Montelukast Sodium
Pronouncation: (mon-te-LOO-kast SOE-dee-um)Class: Leukotriene receptor antagonist
Trade Names:
Singulair
- Tablets 10 mg
- Tablets, chewable 4 mg
- Tablets, chewable 5 mg
- Granules 4 mg/packet
Pharmacology
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Binds to cysteinyl leukotriene type 1 receptors in the upper and lower airways to prevent leukotriene-mediated effects associated with asthma and allergic rhinitis.
Pharmacokinetics
Absorption
T max is 3 to 4 h and bioavailability is 64% for 10 mg oral tablet. T max is 2 to 2.5 h and bioavailability is 73% (63% if taken with food) for 5 mg chewable tablet. T max is 2 h for 4 mg chewable tablet. The 4 mg granule formulation is bioequivalent to the 4 mg chewable tablet when administered in fasted state. Administration of granules with high-fat meal does not affect AUC but prolongs T max to 6.4 h.
Distribution
Protein binding greater than 99%. Vd is 8 to 11 L/kg.
Metabolism
Extensively metabolized; plasma concentrations of metabolites are undetectable at steady state. CYP-450 3A4 and 2C9 are involved in metabolism.
Elimination
Plasma clearance averages 45 mL/min and mean plasma t ½ is 2.7 to 5.5 h; 86% recovered in feces and less than 0.2% in urine.
Special Populations
Hepatic Function ImpairmentAUC increased 41% and t ½ prolonged to 7.4 h in patients with mild to moderate hepatic function impairment.
ElderlyPlasma t ½ is slightly longer.
Indications and Usage
Prophylaxis and chronic treatment of asthma in patients 12 mo of age and older; relief of symptoms of seasonal allergic rhinitis in patients 2 yr of age and older; relief of symptoms of perennial allergic rhinitis in patients 6 mo of age and older.
Prevention of exercise-induced bronchoconstriction (EIB) in patients 15 yr of age and older.
Unlabeled Uses
Chronic urticaria, atopic dermatitis.
Contraindications
Standard considerations.
Dosage and Administration
AsthmaAdults and Children 12 mo of age and older
PO Once daily. Adults and adolescents 15 yr of age and older: 10 mg daily. Children 6 to 14 yr of age: 5 mg daily. Children 12 mo to 5 yr of age: 4 mg daily.
EIBAdults and Children 15 yr of age and older
PO 10 mg 2 h prior to exercise. An additional dose should not be taken within 24 h of the previous dose.
Seasonal Allergic RhinitisAdults and Children 2 yr of age and older
PO Once daily.
Adults and adolescents 15 yr of age and olderPO 10 mg daily.
Children 6 to 14 yr of agePO 5 mg daily.
Children 2 to 5 yr of agePO 4 mg daily.
Perennial Allergic RhinitisAdults and Children 6 mo and older
PO Once daily.
Adults and adolescentsPO 15 yr of age and older: 10 mg daily.
Children 6 to 14 yr of agePO 5 mg daily.
Children 6 mo to 5 yr of agePO 4 mg daily.
General Advice
- Patients taking a daily dose for a particular indication (including chronic asthma) should not take an additional dose to prevent EIB.
- Do not open packet containing granules until ready for use; the full dose must be administered within 15 min after opening packet.
- Granules can be administered directly in the mouth, dissolved in 1 teaspoonful (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 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.
Storage/Stability
Store at controlled room temperature (59° to 86°F). Protect from moisture and light.
Drug Interactions
Phenobarbital, rifampinMay decrease montelukast levels.
Laboratory Test Interactions
None well documented.
Adverse Reactions
Cardiovascular
Cardiac complications, palpitations (postmarketing).
CNS
Headache (18%); asthenia/fatigue, dizziness (2%); abnormal dreams, depression, drowsiness, hallucinations, insomnia, paraesthesia/hypoesthesia, psychomotor hyperactivity (including irritability, agitation, aggressive behavior, restlessness, and tremor), seizures (postmarketing).
Dermatologic
Atopic dermatitis, dermatitis, eczema, skin infection, urticaria (at least 2%); rash (2%); vasculitic rash (postmarketing).
