Montelukast

SINGULAIR is a leukotriene receptor antagonist indicated for: Prophylaxis and chronic treatment of asthma in patients 12 months of age and older. Acute prevention of exercise-induced bronchoconstriction (EIB) in patients 6 years of age and older. Relief of symptoms of allergic rhinitis (AR): seasonal allergic rhinitis (SAR) in patients 2 years of age and older, and perennial allergic rhinitis (PAR) in patients 6 months of age and older. Reserve use for patients who have an inadequate response or intolerance to alternative therapies. Limitations of Use: Not indicated to treat an acute asthma attack.

The cysteinyl leukotrienes (LTC 4, LTD 4, LTE 4 ) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to cysteinyl leukotriene (CysLT) receptors. The CysLT type-1 (CysLT 1 ) receptor is found in the human airway (including airway smooth muscle cells and airway macrophages) and on other pro-inflammatory cells (including eosinophils and certain myeloid stem cells). CysLTs have been correlated with the pathophysiology of asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process. In allergic rhinitis, CysLTs are released from the nasal mucosa after allergen exposure during both early- and late-phase reactions and are associated with symptoms of allergic rhinitis.

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. Dosage (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 or one packet of 4-mg oral granules. 6 to 23 months: one packet of 4-mg oral granules. Patients with both asthma and allergic rhinitis should take only one dose daily in the evening. For oral granules: Must administer within 15 minutes after opening the packet (with or without mixing with food).

SINGULAIR is contraindicated in patients with hypersensitivity to any of its components. Hypersensitivity to any component of SINGULAIR.

Boxed warning (serious neuropsychiatric events): Serious neuropsychiatric (NP) events have been reported with the use of SINGULAIR. The types of events reported were highly variable, and included, but were not limited to, agitation, aggression, depression, sleep disturbances, suicidal thoughts and behavior (including suicide). The mechanisms underlying NP events associated with SINGULAIR use are currently not well understood. Do not prescribe SINGULAIR to treat an acute asthma attack. Advise patients to have appropriate rescue medication available. Inhaled corticosteroid may be reduced gradually. Do not abruptly substitute SINGULAIR for inhaled or oral corticosteroids. Patients with known aspirin sensitivity should continue to avoid aspirin or non-steroidal anti-inflammatory agents while taking SINGULAIR.

The following clinically significant adverse reactions are described elsewhere in the labeling: Neuropsychiatric Events Most common adverse reactions (incidence ≥5% and greater than placebo listed in descending order of frequency): upper respiratory infection, fever, headache, pharyngitis, cough, abdominal pain, diarrhea, otitis media, influenza, rhinorrhea, sinusitis, otitis.

No dose adjustment is needed when SINGULAIR is co-administered with theophylline, prednisone, prednisolone, oral contraceptives, fexofenadine, digoxin, warfarin, gemfibrozil, itraconazole, thyroid hormones, sedative hypnotics, non-steroidal anti-inflammatory agents, benzodiazepines, decongestants, and Cytochrome P450 (CYP) enzyme inducers.

Store SINGULAIR 4-mg oral granules, 4-mg chewable tablets, 5-mg chewable tablets and 10-mg film-coated tablets at 20°C to 25°C (68°F to 77°F), excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from moisture and light. Store in original package.