Zafirlukast
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Classification: Antiasthmatic Action/Kinetics: A selective and competitive antagonist of leukotriene receptors D 4 and E 4, which are components of slow-reacting substance of anaphylaxis. It is believed that cysteinyl leukotriene occupation of receptors causes asthma, including airway edema, smooth muscle constriction, and altered cellular activity associated with the inflammatory process. Zafirlukast inhibits bronchoconstriction caused by sulfur dioxide and cold air in clients with asthma. It also attenuates the early- and late-phase reaction in asthmatics caused by inhalation of antigens such as grass, cat dander, ragweed, and mixed antigens. Rapidly absorbed after PO use; bioavailabilty may be decreased when taken with food. Peak plasma levels: 3 hr. t 1/2, terminal: About 10 hr. Over 99% bound to plasma proteins. Extensively metabolized in the liver, with about 90% excreted in the feces and 10% in the urine. Inhibits certain cytochrome P450 isoenzymes. Uses: Prophylaxis and chronic treatment of asthma in adults and children 7 years of age and older. Contraindications: Use to terminate an acute asthma attack, including status asthmaticus. Lactation. Special Concerns: The clearance is reduced in clients 65 years of age and older. Safety and efficacy have not been determined in children less than 12 years of age. Side Effects: GI: N&V;, diarrhea, abdominal pain, dyspepsia. CNS: Headache, dizziness. Hepatic: Rarely, symptomatic hepatitis and hyperbilirubinemia. Hypersensitivity reactions: Urticaria, angioedema, rashes (with and without blistering). Miscellaneous: Infection, generalized pain, asthenia, accidental injury, myalgia, fever, back pain, systemic eosinophilia with vasculitis consistent with Churg-Strauss syndrome.
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How Supplied: Tablet: 10 mg, 20 mg
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Zafirllukast plasma levels