Montelukast

Abstract

▴ Montelukast is a selective antagonist of the leukotriene D₄ (LTD4) receptor. In patients with asthma, montelukast 5 to 250 mg/day attenuated LTD4-induced bronchoconstriction and, at a dosage of 10mg, significantly reduced early and late airway response to allergen (dust mite extract) relative to placebo. ▴ In studies evaluating the effects of various dosages of montelukast on exercise-induced bronchoconstriction the optimal dose of the drug was found to be 10mg. ▴ Montelukast 10 mg/day controlled asthma significantly more effectively than placebo in a 3-month randomised double-blind study. In a 9-month open extension of this trial, during which patients were randomised to treatment with montelukast 10 mg/day or beclomethasone (≈400 μg/day), daytime symptom score and β-agonist use decreased to a similar extent in each group. ▴ In a further study, treatment with montelukast 10 mg/day permitted clinically significant tapering of corticosteroid dosage in patients with stable asthma. ▴ Montelukast (5 mg/day) has also demonstrated efficacy in childhood asthma. ▴ The tolerability profile of montelukast was similar to that of placebo in placebo-controlled clinical trials in adults and children; the most common adverse event was headache.