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Montelukast (Singulair)

Leukotriene Receptor Antagonistprescriptionoral · predicted

Selective cysteinyl leukotriene receptor antagonist for asthma maintenance and allergic rhinitis. Oral bioavailability ~64%. Extensively metabolized via CYP3A4 and CYP2C9; no active metabolites detected at steady state. Taken once daily in the evening.

Projected serum levels — 10 mg, once daily

Montelukast (Singulair)
Montelukast (Singulair) modeled serum levels, 10 mg once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 1 days. 0 1.3 2.5 3.8 5 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 1

Maintenance schedule: 10 mg once daily (oral).

Modeled steady state after ~1 days: peak ≈ 4.3 mg, trough ≈ 0.43 mg body load. Population-based estimate over 15 days for a 10 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Leukotriene Receptor Antagonist
Route modeled
Oral
Model confidence
predicted
Half-life
4 h
Common dose
10 mg
Suggested maximum
10 mg/day
Reference dose range
5–10 mg (single dose)
Suggested cadence
once daily
Validated against
10 mg oral — Cmax 0.54 mg/L at 3 h

Documented interactions

  • danger
    Clopidogrel (Plavix) + Montelukast (Singulair) CYP inhibition

    Clopidogrel (Plavix) reversible_inhibitor of CYP2C8 predicted to change Montelukast (Singulair) AUC by ~2.07x

  • danger
    Efavirenz (Sustiva) + Montelukast (Singulair) CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Montelukast (Singulair) AUC by ~0.40x

  • danger
    Levothyroxine (Synthroid) + Montelukast (Singulair) Protein binding

    Montelukast (Singulair) may displace Levothyroxine (Synthroid) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free…

  • danger
    Pioglitazone + Montelukast (Singulair) CYP inhibition

    Montelukast (Singulair) reversible_inhibitor of CYP2C8 predicted to change Pioglitazone AUC by ~2.07x

  • danger
    Quercetin + Montelukast (Singulair) CYP inhibition

    Quercetin reversible_inhibitor of CYP2C8 predicted to change Montelukast (Singulair) AUC by ~2.07x

  • danger
    Rifampin + Montelukast (Singulair) CYP induction

    Rifampin inducer of CYP3A4 predicted to change Montelukast (Singulair) AUC by ~0.40x

Serum checks 201 modeled interaction pairings for montelukast (singulair) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Montelukast, a leukotriene receptor antagonist, for the treatment of mild asthma and exercise-induced bronchoconstriction Leff JA et al. · New England Journal of Medicine, 1998 DOI

    Landmark NEJM trial demonstrating montelukast 10 mg daily significantly improved FEV1, reduced beta-agonist use, and protected against exercise-induced bronchoconstriction in mild asthma.

  2. Montelukast, a once-daily leukotriene receptor antagonist, in the treatment of chronic asthma: a multicenter, randomized, double-blind trial Reiss TF et al. · Archives of Internal Medicine, 1998 DOI

    Multicenter double-blind RCT showing montelukast significantly improved FEV1, morning and evening PEFR, and reduced daytime symptoms and beta-agonist use versus placebo in chronic asthma.

  3. Clinical effectiveness and safety of montelukast in asthma. What are the conclusions from clinical trials and meta-analyses? Miligkos M et al. · Drug Design, Development and Therapy, 2014 DOI

    Systematic review confirming montelukast is effective as monotherapy and add-on to ICS in mild-to-moderate asthma, with particular benefit in exercise-induced and aspirin-sensitive phenotypes.

3 published studies referenced in the app, each with a plain-language summary.