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20 patients with pathospermia and asymptomatic bacteriospermia of more than 10(5) bacteria/ml received an oral treatment with 800 mg Norfloxacin daily for ten days. An complete spermiogram including motility assessments with laser-Doppler-spectroscopy, round-cell counts, evaluation of number and types of microorganisms was performed before treatment and within one week after treatment. As results, a statistically significant decrease of number of bacteria and round-cells was observed in the ejaculates, whereas the other spermiogram-parameters remained unchanged.
Norfloxacin, a nalidixic acid analog, is the first of the fluorinated quinolinecarboxylic acids to be marketed in the United States. It demonstrates potent antibacterial activity against aerobic, gram-negative bacteria including the Enterobacteriaceae, gentamicin-resistant Pseudomonas aeruginosa, and penicillin-resistant Neisseria gonorrhoeae. Norfloxacin exhibits good activity against methicillin-resistant and -sensitive Staphylococcus aureus, but less activity against most other aerobic, gram-positive organisms. Anaerobic bacteria are resistant to the drug. Resistance to norfloxacin is not plasmid mediated, but is secondary to bacterial mutation, and occurs less frequently than nalidixic acid resistance. Its pharmacokinetic properties after a 400-mg oral dose consist of a peak serum concentration of 1.3-1.58 micrograms/ml, an elimination half-life of 3-7 hours, and good penetration into kidney and prostatic tissues. Renal excretion is the major route of elimination. Norfloxacin is highly effective in the treatment of uncomplicated and complicated urinary tract infections, and gonococcal urethritis. Adverse effects are generally well tolerated and usually do not require discontinuation of therapy.
The Chinese hamster V79 lung cell in vitro micronucleus assay was adapted to detect and quantify phototoxicity and photogenotoxicity of fluoroquinolones. Using this assay, the quinolones were ranked in terms of decreasing phototoxicity: clinafloxacin > lomefloxacin, sparfloxacin > trovafloxacin, nalidixic acid, ofloxacin, ciprofloxacin > enoxacin, norfloxacin. This rank order agrees well with published studies utilizing various other phototoxicity models and establishes this approach as a fast and sensitive way to characterize the phototoxic potential of quinolones. Nearly complete inhibition of phototoxicity was observed if the cells were pretreated for as little as 1 min with 10-20 mM sodium azide prior to the addition of quinolone. An identical azide effect was seen in unirradiated quinolone- and etoposide-treated cells. These findings are consistent with a model in which sodium azide renders DNA topoisomerase II catalytically inactive. In this state, topoisomerase II cannot initiate DNA strand cleavage and the DNA/topoisomerase complex becomes insensitive to quinolones and other topoisomerase II inhibitors. The fact that azide reduces both UV-dependent and UV-independent toxicity and clastogenicity strongly suggests a common mechanism of toxicity dependent on the formation of topoisomerase-induced DNA double-strand breaks.
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Antibiotics, including members of the tetracycline and fluoroquinolone families, are emerging organic environmental contaminants. Uptake from soil by plants is a means for antibiotics to enter terrestrial food chains. Chemical exchange between plant and the soil/water matrix occurs simultaneously with degradation in the soil/water matrix. In this study, the comparative temporal behaviour of rice (Oryza sativa L.) towards the zwitterionic antibiotics oxytetracycline, chlortetracycline and norfloxacin at initial soil/water concentrations of 10, 20 and 30 μg g(-1) (dry weight) is investigated. This is accomplished within the framework of an activity-based mass-conserving dynamic model. Plant antibiotic concentrations are observed to increase to a maximum then decline. Maximum concentrations in rice are compound-dependent linear functions of initial soil/water concentrations, but the relationships are not related to the compound octan-1-ol/water distribution ratio (DOW). The times required to attain maximal concentrations are independent of initial soil/water levels for a given antibiotic, but again vary between antibiotics and are not related to DOW values. Translocation from root to other tissues is not observed. The magnitudes of Root Concentration Factors (RCFs), the ratio of root and soil/water concentrations, are consistent with significant sorption to soil and consequent relatively low concentrations in interstitial water.
Aquaculture in mangrove wetlands has been developed rapidly, causing various environmental problems (e.g., antibiotic residue). In the present study, the levels and distributions of a well-known class of antibiotics (fluoroquinolones; FQs), including norfloxacin (NOR), ciprofloxacin (CIP), and enrofloxacin (ENR), were examined in sediment and mangrove plant (Aegiceras corniculatum) from a mangrove wetland in the Zhanjiang Mangrove National Nature Reserve, South China. NOR and CIP were detected in all sediment samples, with concentrations ranging from 4.3 to 64.2 ng/g and from 7.62 to 68.5 ng/g on a basis of dry weight (dw), respectively, whereas ENR was found with relatively lower frequency (<78%) and lower concentrations (<19.3 ng/g). Sediments in mangrove rhizosphere area contained considerably higher concentrations of all FQs (except for ENR). FQs were largely varied in mangrove plant tissues; NOR and ENR were not detected in leaf and root samples, respectively. CIP featured an increasing tendency from the root to the upper parts of plants, whereas a decreasing trend was found for NOR. Three bioconcentration factors (BCFs) of FQs, including BCFs for roots (BCFr), branches (BCFb), and leaves (BCFl) were calculated, and most of them exceeded 1. Especially for NOR, its BCFr can reach up to 9.9, indicating that Aegiceras corniculatum has a strong ability to accumulate FQs from sediment and/or surrounding environment. For NOR and CIP, strong positive relationships were observed between BCFr and concentrations in root, but no significant correlations were observed between BCFr and root lipid of mangrove plant. More studies are needed to investigate the uptake mechanism of antibiotics in mangrove plants.
