Montelukast

Pronunciation

(mon te LOO kast)

U.S. Brand Names

Singulair®

Synonyms

Montelukast Sodium

Generic Available

Canadian Brand Names

Singulair®

Use

Prophylaxis and chronic treatment of asthma in adults and children

1 year of age; relief of symptoms of seasonal allergic rhinitis in adults and children

2 years of age

Use - Unlabeled/Investigational

Acute asthma

Pregnancy Risk Factor

Pregnancy Implications

Montelukast was not teratogenic in animal studies, however, there are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if clearly needed. Healthcare providers should report any prenatal exposures to the montelukast pregnancy registry at (800) 986-8999.

Lactation

Excretion in breast milk unknown/use caution

Contraindications

Hypersensitivity to montelukast or any component of the formulation

Warnings/Precautions

Montelukast is not FDA approved for use in the reversal of bronchospasm in acute asthma attacks; some clinicians, however, support its use (Cylly, 2003; Camargo, 2003; Ferreira, 2001). Should not be used as monotherapy for the treatment and management of exercise-induced bronchospasm. Advise patients to have appropriate rescue medication available. Appropriate clinical monitoring and caution are recommended when systemic corticosteroid reduction is considered in patients receiving montelukast. Inform phenylketonuric patients that the chewable tablet contains phenylalanine. Safety and efficacy in children <1 year of age have not been established.

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

(As reported in adults)

>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

No specific antidote

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

Drug Interactions

Substrate (major) of CYP2C8/9, 3A4; Inhibits CYP2C8/9 (weak)

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

Herb/Nutraceutical: St John's wort may decrease montelukast levels.

Stability

Store at room temperature of 15°C to 30°C (59°F to 86°F); protect from moisture and light

Granules: Use within 15 minutes of opening packet.

Mechanism of Action

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.

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

Oral:

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

Take dose in the evening. Granules may be administered directly in the mouth or mixed with applesauce, carrots, rice, or ice cream. Administer within 15 minutes of opening packet. Do not mix in liquids.

Dietary Considerations

Tablet, chewable: 4 mg strength contains phenylalanine 0.674 mg; 5 mg strength contains phenylalanine 0.842 mg

Patient Education

Do not stop other asthma medication unless advised by prescriber. Chewable tablet contains phenylalanine. Take every evening on a continuous basis; do not discontinue even if feeling better (this medication may help reduce incidence of acute attacks). Granules may be administered directly in the mouth or mixed with applesauce, carrots, rice, or ice cream (do not mix in liquids); administer within 15 minutes of opening packet. You may experience mild headache (mild analgesic may help); or fatigue or dizziness (use caution when driving). Report skin rash or itching, abdominal pain or persistent GI upset, unusual cough or congestion, feeling of numbness in arms or legs, flu-like illness, or worsening of asthmatic condition. Breast-feeding precaution: Consult prescriber if breast-feeding.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May cause dizziness or drowsiness

Mental Health: Effects on Psychiatric Treatment

Barbiturates may decrease the effects of montelukast; CYP3A4 substrate; nefazodone may increase effects

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]

References

Camargo CA Jr, Smithline HA, Malice MP, et al, "A Randomized Controlled Trial of Intravenous Montelukast in Acute Asthma," Am J Respir Crit Care Med , 2003, 167(4):528-33.

Cylly A, Kara A, Ozdemir T, et al, "Effects of Oral Montelukast on Airway Function in Acute Asthma," Respir Med , 2003, 97(5):533-6.

Ferreira MB, Santos AS, Pregal AL, et al, "Leukotriene Receptor Antagonists (Montelukast) in the Treatment of Asthma Crisis: Preliminary Results of a Double-Blind Placebo Controlled Randomized Study," Allerg Immunol (Paris) , 2001, 33(8):315-8.

International Brand Names

Lukair® (AR); Lukasm® (IT); Montair® (IN); Montegen® (IT); Singulair® (AR, AT, AU, BE, BR, CA, CH, CL, CO, CR, CZ, DE, DK, EC, ES, FI, FR, GB, GT, HN, HR, HU, IE, IL, IT, MX, NL, NO, NZ, PA, PL, PT, RO, RU, SE, SG, SI, SV, TH, TR, YU)

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