Montelukast detailed information

Montelukast detailed information

Clinical data
Pregnancy category	B (U.S.), B1 (Au)
Routes of administration	Oral
ATC code	R03DC03 (WHO)
Legal status
Legal status	℞-only (U.S.), POM (UK), S4 (Au)
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
Identifiers
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
CAS Number	158966-92-8
PubChem CID	60951
DrugBank	APRD00434
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C35H36ClNO3S
Molar mass	586.184 g/mol
3D model (JSmol)	Interactive image
SMILES Clc1ccc2ccc(/C=C/c3cccc(c3)C(CCc3ccccc3C(C)(C)O)SCC3(CC3)CC(=O)O)nc2c1

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

• Singulair Official Website

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