For the treatment of asthma
Montelukast selectively antagonizes leukotriene D<sub>4</sub> (LTD<sub>4</sub>) at the cysteinyl leukotriene receptor, CysLT<sub>1</sub>, in the human airway. Montelukast inhibits the actions of LTD<sub>4</sub> at the CysLT<sub>1</sub> receptor, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus.
Side effects include headache, abdominal or stomach pain, cough, dental pain, dizziness, fever, heartburn, skin rash, stuffy nose, weakness or unusual tiredness.
Rapidly absorbed following oral administration (bioavailability is 64%)
2.7-5.5 hours
Coupled with estimates of montelukast oral bioavailability, this indicates that montelukast and its metabolites are excreted almost exclusively via the bile.
* 8 to 11 L
* 45 mL/min [healthy adults]