Pharmacology

Binds to cysteinyl leukotriene type 1 (CysLT 1) receptor in the upper and lower airways to prevent
leukotriene-mediated effects associated with asthma and allergic rhinitis.

Pharmacokinetics
Absorption
Rapidly absorbed. T max is 3 to 4 h and bioavailability is 64% for the 10 mg oral tablet in the fasted
state. T max is 2 to 2.5 h and bioavailability is 73% (63% if taken with food) for the 5 mg chewable
tablet. T max is 2 h for the 4 mg chewable tablet taken without food. The 4 mg granule formulation is
bioequivalent to the 4 mg chewable tablet when administered in the fasted state. Administration of
granules with a high-fat meal does not affect AUC, but prolongs T max to 6.4 h and decreases C max by
35%.

Distribution
Protein binding is more than 99%. Vd is 8 to 11 L.

Metabolism
Extensively metabolized; plasma concentrations of metabolites are undetectable at steady state.
CYP-450 3A4 and 2C9 are involved in metabolism.

Elimination
Plasma Cl averages 45 mL/min and mean plasma half-life is 2.7 to 5.5 h; 86% is recovered in feces
and less than 0.2% in urine.

Special Populations
Renal Function Impairment
Pharmacokinetics were not evaluated in patients with renal impairment.
Hepatic Function Impairment

AUC increased 41% and half-life was prolonged to 7.4 h in patients with mild to moderate hepatic
impairment and cirrhosis. Patients with severe hepatic impairment or hepatitis have not been
evaluated.
Elderly
Plasma half-life is slightly longer.
Children
In children 6 to 23 mo of age, the systemic exposure to montelukast is higher than in adults.
Gender
Pharmacokinetics are similar in male and female patients.
Race
Differences have not been studied.

Indications and Usage

Prophylaxis and long-term treatment of asthma in patients 12 mo and older; relief of symptoms of
seasonal allergic rhinitis in patients 2 y and older; relief of symptoms of perennial allergic rhinitis in
patients 6 mo and older; prevention of exercise-induced bronchoconstriction (EIB) in patients 6 y and
older.

Unlabeled Uses
Atopic dermatitis, chronic urticaria.

Contraindications
Hypersensitivity to any component of the product.

Dosage and Administration

Asthma
Adults and adolescents 15 y and older

PO 10 mg daily in the evening.

Children 6 to 14 y of age
PO 5 mg daily in the evening (chewable tablet).
Children 2 to 5 y of age
PO 4 mg daily in the evening (chewable tablet or granules).
Children 12 to 23 mo of age
PO 4 mg daily in the evening (granules).
Exercise-induced bronchoconstriction
Adults and adolescents 15 y and older
PO 10 mg at least 2 h prior to exercise. An additional dose should not be taken within 24 h of the
previous dose.
Children 6 to 14 y of age
PO 5 mg at least 2 h prior to exercise (chewable tablet). An additional dose should not be taken
within 24 h of the previous dose.
Perennial Allergic Rhinitis
Adults and adolescents 15 y and older
PO 10 mg daily.
Children 6 to 14 y of age
PO 5 mg once daily (chewable tablet).
Children 2 to 5 y of age
PO 4 mg daily (chewable tablet or granules).
Children 6 to 23 mo of age
PO 4 mg daily (granules).
Seasonal Allergic Rhinitis
Adults and adolescents 15 y and older
PO 10 mg daily.
Children 6 to 14 y of age
PO 5 mg daily (chewable tablet).

Children 2 to 5 y of age
PO 4 mg daily (chewable tablet or granules).

General Advice

Provide patients with appropriate rescue medication.

Patients taking a daily dose for a particular indication, including chronic asthma, should not
take an additional dose to prevent EIB.

Patients with both asthma and allergic rhinitis should take only 1 tablet daily in the evening.

May be taken with or without food.

Oral granules

Do not open a packet containing granules until ready for use; the full dose must be
administered within 15 min of opening the packet.

Granules can be administered directly in the mouth, dissolved in 5 mL of cold or room

temperature baby formula or breast milk, or mixed with a spoonful of cold or room temperature
soft foods (applesauce, carrots, rice, or ice cream only). If mixing with baby formula, breast milk,
or food, do not prepare it ahead of time or store for future use. Discard any unused portion.

Do not dissolve granules in any liquid other than baby formula or breast milk for
administration; however, liquids can be taken subsequent to administration.

Uses for Montelukast Sodium

Asthma
Prevention and long-term symptomatic management of
asthma.1 31 40 43 45 51 53 54 55 56 57 58 59 6069 70 105 109 110 119 Efficacy for this indication demonstrated when the drug was
administered in the evening.1 31 45
In patients with mild persistent asthma, low-dose orally inhaled corticosteroids considered first-line
agents for long-term control.21 44 45 47 70 8086 92 105 110 119 Alternative agents, including certain leukotriene
modifiers (i.e., montelukast, zafirlukast), may be used44 70 80 86 87 88 91 98 99 105 110 119but are less effective than
inhaled corticosteroids and are not preferred as initial therapy. 110 119 121

