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A prospective randomized study was conducted at an infectious disease hospital in Thailand. Ceftibuten was compared with norfloxacin, both given orally for five days for treatment of acute gastroenteritis in children. One hundred and seventy cases were included in the study. Eighty-eight cases were treated with ceftibuten and eighty-two cases with norfloxacin. The baseline characteristics of the patients in both treatment groups were similar. The results showed that mean durations of diarrhea in the ceftibuten and norfloxacin groups were 2.48 days and 2.29 days, respectively, but there was no statistically significant difference between the two groups (p > 0.05). There were Salmonella spp and Shigella spp isolated in both treatment groups and all were susceptible to both antibiotics. The mean durations of Salmonella diarrhea in the ceftibuten and norfloxacin groups were 2.7 and 2.2 days, respectively, while those of Shigella diarrhea were 2.3 days and 2.0 days, respectively. There were no statistically significant differences in either comparison (p > 0.05). Neither complications nor clinical relapses were observed after both antibiotics' treatment.
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Antistaphylococcal activity of two new quinolones, norfloxacin and pefloxacin, was studied. Minimal inhibitory concentrations (MICs) were determined by the agar dilution technique for 312 staphylococcal strains, all of which were resistant to nalidixic acid. 50% and 90% MICs were respectively 1 and 4 micrograms/ml for norfloxacin and 0.5 and 1 micrograms/ml for pefloxacin. Activities of these two new quinolones proved similar on Staphylococcus aureus and non-coagulase-producing staphylococci, regardless of their response to methicillin. Cross resistance between the two drugs was demonstrated.
Norfloxacin-resistant mutants were isolated and by DNA sequencing the mutations conferring resistance were identified. Mutant fitness was determined by measuring growth rates in vitro. Mutants with reduced growth rates were serially passaged to obtain growth-compensated mutants. The level of DNA supercoiling was determined by isolating plasmid DNA from the susceptible, resistant and compensated mutants and comparing the topoisomer distribution patterns by gel electrophoresis in the presence of chloroquine.
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The in vitro activity of three fluoroquinolones--ciprofloxacin, norfloxacin and ofloxacin--was studied on four laboratory-adapted strains (one chloroquine-resistant) and one fresh isolate of P. falciparum from Delhi by the schizont maturation inhibition microtest. The IC50 concentrations (mean +/- SD) were found to be as: ciprofloxacin 6.38 +/- 1.34 micrograms/ml, norfloxacin 11.24 +/- 1.27 micrograms/ml, and ofloxacin 22.3 +/- 3.11 micrograms/ml, while the MIC values were 32 micrograms/ml, 64 micrograms/ml and 128 micrograms/ml for the three drugs in the same order. The IC50 and MIC values for chloroquine-resistant strain were not significantly different from those for the chloroquine-sensitive strains. We conclude that there is little interstrain variability in the in vitro susceptibility of P. falciparum to fluoroquinolones, and that there is no cross resistance between them and chloroquine. The reported variability in clinical response of falciparum malaria to fluoroquinolones is not likely to be due to variation in parasite sensitivity.
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Thirty-five women (92%) treated with norfloxacin or ciprofloxacin received therapy during the first trimester. The most common indication for therapy (92%) was urinary tract infection. More pregnancies in the quinolone group resulted in cesarean delivery due to reported fetal distress as compared to the controls (P = .005), without clear reason. Children born to mothers treated with quinolones were significantly heavier (P = .05) than the control infants, possibly because of better control of the urinary tract infection. No malformations were found in the quinolone group, whereas one child in the control group had a ventricular septal defect. No differences were detected between the groups in achievement of developmental milestones or in the musculoskeletal system.
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The in vitro antibacterial activity of temafloxacin hydrochloride (TA-167 or A-62254) was evaluated against a wide variety of clinical isolates and compared with those of other fluoroquinolones. The potency (MIC90) of the compound against gram-positive aerobic bacteria was higher or comparable to those of ciprofloxacin, ofloxacin, and norfloxacin. Against most gram-negative enteric bacteria and Pseudomonas species, temafloxacin was less active than ciprofloxacin, but was generally as active as ofloxacin and norfloxacin, except against Proteus species and Morganella morganii. Against obligate anaerobes, it was more active than the reference quinolones. Temafloxacin was bactericidal for one strain each of Staphylococcus aureus. Escherichia coli, and Pseudomonas aeruginosa. The compound inhibited E. coli DNA gyrase activity at a low concentration.
