Inhibition of Enoxacin Absorption By Antacids or Ranitidine

Authors: Grasela TH, Schentag JJ, Sedman AJ, Wilton JH, Thomas DJ, Schultz RW, Lebsack ME, Kinkel AW
Publication: Antimicrob Agents Chemother
Keywords: adolescent, aluminum hydroxide, antacids, anti-infectives, clinical pharmacology, drug combinations, drug effects, drug interactions, enoxacin, female, gastroenterology, gastrointestinal agents, humans, infectious disease, intestinal absorption, magnesium hydroxide, male, New York, pharmacokinetics, pharmacology, ranitidine
Division: Clinical Pharmacology and Pharmacometrics (CPP)

Abstract

Ten normal volunteers participated in a randomized, five-way crossover study to determine the effect of concurrent enoxacin and antacid or ranitidine administration on enoxacin absorption. The bioavailability of a single oral 400-mg enoxacin dose was significantly decreased, by 73 and 49%, when Maalox TC was administered 0.5 and 2 h before enoxacin, respectively. Enoxacin bioavailability was not significantly altered when the antacid was given 8 h before or 2 h after enoxacin administration. Ranitidine, administered intravenously 2 h before enoxacin, also significantly decreased enoxacin bioavailability, by 40%. The correlation between the proximity of antacid administration and the magnitude of the decrease in enoxacin bioavailability supports complexation as the mechanism of the antacid-enoxacin interaction. However, reduction of enoxacin bioavailability by ranitidine suggests that elevated gastric pH may also play a role in the antacid-enoxacin drug-drug interaction.

By Thaddeus H. Grasela, Schentag JJ, Sedman AJ, Wilton JH, Thomas DJ, Schultz RW, Lebsack ME, Kinkel AW