Slideshow: What is Asthma? Causes, Symptoms, and Treatment

In patients with moderate persistent asthma, low-dose inhaled corticosteroids with a long-acting
inhaled 2-agonist bronchodilator (e.g., salmeterol, formoterol) or monotherapy with medium-dose
inhaled corticosteroids preferred.110 119 However, the National Asthma Education and Prevention
Program (NAEPP) recommends that beneficial effects of long-acting inhaled 2-agonists be weighed
carefully against increased risk of severe asthma exacerbations and asthma-related deaths
associated with daily use of such agents. 119
Alternative agents, including certain leukotriene modifiers (i.e., montelukast, zafirlukast), can be
added to a low dosage of inhaled corticosteroid for treatment of moderate persistent asthma, but
these options are less effective. 110 119 Considerations favoring combination with orally inhaled
corticosteroids include intolerance to long-acting 2-adrenergic agonists, marked preference for oral
therapy, and demonstration of superior responsiveness to these leukotriene modifiers. 119
In adults and children 5 years of age with severe persistent asthma, NAEPP and the Global
Initiative for Asthma (GINA) state that maintenance therapy with inhaled corticosteroids at medium to
high dosages and adjunctive therapy with a long-acting inhaled 2-agonist is
preferred.110 119Alternatives to a long-acting inhaled 2-agonist in such patients receiving medium-dose
inhaled corticosteroids include certain leukotriene modifiers (i.e., montelukast, zafirlukast), but these
agents are generally not preferred. 110 119
In infants and children 4 years of age, NAEPP states that an inhaled corticosteroid at medium or
high dosages and adjunctive therapy with either a long-acting inhaled 2-agonist or montelukast is
the only preferred treatment.119
Maintenance therapy with montelukast may be considered in patients who are unable or unwilling to
comply with therapy using inhaled corticosteroids (e.g., young children). 119
Not recommended for relief of acute bronchospasm; however, may continue therapy during acute
asthma exacerbations.1 53 (See Acute Asthma under Cautions.)

Exercise-induced Bronchospasm

Prevention of exercise-induced bronchospasm. 1 48 49 50 52

Leukotriene modifiers not included as first-line agents or as alternative agents to orally inhaled 2adrenergic agonists in current guidelines;22 70 92 110 119 addition of montelukast may provide additional
measure of control in patients currently maintained on long-term controller therapy. 88 9899
Manufacturer states that patients who experience exacerbations of asthma after exercise should
have a short-acting orally inhaled 2-adrenergic agonist available for rescue.1 98 Not established that
daily administration of montelukast for chronic treatment of asthma prevents acute episodes of
exercise-induced bronchospasm.1

Allergic Rhinitis
Symptomatic management of seasonal or perennial allergic rhinitis. 1 87 93 111 Efficacy for this indication
demonstrated when the drug was administered in the morning or evening. 1

Urticaria
Has been used successfully in patients with chronic idiopathic urticaria; beneficial when added to
existing therapy.83

Montelukast Sodium Dosage and Administration

Administration
Oral Administration
Administer at regular intervals (once daily) without regard to meals. 1 31 45
Administer in the evening in patients with asthma with or without coexisting allergic rhinitis. 1 31 45
May individualize time of administration in patients with allergic rhinitis; administer at the same time
each day.1 125
Administer 2 hours before exercise in patients with exercise-induced bronchospasm; do not take an
additional dose within 24 hours of previous dose.1 125

Oral Granules
Generally used in children 12 months to 5 years of age. 1 Do not open packet until ready to use;
administer full dose within 15 minutes of opening packet and without regard to meals. 1 125

Administer directly in the mouth alone or mix with a teaspoonful (5 mL) of cold or room temperature
baby formula, breast milk, or soft food (i.e., applesauce, carrots, rice, ice cream). 1Granules are not
intended to be dissolved in liquid other than baby formula or breast milk prior to administration;
however, liquids can be taken after administration of the granules. 1 125 (See Stability.)
Do not store granules mixed with food for future use; discard any unused portion. 1 125

Dosage
Available as montelukast sodium; dosage expressed in terms of montelukast. 1

Pediatric Patients
Asthma With or Without Allergic Rhinitis
Oral
Children 1223 months: 4 mg once daily as oral granules. 1
Children 25 years of age: 4 mg once daily as chewable tablets or oral granules. 1 109
Children 614 years of age: 5 mg once daily as chewable tablets. 1
Adolescents 15 years of age: 10 mg once daily as film-coated tablets. 1 45
Additional dosage not needed for treatment of allergic rhinitis in patients already receiving chronic
therapy for asthma.1

Exercise-induced Bronchospasm
Prevention
Oral
Children 614 years of age: 5 mg daily has been used for prevention of exercise-induced
bronchospasm.1 48 49 50 52 77 78
Adolescents 15 years of age: 10 mg once daily as film-coated tablets. 1 48 49 50 52 77 78

Seasonal Allergic Rhinitis With or Without Asthma

Oral
Children 25 years of age: 4 mg once daily as chewable tablets or oral granules. 1
Children 614 years of age: 5 mg once daily as chewable tablets. 1
Adolescents 15 years of age: 10 mg once daily as film-coated tablets. 1

Perennial Allergic Rhinitis With or Without Asthma

Oral
Infants 623 months of age: 4 mg once daily as oral granules. 1
Children 25 years of age: 4 mg once daily as chewable tablets or oral granules. 1
Children 614 years of age: 5 mg once daily as chewable tablets. 1
Adolescents 15 years of age: 10 mg once daily as film-coated tablets. 1

Adults
Asthma With or Without Allergic Rhinitis
Oral
10 mg once daily as film-coated tablets. 1
Additional dosage not needed for treatment of allergic rhinitis in patients already receiving chronic
therapy for asthma.1

Exercise-induced Bronchospasm
Prevention
Oral
10 mg as film-coated tablets.1 48 49 50 52 77 78

Seasonal Allergic Rhinitis With or Without Asthma

Oral
10 mg once daily as film-coated tablets. 1

Perennial Allergic Rhinitis With or Without Asthma

Oral
10 mg once daily as film-coated tablets. 1

Urticaria
Oral
520 mg daily.83

Special Populations

Hepatic Impairment
No dosage adjustment required in patients with mild to moderate hepatic impairment. 1 Not evaluated
in patients with severe hepatic impairment or hepatitis. 1

Renal Impairment
No dosage adjustment required. 1