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Home / Drugs / Starting with M / Montelukast
 
Montelukast
 

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.
BrandsMontair
Singulair
Singular
CategoriesAnti-Asthmatic Agents
Antiarrhythmic Agents
Leukotriene Antagonists
ManufacturersMerck research laboratories div merck co inc
Merck and co inc
PackagersAdvanced Pharmaceutical Services Inc.
Apotheca Inc.
AQ Pharmaceuticals Inc.
A-S Medication Solutions LLC
Bryant Ranch Prepack
Cardinal Health
Comprehensive Consultant Services Inc.
Direct Pharmaceuticals Inc.
Dispensing Solutions
Diversified Healthcare Services Inc.
Lake Erie Medical and Surgical Supply
Merck & Co.
Murfreesboro Pharmaceutical Nursing Supply
Nucare Pharmaceuticals Inc.
PD-Rx Pharmaceuticals Inc.
Physicians Total Care Inc.
Prepackage Specialists
Prepak Systems Inc.
Redpharm Drug
Remedy Repack
Resource Optimization and Innovation LLC
Tya Pharmaceuticals
Vangard Labs Inc.

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.

mechanism of action

Montelukast selectively antagonizes leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor, CysLT1, in the human airway. Montelukast inhibits the actions of LTD4 at the CysLT1 receptor, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus.

toxicity

Side effects include headache, abdominal or stomach pain, cough, dental pain, dizziness, fever, heartburn, skin rash, stuffy nose, weakness or unusual tiredness.

biotransformation

Hepatic

absorption

Rapidly absorbed following oral administration (bioavailability is 64%)

half life

2.7-5.5 hours

route of elimination

Coupled with estimates of montelukast oral bioavailability, this indicates that montelukast and its metabolites are excreted almost exclusively via the bile.