Abstract
The effect of proton pump inhibitors and Helicobacter pylori infection on the bioavailability of antibiotics is poorly understood. We determined the effects of 5-day oral administration of 60 mg lansoprazole on the bioavailability of clarithromycin in individuals with and without H. pylori infection. Thirteen H. pylori-infected and 10 non-infected healthy volunteers were enrolled in a study with an open-randomized two-period crossover design and a 21-day washout period between phases. Plasma concentrations of clarithromycin in subjects with and without lansoprazole pre-treatment were measured by liquid chromatography coupled to a tandem mass spectrometer. Clarithromycin Cmax and AUC0-10 h were significantly reduced after lansoprazole administration. In addition, lansoprazole treatment of the H. pylori-positive group resulted in a statistically significant greater reduction in Cmax (40 vs 15%) and AUC0-10 h (30 vs 10%) compared to lansoprazole-treated H. pylori-negative subjects. Thus, treatment with lansoprazole for 5 days reduced bioavailability of clarithromycin, irrespective of H. pylori status. This reduction, however, was even more pronounced in H. pylori-infected individuals.
Highlights
More than 50% of the world population is believed to be infected by Helicobacter pylori, the most common chronic bacterial infection in humans
A 5-day treatment with lansoprazole adversely affected the relative bioavailability of the antibiotic, as indicated by a reduction in the peak plasma concentration (Cmax) of clarithromycin, by the lack of inclusion within the 90% confidence interval for AUC0-10 h CLA, Cmax and the individual AUC0-∞ CLA values in the range of 80-125%, as well as the LANS(-)/LANS(+) ratio for Cmax and AUC0-10 h CLA
Lansoprazole treatment in the H. pylori-positive group resulted in a significant (P < 0.05) reduction in Cmax and AUC0-10 h CLA compared to lansoprazoletreated H. pylori-negative subjects (Table 1)
Summary
More than 50% of the world population is believed to be infected by Helicobacter pylori, the most common chronic bacterial infection in humans. This infection is a major pathogenic factor in gastroduodenal diseases, including chronic active gastritis, peptic ulcers and gastric neoplasm [1]. Anti-secretory drugs such as proton pump inhibitors can potentially alter the pharmacokinetics of antibiotics by reducing the gastric juice viscosity and/or volume [6], affecting the chemical stability of drugs [7], slowing gastric emptying [8], and possibly reducing the dissolution of solid drug formulations. Clarithromycin is commonly prescribed in most anti-H. pylori treatments [9] It is an advanced-generation macrolide with a broad in vitro antimicrobial spectrum. Elevation of the gastric pH might alter the bioavailability and distribution of clarithromycin
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