====== Montelukast ====== ===== Classification ===== * Leukotriene Receptor Antagonist (CysLT1 blocker) Parent class: * [[respiratory:drug_classes:leukotriene_modifiers|Leukotriene Modifiers]] ---- ===== Mechanism of Action ===== Montelukast selectively blocks the CysLT1 receptor. Leukotrienes (LTC4, LTD4, LTE4) normally cause: * Bronchoconstriction * Increased mucus secretion * Increased vascular permeability * Eosinophilic airway inflammation By blocking the receptor: * ↓ Bronchospasm * ↓ Airway inflammation * ↓ Mucus production Does NOT block leukotriene synthesis — only receptor binding. ---- ===== Pharmacokinetics ===== * Oral administration * Once daily dosing * Hepatic metabolism (CYP3A4, CYP2C9) * Eliminated via bile No routine lab monitoring required. ---- ===== Indications ===== * [[respiratory:clinical:asthma|Asthma]] (mild persistent or add-on therapy) * Exercise-induced bronchospasm * [[allergy:clinical:allergic_rhinitis|Allergic Rhinitis]] * Aspirin-exacerbated respiratory disease (AERD) Not first-line for moderate or severe asthma. ---- ===== Dosing (Adult) ===== * 10 mg PO once daily (evening preferred) Pediatric dosing based on age (chewable formulations available). ---- ===== Adverse Effects ===== Common: * Headache * GI upset Serious: * Neuropsychiatric effects (boxed warning) - Agitation - Depression - Sleep disturbances - Suicidal ideation (rare) FDA recommends reserving for patients who cannot tolerate alternative therapy in allergic rhinitis. ---- ===== Contraindications / Cautions ===== * Use caution in patients with history of depression or psychiatric illness * Not effective for acute asthma attacks ---- ===== Clinical Role in Asthma ===== Montelukast: * Less effective than inhaled corticosteroids * Useful as add-on therapy * Helpful in aspirin-sensitive asthma * Useful in patients with both asthma and allergic rhinitis See: * [[respiratory:clinical:asthma|Asthma Management]] ---- ===== Clinical Role in Allergic Rhinitis ===== * Inferior to intranasal corticosteroids * Consider if antihistamines not tolerated * Consider if coexisting asthma See: * [[allergy:clinical:allergic_rhinitis|Allergic Rhinitis]] ---- ===== Comparison Within Class ===== ^ Drug ^ Mechanism ^ Major Risk ^ | [[respiratory:drugs:montelukast|Montelukast]] | CysLT1 receptor blocker | Neuropsychiatric effects | | [[respiratory:drugs:zafirlukast|Zafirlukast]] | CysLT1 receptor blocker | Rare hepatotoxicity | | [[respiratory:drugs:zileuton|Zileuton]] | 5-LO inhibitor | Hepatotoxicity | ---- ===== Clinical Pearls ===== * Leukotrienes are potent bronchoconstrictors. * Useful in aspirin-exacerbated respiratory disease. * Not a rescue medication. * Discuss mental health risks before prescribing. * Often used in pediatric asthma due to oral formulation. ---- ===== Related Pages ===== * [[respiratory:drug_classes:leukotriene_modifiers|Leukotriene Modifiers]] * [[endocrine:drug_classes:corticosteroids|Corticosteroids]] * [[allergy:histamine|Histamine & Antihistamines]]