Transfer of Clarithromycin to Gastric Juice is Enhanced by Omeprazole in Helicobacter pylori -Infected Individuals

Background: The effects of proton-pump inhibitors and Helicobacter pylori infection on the distribution of drugs employed for the eradication of H. pylori are poorly understood. The aim of this study was to investigate the effects of a 7-day oral administration of 20 mg omeprazole on the distributio...

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Bibliographic Details
Published in:Scandinavian journal of gastroenterology 2001, Vol.36 (12), p.1248-1253
Main Author: Pedrazzoli Jr, S. A. Calafatti, R. A. M. Ortiz, F. E. Dias, M. Deguer, F. D. Mendes, A. P. Bento, A. A. Pereira, H. Piovesana, J. G. P. Ferraz, F. Lerner, G. de Nucci, J.
Format: Article
Language:English
Subjects:
Adult
Anti-Bacterial Agents - pharmacokinetics
Anti-Ulcer Agents - pharmacology
Biological and medical sciences
Biological Transport, Active
Chromatography, High Pressure Liquid
Clarithromycin - pharmacokinetics
Clarithromycin Helicobacter Pylori Omeprazole Peptic Ulcer Pharmacokinetics
Cross-Over Studies
Digestive system
Drug Synergism
Gastric Juice - chemistry
Helicobacter Infections - metabolism
Helicobacter pylori
Humans
Male
Medical sciences
Omeprazole - pharmacology
Pharmacology. Drug treatments
Time Factors
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Summary:Background: The effects of proton-pump inhibitors and Helicobacter pylori infection on the distribution of drugs employed for the eradication of H. pylori are poorly understood. The aim of this study was to investigate the effects of a 7-day oral administration of 20 mg omeprazole on the distribution of clarithromycin in the gastric juice of individuals with H. pylori infection. Methods: Eighteen H. pylori infected dyspeptic male volunteers without endoscopic lesions were enrolled in a study with an open, randomized, two-period crossover design and a 21-day washout period between phases. Plasma and gastric juice concentrations of clarithromycin in subjects with and without omeprazole pretreatment were measured by means of liquid chromatography coupled to tandem mass spectrometry. Results: The maximum concentration of clarithromycin (C max ) and the area under the time-concentration curve from 0 to 2 h (AUC 0-2h ) were significantly higher in gastric juice than in plasma. Omeprazole treatment further augmented clarithromycin C max and AUC 0-2h in gastric juice approximately 2-fold ( P < 0.05). Conclusions: Short-term treatment with omeprazole in H. pylori -positive volunteers increases the amount of clarithromycin transferred to the gastric juice, confirming a synergism between these drugs. Our results suggest the presence of an active transport mechanism for clarithromycin from plasma to the gastric lumen, which is influenced by omeprazole.
ISSN:0036-5521
1502-7708
DOI:10.1080/003655201317097074