EENT
Conjunctivitis, ear pain, myopia, otitis, pharyngitis, rhinorrhea, sinusitis, tonsillitis (at least 2%); nasal congestion (2%); epistaxis (at least 1%).
GI
Diarrhea, dyspepsia, gastroenteritis, laryngitis, nausea, tooth infection (at least 2%); dental pain, infectious gastroenteritis (2%); pancreatitis, vomiting (postmarketing).
Hematologic-Lymphatic
Bruising, eosinophilia, increased bleeding tendency (postmarketing).
Hepatic
Cholestatic hepatitis, hepatocellular liver-injury, mixed-pattern liver injury (postmarketing).
Lab Tests
ALT/AST increased (2%); pyuria (1%).
Musculoskeletal
Arthralgia, myalgia including muscle cramps (postmarketing).
Respiratory
Influenza (4%); cough (3%); acute bronchitis, pneumonia, upper respiratory tract infection, wheezing (at least 2%); worsening of pulmonary symptoms (postmarketing).
Miscellaneous
Abdominal pain (3%); fever, varicella, viral infection (at least 2%); trauma (1%); edema, hypersensitivity (including anaphylaxis, pruritus, urticaria, and hepatic eosinophilic infiltration) (postmarketing).
Precautions
Pregnancy
Category B .
Lactation
Undetermined.
Children
Safety and efficacy not established for treatment of asthma in patients younger than 12 mo of age. Safety and efficacy not established for treatment of allergic rhinitis in patients younger than 2 yr of age. Safety and efficacy not established for treatment of perennial allergic rhinitis in patients younger than 6 mo of age. Safety and efficacy not established for treatment of EIB in patients younger than 15 yr of age.
Acute asthma attacks
Do not use for reversal of bronchospasm in acute asthma attacks, including status asthmaticus.
Concurrent corticosteroids
Do not abruptly substitute montelukast for inhaled or oral corticosteroids.
Eosinophilic conditions
Systemic eosinophilia may occur, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome.
Exercise-induced asthma
Do not use montelukast as monotherapy for treatment and management of EIB.
Phenylketonuria
Montelukast chewable tablets contain phenylalanine.
Overdosage
Symptoms
Abdominal pain, headache, hyperkinesia, mydriasis, somnolence, thirst, vomiting.
Patient Information
- Advise patient to read patient information leaflet before using the first time and to reread and check for new information with each refill.
- Caution patient with asthma not to decrease the dose or stop taking any other asthma medications unless advised by health care provider.
- Advise patient that montelukast can be taken without regard to meals, but to take with food if stomach upset occurs.
- Advise patient with asthma or asthma and allergic rhinitis to take prescribed dose once daily in the evening.
- Advise patient with allergic rhinitis to take prescribed dose once daily at a time that is convenient, but at about the same time each day.
- Advise patient or caregiver using granules that packet containing granules should not be opened until ready for use and that the full dose must be administered within 15 min. Granules can be administered directly in the mouth, dissolved in 1 teaspoonful (5 mL) of cold or room temperature formula or breast milk, or mixed with a spoonful of cold or room temperature soft foods (applesauce, carrots, rice, or ice cream only). Caution patient or caregiver mixing granules with baby formula, breast milk, or food not to prepare ahead of time or store for future use. Instruct patient to discard any unused portion.
- Caution patient with asthma that medication is not to be used to treat acute asthma attacks. Instruct patient to always have a short-acting beta-agonist available for acute treatment of asthma symptoms.
- Instruct patient to take montelukast every day as prescribed, even when symptoms have been controlled.
- Caution patient not to increase montelukast dose or frequency of use, but to notify health care provider if symptoms return or worsen, or, for patient with asthma, if the need for rescue medication increases, or if rescue medication does not seem to work as well.
- Advise patient with EIB to use the usual regimen of beta-agonists as prophylaxis unless otherwise instructed by health care provider.
- Advise patient with known aspirin sensitivity to continue avoidance of aspirin and NSAIDs while taking montelukast.
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Hay Fever, Asthma -- Maintenance, Bronchospasm Prophylaxis
