Classifications: bronchodilator (respiratory smooth muscle relaxant); leukotriene receptor antagonist; Therapeutic: bronchodilator; leukotriene receptor antagonist
Pregnancy Category: B
5 mg, 10 mg tablets; 4 mg chewable tablets; 4 mg oral granules
Selective receptor antagonist of leukotriene D4, thus inhibiting bronchoconstriction. Leukotrienes are considered more important than prostaglandins as inflammatory agents;
they induce bronchoconstriction and mucus production. Elevated sputum and blood levels of leukotrienes have been documented
during acute asthma attacks.
Controls asthmatic attacks by inhibiting leukotriene release as well as inflammatory action associated with the attack.
Indicated by improved pulmonary functions and better controlled asthmatic symptoms.
Prophylaxis and chronic treatment of asthma or allergic rhinitis; exercise-induced bronchoconstriction (EIB).
Hypersensitivity to montelukast; acute asthma attacks; bronchoconstriction due to asthma or NSAIDs; status asthmaticus;
children <6 mo; lactation.
Hypersensitivity to other leukotriene receptor antagonists (e.g., zafirlukast, zileuton); severe liver disease; jaundice,
PKU; severe asthma; pregnancy (category B).
Route & Dosage
Adult: PO 10 mg q.d. in evening
Child: PO 12 mo5 y, 4 mg q.d. in evening; 614 y, 5 mg chewable tablet q.d. in evening
Adult/Adolescent (>15 y): PO 10 mg 2 h before exercise (not more than 1 per day)
- Give in the evening for maximum effectiveness.
- Ensure chewable tablets for children are not swallowed whole.
- Store at 15°30° C (59°86° F) in a tightly closed container and protect from light.
Adverse Effects (≥1%)Body as a Whole:
Asthenia, fever, trauma. CNS:
Dizziness, headache. GI:
Abdominal pain, dyspepsia, gastroenteritis, dental pain, abnormal liver function tests (ALT, AST), diarrhea
, nausea. Respiratory:
Nasal congestion, cough, influenza
, laryngitis, pharyngitis, sinusitis
Rapidly absorbed from GI tract, bioavailability 64%. Peak:
34 h for oral tablet, 22.5 h for chewable tablet. Distribution:
>99% protein bound. Metabolism:
Extensively metabolized by cytochromes P450 3A4 and 2C9. Elimination:
In feces. Half-Life:
Assessment & Drug Effects
- Monitor effectiveness carefully when used in combination with phenobarbital or other potent cytochrome P450 enzyme inducers.
- Lab test: Periodic liver function tests.
Patient & Family Education
- Do not use for reversal of an acute asthmatic attack.
- Inform physician if short-acting inhaled bronchodilators are needed more often than usual with montelukast.
- Use chewable tablets (contain phenylalanine) with caution with PKU.