Leukotriene antagonist
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A leukotriene antagonist is a hormone antagonist acting upon leukotrienes.
It has been demonstrated that leukotrienes are implicated in the inflammatory cascade leading to asthma. Leukotriene modifiers are an important therapeutic advance in managing asthma.
There are two main approaches to block the actions of leukotrienes.
- Inhibition of the 5-lipoxygenase pathway
- Antagonism of cysteinyl-leukotriene type 1 receptors
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- Agents such as montelukast and zafirlukast block the actions of cysteinyl leukotrienes at the CysLT1 receptor on target cells such as bronchial smooth muscle.
These modifiers have been shown to improve asthma symptoms, reduce asthma exacerbations and limit markers of inflammation such as eosinophil counts in the peripheral blood and bronchoalveolar lavage fluid. This demonstrates that they have anti-inflammatory properties.
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