Montelukast detailed information
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Clinical data | |
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Pregnancy category | |
Routes of administration | Oral |
ATC code | |
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Pharmacokinetic data | |
Bioavailability | 63% to 73% |
Protein binding | 99% |
Metabolism | Hepatic (CYP3A4 and CYP2C9-mediated) |
Elimination half-life | 2.7-5.5 hours |
Excretion | Biliary |
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CAS Number | |
PubChem CID | |
DrugBank | |
E number | {{#property:P628}} |
ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value). |
Chemical and physical data | |
Formula | C35H36ClNO3S |
Molar mass | 586.184 g/mol |
3D model (JSmol) | |
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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Overview
Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. It is usually administered orally. Montelukast blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation. Because of its method of operation, it is not useful for the treatment of acute asthma attacks. Again because of its very specific focus of operation, it does not interact with other allergy medications such as theophylline.
Montelukast is marketed in United States and many other countries by Merck & Co. with the brand name Singulair®. It is available as oral tablets, chewable tablets, and oral granules. In India and other countries, it is also marketed under the brand name Montair®, produced by Indian company Cipla.
Side effects
Side effects include gastrointestinal disturbances, hypersensitivity reactions, sleep disorders and increased bleeding tendency, aside from many other generic adverse reactions. Its use is associated with a higher incidence of Churg-Strauss syndrome (whether or not this drug is 'unmasking' subclinical Churg-Strauss is as yet uncertain).
References
- Lipkowitz, Myron A. and Navarra, Tova (2001) The Encyclopedia of Allergies (2nd ed.) Facts on File, New York, p. 178, ISBN 0-8160-4404-X
External links
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- Leukotriene antagonists