Aeromax Mechanism of Action

Pharmacology: Montelukast (Aeromax) is a selective and orally active leukotriene receptor antagonist that inhibits the cysteinyl leukotriene (CysLT₁) receptor. It binds with affinity and selectivity to the CysLT₁ receptor (in preference to other pharmacologically important airway receptors, such as prostanoid, cholinergic, or beta-adrenergic receptor).
Montelukast inhibits physiologic actions of LTD₄ at the CysLT₁ receptor without any agonist activity.
The cysteinyl leukotrienes (LTC₄, LTD₄, LTE₄) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to CysLT receptors found in the human airway. Cysteinyl leukotrienes and leukotriene receptor occupation have been correlated with the pathophysiology of asthma and allergic rhinitis.
Pharmacokinetics: Peak plasma concentrations of montelukast are achieved in 2 to 4 hours after oral doses. The mean oral bioavailability is 64%. Montelukast is more than 99% bound to plasma proteins. It is extensively metabolized in the liver by cytochrome P450 isoenzymes CYP3A4, CYP2A6, and CYP2C9, and is excreted principally in the faeces via the bile. Metabolism was reduced and the elimination half-life prolonged in patients with mild to moderate hepatic impairment.