Montelukast
Unchecked
Montelukast
Singulair
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Summary
Common uses
Asthma (controller)0, Exercise-induced bronchospasm0, Allergic rhinitis0
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[1]
Bioavailability
~64% (oral; not significantly affected by food)[1]
Pregnancy
Generally considered safe; pregnancy registries do not show increased major malformation risk.[citation needed]
Legal status
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[1].
References
[edit | edit source]- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Singulair (montelukast sodium), Merck, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020829s072,020830s076,021409s050lbl.pdf