BSN Tracker

montelukast

Brand: Singulair

⚠ BBW Prototype Drug
Drug Class: leukotriene receptor antagonist (LTRA)
Drug Family: leukotriene modifier
Subclass: cysteinyl leukotriene CysLT1 receptor antagonist
Organ Systems: respiratoryimmunology

Mechanism of Action

Blocks CysLT1 receptors preventing leukotriene D4 (LTD4)-mediated bronchoconstriction, mucus secretion, and eosinophil recruitment; anti-inflammatory bronchodilation.

cysteinyl leukotriene receptor 1 (CysLT1)

Indications

  • asthma (mild persistent — adjunct to ICS)
  • exercise-induced bronchospasm
  • allergic rhinitis
  • aspirin-exacerbated respiratory disease
  • eosinophilic esophagitis (off-label)

Contraindications

  • phenylketonuria (chewable tablet contains aspartame)

Adverse Effects

Common

  • headache
  • GI upset
  • upper respiratory infection

Serious

  • neuropsychiatric events (depression, suicidal ideation — BBW added 2020)
  • hypersensitivity

Pharmacokinetics (ADME)

Absorption ~64-73% oral bioavailability
Distribution large Vd
Metabolism extensive hepatic CYP3A4 and CYP2C9
Excretion fecal ~86%
Half-life 5.3-5.5 hours
Onset 3-4 hours
Peak 3-4 hours
Duration 24 hours
Protein Binding 99%
Vd 8-11 L/kg

Drug Interactions

Drug / Agent Mechanism Severity
strong CYP3A4/2C9 inducers (rifampin, phenobarbital) reduce montelukast levels moderate

Nursing Considerations

  1. FDA BBW (2020): warn patients about neuropsychiatric effects including depression and suicidality
  2. Reserve for patients who benefit from oral therapy (needle-phobia, rhinitis overlap) or aspirin-exacerbated asthma
  3. Evening dosing preferred (leukotrienes peak at night)
  4. Counsel patients and caregivers to report mood/behavior changes immediately

Clinical Pearls

  • Less effective than ICS for asthma control but preferred for aspirin-exacerbated respiratory disease and allergic rhinitis combination
  • Neuropsychiatric BBW: mood changes, suicidal ideation — FDA mandated Black Box Warning 2020

Safety Profile

Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required
Guideline Update pending

Concordance Terms

Cross-referenced clinical concepts — click any term to see all content where it appears.

Allergic Rhinitis Aspirin-exacerbated Respiratory Disease Asthma (mild Persistent — Adjunct To ICS) Eosinophilic Esophagitis (off-label) Exercise-induced Bronchospasm Leukotriene Receptor Antagonist (LTRA)
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