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Leukotriene Modifiers

Leukotrienes are inflammatory mediators released from mast cells and eosinophils during the allergic cascade, driving bronchoconstriction, mucus secretion, and airway edema. Montelukast blocks the leukotriene receptor (CysLT1), shutting down that downstream inflammation. It does NOT bronchodilate acutely — it is a long-term oral CONTROLLER for prophylaxis of mild persistent asthma and exercise-induced bronchospasm (often add-on when an inhaled corticosteroid alone is insufficient) and also treats allergic rhinitis. Signature trio: by mouth, in the evening, and watch the brain (neuropsychiatric boxed warning). It must never replace a short-acting bronchodilator in an acute attack.

montelukastPrototype
Singulair; CysLT1 receptor antagonist; once daily in the evening
zafirlukast
leukotriene receptor antagonist; taken on empty stomach
zileuton
5-lipoxygenase inhibitor — different target; requires liver function monitoring
mild persistent asthma prophylaxis
controller, not rescue
exercise-induced bronchospasm
add-on to inhaled corticosteroid
when ICS alone is insufficient — adjunct, not a replacement
allergic rhinitis
headache
abdominal pain
drowsiness
mild, non-urgent
acute bronchospasm rescue use
NOT a rescue drug — never substitute for a short-acting bronchodilator during an attack
active or history of mental health disorder
relative; weigh risk given neuropsychiatric boxed warning and assess baseline mental status
assess baseline mental health status
before starting and at follow-up — boxed-warning surveillance
give once daily in the evening
bedtime dosing for asthma control
use age-appropriate formulation
chewable tablets ages 2–14; granules 6–23 months
verify a rescue inhaler is available
montelukast does not cover acute attacks
report mood or behavior changes immediately
agitation, depression, nightmares, aggression — boxed-warning symptoms
report thoughts of self-harm immediately
take every evening even when symptom-free
daily controller, not as-needed
do not use for an acute attack
use the prescribed rescue inhaler instead
do not stop the inhaled corticosteroid
montelukast is add-on, not a replacement
Report Nowescalate immediately
neuropsychiatric events HallmarkBlack Box
FDA boxed warning (2020): mood changes, agitation, depression, suicidal ideation, hallucinations, nightmares, aggression — notify provider promptly, consider discontinuation
suicidal ideation
component of the boxed warning; report immediately

Clinical Pearl

Bedtime, by mouth, and watch the brain — montelukast's three signatures are evening dosing, oral route, and the neuropsychiatric boxed warning. It controls, it never rescues.

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