Ciprofloxacin is one of a new generation of fluorinated quinolones structurally related to nalidixic acid. The primary mechanism of action of ciprofloxacin is inhibition of bacterial DNA gyrase. It is a broad spectrum antibacterial drug to which most Gram-negative bacteria are highly susceptible in vitro and many Gram-positive bacteria are susceptible or moderately susceptible. Unlike most broad spectrum antibacterial drugs, ciprofloxacin is effective after oral or intravenous administration. Ciprofloxacin has been most extensively studied following oral administration. It attains concentrations in most tissues and body fluids which are at least equivalent to the minimum inhibitory concentration designated as the breakpoint for bacterial susceptibility in vitro. The results of clinical trials with orally and intravenously administered ciprofloxacin have confirmed the potential for its use in a wide range of infections, which was suggested by its in vitro antibacterial and pharmacokinetic profiles. It has proven an effective treatment for many types of systemic infections as well as for both acute and chronic infections of the urinary tract. Ciprofloxacin generally appeared to be at least as effective as alternative orally administered antibacterial drugs in the indications in which they were compared, and in some indications, to parenterally administered antibacterial therapy. However, further studies are needed to fully clarify the comparative efficacy of ciprofloxacin and standard antibacterial therapies. Bacterial resistance to ciprofloxacin develops infrequently, both in vitro and clinically, except in the setting of pseudomonal respiratory tract infections in cystic fibrosis patients. The drug is also well tolerated. Thus, as an orally active, broad spectrum and potent antibacterial drug, ciprofloxacin offers a valuable alternative to broad spectrum parenterally administered antibacterial drugs for use in a wide range of clinical infections, including difficult infections due to multiresistant pathogens.

Ciprofloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.

Previous work revealed genotoxic effects in the wastewater of a large university hospital using a bacterial short-term genotoxicity assay, based on a umuC::lacZ fusion gene (umuC assay). These studies ruled out disinfectants and detergents as main causative agents of the genotoxic effects. This paper focuses on specific hospital-related drugs as the cause. The ratio of theoretical mean wastewater concentrations (derived from consumption data) and lowest observable effect concentrations of selected pharmaceuticals were used to calculate umuC induction probabilities. The fluoroquinolone antibiotics Ciproxin® and Noroxin® showed the highest induction probabilities and exceeded all other investigated drugs by at least one order of magnitude in significance. Antineoplastic drugs, originally thought to be the main effectors, were found to be of marginal significance using the umuC assay. These findings were further supported by investigation of urine samples of hospital patients with the umuC assay. The determination of ciprofloxacin in native hospital wastewater by reversed-phase high-performance liquid chromatography and fluorescence detection revealed concentrations from 3 to 87 μg/L. umuC induction factor and ciprofloxacin concentrations in 16 hospital wastewater samples showed a log-linear correlation (r2 = 0.84, p < 0.0001). These results suggest that the previously measured umuC genotoxicity in the wastewater of the hospital under investigation is caused mainly by fluoroquinolone antibiotics, especially by ciprofloxacin. On the basis of these findings, the role of the umuC assay as a screening tool for wastewater genotoxicity assessment is discussed.

Identification of fluoroquinolone antibiotics as the main source of umuC genotoxicity in native hospital wastewater

Analysis of fluoroquinolones in biological fluids by high-performance liquid chromatography.

Chromatography as an analytical tool for selected antibiotic classes : a reappraisal addressed to pharmacokinetic applications

Determination of BAY 12-8039, a new 8-methoxyquinolone, in human body fluids by high-performance liquid chromatography with fluorescence detection using on-column focusing.

Sensitive and selective determination of picogram amounts of ciprofloxacin and its metabolites in biological samples using high-performance liquid chromatography and photothermal post-column derivatization.

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Sensitive and selective determination of picogram amounts of ciprofloxacin and its metabolites in biological samples using high-performance liquid chromatography and photothermal post-column derivatization.