Montelukast dose selection in children ages 2 to 5 years: Comparison of population pharmacokinetics between children and adults

Montelukast, a leukotriene receptor antagonist, has demonstrated efficacy a nd tolerability in the treatment of asthma in patients age 6 years and olde r. The purpose of this open, one-period, multicenter population pharmacokin etic study was to identify a chewable tablet (CT) dose of montelukast for a dministration to children ages 2 to 5 years with asthma, yielding a single- dose pharmacokinetic profile (area under the plasma concentration-time curv e [AUC]) comparable to that of the 10 mg film-coated tablet (FCT) dose in a dults. Because patient numbers were small and the volume of blood that coul d be collected from individual 2- to 5-year-old patients was limited, a pop ulation pharmacokinetic approach was used to estimate population AUC (AUC(p op)). The 4 mg CT dose of montelukast was well tolerated and yielded on AUC (pop) (2721 ng.h/ml) similar to that of the adult AUC(pop) (2595 ng.h/mL) o bserved after a 10 mg FCT dose. These results support the selection of a 4 mg once-daily CT dose of montelukast for future efficacy and safety studies in children ages 2 to 5 years with asthma. (C) 2001 the American College o f Clinical Pharmacology.