Trade Names:Accolate- Tablets 10 mg- Tablets 20 mg
Inhibits 3 leukotriene receptor types. Leukotrienes have been associated with the longer, inflammatory component of asthma.
Rapidly absorbed. T max is 3 h. Bioavailability is unknown. Administration with food reduced the mean bioavailability about 40%.
At least 99% bound to proteins (predominantly albumin). Vd is 70 L. Minimal distribution across blood-brain barrier.
Extensively metabolized. Most common metabolic products are hydroxylated metabolites, which are excreted in feces. These metabolites are formed through the CYP-450 2C9 pathway. Inhibits CYP3A4 and CYP2C9 isoenzymes.
Oral Cl is about 20 L/h. Biliary route is primary route of excretion. Urinary excretion accounts for about 10% of the dose, while the rest is excreted in feces. The terminal t ½ is about 10 h. The plasma t ½ is about 8 to 16 h.
Approximately 50% to 60% greater C max and AUC compared with healthy subjects.Elderly
Oral Cl decreases with age. In patients older than 65 yr of age, there are about 2- to 3-fold greater C max and AUC compared with young adults.
Prophylaxis and chronic treatment of asthma in adults and children 5 yr of age and older.
PO 20 mg twice daily.Children 5 to 11 yr of age
PO 10 mg twice daily.
Store tablets at controlled room temperature (68° to 77°F). Protect from light and moisture.
Increased zafirlukast plasma levels.Erythromycin, theophylline
Lowered zafirlukast plasma concentrations.Warfarin
Zafirlukast potentiates the hypoprothrombinemic effect of warfarin. Significant increase in the PT may result.
None well documented.
Headache (13%); dizziness (2%).
Nausea, diarrhea (3%); vomiting (2%); dyspepsia (1%).
ALT elevations (2%).
Hypersensitivity (including urticaria, angioedema, rashes).
Infection (4%); pain, asthenia, abdominal pain, accidental injury, fever, back pain (2%).
Category B .
Excreted in breast milk.
Safety and efficacy in children younger than 5 yr of age not established.
Drug Cl decreases with age.
Zafirlukast is not effective in treating acute asthmatic symptoms, but it can be continued during these times.
Elderly patients experienced an increased frequency of infections (primarily respiratory) compared with placebo-treated patients. These appeared to be associated with coadministration of inhaled corticosteroids.
Rash, upset stomach.
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