USMLE

Montelukast & Zafirlukast

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Respiratory Pharm
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  6. Montelukast & Zafirlukast
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  13. Theophylline

Summary

Montelukast and Zafirlukast are drugs used to treat asthma. They work as antagonists or blockers of leukotriene receptors. When administered in an inhaled formulation, these drugs can treat asthma by blocking the actions of leukotrienes at the airways, reducing inflammation and bronchoconstriction.

Key Points

  • Montelukast, Zafirlukast
    • Drug Names
      • -lukast (montelukast, zafirlukast)
    • Mechanism
      • Acts as antagonist of leukotriene receptors
        • Specifically blocks leukotriene D4  receptor
          • Prevents signaling by leukotrienes, which induces inflammation and bronchoconstriction
    • Indications
      • Asthma
        • Treats atopic, aspirin-induced, and exercise-induced asthma
          • Used for chronic asthma prophylaxis by increasing airway caliber and reducing mucosal inflammation