Montelukast pharmacokinetics and molecular data

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1] Phone:617-525-6884

Pharmacokinetics

Mechanism

Effect on eosinophils in peripheral blood

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Mechanism

Montelukast causes inhibition of airway cysteinyl leukotriene receptors as demonstrated by the ability to inhibit bronchoconstriction due to inhaled LTD4 in asthmatics. Doses as low as 5 mg cause substantial blockage of LTD4-induced bronchoconstriction. In a placebo-controlled, crossover study (n=12), Montelukast inhibited early- and late-phase bronchoconstriction due to antigen challenge by 75% and 57%, respectively. Return to top

Effect on eosinophils in peripheral blood

The effect of Montelukast on eosinophils in the peripheral blood was examined in clinical trials. In patients with asthma aged 2 years and older who received Montelukast, a decrease in mean peripheral blood eosinophil counts ranging from 9% to 15% was noted, compared with placebo, over the double-blind treatment periods. In patients with seasonal allergic rhinitis aged 15 years and older who received Montelukast, a mean increase of 0.2% in peripheral blood eosinophil counts was noted, compared with a mean increase of 12.5% in placebo-treated patients, over the double-blind treatment periods; this reflects a mean difference of 12.3% in favor of Montelukast. The relationship between these observations and the clinical benefits of montelukast noted in the clinical trials is not known. Return to top

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The content of this page is taken from the FDA package insert for this drug and should not be edited.