Single-dose pharmacokinetics of nizatidine (Axid) in children

J Clin Pharmacol. 2002 Oct;42(10):1089-96. doi: 10.1177/009127002401382687.

Abstract

The pharmacokinetics of nizatidine following a single 5.0 mg/kg oral dose given as an extemporaneous liquid formulation in apple juice was examined in 12 healthy children (8.0 +/- 2.4 years, 30.7 +/- 8.4 kg). Nizatidine and N-desmethylnizatidine were quantitated by HPLC/MS from five post dose blood samples taken over a 12-hour period. The apparent terminal elimination rate constant for nizatidine in the pediatric subjects (0.58 +/- 0.8h(-1)) was virtually identical to that (0.54 +/- 0.13 h(-1)) previously reported from adult studies. When corrected for an estimated 30% reduction in nizatidine oral bioavailability observed in adults upon coingestion of the drug with other fruit/vegetable juices, nizatidine pharmacokinetic parameter estimates (e.g., Cmax, CL/F, Vss/F) in our pediatric subjects were similar to those previously reported in adults who were administered dimensionally similar (e.g., approximately 4 mg/kg) solid oral doses of the drug. Examination of the mean area under the curve (i.e., AUC0-infinity for nizatidine and N-desmethylnizatidine suggested an approximate 15% metabolic conversion of the parent drug. Finally, nizatidine plasma concentrations in pediatric patients following a single 5.0 mg/kg oral dose exceeded the EC50 value of the drug for gastric acid suppression determined from adult studies for approximately 6 hours.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Administration, Oral
  • Area Under Curve
  • Child
  • Child, Preschool
  • Chromatography, High Pressure Liquid
  • Female
  • Half-Life
  • Histamine H2 Antagonists / administration & dosage
  • Histamine H2 Antagonists / blood
  • Histamine H2 Antagonists / pharmacokinetics*
  • Humans
  • Infant
  • Male
  • Nizatidine / administration & dosage
  • Nizatidine / analogs & derivatives*
  • Nizatidine / blood
  • Nizatidine / pharmacokinetics*

Substances

  • Histamine H2 Antagonists
  • N-desmethylnizatidine
  • Nizatidine