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Thirty-nine trials were included in this review with 4623 participants. Antimicrobials versus placebo or no treatment Overall, antimicrobial therapy shortened the mean duration of diarrhoea by about a day and a half compared to placebo or no treatment (MD -36.77 hours, 95% CI -43.51 to -30.03, 19 trials, 1013 participants, moderate quality evidence). Antimicrobial therapy also reduced the total stool volume by 50% (ROM 0.5, 95% CI 0.45 to 0.56, 18 trials, 1042 participants, moderate quality evidence) and reduced the amount of rehydration fluids required by 40% (ROM 0.60, 95% CI 0.53 to 0.68, 11 trials, 1201 participants, moderate quality evidence). The mean duration of fecal excretion of vibrios was reduced by almost three days (MD 2.74 days, 95% CI -3.07 to -2.40, 12 trials, 740 participants, moderate quality evidence).There was substantial heterogeneity in the size of these benefits, probably due to differences in the antibiotic used, the trial methods (particularly effective randomization), and the timing of outcome assessment. The benefits of antibiotics were seen both in trials recruiting only patients with severe dehydration and in those recruiting patients with mixed levels of dehydration. Comparisons of antimicrobials In head-to-head comparisons, there were no differences detected in diarrhoea duration or stool volume for tetracycline compared to doxycycline (three trials, 230 participants, very low quality evidence); or tetracycline compared to ciprofloxacin or norfloxacin (three trials, 259 participants, moderate quality evidence). In indirect comparisons with substantially more trials, tetracycline appeared to have larger benefits than doxycycline, norfloxacin and trimethoprim-sulfamethoxazole for the primary review outcomes.Single dose azithromycin shortened the duration of diarrhoea by over a day compared to ciprofloxacin (MD -32.43, 95% CI -62.90 to -1.95, two trials, 375 participants, moderate quality evidence) and by half a day compared to erythromycin (MD -12.05, 95% CI -22.02 to -2.08, two trials, 179 participants, moderate quality evidence). It was not compared with tetracycline.
Kidney transplanted patients are often treated with immunosuppressive, antihypertensive, and antibiotic drugs such as cyclosporine A (CsA), β-blockers, and fluoroquinolones, respectively. Organic cation transporters (OCT) expressed in the basolateral membrane of proximal tubules represent an important drug excretion route. In this work, the renal expression of OCT after syngeneic and allogeneic kidney transplantation in rats with or without CsA immunosuppression was studied. Moreover, the interactions of CsA, β-blockers (pindolol/atenolol), and fluoroquinolones (ofloxacin/norfloxacin) with rOCT1, rOCT2, hOCT1, and hOCT2 in stably transfected HEK293-cells were studied. Kidney transplantation was associated with reduced expression of rOCT1, while rOCT2 showed only reduced expression after allogeneic transplantation. All drugs interacted subtype- and species-dependently with OCT. However, only atenolol, pindolol, and ofloxacin were transported by hOCT2, the main OCT in human kidneys. While CsA is not an OCT substrate, it exerts a short-term effect on OCT activity, changing their affinity for some substrates. In conclusion, appropriate drug dosing in transplanted patients is difficult partly because OCT are down-regulated and because concomitant CsA treatment may influence the affinity of the transporters. Moreover, drug-drug competition at the transporter can also alter drug excretion rate.
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The aim of this study was to evaluate the species distribution, antibiotic-resistance profile and presence of enterotoxin (SE) genes in staphylococci isolated from the Dilúvio stream in South Brazil. Eighty-eight staphylococci were identified, 93.18% were identified as coagulase-negative (CNS) and 6.82% coagulase-positive (CPS). Fourteen Staphylococcus species were detected and the most frequently were Staphylococcus cohnii (30.48%) and S. haemolyticus (21.95%). Resistance to erythromycin was verified in 37.50% of the strains, followed by 27.27% to penicillin, 12.50% to clindamycin, 6.81% to trimethoprim-sulfamethoxazole, 5.68% to chloramphenicol and 2.27% to norfloxacin. None of the investigated strains showed gentamicin and ciprofloxacin resistance. The strains were tested for the presence of sea, seb, sec, sed and see genes by PCR and only CNS strains (43.18%) showed positive results to one or more SE genes. The scientific importance of our results is due to the lack of data about these topics in polluted waters in Brazil. In conclusion, polluted waters from the Dilúvio stream may constitute a reservoir for disseminating antibiotic-resistance and enterotoxin into the community. In addition, the detection of staphylococci in the polluted waters of the Dilúvio stream indicated a situation of environmental contamination and poor sanitation conditions.
From 1986 to 1994, 812 P. aeruginosa, 1997 E. coli, 437 P. mirabilis, 400 Klebsiella spp., 238 Enterobacter spp., 130 Serratia spp. strains were isolated from clinical materials in the Microbiology laboratory of the Infectious Diseases Institute of Policlinico Monteluce, Perugia University. During the study period the Authors observed the following variations in the susceptibility patterns: increased resistance of P. aeruginosa to piperacillin from 20.8% to 27.2% (P<0.05), amikacin from 11.9% to 17.5% (P<0.05), netilmicin from 11.8% to 28.6% (P<0.01), pefloxacin from 74.4% to 87.8% (P<0.01); E. coli to norfloxacin, ciprofloxacin and pefloxacin, respectively from 1.3% to 3.6% (P<0.001), from 1.5% to 3.6% (P<0.05) and from 3.2% to 9% (P<0.001); Serratia spp. to ceftazidime from 14% to 33.3% (P<0.05); Enterobacter spp. to norfloxacin from 5.1% to 13.6% (P<0.05), cotrimoxazole from 12.8% to 23.5% (P<0.05) and chloramphenicol from 19.4% to 31.8% (P<0.05). Moreover cephalotin resistant strains of E. coli decreased from 29.3% to 21.3% in the last 4 years (P<0.001).