Leukotriene Receptor Antagonists - Asthma & Allergy Treatment

Leukotriene receptor antagonists are medications that help control asthma and allergic rhinitis by blocking the action of leukotrienes in the body.

Leukotriene Receptor Antagonists FAQ

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What are leukotriene receptor antagonists?

Leukotriene receptor antagonists are sometimes colloquially referred to as leukasts . Leukotriene receptor antagonists, such as montelukast, zafirlukast, and pranlukast, and 5-lipoxygenase inhibitors, like zileuton and Hypericum perforatum, can be used to treat these diseases.

What is a leukotriene synthesis inhibitor?

Leukotriene-receptor antagonists, such as montelukast and zafirlukast, prevent leukotrienes from binding to their receptors Leukotriene synthesis inhibitors, such as zileuton, block the enzyme, 5-lipoxygenase, which is necessary for the formation of leukotrienes. Montelukast, zafirlukast, and zileuton may be considered for the treatment of asthma.

What is the rationale for leukotriene receptor antagonists (LTRAs)?

LTRAs inhibit the effects of the cysteinyl leukotrienes, which represent 3 of a large number of chemical mediators of asthma. Leukotrienes are released by several types of cells and can cause bronchoconstriction and inflammation 1, 2.

Which leukotriene modifiers are used for allergic rhinitis?

Names of specific leukotriene modifiers include: Montelukast (Singulair®). Zafirlukast (Accolate®). Zileuton (Zyflo®). All three are used to treat asthma, but only montelukast is approved to treat allergic rhinitis. How do leukotriene modifiers work? Montelukast and zafirlukast are leukotriene receptor antagonists.

Are leukotrienes a treatment for asthma and rhinitis?

This topic reviews the biology of the leukotrienes, their role in asthma and inflammation, and the use of 5-lipoxygenase (5-LO) inhibitors and cysteinyl leukotriene (CysLT) receptor antagonists as treatments for asthma, rhinitis, and other allergic diseases.

Which leukotriene receptor antagonist should be stopped?

If a person develops an eosinophilic condition, or a Churg-Strauss syndrome-type illness, the leukotriene receptor antagonist should be stopped. Phenytoin, phenobarbital and rifampicin — These are inducers of CYP 3A4, 2C8 and 2C9 which also metabolise montelukast.