(mon te LOO kast)
Prophylaxis and chronic treatment of asthma; relief of symptoms of seasonal allergic rhinitis and perennial allergic rhinitis; prevention of exercise-induced bronchoconstriction.
Note: American Academy of Otolaryngology, Head and Neck Surgery (AAO-HNS) guidelines recommend against montelukast use as first-line therapy for allergic rhinitis (except in patients with concurrent asthma) (Seidman, 2015 [AAO-HNS, 2015]).
Hypersensitivity to montelukast or any component of the formulation
Note: Patients with both asthma and allergic rhinitis should take only one dose in the evening.
Allergic rhinitis (perennial or seasonal): Oral: 10 mg once daily
Asthma: Oral: 10 mg once daily (in the evening)
Bronchoconstriction, exercise-induced (prevention): Oral: 10 mg at least 2 hours prior to exercise. Note: Additional doses should not be administered within 24 hours. Daily administration to prevent exercise-induced bronchoconstriction has not been evaluated. Patients receiving montelukast for another indication should not take an additional dose to prevent exercise-induced bronchoconstriction.
Chronic urticaria (off-label use): Oral: 10 mg once daily (DiLorenzo 2004; Nettis 2004)
Urticaria (nonsteroidal anti-inflammatory drug " “induced) (off-label use): Oral: 10 mg once daily (Pacor 2001)
Refer to adult dosing.
Note: Patients with both asthma and allergic rhinitis should take only one dose in the evening.
Asthma: Oral:
Children ≥1 to <2 years: 4 mg (oral granules) once daily (in the evening)
Children ≥2 to <6 years: 4 mg (chewable tablet or oral granules) once daily (in the evening)
Children ≥6 years and Adolescents <15 years: 5 mg (chewable tablet) once daily (in the evening)
Adolescents ≥15 years: 10 mg once daily (in the evening)
Bronchoconstriction, exercise-induced (prevention): Note: Additional doses should not be administered within 24 hours. Daily administration to prevent exercise-induced bronchoconstriction has not been evaluated. Patients receiving montelukast for another indication should not take an additional dose to prevent exercise-induced bronchoconstriction. Oral:
Children ≥6 years and Adolescents <15 years: 5 mg (chewable tablet) at least 2 hours prior to exercise
Adolescents ≥15 years: 10 mg once daily at least 2 hours prior to exercise
Perennial allergic rhinitis: Oral:
Children 6 months to <2 years: 4 mg (oral granules) once daily
Children ≥2 to <6 years: 4 mg (chewable tablet or oral granules) once daily
Children ≥6 years and Adolescents <15 years: 5 mg (chewable tablet) once daily
Adolescents ≥15 years: 10 mg once daily
Seasonal allergic rhinitis: Oral:
Children ≥2 to <6 years: 4 mg (chewable tablet or oral granules) once daily
Children ≥6 years and Adolescents <15 years: 5 mg (chewable tablet) once daily
Adolescents ≥15 years: 10 mg once daily
Urticaria (nonsteroidal anti-inflammatory drug-induced) (off-label use): Oral: Adolescents ≥15 years: 10 mg once daily (Pacor 2001)
No dosage adjustment necessary.
Mild-to-moderate impairment: No dosage adjustment necessary.
Severe impairment: No dosage adjustment provided in manufacturer 's labeling; has not been studied.
When treating asthma, administer dose in the evening. Patients with allergic rhinitis may individualize administration time (morning or evening). Patients with both asthma and allergic rhinitis should take a single dose in the evening. May administer without regard to food or meals.
Granules: May be administered directly in the mouth, dissolved in 5 mL of baby formula or breast milk, or mixed with a spoonful of applesauce, carrots, rice, or ice cream; do not add to any other liquids or foods. Administer within 15 minutes of opening packet.
Some products may contain phenylalanine.
Store at room temperature of 25 ‚ °C (77 ‚ °F); excursions permitted to 15 ‚ °C to 30 ‚ °C (59 ‚ °F to 86 ‚ °F). Store in original package. Protect from moisture and light. Granules must be used within 15 minutes of opening packet.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Packet, Oral:
Singulair: 4 mg (30 ea)
Generic: 4 mg (1 ea, 30 ea)
Tablet, Oral:
Singulair: 10 mg
Generic: 10 mg
Tablet Chewable, Oral:
Singulair: 4 mg [contains aspartame]
Singulair: 4 mg [DSC] [contains aspartame; cherry flavor]
Singulair: 5 mg [contains aspartame]
Singulair: 5 mg [DSC] [contains aspartame; cherry flavor]
Generic: 4 mg, 5 mg
Amodiaquine: CYP2C8 Inhibitors may increase the serum concentration of Amodiaquine. Avoid combination
Gemfibrozil: May increase the serum concentration of Montelukast. Monitor therapy
Loxapine: Agents to Treat Airway Disease may enhance the adverse/toxic effect of Loxapine. More specifically, the use of Agents to Treat Airway Disease is likely a marker of patients who are likely at a greater risk for experiencing significant bronchospasm from use of inhaled loxapine. Management: This is specific to the Adasuve brand of loxapine, which is an inhaled formulation. This does not apply to non-inhaled formulations of loxapine. Avoid combination
Lumacaftor: May decrease the serum concentration of Montelukast. Monitor therapy
Mood or behavior changes, including suicidal thinking/behavior
Children ≥15 years and Adults:
>10%: Central nervous system: Headache (18%)
1% to 10%:
Central nervous system: Dizziness (2%), fatigue (2%), fever (2%)
Dermatologic: Skin rash (2%)
Gastrointestinal: Dyspepsia (2%), gastroenteritis (2%), toothache (2%)
Hepatic: Increased serum AST (2%), increased serum ALT ( ≥1%)
Neuromuscular & skeletal: Weakness (2%)
Respiratory: Nasal congestion (2%), cough ( ≥1%), epistaxis ( ≥1%), sinusitis ( ≥1%), upper respiratory tract infection ( ≥1%)
Children 2 to ≤14 years: ≥2%:
Central nervous system: Fever, headache
Dermatologic: Dermatitis, eczema, skin rash, urticaria
Gastrointestinal: Abdominal pain, dyspepsia, gastroenteritis, nausea
Infection: Influenza, varicella, viral infection
Ophthalmic: Conjunctivitis
Otic: Otalgia, otitis
Respiratory: Laryngitis, pharyngitis, pneumonia, rhinorrhea, sinusitis, upper respiratory tract infection
Children 6 to 23 months: ≥2%:
Respiratory: Cough, otitis media, pharyngitis, rhinitis, tonsillitis, upper respiratory tract infection, wheezing
Postmarketing and/or case reports (Limited to important or life-threatening): Churg-Strauss syndrome, depression, disorientation, eosinophilia (systemic), eosinophilic pneumonitis, erythema multiforme, erythema nodosum, hallucination, hepatic eosinophilic infiltration, hepatitis (mixed pattern, hepatocellular, and cholestatic), hypersensitivity, insomnia, memory impairment, pancreatitis, paresthesia, seizure, somnambulism, Stevens-Johnson syndrome, suicidal ideation, suicidal tendencies, thrombocytopenia, toxic epidermal necrolysis, urinary incontinence (children)
Following a single 10 mg dose, AUC increased 41% and half-life was prolonged to 7.4 hours in patients with mild-to-moderate hepatic impairment and cirrhosis. Patients with severe hepatic impairment or hepatitis have not been evaluated.
Plasma half-life is slightly longer in elderly patients.
In children 6-23 months of age, the systemic exposure to montelukast is higher than in adults.
Concerns related to adverse effects:
- Eosinophilia and vasculitis: In rare cases, patients may present with systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition which is often treated with systemic corticosteroid therapy. Healthcare providers should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients. A causal association between montelukast and these underlying conditions has not been established.
