Leukotriene Inhibitors

Leukotriene inhibitors are asthma medications that inhibit the action of leukotrienes, which are produced by mast cells (like histamine) and released when the cells are activated. When leukotrienes are released, inflammation develops in the broncial tubes causing worsening of the diseases. The medications counteract the effects of leukotrienes.

Brand Names Generic Names

Zyflo Zileuton
Accolate Zarfirlukast
Singulair Montelukast

Drug Action

Zyflo interferes with the early formation of leukotrienes in the body, thus lessening the amount of inflammation present in the bronchial tubes.

Accolate is a leuktriene receptor antagonist. It competes with leukotriene receptor sites in the body, in turn preventing leukotrienes from working in the bronchial tubes is prevented.

Side Effects

Zyflo is generally well tolerated. Side effects may include abdominal pain, indigestion, and nausea. A small number of people may experience an increase in liver enzymes.

Accolate is also well tolerated. Side effects may include headaches.


Zyflo dosing is 600 mg (1 tablet) 4 times a day.

Accolate dosing is 20 mg (1 tablet) 2 times a day. Accolate should be taken 1 hour before or 2 hours after meals. Neither is yet indiacted for children less than 12 years old.

Available Forms

Both are available in tablet form only.

Indications for Use

Both are to be used as preventative medication, to be taken regularly. Neither will relieve symptoms of an asthma attack.

Additional Comments

  • Both Zyflo and Accolate may need to be taken for several weeks to evaluate their effectiveness.
  • Zyflo is contraindicated in people in people with active liver disease. Even in normal people, liver enzymes need to be checked routinely.
  • Caution should be taken when giving Accolate in people with liver disease. It is not contraindicated, but dosages should be monitored closely.

Drug Interactions

Zyflo may increase levels theophylline in the body. Therefore, the dose of theophylline should be decreased and blood levels should be monitored.

Caution should betaken wit the co-administration of Zyflo with propanalol (Inderal), calcium channel blockers, cyclosporine, cisapride (Propulsid), and astemizole (Hismanal).

Caution should also be taken with the administration of Accolate or Zyflo with Warfarin (Coumadin). Warfarin levels should be closely monitored.

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