Effects of ciprofloxacin on testosterone and cortisol concentrations in healthy males

Abstract

Several inhibitors of oxidative drug metabolism inhibit the synthesis of endogenous compounds such as testosterone and cortisol. Since ciprofloxacin is a potent inhibitor of the metabolism of a number of drugs, we studied its effect on serum testosterone and cortisol concentrations in eight healthy male subjects. Blood samples were collected over a 12-h period under baseline conditions and following the first and final doses of ciprofloxacin (500 mg orally every 12 h for 4 days). No significant differences in concentrations or area under the concentration-time curve were found when baseline values were compared with those observed for either testosterone or cortisol after ciprofloxacin administration. These results suggest that ciprofloxacin is unlikely to have either antiandrogenic side effects or clinical utility in lowering testosterone or cortisol concentration.Ciprofloxacin is a member of a promising new class of antimicrobial agents known as the fluoroquinolones. These drugs are expected to be widely used because of their broad spectra of activity and favorable pharmacokinetic profiles, which allow for oral administration and prolonged dosing intervals. While clinical experience with these drugs has shown them to be relatively well tolerated, with a 3 to 10% incidence of adverse effects (20), numerous studies have documented their abilities to inhibit oxidative drug metabolism (6). Ciprofloxacin appears to be comparable to cimetidine in its ability to inhibit the metabolism of classical substrates such as antipyrine and theophylline (12,19), while the related quinolones enoxacin and pipemidic acid have even greater effects.Oxidative biotransformation is important not only for the metabolism of drugs but also for the activation and degradation of a number of endogenous substances. Several compounds such as ketoconazole, metyrapone, and omeprazole (1,4,7,8)

Effect of Quinolones on Serum Testosterone Level in Male Albino Rats

“…It was seen by Nancy et al (1989) that fluoroquinolone such as ciprofloxacin, which causes inhibition of oxidative drug metabolism has no anti-steroidogenic side effects. 13 No significant effect was found on concentration of testosterone with ciprofloxacin, when the baseline concentrations of testosterone were compared with the concentrations obtained after single and multiple doses administrations of ciprofloxacin. The absence of the effect in case of ciprofloxacin at therapeutic doses could be due to its relative selectivity for P450 isozyme or low inhibitory potency, but at the end of the study testosterone assay showed significant decrease in the serum testosterone hormone levels in all experimental groups having P < 0.05 which is significant.…”