Za Pharmacy

Drugs, Supplies and Delivery

Montelukast

Montelukast is a cornerstone therapy for asthma and allergic rhinitis, offering targeted anti-inflammatory benefits. However, its association with neuropsychiatric adverse effects necessitates vigilant monitoring. Adherence to BNF dosing guidelines, patient education, and awareness of rare side effects ensure safe and effective use.

Montelukast is a leukotriene receptor antagonist that selectively blocks the action of cysteinyl leukotrienes (CysLTs), inflammatory mediators involved in asthma and allergic reactions. Key actions include:

  1. Inhibition of Leukotriene D₄ (LTD₄): Binds to CysLT₁ receptors in the airways, preventing bronchoconstriction, mucus secretion, and vascular permeability (Lippincott).
  2. Anti-inflammatory Effects: Reduces eosinophil recruitment and airway inflammation.
  3. Prophylactic Role: Prevents asthma symptoms triggered by allergens, exercise, or aspirin.

Montelukast is approved for:

  1. Asthma:
    • Prophylaxis and chronic treatment in adults and children ≥6 months (BNF).
    • Adjunct therapy for patients inadequately controlled by inhaled corticosteroids.
  2. Allergic Rhinitis:
    • Seasonal and perennial allergic rhinitis (≥2 years).
  3. Exercise-Induced Bronchoconstriction (EIB):
    • Prevention in patients ≥6 years.
  4. Off-Label Uses:
    • Aspirin-exacerbated respiratory disease (AERD).
    • Chronic urticaria (limited evidence).

Adults and Adolescents (≥15 years):

  • Asthma/Allergic Rhinitis: 10 mg once daily, taken in the evening.

Children:

  • 6–14 years: 5 mg once daily (chewable tablet or granules).
  • 2–5 years: 4 mg once daily (oral granules or chewable tablet).
  • 6 months–5 years: 4 mg oral granules once daily (BNF).

Exercise-Induced Bronchoconstriction:

  • 10 mg taken ≥2 hours before exercise (do not take another dose within 24 hours).

Special Populations:

  • Renal/Hepatic Impairment: No dose adjustment required.

Elderly: No specific recommendations; use standard dosing

  • Common (≥1%): Headache, abdominal pain, thirst, dizziness.
  • Serious (Rare):
    • Neuropsychiatric effects: Agitation, depression, suicidal ideation (boxed warning).
    • Eosinophilia (with systemic symptoms).
    • Hypersensitivity reactions (angioedema, anaphylaxis).
    • Hepatic dysfunction (elevated ALT/AST).
  1. Contraindications:
    • Hypersensitivity to montelukast or components.
  2. Neuropsychiatric Risks:
    • Monitor for mood changes, sleep disturbances, or suicidal thoughts; discontinue if symptoms occur.
  3. Pregnancy/Lactation:
    • BNF Category: Use only if benefits outweigh risks (limited human data).
    • Excreted in breast milk; avoid during lactation.

Aspirin Sensitivity: Not a substitute for aspirin avoidance in AERD

Montelukast has minimal interactions due to hepatic metabolism via CYP2C8/3A4 and renal excretion. Notable considerations:

  • CYP Inducers:
    • Rifampicin, Phenobarbital: Reduce montelukast levels (monitor efficacy).
  • Gemfibrozil: Inhibits CYP2C8, increasing montelukast exposure (clinical significance unclear).
  • Prednisone, Theophylline: No significant interactions (Lange).

Generic & Brand Names

  • Generic: Montelukast Sodium.
  • Brand Names: Singulair®, Montair®, Lukast®.

Book Now

Order Your Medications with Ease

We provide fast and secure prescription reservations—place your order now and pick it up from the nearest pharmacy!