Zileuton is an antiinflammatory drug sometimes used to treat asthma. It works by blocking the enzyme 5-LOX, which reduces the production of leukotrienes from arachidonic acid. This leukotriene reduction is helpful in preventing exacerbations in patients with asthma - also known as asthma attacks. One side effect of zileuton to know is hepatotoxicity.

Key Points

  • Zileuton
    • Mechanism
      • Decreased production of leukotrienes
        • Inhibits 5-lipoxygenase (5-LOX), thereby blocking the conversion of arachidonic acid to inflammatory leukotrienes.
          • LTC4, LTD4, LTE4 cause bronchoconstriction. By inhibiting their formation, zileuton can prevent asthma episodes.  
        • Leukotrienes are synthesized from arachidonic acid via the lipoxygenase pathway. Zileuton inhibits this pathway, thus reducing leukotriene production.
    • Clinical indications
      • Asthma
        • Zileuton is used as a prophylactic therapy for asthma.
        • Lipoxygenase inhibitors (eg, zileuton) decrease production of pro-inflammatory leukotrienes and are indicated for treatment of asthma
    • Adverse effects
      • Hepatotoxicity