PHARMACOLOGY The cysteinyl leukotrienes (LTC4 , LTD4 , LTE4 ) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to cysteinyl leukotriene receptors (CysLT) found in the human airway. Montelukast is an orally active compound that binds with high affinity and selectivity to the CysLT1 receptor. Montelukast inhibits physiologic actions of LTD4 at the CysLT1 receptor without any agonist activity.
DOSAGE & ADMINISTRATION
By indications • Asthma: Once daily in the evening for patients 12 months and older. • Acute prevention of EIB: One tablet at least 2 hours before exercise for patients 6 years of age and older. • Seasonal Allergic Rhinitis: Once daily for patients 2 years and older. • Perennial Allergic Rhinitis: Once daily for patients 6 months and older. By age • 15 years and older: One 10-mg tablet. • 6 to 14 years: One 5-mg chewable tablet. • 2 to 5 years: One 4-mg chewable tablet.
ADVERSE EFFECT
Montelukast appears to be well tolerated. In clinical trials, the most common adverse effect reported was headache, occurring in approximately 18% of patients. Rash, dyspepsia, dizziness, and abdominal pain were all reported in less than 2% of patients. Elevated liver transaminases have been reported with montelukast use, but not at a greater incidence than with placebo. A small percentage of pediatric patients have experienced diarrhea, sinusitis and otitis media during montelukast clinical trials. PRECAUTION Montelukast is not indicated for use in the reversal of bronchospasm in acute asthma attacks, including status asthmaticus. Patients should be advised to have appropriate rescue medication available.
DRUG INTERACTION
Montelukast may be administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma. In drug-interactions studies, the recommended clinical dose of montelukast did not have clinically important effects on the following medicinal products: theophylline, prednisone, prednisolone, oral contraceptives, terfenadine, digoxin and warfarin. Caution should be exercised, particularly in children, when montelukast is co-administered with phenytoin, phenobarbital and rifampicin
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