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Montelukast

Medically reviewed by Drugs.com. Last updated on Jul 11, 2020.

Pronunciation

(mon te LOO kast)

Index Terms

  • Montelukast Sodium

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

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, 5 mg [contains aspartame]

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

Use: Labeled Indications

Allergic rhinitis (perennial or seasonal): Relief of symptoms of seasonal allergic rhinitis in adults and pediatric patients ≥2 years of age and perennial allergic rhinitis in adults and pediatric patients ≥6 months of age. Because the benefits may not outweigh the risk of neuropsychiatric symptoms in patients with allergic rhinitis, reserve use for patients who have had an inadequate response or intolerance to alternative therapies.

Asthma: Prophylaxis and chronic treatment of asthma.

Bronchoconstriction, exercise-induced (prevention): Prevention of exercise-induced bronchoconstriction.

Note: American Academy of Otolaryngology, Head and Neck Surgery (AAO-HNS) and American Academy of Allergy, Asthma, and Immunology (AAAAI) and American College of Allergy, Asthma, and Immunology (ACAAI) guidelines recommend against montelukast use as first-line therapy for allergic rhinitis (except in patients with concurrent asthma) (Dykewicz 2017; Seidman 2015). The Global Initiative for Asthma recommends montelukast in patients with concomitant allergic rhinitis or those who cannot take inhaled corticosteroids (GINA 2020).

Off Label Uses

Chronic urticaria

Data from controlled, double-blind trials regarding the use of montelukast in combination with antihistamines for the management of chronic urticaria are conflicting [Di Lorenzo 2004], [Nettis 2004], [Wan 2009].

Based on clinical practice guidelines from the American Academy of Allergy, Asthma and Immunology (AAAAI); the American College of Allergy, Asthma, and Immunology (ACAAI); the Joint Council of Allergy, Asthma and Immunology (JCAAI); and the World Allergy Organization for the diagnosis and management of acute and chronic urticaria, a leukotriene receptor antagonist may be added to antihistamine therapy in patients who do not respond to antihistamines [AAAAI [Bernstein 2014]], [WAO [Sánchez-Borges 2012]].

Urticaria (nonsteroidal anti-inflammatory drug-induced)

Data from a double-blind, placebo-controlled comparison of montelukast and cetirizine in patients with chronic urticaria and intolerance to food additives and/or aspirin supports the use of montelukast in the treatment of patients experiencing urticaria related to the use of nonsteroidal anti-inflammatory drugs [Pacor 2001].

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)

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Note: Due to risk of neuropsychiatric adverse effects, the benefits and risks of montelukast should be assessed prior to therapy initiation. Patients with both asthma and allergic rhinitis should take only 1 dose in the evening.

Allergic rhinitis:

Perennial:

Infants ≥6 months and Children <6 years: Oral: 4 mg once daily.

Children ≥6 years and Adolescents <15 years: Oral: 5 mg once daily.

Adolescents ≥15 years: Oral: 10 mg once daily.

Seasonal:

Children 2 to 5 years: Oral: 4 mg once daily.

Children ≥6 years and Adolescents <15 years: Oral: 5 mg once daily.

Adolescents ≥15 years: Oral: 10 mg once daily.

Asthma, maintenance therapy: Note: Not preferred therapy for any level of asthma severity; may be considered an alternative option for Step 2 or greater management; inhaled corticosteroids are preferred (GINA 2020).

12 months to 5 years: Oral: 4 mg once daily in the evening.

6 to 14 years: Oral: 5 mg once daily in the evening.

≥15 years: Oral: 10 mg once daily in the evening.

Exercise-induced bronchospasm, prevention:

Note: Additional doses should not be administered within 24 hours. Daily administration to prevent exercise-induced bronchospasm has not been evaluated. Patients receiving montelukast for another indication should not take an additional dose to prevent exercise-induced bronchoconstriction.

Children ≥6 years and Adolescents <15 years: Oral: 5 mg at least 2 hours prior to exercise.

Adolescents ≥15 years: Tablet: Oral: 10 mg at least 2 hours prior to exercise.

