Quinolones News

#10 May 2, 2017

Levofloxacin given as a prodrug avoids interaction with metal-containing drugs

Fluoroquinolones form chelates when administered concomitantly with antacids containing aluminium, magnesium or calcium salts, resulting in less active drug, therefore recommendations have been to stagger administration to two hours between each agent. Researchers have reported on a novel method to overcome this interaction, in which they prepared an ethoxycarbonyl 1-ethyl hemiacetal ester of levofloxacin (LVFX-EHE) as a prodrug.

This study assessed the effects of aluminium hydroxide on the bioavailability of levofloxacin (LVFX) following oral administration of LVFX-EHE in rats. In addition, drug absorption of LVFX and LVFX-EHE from the small intestine following addition of aluminium hydroxide was assessed using an in situ everted gut sac. Finally the MICs of LVFX and LVFX-EHE for various intestinal bacteria were measured.

Researchers reported promising results; when the pro-drug was administered with and without aluminium hydroxide, the AUC0-4 h values of LVFX hydrolysed from LVFX-EHE were similar to that of LVFX alone. The in vitro gut sac experiment also demonstrated that when levofloxacin was administered with aluminium its absorption was significantly reduced. In contrast when LVFX-EHE was administered with aluminium, it maintained absorption even after 1 h of incubation.

Researchers drew attention to the fact that MIC values of LVFX-EHE were far higher than LVFX and concluded that the new prodrug form of levofloxacin is able to avoid chelate formation when administered with aluminium, and retains enhanced antimicrobial activity.

PMID: 27774590

J Pharm Pharmacol. 2016 Dec;68(12):1527-1534. doi: 10.1111/jphp.12642.

Source: https://www.ncbi.n

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