Amoxicillin and ampicillin are not transferred to gastric juice irrespective of Helicobacter pylori status or acid blockade by omeprazole

Aliment Pharmacol Ther. 2002 Jun;16(6):1163-70. doi: 10.1046/j.1365-2036.2002.01262.x.

Abstract

Background: The effects of proton pump inhibitors and Helicobacter pylori infection on the distribution of drugs used for the eradication of the bacteria are poorly understood.

Aim: The aim of this study was to investigate the effects of a 7-day administration of 20 mg of omeprazole on the pharmacokinetics of amoxicillin and ampicillin in the plasma, saliva and gastric juice of individuals with and without H. pylori infection.

Methods: Fifty-four healthy volunteers without endoscopic lesions were enrolled. Twenty-six volunteers were included in the amoxicillin study and 28 individuals in the ampicillin study. Each study had an open randomized two-period crossover design and a 21-day washout period between phases. Plasma, saliva and gastric juice concentrations of amoxicillin and ampicillin in subjects with and without omeprazole pre-treatment were measured by reversed-phase HPLC using UV detection.

Results: Neither pre-treatment with omeprazole nor H. pylori infection interfered with the plasma bioavailability of amoxicillin or ampicillin, as assessed by the AUC0-2 h. Neither ampicillin nor amoxicillin were detected in saliva or gastric juice in any study phase.

Conclusion: Short-term treatment with omeprazole does not interfere with the pharmacokinetics of amoxicillin or ampicillin. Our results also exclude the presence of a transfer mechanism for amoxicillin or ampicillin from the plasma to the gastric lumen.

Publication types

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

MeSH terms

  • Adult
  • Amoxicillin / administration & dosage
  • Amoxicillin / pharmacokinetics*
  • Ampicillin / administration & dosage
  • Ampicillin / pharmacokinetics*
  • Area Under Curve
  • Biological Availability
  • Chromatography, High Pressure Liquid
  • Cross-Over Studies
  • Enzyme Inhibitors / pharmacology*
  • Female
  • Gastric Juice / chemistry
  • Helicobacter Infections / drug therapy*
  • Helicobacter pylori / pathogenicity*
  • Humans
  • Male
  • Omeprazole / pharmacology*
  • Penicillins / administration & dosage
  • Penicillins / pharmacokinetics*
  • Proton Pump Inhibitors*
  • Saliva / chemistry

Substances

  • Enzyme Inhibitors
  • Penicillins
  • Proton Pump Inhibitors
  • Ampicillin
  • Amoxicillin
  • Omeprazole