Montelukast has high affinity and selectivity for receptor binding cysteinyl leukotrienes. The use of montelukast inhibits the early and late phase bronchoconstriction. Montelukast decreases bronchoconstriction even at very low doses (5 mg). Bronchodilation lasts for 2 hours after ingestion of the drug.Bronchodilation effect caused by a beta-adrenergic agonist, increases the effects caused by montelukast. Montelukast reduces the number of eosinophils in peripheral blood and in the airways (sputum) children and adults and improves the clinical course of the control of asthma. In adult patients, montelukast significantly improves the morning forced expiratory volume masteron hair loss for 1 second. Montelukast enhances the clinical effect of inhaled glucocorticosteroids.Montelukast reduces the severity of daytime (including coughing, wheezing, shortness of breath and limitation of activity) and nighttime symptoms of asthma.Montelukast reduces the need for beta-adrenergic agonist and a glucocorticosteroid, used if necessary (for deterioration). Patients receiving montelukast, there is a long-term remission than patients who did not take it. The therapeutic effect was observed after the first dose. In children aged from 2 years with asthma mild and episodic exacerbations, montelukast significantly reduced the frequency of episodes of bronchial asthma exacerbations and improves respiratory function.
Weakened bronchoconstriction that occurs on a background of physical activity. In patients with bronchial asthma, aspirin-sensitive and receiving concomitant therapy with inhaled and / or oral corticosteroids, montelukast treatment leads to a significant improvement of the control of asthma symptoms.
maximum substance concentration in plasma achieved in children aged from 2 to 5 years after 2 hours after administration on an empty stomach at a dose of 4 mg. The average Cmax was 66% higher, while Cmin mean was lower than in adults after taking a dose of 10 mg.
In adult patients when taken on an empty stomach achieved within 2 hours after intake. The average bioavailability of 73%; it is reduced to 63% when taking the drug after the normal meal.
Montelukast is more than 99% bound to plasma proteins. Montelukast volume of distribution at steady state an average of 8-11 liters. Poorly penetrates the blood-brain barrier.
Montelukast active undergoes metabolism in the liver. In the equilibrium state after administration of therapeutic doses in children and adults, the concentration of montelukast metabolites in the plasma are not defined.
Isozyme of cytochrome are involved in the montelukast metabolism, but at therapeutic concentrations of montelukast do not inhibit cytochrome masteron hair lossand .Montelukast metabolites have negligible pharmacological activity.
clearance from plasma montelukast in healthy adults is 45 ml / min. After oral administration of montelukast labeled 86% of the drug excreted for five days through the intestines and at least 0.2% – kidneys.This indicates that the drug and its metabolites are excreted mainly in the bile. The masteron hair loss montelukast in young patients of between 2.7 to 5.5 hours. The pharmacokinetics of montelukast retains substantially linear ingestion of doses above 50 mg.
Special groups of patients
No studies have been conducted in patients with renal insufficiency.
Because montelukast and its metabolites are excreted in the bile, dose adjustment in patients with renal impairment is not required.
On the pharmacokinetics of montelukast data in patients with severe hepatic insufficiency (score> 9 on the scale of Child-Pugh ) are absent.
Indications for use:
The drug is indicated for children 6-14 years old for:
- long-term treatment and prevention of asthma (including warning of daytime and nighttime symptoms);
- the treatment of asthma masteron hair loss in patients with hypersensitivity to aspirin and prevention of bronchospasm physical effort.
- Hypersensitivity to the active substance or to any of the excipients.
- Children under 6 years of age.
- Phenylketonuria (medication contains aspartame).
- Severe liver dysfunction.