15 Facts About Zafirlukast

Zafirlukast is an orally administered leukotriene receptor antagonist used for the chronic treatment of asthma.

Zafirlukast is extensively hepatically metabolized by an enzyme called CYP2C9.

Zafirlukast was the first cysteinyl leukotriene receptor antagonist approved in the United States.

Zafirlukast is FDA-approved for the prevention and treatment of asthma in adults and children older than 5 years old.

Zafirlukast is considered to be "pregnancy category B " This is due, in part, to the wide safety margin of zafirlukast in animal studies investigating teratogenicity.

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Zafirlukast is contraindicated in people that are hypersensitive or allergic to it.

Zafirlukast is generally well tolerated, though headache and gastrointestinal upset can occur.

Zafirlukast-induced hepatotoxicity is characterized by a spectrum of liver damage symptoms, including fatigue, nausea, and right upper quadrant pain followed by dark urine, jaundice and pruritus.

Zafirlukast is an inhibitor of the hepatic drug-metabolizing enzyme cytochrome P450 family 3 subfamily A member 4 .

Zafirlukast is an antagonist of cysteinyl leukotriene receptor 1, a receptor found throughout the smooth muscle of the lungs, within interstitial lung macrophages, and rarely in epithelial cells.

Zafirlukast is rapidly absorbed into the bloodstream following oral administration, reaching peak plasma levels within 3 hours of taking the dose.

Zafirlukast is moderately distributed into the body's tissues, with an apparent steady state volume of distribution of 70 liters.

Zafirlukast is primarily metabolized by the enzyme CYP2C9 to a hydroxylated metabolite.

Zafirlukast was the first cysteinyl leukotriene receptor antagonist approved in the United States.

Zafirlukast is sometimes used for the treatment of bronchial asthma in cats.