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.
Approaches
There are two main approaches to block the actions of leukotrienes.
Inhibition of the 5-lipoxygenase pathway
Drugs such as zileuton block 5-lipoxygenase, inhibiting the synthetic pathway of leukotriene metabolism, whereas drugs such as MK-886 block the 5-lipoxygenase activating protein (FLAP) and may help in treating atherosclerosis. [1]
Antagonism of cysteinyl-leukotriene type 1 receptors
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.
References
- ↑ Jawien J, Gajda M, Rudling M, et al (2006). "Inhibition of five lipoxygenase activating protein (FLAP) by MK-886 decreases atherosclerosis in apoE/LDLR-double knockout mice". Eur. J. Clin. Invest. 36 (3): 141-6. doi:10.1111/j..2006.01606.x.
External links
Drugs for obstructive airway diseases: asthma/COPD (R03) | |
|---|---|
| Adrenergics, inhalants | Short acting β2-agonists: Salbutamol/Levosalbutamol • Fenoterol • Terbutaline Long acting β2-agonists (LABA): Bambuterol • Clenbuterol • Formoterol • Salmeterol other: Epinephrine • Isoproterenol • Orciprenaline |
| Glucocorticoids | Beclometasone • Budesonide • Ciclesonide • Fluticasone • Mometasone |
| Anticholinergics | Ipratropium • Tiotropium |
| Mast cell stabilizers | Cromoglicate • Nedocromil |
| Xanthines | Aminophylline • Theobromine • Theophylline |
| Leukotriene antagonists | Montelukast • Pranlukast • Zafirlukast |
| Combination products | Budesonide/formoterol • Fluticasone/salmeterol • Ipratropium/salbutamol |
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
