Leukotriene modifiers are one of the newer classes of drugs for the treatment of asthma. Leukotrienes are chemicals that are released during inflammation. They help to maintain inflammation, increase the production of mucus, and contribute to swelling in the lungs. Individuals who have asthma are more sensitive to the effects of leukotrienes than people without asthma.

Leukotriene modifiers block the body's production or use of leukotrienes?preventing or lessening inflammation and helping to keep airways open.

Drugs in this Class
Zileuton Extended-Release Tablets (Zyflo CR Extended-Release Tablet)
Montelukast Tablets (Montelukast Sodium Tablets, Singulair Tablets)
Zafirlukast (Accolate)

Summarizing the Evidence

• While no clinical trials have compared montelukast, zafirlukast, and zileuton; all three leukotriene modifiers have been shown to be more effective than placebo (inactive sugar pills) in the treatment of asthma.
• In general, however, leukotriene modifiers are not as effective as inhaled corticosteroids or long-acting beta-2 agonists for controlling asthma symptoms.
• Some asthma patients may find taking an oral drug more convenient than using an inhaled asthma medication.
• Usually, the selection of a leukotriene modifier typically depends on the doctor's preference, the patient?s experience with previous treatment, and other medications the patient may be taking (to avoid potential drug interactions).
• The most recent update to national asthma guidelines ?released in 2002 by the National Asthma Education and Prevention Program (NAEPP) and the National Heart, Lung, Blood Institute (NHLBI) Expert Panel ? state that leukotriene modifiers provide an alternative option for patients with mild persistent asthma. The report also advises that leukotriene modifiers can be utilized in combination with low-dose or medium-dose inhaled corticosteroids for moderate persistent asthma.

Dosing and Administration

• Montelukast comes in tablets, chewable tablets, and oral granules which are mixed with a soft food, such as applesauce or ice cream. Usually, montelukast is taken once daily in the evening. Montelukast can be used by children as young as 6 months old, as well as by older children and adults.
• Zafirlukast is available as tablets that typically are taken twice daily, at least one hour before a meal or two hours after a meal. Zafirlukast can be used for individuals who are age 5 or older.
• Zileuton also comes in tablets. It is taken four times per day with meals and at bedtime. Zileuton is for adults and children at least 12 years of age.

Generic Availability

• No generics are available for any of the leukotriene modifiers.

Drug Interactions

Some interactions between medications can be more severe than others. The best way for you to avoid harmful interactions is to tell your doctor and/or pharmacist what medications you are currently taking, including any over-the-counter products, vitamins, and herbals. For specific information on how the drugs interact and the severity of the interaction, please use our Drug Interactions Checker.

Side Effects

To view specific side effect information, please use our Side Effect Checker.

Additional Information

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Last Updated: May 2007

Note: The above information is intended to supplement, not substitute for, the expertise and judgment of your physician, pharmacist, or other healthcare professional. It should not be construed to indicate that the use of the product is safe, appropriate, or effective for you. Consult your healthcare professional before taking any medication.

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