Pharmacokinetic properties of esomeprazole in adolescent patients aged 12 to 17 years with symptoms of gastroesophageal reflux disease: A randomized, open-label study.

ABSTRACT

OBJECTIVE: The aim of this study was to assess the pharmacokinetic (PK) properties and tolerability of esomeprazole 20 and 40 mg after single and repeated oral doses in adolescents with symptoms of gastroesophageal reflux disease (GERD). RESULTS: The study included 15 boys and 13 girls (mean age, 14.3 years). Geometric mean AUC(0-infinity) values (overall drug exposure) were 1.58 and 5.57 micromol . h/L (0.027 and 0.083 pmol x h x L(-1)/kg) after single-dose administration of esomeprazole 20 and 40 mg, respectively, on day 1. Corresponding values with repeated doses (day 8) were 3.65 and 13.86 micromol x h/L (0.064 and 0.207 micromol x h x L(-1)/kg). Geometric mean Cmax values were 0.67 and 2.78 micromol/L (0.012 and 0.041 micromol/L x kg(-1)) with single-dose administration of esomeprazole 20 and 40 mg, respectively, and 1.45 and 5.13 micromol/L (0.026 and 0.075 micromol/L x kg(-1)), respectively, with repeated doses (day 8). These mean AUC(0-infinity) and CmaX values were >2-fold with the 40 mg dose compared with the 20-mg dose with single- and repeated-dose administration. The most common adverse event was headache (2 [7.1%] patients). CONCLUSIONS: The results of this study suggest that the PK parameters of esomeprazole were both dose- and time-dependent in these adolescents with GERD. Both doses of esomeprazole were well tolerated in this study population.