Everyone Healthy medication library
Leukotriene receptor antagonist Drug Class
Medicines in this drug class are grouped together in the Everyone Healthy medication database. This page is educational only and should not be used as personal prescribing advice.
Drug class overview
Leukotriene receptor antagonist overview
Leukotriene antagonist
Aleukotriene antagonist is a drug that inhibits leukotrienes, which are fatty compounds produced by the immune system that cause inflammation in asthma and bronchitis, and constrict airways.
Leukotriene inhibitors (or modifiers), such as montelukast, zafirlukast and zileuton, are used to treat those diseases. Leukotriene inhibitors are less effective than corticosteroids, but have virtually no side effects, so they are often used to treat children.[1]
Approaches
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| Systematic (IUPAC) name | |
|---|---|
| 2-[1-[[(1R)-1-[3-[2-(7-chloroquinolin-2-yl)ethenyl] phenyl]-3-[2-(2-hydroxypropan-2-yl)phenyl]propyl] sulfanylmethyl]cyclopropyl]acetic acid |
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| Identifiers | |
| CAS number | 158966-92-8 |
| ATC code | R03DC03 |
| PubChem | 60951 |
| DrugBank | APRD00434 |
| Chemical data | |
| Formula | C35H36ClNO3S |
| Mol. mass | 586.184 g/mol |
| SMILES | eMolecules & PubChem |
| Pharmacokinetic data | |
| Bioavailability | 63% to 73% |
| Protein binding | 99% |
| Metabolism | Hepatic (CYP3A4 and CYP2C9-mediated) |
| Half life | 2.7-5.5 hours |
| Excretion | Biliary |
| Therapeutic considerations | |
| Pregnancy cat. | B (U.S.), B1 (Au) |
| Legal status | ℞-only (U.S.), POM (UK), S4 (Au) |
| Routes | Oral
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There are two main approaches to block the actions of leukotrienes.
Inhibition of the 5-lipoxygenase pathway
Drugs such as zileuton block 9998 lipo protein oxydatenase 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. [2]
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
- ^ NEJM 360:1002
- ^ 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:. http://www.blackwell-synergy.com/doi/abs/10.1111/j..2006.01606.x.
External links
Linked medicines