Absorption interactions with fluoroquinolones. 1995 update

The utility of the fluoroquinolone class of antibiotics is rapidly expanding due to their favourable pharmacokinetic profile and the continuing development of new compounds. These agents are often used for indications not successfully treated with other orally available antimicrobials in the past, or for ‘step-down’ therapy in patients originally treated with intravenous agents. As the usage of these agents expands for serious systemic infections, knowledge of absorptive interactions with fluoroquinolones becomes paramount. Fluoroquinolones are often utilised in dosages and against modestly susceptible pathogens which allow a narrow margin for acceptable decreases in bioavailability. Chelation interactions with multivalent cations can result in inactivation of the fluoroquinolone with ramifications in vitro and in vivo. Chelation interactions have been reported to occur in between 22 and 76% of patients prescribed fluoroquinolones. Concurrent administration of magnesium-aluminium antacids and sucralfate has the greatest effect on the bioavailability of quinolones followed by iron, calcium and zinc. Spacing doses of fluoroquinolones and interactants has been suggested as a method of ensuring adequate quinolone absorption, but this can make optimal administration of the cation interactant difficult, if not imposible.