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Montelukast
- indication:For the treatment of asthma
- pharmacologypharmacology:
- mechanism: 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.
- toxicity: Side effects include headache, abdominal or stomach pain, cough, dental pain, dizziness, fever, heartburn, skin rash, stuffy nose, weakness or unusual tiredness.
- absorprion: Rapidly absorbed following oral administration (bioavailability is 64%)
- halflife: 2.7-5.5 hours
- roouteelimination: Coupled with estimates of montelukast oral bioavailability, this indicates that montelukast and its metabolites are excreted almost exclusively via the bile.
- volumedistribution: * 8 to 11 L
- clearance: * 45 mL/min [healthy adults]