title: Single-dose pharmacokinetic properties of esomeprazole in children aged 1 - 11 years with endoscopically proven GERD: a randomized, open-label study.
abstract: OBJECTIVE
  To assess the overall exposure after a single dose of esomeprazole in children with gastroesophageal reflux disease (GERD).
  
  
  METHODS
  Oral esomeprazole administered as an intact capsule with 30 - 180 mL of water, or as an opened capsule mixed with as much as 1 tablespoon of applesauce followed by 30 - 180 mL of water.
  
  
  METHODS
  In this randomized, open-label study of children aged 1 - 11 years with endoscopically proven GERD, patients weighing 8 - < 20 kg were randomized to a single 5- or 10-mg oral dose of esomeprazole, and patients weighing >= 20 kg were randomized to a single 10- or 20-mg oral dose of esomeprazole. Esomeprazole exposure (AUC(0-∞)), AUC from zero to last measurable concentration (AUC(0-t)), maximum plasma concentration (C(max)), time to C(max) (t(max)), terminal-phase half-life, apparent oral clearance, and apparent volume of distribution were determined.
  
  
  RESULTS
  28 patients were randomized to receive esomeprazole: 14 patients weighing 8 to < 20 kg received esomeprazole 5 mg (n = 7) or 10 mg (n = 7), and 14 patients weighing ≥20 kg received esomeprazole 10 mg (n = 6) or 20 mg (n = 8). Children weighing 8 - < 20 kg had a 1.8-fold higher exposure with the 10-mg vs. 5-mg dose (AUC(0-∞), 1.32 vs. 0.73 μmol·h/L, respectively); children weighing ≥ 20 kg had a 4.4-fold higher exposure with the 20-mg vs. 10-mg dose (AUC(0-∞), 3.06 vs. 0.69 μmol·h/L). C(max) was 2.2-fold higher for the 10-mg vs. 5-mg dose (8 to < 20 kg) and 2.4-fold higher for the 20-mg vs.10-mg dose (>= 20 kg).
  
  
  CONCLUSIONS
  The pharmacokinetics of single-dose esomeprazole were dose-dependent in children weighing >= 20 kg but not in children weighing 8 to < 20 kg.
authors.forename: Nader N
authors.initials: NN
authors.lastname: Youssef
authors.forename: Eduardo
authors.initials: E
authors.lastname: Tron
authors.forename: Vasundhara
authors.initials: V
authors.lastname: Tolia
authors.forename: Jennifer E
authors.initials: JE
authors.lastname: Hamer-Maansson
authors.forename: Per
authors.initials: P
authors.lastname: Lundborg
authors.forename: Marta
authors.initials: M
authors.lastname: Illueca
mesh_terms: D000897:Anti-Ulcer Agents / Q000009:adverse effects / Q000493:pharmacokinetics*; D002648:Child; D002675:Child, Preschool; D064098:Esomeprazole / Q000009:adverse effects / Q000493:pharmacokinetics*; D005260:Female; D005764:Gastroesophageal Reflux / Q000188:drug therapy*; D006801:Humans; D007223:Infant; D008297:Male
chemical_list: D000897:Anti-Ulcer Agents; D064098:Esomeprazole