Pharmacokinetics of montelukast in asthmatic patients 6 to 24 months old

J Clin Pharmacol. 2004 May;44(5):487-94. doi: 10.1177/0091270004264970.

Abstract

Montelukast is a cysteinyl leukotriene receptor antagonist approved for the treatment of asthma for those ages 1 year old to adult. The purpose of this study was to evaluate the pharmacokinetic comparability of a 4-mg dose of montelukast oral granules in patients > or = 6 to < 24 months old to the 10-mg approved dose in adults. This was an open-label study in 32 patients. Population pharmacokinetic parameters included estimates of AUC(pop), C(max), and t(max). Results were compared with estimates from adults (10-mg film-coated tablet [FCT]). Dose selection criteria were for the 95% confidence interval (CI) for the AUC(pop) estimate ratio (pediatric/adult 10 mg FCT) to be within comparability bounds of (0.5, 2.00). The AUC(pop) ratio and the 95% CI for children compared with adults were within the predefined comparability bounds. Observed plasma concentrations were also similar. Based on systemic exposure of montelukast, a 4-mg dose of montelukast appears appropriate for children as young as 6 months of age.

Publication types

  • Clinical Trial
  • Comparative Study
  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetates / blood
  • Acetates / pharmacokinetics*
  • Acetates / therapeutic use
  • Administration, Oral
  • Area Under Curve
  • Asthma / blood
  • Asthma / drug therapy*
  • Asthma / physiopathology
  • Blood Urea Nitrogen
  • Chemistry, Pharmaceutical
  • Child, Preschool
  • Cyclopropanes
  • Diarrhea / chemically induced
  • Half-Life
  • Humans
  • Infant
  • Male
  • Mastication
  • Quinolines / blood
  • Quinolines / pharmacokinetics*
  • Quinolines / therapeutic use
  • Receptors, Leukotriene B4 / administration & dosage
  • Receptors, Leukotriene B4 / antagonists & inhibitors
  • Receptors, Leukotriene B4 / therapeutic use
  • Sulfides
  • Tablets

Substances

  • Acetates
  • Cyclopropanes
  • Quinolines
  • Receptors, Leukotriene B4
  • Sulfides
  • Tablets
  • montelukast