- Neuropsychiatric events: Postmarketing reports of behavioral changes (eg, abnormal dreams, agitation, aggression, anxiety, attention deficit, depression, disorientation, hallucinations, hostility, insomnia, irritability, memory disturbances, restlessness, sleep disturbance, suicide ideation/behavior, and tremor) have been noted in pediatric, adolescent, and adult patients. In a retrospective analysis performed by Merck, serious behavior-related events were rare (Philip, 2009a); assess patients for behavioral changes. Patients should be instructed to notify the prescriber if behavioral changes occur.
Disease related concerns:
- Acute asthma/bronchospasm: Not FDA approved for use in the reversal of bronchospasm in acute asthma attacks, including status asthmaticus. Some studies, however, support its use as adjunctive therapy (Cylly, 2003; Ferreira, 2001; Harmancik, 2006). Appropriate rescue medication should be available. Montelukast treatment should continue during acute asthma exacerbation.
- Aspirin-sensitive asthmatics: Montelukast will not interrupt bronchoconstrictor response to aspirin or other NSAIDs. Patients with known aspirin sensitivity should continue to avoid these agents.
Concurrent drug therapy issues:
- Corticosteroids: When inhaled or systemic corticosteroid reduction is considered in patients initiating or receiving montelukast, appropriate clinical monitoring and a gradual dose reduction of the steroid are recommended.
- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Dosage form specific issues:
- Chewable tablet: Contains phenylalanine.
B
Adverse events have not been observed in animal reproduction studies. Structural defects have been reported in neonates exposed to montelukast in utero; however, a specific pattern and relationship to montelukast has not been established. Based on available data, an increased risk of teratogenic effects has not been observed with montelukast use in pregnancy (Bakhireva 2007; Nelsen 2012; Sarkar 2009). Uncontrolled asthma is associated with adverse events on pregnancy (increased risk of perinatal mortality, pre-eclampsia, preterm birth, low birth weight infants). Montelukast may be considered for use in women who had a favorable response prior to becoming pregnant; however, initiating a leukotriene receptor antagonist during pregnancy is an alternative (but not preferred) treatment option for mild persistent asthma (NAEPP 2005).
Selective leukotriene receptor antagonist that inhibits the cysteinyl leukotriene receptor. Cysteinyl leukotrienes and leukotriene receptor occupation have been correlated with the pathophysiology of asthma, including airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma. Cysteinyl leukotrienes are also released from the nasal mucosa following allergen exposure leading to symptoms associated with allergic rhinitis (Jarvis, 2000).
Rapid
Vd: 8-11 L
Extensively hepatic via CYP3A4, 2C8, and 2C9
Feces (86%); urine (<0.2%)
Tablet: 10 mg: 3 to 4 hours (fasting); Chewable tablet: 4 mg (children 2 to 5 years): 2 hours (fasting); Chewable tablet 5 mg: 2 to 2.5 hours (fasting); Granules: 2.3 ‚ ± 1 hours (fasting) and 6.4 ‚ ± 2.9 hours (with high-fat meal)
>24 hours
2.7-5.5 hours; Mild-to-moderate hepatic impairment: 7.4 hours
Plasma: >99%
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience cough, diarrhea, headache, pharyngitis, abdominal pain, rhinitis, rhinorrhea, or loss of strength and energy. Have patient report immediately to prescriber signs of depression (suicidal ideation, anxiety, emotional instability, or illogical thinking), signs of liver problems (dark urine, feeling tired, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin or eyes), signs of pancreatitis (severe abdominal pain, severe back pain, severe nausea, or vomiting), hallucinations, behavioral changes, memory impairment, difficulty breathing, flu-like symptoms, seizures, arrhythmia, angina, confusion, burning or numbness feeling, bruising, bleeding, ear pain, tremors, or insomnia (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.