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Leukotrienes

LEUKOTRIENE INHIBITORS

 

Leukotriene inhibitors block 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 bronchial tubes causing worsening of the diseases.  These medications have been found to be useful in the treatment of asthma, nasal allergies and excercise induced bronchocontriction.

 

Common leukotriene inhibitors

Zyflo – Zileuton

Accolate – Zarfirlukas

Singulair - Montelukast

 

Drug Action
Zyflo interferes with the early formation of leukotrienes in the body by blocking an enzyme, thus lessening the amount of inflammation present in the bronchial tubes.

 

Accolate and Singulair are eukotriene receptor antagonists. They compete with leukotrienes at the receptor sites in the body; in turn preventing leukotrienes from having an affect in the bronchial tubes.

 

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 and therefore, blood tests for liver function should be monitored occasionally.

 

Accolate is also well tolerated.  Side effects may include headaches and elevation in liver enzymes.  Blood test to check liver function should be monitored periodically.

 

Singulair is also well tolerated.  Side effects are rare and may include headaches and sore throat.

 

Dosing

Zyflo is usually taken 4 times a day. 

 

Accolate is usually taken twice a day and should be taken 1 hour before or 2 hours after meals. 

 

Singulair is given once a day and works best when taken in the evening.  It is approved for patients ages 1 year and over.

 

Indications for Use (of all leukotriene inhibitors)
All three drugs are intended to be used as preventative medication and are indicated in the treatment of acute asthma attacks.

 

Additional Comment

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 (of all leukotriene inhibitors)

Zyflo may increase levels theophylline in the body.   Therefore, the dose of theophylline should be decreased and blood levels should be monitored.  Caution should be taken 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) and Warfarin levels should be closely monitored.

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This site was last updated 07/18/08