Urticaria (nonsteroidal anti-inflammatory drug-induced): Limited data available: Adolescents ≥15 years: Oral: 10 mg once daily (Pacor 2001).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

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, or mixed with a spoonful of cold or room temperature 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 20°C to 25°C (68°F to 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

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 and Ivacaftor: May decrease the serum concentration of Montelukast. Monitor therapy

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

1% to 10%:

Central nervous system: Headache (children and adolescents: ≥2%), dizziness (adolescents and adults: 2%), fatigue (adolescents and adults: ≤2%)

Dermatologic: Atopic dermatitis (children: ≥2%), dermatitis (children: ≥2%), eczema (children: ≥2%), skin infection (children: ≥2%), urticaria (children: ≥2%), skin rash (2%)

Gastrointestinal: Abdominal pain (children: ≥2%), diarrhea (children and adolescents: ≥2%), nausea (children and adolescents: ≥2%), tooth infection (children: ≥2%), dyspepsia (2%), gastroenteritis (2%), toothache (adolescents and adults: 2%)

Genitourinary: Pyuria (adolescents and adults: 1%)

Hepatic: Increased serum aspartate aminotransferase (adolescents and adults: 2%), increased serum alanine aminotransferase (adolescents and adults: ≥1%)

Infection: Influenza (children and adolescents: ≥2%), varicella zoster infection (children: ≥2%), viral infection (children and adolescents: ≥2%)

Neuromuscular & skeletal: Asthenia (adolescents and adults: ≤2%)

Ophthalmic: Conjunctivitis (children: ≥2%), myopia (children: ≥2%)

Otic: Otalgia (children: ≥2%), otitis (children and adolescents: ≥2%), otitis media (children and adolescents: ≥2%)

Respiratory: Cough (3%), acute bronchitis (children: ≥2%), laryngitis (children and adolescents: ≥2%), pharyngitis (children: ≥2%), pneumonia (children: ≥2%), rhinitis (infective; children: ≥2%), rhinorrhea (children: ≥2%), nasal congestion (adolescents and adults: 2%), epistaxis (adolescents and adults: ≥1%), sinus headache (adolescents and adults: ≥1%), sinusitis (≥1%), upper respiratory tract infection (≥1%)

Miscellaneous: Fever (2%), trauma (adolescents and adults: 1%)

<1%, postmarketing and/or case reports: Abnormal dreams, aggressive behavior, agitation, anaphylaxis, angioedema, anxiety, arthralgia, behavioral changes, bleeding tendency disorder, bruise, depression, diarrhea, disorientation, drowsiness, edema, eosinophilia (systemic), eosinophilic granulomatosis with polyangiitis, eosinophilic pneumonitis, epistaxis, erythema multiforme, erythema nodosum, hallucination, hepatic eosinophilic infiltration, hepatitis (mixed pattern, hepatocellular, and cholestatic), hostility, hypersensitivity reaction, hypoesthesia, insomnia, irritability, lack of concentration, memory impairment, mood changes, muscle cramps, myalgia, nausea, obsessive compulsive disorder, palpitations, pancreatitis, paresthesia, pruritus, restlessness, seizure, somnambulism, Stevens-Johnson syndrome, stuttering, suicidal ideation, suicidal tendencies, thrombocytopenia, tic disorder, toxic epidermal necrolysis, tremor, urinary incontinence, urticaria, vasculitis, vomiting

ALERT: U.S. Boxed Warning

Serious neuropsychiatric events:

Serious neuropsychiatric (NP) events have been reported with the use of montelukast. The types of events reported were highly variable, and included, but were not limited to, agitation, aggression, depression, sleep disturbances, suicidal thoughts and behavior (including suicide). The mechanisms underlying NP events associated with montelukast use are currently not well understood.

Because of the risk of NP events, the benefits of montelukast may not outweigh the risks in some patients, particularly when the symptoms of disease may be mild and adequately treated with alternative therapies. Reserve use of montelukast for patients with allergic rhinitis who have an inadequate response or intolerance to alternative therapies. In patients with asthma or exercise-induced bronchoconstriction, consider the benefits and risks before prescribing montelukast.

