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Leukotriene Modifiers

Description:
Leukotrienes are very powerful chemical mediators synthesized and released by mast cells in the respiratory tract that result in bronchospasm, tissue edema (swelling) and attraction of inflammatory cells such as eosinophils. Leukotrienes have long been identified as an important cause in asthma. Studies have shown that leukotrienes are formed from fatty acids through a specific series of chemical reactions referred to as the leukotriene pathway or more specifically where leukotriene modifiers are concerned, the 5-lipoxygenase pathway. As more leukotrienes accumulate at the end of this pathway, symptoms of asthma develop. Leukotriene modifiers either interfere with the sequence of chemical reactions in the 5-lipoxygenase pathway, or interfere with the binding of leukotrienes with their corresponding receptors in the airways and thus limit their ability to cause asthmatic symptoms.

TABLE 11

Leukotriene Modifiers

Brand Name
Generic Name
Dose
Other Instructions
Accolate® zafirlukast 20mg tablet twice a day use 1 hour before, or
2 hours after meals
10mg tablet twice a day
(5 - 11 years)
Singulair® montelukast 10mg tablet once a day, not affected by meals
(ages 15 years and older)
5mg tablet once a day,
(6 - 14 yrs)
4mg chewable tablet once
a day (2 - 5 years)
4mg granules once a day
(12 - 24 months)

Use:
Treatment of asthma with leukotriene modifiers can improve lung function, decrease the need for sympathomimetic inhalers (e.g. albuterol) and reduce symptoms. Although these medications are effective, they do not appear to be quite as effective as oral or inhaled corticosteroids in controlling asthma. Further, there is no clear evidence that leukotriene modifiers prevent remodeling of the airways as does treatment with corticosteroids.

Additionally, leukotriene modifiers may be very effective in treating some individuals with asthma, while having little or no effect in others. In contrast, corticosteroids are effective in controlling asthmatic symptoms in the vast majority of individuals. That being said, The Asthma Center specialists have found the combination of corticosteroids and leukotriene modifiers to be beneficial. Use of both leukotriene modifiers and corticosteroids can result in better control of asthmatic symptoms than with either medication alone in some individuals, while also allowing reduction of the dose of corticosteroids needed to achieve good clinical control of asthmatic symptoms.

Leukotriene modifiers include the leukotriene-receptor antagonists montelukast (Singulair®) and zafirlukast (Accolate®).

Risks and Precautions:
Side effects are uncommon but include: headache, nausea, stomach upset, pain, fever, muscle ache, fatigue, sore throat, laryngitis and liver enzyme elevation. These medications are usually well tolerated. Churg Strauss syndrome, a form of vascular inflammation, rarely is noted with these medications and can include vague symptoms of fever, fatigue, weight loss, vasculitis leading to kidney disease, hypotension, abdominal pain, bowel damage, heart disease, muscle aches and wasting, nervous system damage and arthritis. Liver function abnormalities have been reported with all of these agents and should be periodically monitored.

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