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Montelukast



Montelukast
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
Identifiers
CAS number 158966-92-8
ATC code R03DC03
PubChem 60951
DrugBank APRD00434
Chemical data
Formula C35H36ClNO3S 
Mol. mass 586.184 g/mol
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

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.

Additional recommended knowledge

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
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Montelukast". A list of authors is available in Wikipedia.
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