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Montelukast

Catalog No. DB00471 Name DrugBank
CAS Number 158966-92-8 Website http://www.ualberta.ca/
M. F. C35H36ClNO3S Telephone (780) 492-3111
M. W. 586.18324 Fax (780) 492-1071
Purity Email david.wishart@ualberta.ca
Storage Chembase ID: 354

SYNONYMS

IUPAC name
2-[1-({[(1R)-1-{3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl}-3-[2-(2-hydroxypropan-2-yl)phenyl]propyl]sulfanyl}methyl)cyclopropyl]acetic acid
IUPAC Traditional name
montelukast
Brand Name
Montair
Singulair
Singular

DATABASE IDS

CAS Number 158966-92-8
PubChem SID 46505585
PubChem CID 5281040

PROPERTIES

Hydrophobicity(logP) 7.9

DETAILS

Description (English)
Item Information
Drug Groups approved
Description 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 locus 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.
Indication For the treatment of asthma
Pharmacology Montelukast, like zafirlukast, is a leukotriene receptor antagonist used as an alternative to anti-inflammatory medications in the management and chronic treatment of asthma and exercise-induced bronchospasm (EIB). Unlike zafirlukast, montelukast does not inhibit CYP2C9 or CYP3A4 and is, therefore, not expected to affect the hepatic clearance of drugs metabolized by these enzymes.
Toxicity Side effects include headache, abdominal or stomach pain, cough, dental pain, dizziness, fever, heartburn, skin rash, stuffy nose, weakness or unusual tiredness.
Affected Organisms
Humans and other mammals
Biotransformation Hepatic
Absorption Rapidly absorbed following oral administration (bioavailability is 64%)
Half Life 2.7-5.5 hours
Protein Binding 99% (to plasma proteins)
Elimination Coupled with estimates of montelukast oral bioavailability, this indicates that montelukast and its metabolites are excreted almost exclusively via the bile.
Distribution * 8 to 11 L
Clearance * 45 mL/min [healthy adults]
External Links
Wikipedia
RxList
Drugs.com

REFERENCES