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
S 
mol
Pharmacokinetic data
Bioavailability 63% to 73%
Protein binding 99%
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 theophylline.

Montelukast is marketed in United States and many other countries by 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
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Drugs for obstructive airway diseases: asthma/COPD (Ipratropium/salbutamol
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The Merck Manual
Annual Revenue: $22.9 billion USD (2% FY 2004) · Employees: 63,000 · Stock Symbol: NYSE: MRK · Website: www.merck.com
 
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