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PharmSpace

Class Explorer · Respiratory

Leukotriene receptor antagonists

Block the cysteinyl leukotriene receptor, cutting the bronchoconstriction, mucus and eosinophil recruitment that arachidonic acid's other branch produces.

Members

Also in this class: Zafirlukast. Full pages arrive as the library grows.

Compare the members

Montelukast
Role
Add-on controller
Key warning
Neuropsychiatric effects

Shared across the class

Indications
Asthma, as add-on therapy · Allergic rhinitis · Exercise-induced bronchoconstriction · Aspirin-exacerbated respiratory disease
Adverse effects
Headache · Neuropsychiatric events including mood change, sleep disturbance, and suicidality
Contraindications
Not for acute bronchospasm
Monitoring
Symptom control · Mood, sleep and behaviour, especially in children and adolescents

What makes each agent different

  • Montelukast is once daily and by far the most used; zafirlukast has food and interaction constraints that make it awkward.

The neuropsychiatric warning is a boxed one in several jurisdictions and is regularly missed at counselling. Parents should be told what to watch for.

Never a substitute for an inhaled corticosteroid in persistent asthma; it is an addition, and a weaker one.

Last reviewed 2026-08-16 · Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed.