- Leukotriene antagonist
A leukotriene antagonist is a
hormone antagonistacting upon leukotrienes.
It has been demonstrated that leukotrienes are implicated in
bronchoconstrictionand 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
Drugs such as
zileutonblock 5-lipoxygenase, inhibiting the synthetic pathway of leukotriene metabolism, whereas drugs such as MK-886block the 5-lipoxygenase activating protein(FLAP) and may help in treating atherosclerosis. [cite journal |author=Jawien J, Gajda M, Rudling M, "et al" |title=Inhibition of five lipoxygenase activating protein (FLAP) by MK-886 decreases atherosclerosis in apoE/LDLR-double knockout mice |journal=Eur. J. Clin. Invest. |volume=36 |issue=3 |pages=141–6 |year=2006 |pmid= |doi=10.1111/j..2006.01606.x |url=http://www.blackwell-synergy.com/doi/abs/10.1111/j..2006.01606.x]
Antagonism of cysteinyl-leukotriene type 1 receptors
Agents such as
montelukastand zafirlukastblock the actions of cysteinyl leukotrienes at the CysLT1receptor 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 lavagefluid. This demonstrates that they have anti-inflammatory properties.
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