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Antibacterial activity of fleroxacin (FLRX), a new quinolone antimicrobial, against 36 strains of Shigella app., 14 strains of Salmonella spp., 11 strains of Escherichia coli, 9 strains of Vibrio spp. (including 2 strains of V. cholerae O1), 14 strains of Campylobacter jejuni/coli, 3 strains of Aeromonas spp. and 1 strain of Plesiomonas shigelloides isolated from infectious enteritis patients in this study was determined. Its activity was compared with that of ciprofloxacin (CPFX), norfloxacin (NFLX) and nalidixic acid (NA). The MIC90 values of FLRX were 0.1 microgram/ml against Shigella spp. and E. coli, 0.2 microgram/ml against Salmonella spp. and Vibrio spp., and 12.5 micrograms/ml against C. jejuni/coli MIC90 of FLRX was comparable to that of CPFX and NFLX against Vibrio spp.. Against other species, MIC90 of FLRX were 2- to 4-fold higher than those of CPFX, whereas equal to or 2-fold lower than NFLX. FLRX demonstrated excellent activity against an NA-resistant (MIC: > 100 micrograms/ml) isolate of E. coli, with MIC 0.78 microgram/ml. FLRX showed 8-fold higher activity than NA against other strains. The antibacterial activity of FLRX was compared with that of NA against stocked strains (clinical isolates from August 1989 to February 1991), consisting of 11 strains of Shigella spp., 10 strains of Salmonella spp., 8 strains of E. coli, 10 strains of V. cholerae O1, 10 strains of V. parahaemolyticus and 14 strains of C. jejuni/coli. MICs of FLRX were 0.78 and 12.5-25 micrograms/ml against Shigella spp. and C. jejuni/coli that showed resistance of NA (MIC: > or = 100 micrograms/ml), respectively. Based on the above, although the absolute MICs are low against E. coli and shigella spp., a value of 0.78 micrograms/ml for FLRX suggested that such strains should be considered to be resistant.
Phytochemical analysis showed the presence of alkaloids, phenols and tannins in all plants extracts. The results of the antibacterial assays indicated that all tested extracts exert antibacterial activities, with the minimum inhibitory concentration (MIC) values varying from 32 to 1024 μg/ml. The extracts from Dichrostachys glomerata, Beilschmiedia cinnamomea, Aframomum citratum, Piper capense, Echinops giganteus, Fagara xanthoxyloïdes and Olax subscorpioïdea were the most active. In the presence of efflux pump inhibitor, PAßN, the activity of the extract from D. glomerata significantly increased on 69.2% of the tested MDR bacteria. At MIC/5, synergistic effects were noted with the extract of D. glomerata on 75% of the tested bacteria for chloramphenicol (CHL), tetracycline (TET) and norfloxacin (NOR). With B. cinnamomea synergy were observed on 62.5% of the studied MDR bacteria with CHL, cefepime (FEP), NOR and ciprofloxacin (CIP) and 75% with erythromycin (ERY).
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The purpose of this study was to determine the effectiveness and tolerability of norfloxacin, cinoxacin and oxolinic acid in the treatment of urinary tract infections (UTI) in comparison to nalidixic acid. 125 patients were given the drugs in the appropriate doses for 10-14 days and 30 patients were treated for six weeks. Clinical, bacteriological, hematological and chemical checks were made on all patients before and after treatment. It was found that norfloxacin, cinoxacin and oxolinic acid are safe and effective against Escherichia coli, Klebsiella and Proteus, the commonly encountered organisms in urinary tract infections. The cure rate for norfloxacin was 93%, for cinoxacin 83%, for oxolinic acid 80% and for nalidixic acid 70% in the short course. However, these differences were not statistically significant. Oxolinic acid, cinoxacin and norfloxacin have the advantage over nalidixic acid of being administered only twice daily.
The current drugs recommended for treatment of melioidosis are tetracycline, chloramphenicol and cotrimoxazole. Unfortunately these drugs are not the drug of choice in an acutely ill patient with septicaemia prior to the availability of laboratory results. With the discovery of the new cephalosporins which have a broad spectrum of activity clinicians are using them either alone or in combination with other antibiotics in such critical situations. Hence, an in-vitro study was carried out on the susceptibility of 41 strains of P. pseudomallei isolated in Malaysia, to these new cephalosporins and a new quinolone. The results showed that all the cephalosporins tested had some activity on the strains tested, with ceftazidime being the most active drug. Pefloxacin had very poor activity. However, further clinical studies are required to determine the duration, dosage and in-vivo activity of the antibiotics.