable tablets, 4 or 5 mg);
– rare hereditary diseases such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption (for film-coated tablets, 10 mg);
– children under 2 years of age (for chewable tablets, 4 mg); up to 6 years (for chewable tablets, 5 mg); children under 15 years of age (for film-coated tablets, 10 mg).

Side Effects

From the side of the central nervous system: often – headache.

From the gastrointestinal tract: often – pain in the abdominal area.

Post-marketing observations

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

From the side of hemostasis: increased tendency to bleeding, incl. nosebleeds, bruises.

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

From the skin and subcutaneous tissues: often – rash; uncommon – tendency to form hematomas, urticaria, itching; very rarely – erythema nodosum, erythema multiforme.

From the side of the central nervous system: infrequently – headache, dizziness, drowsiness, paresthesia/hypoesthesia, convulsions, hyperkinesia.

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

From the cardiovascular system: rarely – palpitations.

From the blood and lymphatic system: rarely – increased tendency to bleeding.

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

From the liver and biliary tract: often – increased activity of hepatic transaminases (ALT, AST); very rarely – cholestatic hepatitis, damage to hepatocytes, most often due to concomitant drug therapy or existing liver pathology (various forms of hepatitis).

From the musculoskeletal and connective tissue side: infrequently – arthralgia, myalgia, including muscle spasms.

From the respiratory system: infrequently – nosebleeds; very rarely – Churg-Strauss syndrome.

From the senses: otitis media (including medial).

Other: uncommon – 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 AUC value decreases in individuals concomitantly receiving phenobarbital (by approximately 40%), however, no adjustment of the montelukast dosage regimen is required in such patients. In vitro studies have shown that montelukast is a potential inhibitor of the CYP2C8 isoenzyme of the cytochrome P450 system, however, data from clinical drug-drug interaction studies involving montelukast and rosiglitazone (a pre-substrate of drugs primarily metabolized by the CYP2C8 isoenzyme) have shown that doses of montelukast do not inhibit the CYP2C8 isoenzyme in vivo. Therefore, montelukast does not have a significant effect on the metabolism of medications 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 of montelukast and gemfibrozil (an inhibitor of both CYP2C8 and CYP2C9) demonstrate that gemfibrozil increases the effect of systemic exposure to montelukast by 4.4 times.

Co-administration of intraconazole, a strong CYP3A4 inhibitor, with gemfibrozil and montelukast did not result in an additional increase in the effect of systemic exposure to montelukast. The effect of gemfibrozil on the systemic exposure of montelukast may not be considered clinically significant based on safety data when used at doses higher than the approved dose of 10 mg in adult patients (e.g., 200 mg/day in adult patients for 22 weeks and up to 900 mg/day in patients taking the drug for approximately one week, no clinically significant adverse effects were observed).

Therefore, no dosage adjustment of montelukast is required when coadministered with gemfibrozil.

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

Combination treatment with bronchodilators

Montelar® is a reasonable addition to monotherapy with bronchodilators if the latter do not provide adequate control of bronchial asthma. Once a therapeutic effect has been achieved (usually after the first dose) from treatment with Montelar®, a gradual reduction in the dose of bronchodilators can begin.

Combined treatment with inhaled corticosteroids

Treatment with Montelar® provides an additional therapeutic effect to patients using inhaled corticosteroids. Once the condition has stabilized, you can begin to gradually reduce the dose of GCS under the supervision of a physician. In some cases, complete abolition of inhaled corticosteroids is acceptable, but abrupt replacement of inhaled corticosteroids with Montelar® 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.

Overdose

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

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

Storage conditions

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

Shelf life

2 years

Manufacturer

Genveon Ilac Sanayi Ve Ticaret Anonymous Shirketi, Türkiye