No

Leukotriene Receptor Antagonist

Prophylaxis and chronic treatment of asthma in adults and children greater than or equal to 2 years of age

B

Hypersensitivity to any component

Montelukast is not indicated for use in the reversal of bronchospasm in acute asthma attacks, including status asthmaticus. 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 0.842 mg/5 mg chewable tablet.

>10%: Central nervous system: Headache

1% to 10%:

Central nervous system: Dizziness, fatigue, fever

Dermatologic: Rash

Gastrointestinal: Dyspepsia, dental pain, gastroenteritis, diarrhea, nausea, abdominal pain

Neuromuscular & skeletal: Weakness

Respiratory: Cough, nasal congestion, laryngitis, pharyngitis

Miscellaneous: Flu-like symptoms, trauma

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. Physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients. A casual association between montelukast and these underlying conditions has not been established.

No specific antidote

CYP2A6, and 2C9, 3A3/4, enzyme substrate

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.

Duration: >24 hours

Distribution: V_d: 8-11 L

Protein binding, plasma: >99%

Metabolism: Extensively by cytochrome P-450 3A4 and 2C9

Bioavailability: Oral: Mean: 64% for 10 mg tablet and 63% to 73% for 5 mg tablet

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

Time to peak serum concentration: 3-4 hours for 10 mg tablet and 2-2.5 hours for 5 mg tablet

Elimination: Almost exclusively in the bile; fecal (86%), urine (<0.2%)

Oral:

<2 years: Safety and efficacy have not been established

2-5 years: Chew one 4 mg chewable tablet/day, taken in the evening

6 to 14 years: Chew one 5 mg chewable tablet/day, taken in the evening

Children greater than or equal to 15 years and Adults: 10 mg/day, taken in the evening

Dosing adjustment in hepatic impairment: Mild moderate: No adjustment necessary

May cause dizziness or drowsiness

Barbiturates may decrease the effects of montelukast; CYP3A3/4 substrate; nefazodone may increase effects

No information available to require special precautions

No effects or complications reported

This medication is not for an acute asthmatic attack; in acute attack, follow instructions of prescriber. Do not stop other asthma medication unless advised by prescriber. Take every evening on a continuous basis; do not discontinue even if feeling better (this medication may help reduce incidence of acute attacks). You may experience mild headache (mild analgesic may help); fatigue or dizziness (use caution when driving). Report skin rash or itching, abdominal pain or persistent GI upset, unusual cough or congestion, or worsening of asthmatic condition. Breast-feeding precautions: Consult prescriber if breast-feeding.

Tablet, as sodium: 10 mg

Tablet, chewable (cherry), as sodium: 4 mg, 5 mg