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ACUTE EXPOSURE INFORMATION

  1. USES: Montelukast is indicated for the prophylaxis and chronic treatment of asthma and acute prevention of exercise-induced bronchoconstriction. It is also indicated for the relief of symptoms of seasonal or perennial allergic rhinitis.
  1. PHARMACOLOGY: Montelukast sodium is a selective and active leukotriene (LTD4, LTE4) receptor antagonist. It binds to cysteinyl leukotrienes (CysLT) type-1 receptors found in the human airway (smooth muscle cells and macrophages), which prevents airway edema, smooth muscle contraction and other respiratory inflammation. The leukotrienes are also released from the nasal mucosa after allergen exposure where montelukast sodium may inhibit symptoms of allergic rhinitis.
  1. EPIDEMIOLOGY: Exposure is common but significant toxicity is rare.
  1. WITH THERAPEUTIC USE
    1. Adverse effects associated with therapeutic montelukast use include fatigue, maculopapular rash, fever, dyspepsia, gastroenteritis, headache, nasal congestion, upper respiratory infection, cough, eosinophilia, elevated liver enzymes, palpitations, vomiting, pancreatitis, paresthesia, hypoesthesia, insomnia, tremor, drowsiness, abnormal dreams, seizures, agitation, suicidal thinking and behavior, and hallucinations. Montelukast and the other leukotriene antagonists have rarely been associated with the development of Churg-Strauss syndrome, a potentially fatal eosinophilic vasculitis, during therapeutic use. This occurred in adult asthma patients, in most of whom concomitant oral steroid doses were reduced. Effects have included worsening pulmonary symptoms, eosinophilia, vasculitic rash, cardiac complications, and neuropathy.
  1. WITH POISONING/EXPOSURE
    1. No clinical effects have been reported in the majority of overdose reports. The most common effects following pediatric overdose include thirst, somnolence, mydriasis, hyperkinesia, and abdominal pain. In postmarketing experience and clinical studies, abdominal pain, somnolence, thirst, headache, vomiting, and psychomotor hyperactivity were reported in adults and children after ingesting montelukast doses as high as 1000 mg.
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