Monarin Mechanism of Action

Pharmacology: Montelukast is a leukotriene receptor antagonist which binds with high affinity and selectivity to the CysLT1 (cysteinyl leukotrienes) receptor. The cysteinyl leukotrienes (LTC4, LTD4, LTE4) are inflammatory eicosanoids released from various cells including mast cells and eosinophils. These eicosanoids bind to cysteinyl leukotriene receptors. The CysLT1 receptor is found in the human airway. CysLTs have been correlated with the pathophysiology of asthma. In asthma, leukotrienes-mediated effects include bronchoconstriction, mucous secretion, vascular permeability, and eosinophil recruitement. Treatment with montelukast inhibited both early- and late-phase bronchoconstriction due to antigen challenge. Montelukast decreased peripheral blood eosinophils in adult patients.
Pharmacokinetics: Montelukast is rapidly absorbed following oral administration. The mean oral bioavailabilty is 64% and not influenced by a standard meal.
Montelukast is more than 99% bound to plasma proteins. The steady-state volume of distribution of montelukast averages 8-11 litres. It is extremely metabolized in the liver that involve the cytochromes P450 3A4, 2A6 and 2C9. Montelukast and its metabolites are excreted almost exclusively via the bile.