Montelukast

Leukotriene receptor antagonist, Antiasthmatic

Montelukast

Singulair

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Summary

Classes

Leukotriene receptor antagonist, Antiasthmatic

Common uses

Asthma (controller)▲0▼, Exercise-induced bronchospasm▲0▼, Allergic rhinitis▲0▼

Pharmacy

Starting dose

10 mg PO once daily in the evening (adults); 4-5 mg in children

Preparations

10 mg tablets; 4 mg, 5 mg chewables; 4 mg granules

US FDA Max

10 mg/d (adults)

Pharmacology

Routes

Oral

Onset

Bronchodilation within 1-2 hours; full controller effect 1-2 weeks

Duration

24 hours

Half-life

2.7-5.5 hours

Bioavailability

~64% (oral; not significantly affected by food)

Pregnancy

Generally considered safe; pregnancy registries do not show increased major malformation risk.^{[citation needed]}

Legal status

Rx-only in US. FDA Boxed Warning (2020): neuropsychiatric events including agitation, depression, sleep disturbance, and suicidal thoughts; benefit-risk should be reassessed regularly.

Purported mechanism

Montelukast is a selective antagonist of the CysLT1 receptor; blocking leukotriene D4 (and to a lesser extent C4 and E4) binding reduces airway smooth muscle contraction, vascular permeability, and eosinophilic inflammation downstream of 5-lipoxygenase activation.▲0▼ Metabolized primarily via CYP2C8 with CYP3A4 contribution; the boxed warning was added after post-marketing reports of neuropsychiatric events were judged by FDA to outweigh the modest controller benefit relative to inhaled corticosteroids.