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Montelukast is an oral leukotriene receptor antagonist (LTRA)

Leukotrienes are a family of eicosanoid inflammatory mediators of asthma. They are generated from arachidonic acid as a result of the 5-lipoxygenase action in multiple inflammatory cells, particularly mast cells, basophils, eosinophils, neutrophils and macrophages.

Leukotrienes bind to cysteinyl leukotriene (CysLT) receptors. The CysLT type-1 (CysLT1) receptor is found in the human airway, its activation is responsible for smooth muscle contraction (bronchospasm), increase in bronchial reactivity (mucus secretion), in vascular permeability and in eosinophil recruitment in asthmatics.

Montelukast acts as an antagonist of the cysteinyl-leukotriene-receptor CysLT1, and then is able to attenuate the bronchoconstriction.

Another drug of the leukotriene receptor antagonist (LTRA) class is Zafirlukast (Accolate®). Montelukast is the preferred drug of its class due to its once daily dosing regimen, lack of pharmacokinetic interactions and unaltered food bioavailability.


FDA approved:

  • Prophylaxis and chronic treatment of asthma in patients 12 months of age and older. (Montelukast is not indicated for use in acute asthma attacks)
  • Acute prevention of exercise-induced bronchoconstriction (EIB) in patients 6 years of age and older.
  • Relief of symptoms of allergic rhinitis (AR): seasonal allergic rhinitis (SAR) in patients 2 years of age and older, and perennial allergic rhinitis (PAR) in patients 6 months of age and older.

[edit] DOSAGE


15 years and older:

  • Asthma, seasonal or perennial allergic rhinitis: 10 mg/day, taken in the evening.
  • Acute prevention of exercise-induced bronchoconstriction: 10 mg at least 2 hours before exercise

6-14 years:

  • Asthma, seasonal or perennial allergic rhinitis: 5 mg chewable tablet/day, taken in the evening
  • Acute prevention of exercise-induced bronchoconstriction: 5 mg at least 2 hours before exercise

2-5 years:

  • Asthma, seasonal or perennial allergic rhinitis: 4 mg chewable tablet or one packet of 4-mg oral granules, taken in the evening

12-23 months:

  • Asthma or perennial allergic rhinitis: one packet of 4-mg oral granules, taken in the evening

6-12 months:

  • Perennial allergic rhinitis: one packet of 4-mg oral granules, taken in the evening


  • 10 mg Film Coated Tablets
  • 5 mg and 4 mg Chewable Tablets
  • 4 mg Oral Granules


  • Hypersensitivity to any component of this product


  • Concomitant Corticosteroid Use: While the dose of inhaled corticosteroid may be reduced gradually under medical supervision, Montelukast should not be abruptly substituted for inhaled or oral corticosteroids.
  • Neuropsychiatric events have been reported in adult, adolescent, and pediatric patients taking Montelukast. Post-marketing reports with Montelukast use include agitation, aggressive behavior or hostility, anxiousness, depression, disorientation, disturbance in attention, dream abnormalities,hallucinations, insomnia, irritability, memory impairment, restlessness, somnambulism, suicidal thinking and behavior (including suicide), and tremor.


No dose adjustment is needed when Montelukast is co-administered with theophylline, prednisone, prednisolone, oral contraceptives, terfenadine, digoxin, warfarin, gemfibrozil, itraconazole, thyroid hormones, sedative hypnotics, NSAIDs, benzodiazepines, decongestants, and Cytochrome P450 enzyme inducers.


  • Pregnancy Category B (US). There are no adequate and well-controlled studies in pregnant women. Montelukast should be used during pregnancy only if clearly needed.
  • Nursing Mothers: It is not known if montelukast is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Montelukast is given to a nursing mother.


Possible common adverse reactions : upper respiratory infection, headache, cough, epistaxis, increased ALT and somnolence.




Asthma / Chronic obstructive pulmonary disease (COPD)
Adrenergics, inhalants Short acting β2-agonists Fenoterol (Berotec)   Levosalbutamol (Xopenex)   Salbutamol (Ventolin)   Terbutaline (Bricanyl)
Long acting β2-agonists (LABA) Arformoterol (Brovana)   Clenbuterol (Spiropent)   Formoterol (Foradil)   Salmeterol (Serevent)
Ultra long acting β2-agonists Indacaterol   Olodaterol   Vilanterol
Inhaled corticosteroids Beclomethasone (Inhaler)   Budesonide (Inhaler)   Ciclesonide (Inhaler)   Flunisolide (Inhalation suspension)   Fluticasone (Inhaler)   Mometasone (Inhaler)
Anticholinergics (Muscarinic antagonists) Aclidinium bromide   Glycopyrronium bromide   Ipratropium bromide   Oxitropium bromide (Inhalation suspension)   Tiotropium bromide
Mast cell stabilizers Cromoglicate   Nedocromil
Monoclonal anti-IgE antibody Omalizumab
Xanthine derivatives Aminophylline   Bamifylline   Doxofylline   Dyphylline   Theophylline
Eicosanoid inhibition Leukotriene antagonists Montelukast   Pranlukast   Zafirlukast
Thromboxane receptor antagonists Ramatroban   Seratrodast
Non-xanthine PDE4 inhibitors Ibudilast   Roflumilast
Combination products Corticosteroid + Long acting Beta2 agonist Beclomethasone/Formoterol (Inhaler)   Fluticasone/Salmeterol (Inhaler)   Fluticasone/Vilanterol   Mometasone/Formoterol
Corticosteroid + Short acting Beta2 agonist Beclomethasone/Salbutamol   Salbutamol/Flunisolide (Inhalation suspension)   Salbutamol/Flunisolide (Inhaler)
Short acting Beta2 agonist + Muscarinic antagonist Fenoterol/Ipratropium bromide (Inhaler)   Levosalbutamol/Ipratropium   Salbutamol/Ipratropium bromide