Montelukast

Indications
Oral
Chronic asthma
Adult: 10 mg once daily in the evening.
Child: 2-5 yr: 4 mg daily; 6-14 yr: 5 mg daily; ≥15 yr: 10 mg once daily. All doses to be taken in the evening.
Oral
Allergic rhinitis
Adult: 10 mg once daily in the evening.
Oral
Prophylaxis of exercise-induced asthma
Adult: 10 mg at least 2 hr prior to exercise; do not admin additional doses within 24 hr.
Child: ≥15 yr: 10 mg at least 2 hr prior to exercise; do not admin additional doses within 24 hr.
Warnings / Precautions
Not for the relief of acute bronchospasm. Not to be used as monotherapy for the prevention of exercise-induced bronchospasm. Patients in whom asthma is precipitated by aspirin or other NSAIDs should continue to avoid aspirin and NSAIDs. Do not abruptly substitute for oral or inhaled corticosteroids. Be alert for any signs of Churg-Strauss syndrome. Pregnancy and lactation. Children <6 mth.
Adverse Reactions
Dizziness, fatigue, fever; rash; abdominal pain, dyspepsia, dental pain, gastroenteritis; increased AST; weakness; cough, nasal congestion. Aggression, agitation, angioedema, arthralgia, bleeding tendency, bruising, cholestasis, diarrhoea, dream abnormalities, drowsiness, oedema, eosinophilia, hallucinations, hepatic eosinophilic infiltration (rare), hepatitis, hypersensitivity, hypoaesthesia, insomnia, irritability, muscle cramps, myalgia, nausea, palpitation, pancreatitis, paraesthesia, pruritus, restlessness, seizure, urticaria, vasculitis, vomiting.
Potentially Fatal: Anaphylaxis, Churg-Strauss syndrome.
Overdose Reactions
Symptoms: Abdominal pain, headache, psychomotor hyperactivity, vomiting, somnolence, thirst. Management: Symptom-directed and supportive. Not known if dialysis would be helpful.
Drug Interactions
Metabolism may be increased with rifampicin, phenobarbital, phenytoin. Peripheral oedema may occur with prednisone.
See Below for More montelukast Drug Interactions
Food Interactions
Serum levels may be reduced with St John's wort.
Mechanism of Actions
Montelukast is a selective leukotriene receptor antagonist that blocks the effects of cysteinyl leukotrienes in the airways.
Absorption: Rapidly absorbed from the GI tract (oral). Peak plasma concentrations in 2-4 hr. Mean oral bioavailability: 64%.
Distribution: Protein-binding: >99%.
Metabolism: Extensively hepatic by CYP3A4, CYP2A6 and CYP2C9 isoenzymes.
Excretion: Principally via faeces; elimination half-life prolonged in mild to moderate hepatic impairment.
Storage Conditions
Oral: Store at 15-30°C (59-86°F). Protect from moisture and light.
ATC Classification
R03DC03 - montelukast ; Belongs to the class of leukotriene receptor antagonists. Used in the systemic treatment of obstructive airway diseases.
Storage
Oral: Store at 15-30°C (59-86°F). Protect from moisture and light.
Available As
  • Montelukast 10 mg
  • Montelukast Sodium 10 mg
  • Montelukast 2.5 mg
  • Montelukast 4 mg
  • Montelukast Sodium 4 mg
  • Montelukast 5 mg
  • Montelukast Sodium 5 mg
  • Montelukast 8 mg
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