Discuss the benefits and risks of montelukast with patients and caregivers when prescribing montelukast. Advise patients and/or caregivers to be alert for changes in behavior or new NP symptoms when taking montelukast. If changes in behavior are observed, or if new NP symptoms or suicidal thoughts and/or behavior occur, advise patients to discontinue montelukast and contact a health care provider immediately.

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 eosinophilic granulomatosis with polyangiitis (formerly known as Churg-Strauss), a condition which is often treated with systemic corticosteroid therapy. Health care 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: [US Boxed Warning]: Serious neuropsychiatric (NP) events have been reported with variable effects, including, but not limited to, agitation, aggression, depression, sleep disturbances, suicidal thoughts and behavior (including suicide). The benefits of montelukast may not outweigh the risks in some patients, particularly when the symptoms of disease may be mild and adequately treated with alternative therapies. Reserve use for patients with allergic rhinitis who have an inadequate response or intolerance to alternative therapies. In patients with asthma or exercise-induced bronchoconstriction, consider the benefits and risks before use. NP events have been reported in patients with and without a previous history of psychiatric disorder; most cases occurred during treatment, but some cases were reported after discontinuation of therapy. Symptoms typically resolved after discontinuation of therapy. Discuss benefits and risks of montelukast with patients and caregivers and advise patients and/or caregivers to be alert for changes in behavior or new NP symptoms. Discontinue use and contact a health care provider immediately if changes in behavior are observed, or if new NP symptoms or suicidal thoughts and/or behavior 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.

Dosage form specific issues:

• Chewable tablet: Contains phenylalanine.

Monitoring Parameters

Mood or behavior changes, including suicidal thinking/behavior

Pregnancy Considerations

Based on available data, an increased risk of teratogenic effects has not been observed with montelukast use in pregnancy (GINA 2020).

Uncontrolled asthma is associated with adverse events on pregnancy (increased risk of perinatal mortality, preeclampsia, preterm birth, low-birth-weight infants, cesarean delivery, and the development of gestational diabetes). Poorly controlled asthma or asthma exacerbations may have a greater fetal/maternal risk than what is associated with appropriately used asthma medications. Maternal treatment improves pregnancy outcomes by reducing the risk of some adverse events (eg, preterm birth, gestational diabetes). Maternal asthma symptoms should be monitored monthly during pregnancy. Montelukast should not be withheld during pregnancy when clinically indicated (ERS/TSANZ [Middleton 2020]; GINA 2020).

Data collection to monitor pregnancy and infant outcomes associated with asthma and the medications used to treat asthma in pregnancy is ongoing. Health care providers are encouraged to enroll exposed pregnant females in the MotherToBaby Pregnancy Studies conducted by the Organization of Teratology Information Specialists (OTIS) (877-311-8972 or http://mothertobaby.org). Patients may also enroll themselves.

Patient Education

What is this drug used for?

• It is used to prevent breathing problems that happen with exercise.

• It is used to ease allergy signs.

• It is used to treat or prevent asthma.

• It may be given to you for other reasons. Talk with the doctor.

For breathing problems:

• This drug is not to be used to treat intense flare-ups of shortness of breath. Use a rescue inhaler. Talk with the doctor.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Cough

• Diarrhea

• Headache

• Common cold symptoms

• Abdominal pain

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Depression like thoughts of suicide, anxiety, agitation, irritability, panic attacks, mood changes, behavioral changes, or confusion

• Sleepwalking

• Sensing things that seem real but are not

• Trouble with memory

• Nightmares

• Restlessness

• Trouble focusing

• Abnormal movements

• Trouble breathing

• Flu-like symptoms

• Sinus pain

• Burning or numbness feeling

• Ear pain

• Tremors

• Trouble speaking

• Trouble sleeping

• Stevens-Johnson syndrome/toxic epidermal necrolysis like red, swollen, blistered, or peeling skin (with or without fever); red or irritated eyes; or sores in mouth, throat, nose, or eyes

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

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