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ACUTE EXPOSURE INFORMATION

  1. USES: Zafirlukast is used for the prophylaxis and chronic treatment of asthma in adults and children 5 years of age and older.
  1. PHARMACOLOGY: Zafirlukast is a selective and competitive receptor antagonist of the cysteinyl leukotrienes D4 and E4. The cysteinyl leukotrienes, originally described as slow-reacting substances of anaphylaxis, produce airway edema, smooth muscle constriction, and altered cellular activity associated with the inflammatory process, all of which are associated with the pathophysiology of asthma.
  1. EPIDEMIOLOGY: Exposure is common, but severe toxicity is rare.
  1. WITH THERAPEUTIC USE
    1. ADVERSE EFFECT: Adverse effects associated with therapeutic zafirlukast use include headache, somnolence, pharyngitis, rhinitis, gastritis, elevation of liver enzymes, and asthma exacerbation; however, the incidence of most of these effects has been similar in placebo-treated patients.
    1. Zafirlukast and the other leukotriene antagonists have been associated with the development of Churg-Strauss Syndrome, a potentially fatal eosinophilic vasculitis, in adult asthma patients in most of whom concomitant oral steroid dose was reduced. Effects have included worsening pulmonary symptoms, eosinophilia, vasculitic rash, cardiac complications and/or neuropathy. This is a rare effect.
  1. WITH POISONING/EXPOSURE
    1. TOXICITY: Four patients developed minimal adverse effects (eg, rash, upset stomach) after ingesting zafirlukast doses as high as 200 mg.
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