Effect of Helicobacter pylori infection and acid blockade by lansoprazole on clarithromycin bioavailability.
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.
Ortiz
R A M
RA
Unidade Integrada de Farmacologia e Gastroenterologia, Universidade São Francisco, Av. São Francisco de Assis 218, 12916-900 Bragança Paulista, SP, Brazil.
Calafatti
S A
SA
Moraes
L A
LA
Deguer
M
M
Ecclissato
C C
CC
Marchioretto
M A M
MA
Ribeiro
M L
ML
Bernasconi
G
G
Pedrazzoli
J
J
D053799:2-Pyridinylmethylsulfinylbenzimidazoles / Q000008:administration & dosage*; D000328:Adult; D000900:Anti-Bacterial Agents / Q000493:pharmacokinetics* / Q000627:therapeutic use; D000897:Anti-Ulcer Agents / Q000008:administration & dosage*; D019540:Area Under Curve; D001682:Biological Availability; D016022:Case-Control Studies; D002851:Chromatography, High Pressure Liquid; D017291:Clarithromycin / Q000493:pharmacokinetics* / Q000627:therapeutic use; D018592:Cross-Over Studies; D004357:Drug Synergism; D016481:Helicobacter Infections / Q000188:drug therapy* / Q000378:metabolism; D016480:Helicobacter pylori; D006801:Humans; D064747:Lansoprazole; D054328:Proton Pump Inhibitors; D013997:Time Factors
D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D000900:Anti-Bacterial Agents; D000897:Anti-Ulcer Agents; D054328:Proton Pump Inhibitors; D064747:Lansoprazole; D017291:Clarithromycin