What is Montelukast (Singulair)?

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From the Guidelines

Montelukast (Singulair) is a leukotriene receptor antagonist used to treat asthma and allergic rhinitis, with a standard adult dose of 10 mg once daily.

Key Points

  • Montelukast works by blocking leukotriene receptors, reducing inflammation in the airways and preventing asthma symptoms or allergic reactions 1.
  • It is particularly effective for exercise-induced asthma when taken at least 2 hours before physical activity.
  • The medication should be taken regularly, even when symptom-free, for maximum effectiveness.
  • Common side effects include headache, digestive issues, and upper respiratory infections.
  • More serious but rare side effects can include mood changes, behavior problems, and suicidal thoughts, particularly in children and adolescents.
  • According to the most recent guidance, for initial treatment of seasonal allergic rhinitis in persons aged 15 years or older, an intranasal corticosteroid is recommended over a leukotriene receptor antagonist, such as montelukast 1.

Usage and Dosage

  • The standard adult dose is 10 mg once daily, taken in the evening.
  • Children aged 6-14 typically receive 5 mg daily, and children 2-5 years old take 4 mg daily.
  • Patients should continue their other asthma medications unless directed otherwise by their healthcare provider, as montelukast is typically used as an add-on therapy rather than a replacement for inhaled corticosteroids or rescue inhalers.

Clinical Considerations

  • Montelukast may be prescribed for patients with a concurrent diagnosis of mild persistent asthma, as it may also provide benefit for seasonal allergic rhinitis 1.
  • However, it is not the preferred agent for a patient with either condition, and an intranasal corticosteroid is generally recommended as the first-line treatment 1.

From the FDA Drug Label

Montelukast is an orally active compound that binds with high affinity and selectivity to the CysLT1 receptor (in preference to other pharmacologically important airway receptors, such as the prostanoid, cholinergic, or β-adrenergic receptor). Montelukast sodium, the active ingredient in SINGULAIR1, is a selective and orally active leukotriene receptor antagonist that inhibits the cysteinyl leukotriene CysLT1 receptor.

Montelukast (Singulair) is a leukotriene receptor antagonist that binds to the CysLT1 receptor, inhibiting the actions of cysteinyl leukotrienes, which are involved in the pathophysiology of asthma and allergic rhinitis 2 2.

From the Research

Definition and Mechanism of Action

  • Montelukast is a cysteinyl leukotriene receptor antagonist used to treat persistent asthma in patients aged ≥ 6 years 3.
  • It is a selective antagonist of the leukotriene D4 (LTD4) receptor, which plays a role in asthma pathophysiology 4.
  • Montelukast works by blocking the action of leukotrienes, which are chemical messengers involved in inflammation and airway constriction.

Clinical Efficacy

  • Montelukast has been shown to improve lung function, reduce symptoms, and decrease the need for rescue medication in patients with persistent asthma 3, 5, 4, 6.
  • It has been found to be effective in adults and children aged ≥ 6 years with persistent asthma, including those with exercise-induced bronchoconstriction and/or aspirin sensitivity 3, 6.
  • Montelukast has also been shown to have glucocorticoid sparing properties, allowing for the reduction of inhaled corticosteroid doses while maintaining clinical stability 3, 6.

Dosage and Administration

  • The recommended dose of montelukast is 10 mg once daily for adults and adolescents ≥ 15 years, and 5 mg once daily for children aged 6-14 years 5, 6.
  • The drug is administered orally, and its efficacy has been demonstrated in clinical trials with once-daily dosing 3, 5, 4, 6.

Safety and Tolerability

  • Montelukast has been found to be well-tolerated, with a safety profile similar to that of placebo in clinical trials 3, 7, 4, 6.
  • The most common adverse event reported with montelukast is headache, and the frequency of adverse events is similar to that of placebo 7, 4.

References

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Research

Montelukast.

Drugs, 1998

Research

Clinical safety and tolerability of montelukast, a leukotriene receptor antagonist, in controlled clinical trials in patients aged > or = 6 years.

Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology, 2001

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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