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Montelukast

Pronunciation

Pronunciation

(mon te LOO kast)

Index Terms

  • Montelukast Sodium

Dosage Forms

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

Brand Names: U.S.

  • Singulair

Pharmacologic Category

  • Leukotriene-Receptor Antagonist

Pharmacology

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).

Absorption

Rapid

Distribution

Vd: 8-11 L

Metabolism

Extensively hepatic via CYP3A4, 2C8, and 2C9

Excretion

Feces (86%); urine (<0.2%)

Time to Peak

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)

Duration of Action

>24 hours

Half-Life Elimination

2.7-5.5 hours; Mild-to-moderate hepatic impairment: 7.4 hours

Protein Binding

Plasma: >99%

Special Populations: Hepatic Function Impairment

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.

Special Populations: Elderly

Plasma half-life is slightly longer in elderly patients.

Special Populations: Children

In children 6-23 months of age, the systemic exposure to montelukast is higher than in adults.

Use: Labeled Indications

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]).

Use: Unlabeled

Urticaria (nonsteroidal anti-inflammatory drug–induced)

Contraindications

Hypersensitivity to montelukast or any component of the formulation

Dosing: Adult

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)

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

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)

Dosing: Renal Impairment

No dosage adjustment necessary.

Dosing: Hepatic Impairment

Mild-to-moderate impairment: No dosage adjustment necessary.

Severe impairment: No dosage adjustment provided in manufacturer’s labeling; has not been studied.

Administration

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.

Dietary Considerations

Some products may contain phenylalanine.

Storage

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.

Drug Interactions

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

Adverse Reactions

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)

Warnings/Precautions

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.

Monitoring Parameters

Mood or behavior changes, including suicidal thinking/behavior

Pregnancy Risk Factor

B

Pregnancy Considerations

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).

Patient Education

• 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.

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