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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
SMILES eMolecules & PubChem
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 Rx Only (U.S.), POM (UK), S4 (Au)
Routes Oral

Montelukast (trade name Singulair)is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies.[1] It is usually administered orally. Montelukast is a CysLT1 antagonist; that is it 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.

Another leukotriene receptor antagonist is zafirlukast (Accolate), taken twice daily. Zileuton (Zyflo), an asthma drug taken four times per day, blocks leukotriene synthesis by inhibiting 5-lipoxygenase, an enzyme of the eicosanoid synthesis pathway.

The Mont in Montelukast stands for Montreal, the place where Merck developed the drug [2]

Contents

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). In March, 2008 the FDA announced that it would investigate whether mood changes and suicidal thoughts are possible side effects of drugs in this class, including the popular drug Singulair, which currently lists these side effects.[3]

On June 12, 2009 the Food and Drug Administration concluded their review into the possibility of neuropsychiatric side effects with leukotriene modulator drugs. Although clinical trials only revealed an increased risk of insomnia, post-marketing surveillance showed that the drugs are associated with a possible increase in suicidal behaviour and other side effects such as agitation, aggression, anxiousness, dream abnormalities and hallucinations, depression, irritability, restlessness and tremor.[4]

Use with loratadine

Schering-Plough and Merck have sought permission to market a combined tablet with loratadine (Claritin) and montelukast (Singulair), as many patients combine the two themselves. However, the FDA has found no benefit from a combined pill for seasonal allergies over taking the two drugs in combination,[5] and on April 25, 2008, issued a "not approvable" letter for the combination.[6]

Patent(s)

Singulair is covered by U.S. Patent No. 5,565,473[7] which is set to expire (by pediatric extension) on August 3, 2012[8].

References

External links








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