Pronunciation:

(mon te LOO kast)

U.S. Brand Names:

Synonyms:

Generic Available:

Canadian Brand Names:

Use:

Use - Unlabeled/Investigational:

Pregnancy Risk Factor:

Pregnancy Implications:

Lactation:

Contraindications:

Warnings/Precautions:

In rare cases, patients on therapy with montelukast 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.

Adverse Reactions:

>10%: Central nervous system: Headache (18%)

1% to 10%:

Central nervous system: Dizziness (2%), fatigue (2%), fever (2%)

Dermatologic: Rash (2%)

Gastrointestinal: Dyspepsia (2%), dental pain (2%), gastroenteritis (2%), abdominal pain (3%)

Neuromuscular & skeletal: Weakness (2%)

Respiratory: Cough (3%), nasal congestion (2%), upper respiratory infection (2%)

Miscellaneous: Flu-like symptoms (4%), trauma (1%)

Postmarketing and/or case reports: Agitation, anaphylaxis, angioedema, arthralgia, bleeding tendency, bruising, cholestasis (rare), diarrhea, dream abnormalities, drowsiness, edema, eosinophilia, hallucinations, hepatic eosinophilic infiltration (rare), hepatitis, hypoesthesia, insomnia, irritability, muscle cramps, myalgia, nausea, palpitation, pancreatitis, paresthesia, pruritus, restlessness, seizure, urticaria, vasculitis, vomiting

Overdosage/Toxicology:

Remove unabsorbed material from the GI tract, employ clinical monitoring and institute supportive therapy if required

Drug Interactions:

CYP2C8/9 inducers: May decrease the levels/effects of montelukast. Example inducers include carbamazepine, phenobarbital, phenytoin, rifampin, rifapentine, and secobarbital.

CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of montelukast. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.

Ethanol/Nutrition/Herb Interactions:

Stability:

Granules: Use within 15 minutes of opening packet.

Mechanism of Action:

Pharmacodynamics/Kinetics:

Duration: >24 hours

Absorption: Rapid

Distribution: Vd: 8-11 L

Protein binding, plasma: >99%

Metabolism: Extensively hepatic via CYP3A4 and 2C8/9

Bioavailability: Tablet: 10 mg: Mean: 64%; 5 mg: 63% to 73%

Half-life elimination, plasma: Mean: 2.7-5.5 hours

Time to peak, serum: Tablet: 10 mg: 3-4 hours; 5 mg: 2-2.5 hours; 4 mg: 2 hours

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

Dosage:

Children:

6-11 months: Asthma (unlabeled use): 4 mg (oral granules) once daily, taken in the evening

12-23 months: Asthma: 4 mg (oral granules) once daily, taken in the evening

2-5 years: Asthma or seasonal allergic rhinitis: 4 mg (chewable tablet or oral granules) once daily, taken in the evening

6-14 years: Asthma or seasonal allergic rhinitis: Chew one 5 mg chewable tablet/day, taken in the evening

Children 15 years and Adults:

Asthma or seasonal allergic rhinitis: 10 mg/day, taken in the evening

Asthma, acute (unlabeled use): 10 mg as a single dose administered with first-line therapy

Dosing adjustment in renal impairment: No adjustment necessary

Dosing adjustment in hepatic impairment: Mild-to-moderate: No adjustment necessary. Patients with severe hepatic disease were not studied.

Administration:

Dietary Considerations:

Patient Education:

Dental Health: Effects on Dental Treatment:

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

Mental Health: Effects on Mental Status:

Mental Health: Effects on Psychiatric Treatment:

Dosage Forms:

Granules: 4 mg/packet

Tablet: 10 mg

Tablet, chewable: 4 mg [contains phenylalanine 0.674 mg; cherry flavor]; 5 mg [contains phenylalanine 0.842 mg; cherry flavor]

International Brand Names: