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In a double-blind clinical study, 109 adult Egyptian patients infected with Shigella spp. and 45 infected with Salmonella spp. were randomly assigned to three treatment groups: 1) norfloxacin in a single 800-mg dose, 2) norfloxacin, 400 mg twice a day for three days, and 3) trimethoprim (160 mg)-sulfamethoxazole (800 mg) (TMP-SMX), twice a day for three days. Among Shigella-infected patients, diarrheal symptoms had resolved in 86-97% and bacteriologic failure (repeat positive stool culture) occurred in only two patients five days after the start of the three treatment regimens. Among Salmonella-infected patients, diarrheal symptoms had resolved in 76-82% of patients and bacteriologic failure was common (18-36%) five days after the start of therapy. These data indicate that short-course therapy with either norfloxacin or TMP-SMX can be effectively used to treat shigellosis in adults in developing countries. However, for uncomplicated Salmonella spp. infection, short-course therapy with norfloxacin and TMP-SMX may not lead to a rapid resolution of symptoms or consistently eliminate this enteropathogen. more...

A double blind, prospective study was undertaken to compare aqueous humour penetration of topical 0.3% norfloxacin and 0.3% ciprofloxacin and their effect upon normal eyelid flora in 39 patients undergoing cataract surgery. Lid swabs were taken before and after six 1 hourly applications of single drops of ciprofloxacin or norfloxacin given before surgery. Aqueous humour was aspirated at surgery and antibiotic concentration assayed using high performance liquid chromatography. The mean aqueous humour concentrations were: ciprofloxacin 220 ng ml-1, norfloxacin 140 ng ml-1. Although this difference was not statistically significant (p = 0.112) the trend demonstrated may be relevant clinically, especially considering the greater activity of ciprofloxacin. Both coagulase negative staphylococcal (p = 0.004) and total bacterial (p = 0.019) lid counts dropped sixfold after ciprofloxacin treatment but the smaller reductions noted after norfloxacin application did not achieve statistical significance (p > 0.1). The reduction of external eye flora experienced with ciprofloxacin suggests that this may be a useful presurgical prophylactic agent. more...

Three clinically normal pigs were given a single intramuscular injection of an aqueous solution of norfloxacin nicotinate (NFN) at 14 mg/kg body weight. Animals were killed 4 h after treatment and the concentrations of norfloxacin in various biological fluids and tissues were determined by chemical (high performance liquid chromatography, HPLC) and microbiological assay methods. Drug distribution throughout the body was presented as actual concentrations (micrograms/ml and ppm) in each sample and as the ratio of drug concentration in tissue to drug concentration in plasma. Highest concentrations were found in the urine, kidney, liver and bile. The drug was not detected in ocular fluid, brain tissue (by microbiological assay), fat (by HPLC) and skin (by HPLC). Tissue-to-plasma concentrations ratios were near to, or greater than, 1.0 (HPLC assay) for the kidney, liver, spleen, muscle, lung, adrenals, salivary glands, pleural and synovial fluid, and smaller than 1.0 for cerebrospinal fluid, brain tissue and lymph nodes. Agreement between the chemical and microbiological assay results was variable, depending on the type of tissue and biological fluid tested. Binding of norfloxacin to plasma proteins in pig is low (23%-29%). The distribution pattern of the drug in pig, laboratory animals and humans is very similar; it can be characterized as extensive, with tissue-to-serum ratios reaching 2:1 or more in certain non-excretory organs. These values may reflect intracellular concentrations of the drug. more...

Purpose: To determine the intraocular penetration of topically applied fluoroquinolone antibiotics into aqueous humor., Methods: Thirty-two patients undergoing cataract extraction received either 0.3% ciprofloxacin, 0.3% norfloxacin, or 0.3% ofloxacin topical drops. The patients were given two drops 90 minutes preoperatively and two drops 30 minutes preoperatively. At the time of surgery, 0.1 ml aqueous fluid was aspirated from the anterior chamber and immediately stored at -70 degrees C., Results: Concentrations of ciprofloxacin, norfloxacin, and ofloxacin were determined using a broth dilution bioassay. Morganella morganii with a known minimal inhibitory concentration was used to assay ciprofloxacin and norfloxacin levels. Salmonella enteritidis with a known minimal inhibitory concentration was used to assay ofloxacin levels. Topically applied ciprofloxacin achieved a mean aqueous level of 0.072 microgram/ml (range, 0.02-0.153 microgram/ml). One sample was below the sensitivity of the bioassay. Topical norfloxacin achieved a mean aqueous level of 0.0570 microgram/ml (range, 0.046-0.10 microgram/ml). Seven samples did not reach the sensitivity of the bioassay. Topical ofloxacin achieved a mean level in the aqueous humor of 0.338 microgram/ml (range, 0.078-0.625 microgram/ml). There was no statistically significant difference in intraocular aqueous humor levels of ciprofloxacin versus norfloxacin (P > 0.05). Topical ofloxacin achieved aqueous humor levels significantly higher than either ciprofloxacin or norfloxacin (P < 0.004)., Conclusion: Of the currently available topical fluoroquinolone antibiotics, ofloxacin achieves the highest aqueous humor concentrations. more...

Background: The aim of this study was to test whether the spontaneous cure rate is higher in dysuric women with low urinary colony counts (10(2) to 10(4) colony-forming units [cfu] per milliliter) than in women with high colony counts (> or = 10(5) cfu/mL) and whether the response of patients with low colony counts to single-dose treatment is better than those with high colony counts., Methods: Dysuric women underwent a clinical interview, examination, urine culture, and microscopic examination of urine, and were asked to postpone treatment for 2 days. At that time, the urine tests were repeated. Women with bacterial urinary tract infection were randomized to a group given a single dose of 1200 mg of norfloxacin and to a group treated with 400 mg of norfloxacin twice daily for 7 days. Cure rates were tested at 1 and 5 weeks after treatment., Results: Of 146 women with urinary tract complaints, 113 (25 patients with sterile urine cultures, 21 with low colony counts, and 67 with high colony counts) agreed to postpone antibiotic treatment. Two days after the initial urine culture, only one patient with a low initial colony count had a sterile urine culture (5%, 95% confidence interval, 0% to 14%); and 10 patients (48%, 95% confidence interval, 27% to 69%) had a colony count of 10(5) cfu/mL or more. The rate of spontaneous cure in women with high initial colony count was 7%, 95% confidence interval, 1% to 13%. One week after treatment, the cure rates were 48 (84%) of 57 patients given single-dose treatment vs 49 (98%) of 50 patients treated for 7 days. Five weeks after treatment the rates were 63% and 83%, respectively. The efficacy of single-dose treatment in patients with low urinary counts were similar to those with high counts, and less than that achieved by 7 days of treatment., Conclusions: The spontaneous cure rate for a 2-day period is minimal in patients with both a low and a high colony count, but half of the patients with low urinary counts will have high colony counts after this interval. The response to single-dose treatment is similar in patients with low and high colony counts, and lower than with multiday treatment. more...

The effect of sucralfate on the pharmacokinetics of norfloxacin and ofloxacin was assessed in two separate crossover studies with healthy volunteers. In both studies, eight subjects were randomized to one of the following three regimens: a 400-mg dose of norfloxacin or ofloxacin alone, norfloxacin or ofloxacin given simultaneously with sucralfate (1 g), or norfloxacin or ofloxacin given 2 h before sucralfate. Coadministration of sucralfate reduced the bioavailability of norfloxacin and ofloxacin by 91% (P < 0.001) and 61% (P < 0.001), respectively. However, when norfloxacin and ofloxacin were given 2 h before sucralfate, there were no significant alterations in the pharmacokinetics of either fluoroquinolone. Similar results were obtained when the cumulative amount of each fluoroquinolone recovered in the urine was used to calculate bioavailability. To avoid these interactions and potential therapeutic failures, norfloxacin and ofloxacin should not be used concurrently with sucralfate. The interaction can be minimized by maximizing the time between the fluoroquinolone dose and the previous sucralfate dose and giving the fluoroquinolone at least 2 h before another sucralfate dose. more...

Pharmacokinetic behavior involved in the entry of four quinolone antibacterial agents, norfloxacin (NFLX), ciprofloxacin (CPFX), ofloxacin (OFLX) and nalidixic acid (NA), into cerebrospinal fluid (CSF) was comparatively investigated in rats. Periodically, after the bolus i.v. dose of each quinolone (10 mg/kg), aliquots of CSF were collected by cisternal puncture and blood samples were then withdrawn from the jugular vein. CSF and serum (total and unbound) levels of the drugs were determined by HPLC method. Transport parameters for three new quinolones (NFLX, CPFX, OFLX) into CSF were obtained by physiological model analysis. Serum levels of OFLX and NFLX declined bi-exponentially with time, whereas the serum levels of NA and CPFX declined in mono-exponential and tri-exponential fashion, respectively. Fractions of each quinolone unbound to serum protein (approximately 0.7 for NFLX, CPFX, and OFLX, 0.12 for NA) were almost the same at any point in time. The CSF levels of these quinolones rose quite rapidly after drug administration, and then declined, along with their serum levels. Both the CSF level and the ratio of CSF concentration to serum unbound concentration were the highest for NA, followed by OFLX, CPFX and NFLX. These values of the four quinolones were almost proportional to the apparent partition coefficient (Papp) between n-octanol and phosphate buffer (pH 7.0) values of each reported in a previous paper [Tsuji et al., Antimicrob. Agents Chemother., 32, 190 (1988)]. In the three new quinolones, OFLX had a larger value of apparent diffusional clearance between blood and CSF (PAc) than CPFX and NFLX.(ABSTRACT TRUNCATED AT 250 WORDS) more...

Consecutively collected semen samples from a breeding bull were found to be contaminated with Pseudomonas aeruginosa. Palpation through the bull's scrotum revealed inflammatory changes suggestive of chronic orchiepididymitis in one testicle. For 10 months, all the bull's 13 ejaculates were discarded because the post-thaw viability was < 20%. Norfloxacin nicotinate was injected intramuscularly into the bull at 5 mg/kg daily for 7 days. Serum and semen samples were collected at 24-h intervals during the course of treatment and afterwards and were assayed for NFN concentrations. Drug concentrations in the semen, by microbiological assay, during treatment and up to 120 h after the last treatment ranged from 2.6 to 5.1 micrograms/ml, 14.2 to 43.2 times the corresponding serum drug levels. P. aeruginosa was not isolated from the semen 4 or 15 days after the last injection but was re-isolated after 32 and 64 days. A second similar course of NFN was administered and P. aeruginosa was not isolated from semen samples collected on four occasions, 6, 22, 44 and 94 days after the last treatment. more...

The effect of hemodialysis on norfloxacin removal was evaluated in 7 patients. Single 800-mg doses of the drug were given to the subjects prior to dialysis using cuprophan hollow fiber dialyzers. Arterial and venous sample pairs were obtained at hourly intervals during treatment. Norfloxacin plasma concentrations were determined by HPLC. The mean hemodialysis clearance and extraction ratio were 38.84 +/- 10.92 ml/min and 0.19 +/- 0.06, respectively. Small differences in these parameters were observed between dialyzers with different surface areas (p > 0.05) and also between treatments using different blood flow rates (p > 0.05). Since a relatively small amount of norfloxacin is removed by hemodialysis, dosage adjustment is not necessary to compensate for the extracorporeal removal. more...

The effect of a combination regimen using norfloxacin (NFLX) and amphotericin B (AMPH-B) for prevention of infections in patients with acute leukemia being treated by remission-induction chemotherapy in a randomized, controlled trial was studied. One hundred and six consecutive, evaluable patients were randomly assigned to receive orally 200 mg of norfloxacin two or four times daily and 200 mg of amphotericin B four times daily, or amphotericin B only. A smaller percentage of patients with bacteriologically-documented infections was observed in the study group compared with the control group (34.6% vs 56.9%; P < 0.05). The mean number of days that the patients received empirical antibiotic therapy was shorter in the study group (23 days vs 30 days; P < 0.05). The percentage of patients with a gram-negative bacterial infection (9.6% vs 27.5%; P < 0.05) or a fungal infection (17.3% vs 37.3%; P < 0.05) was decreased in the study group. This new combination antimicrobial regimen is safe and effective for prevention of gram-negative bacterial as well as fungal infections in patients with acute leukemia being treated with cytotoxic remission-induction chemotherapy. more...

Fifteen patients of uncomplicated falciparum malaria from Delhi were treated with norfloxacin (10 with 400 mg, 5 with 800 mg, both twice daily) for 3 days and the response was measured according to the WHO extended in vivo test criteria. The lower dose produced S response in two, RII response in five and RIII response in three patients, while the higher dose produced S response in four and RI response in one patient. In patients with S or RI response, the parasite clearance time was 68.6 +/- 9.1 h the defervescence time being 48 h. Thus, norfloxacin did reveal in vivo activity in falciparum malaria, but a dose of 400 mg twice daily proved to be curative only in a small percentage of cases and not consistently. Nausea and bitter taste were the only side effects noted in two patients. more...

The efficacy of the antimicrobial drug norfloxacin for treating infectious coryza was examined in 26-week-old male broiler breeders. Chickens were inoculated in the infraorbital sinus with the causal organism, Haemophilus paragallinarum. Four experimental groups were set up: control uninfected chickens, infected untreated chickens, and infected chickens treated for 5 days with either 20 mg norfloxacin/kg body weight or 40 mg norfloxacin/kg body weight. The first clinical signs were seen 24 hr postinfection. Of the observed clinical signs, sinus edema was ameliorated by the treatment, and the percentage of birds presenting sinus edema, sneezing, and increased lacrimation was significantly reduced after treatment. Clinical signs disappeared rapidly and were gone by the second day of treatment. The other signs disappeared gradually over 2 weeks after treatment began. There were no significant differences between the two dosage levels. H. paragallinarum was not reisolated from the infected infraorbital sinuses of birds treated with the higher dose of the drug, whereas the reisolation rate was 17% from those treated with the lower dose and 86% from the infected untreated birds. more...

Objective: To study the effectiveness of single-dose norfloxacin and ofloxacin in the treatment of gonococcal urethritis in men, and to monitor in vitro antimicrobial susceptibility to these antibiotics over time., Setting: Centre Médico-Social de Bilyogo, Kigali, Rwanda. The only clinic in Rwanda using quinolones for the treatment of gonorrhoea., Methods: As part of a monitoring programme, men with gonococcal urethritis were evaluated after treatment with norfloxacin (800 mg) in 1986 and 1987, and after treatment with ofloxacin (400 mg) in 1989., Results: Neisseria gonorrhoeae was eradicated from the urethra from 96.0% (189/197) and from 97.1% (166/171) men treated with norfloxacin and ofloxacin, respectively. Overall 38.2% of the pretreatment isolates produced penicillinase (PPNG isolates) and 20.4% (44/216) of the tested non-PPNG isolates were chromosomally resistant to penicillin (MIC > or = 2.0 mg/l). Resistance to tetracycline and thiamphenicol was common in both PPNG and non-PPNG and increased considerably in 1989. All isolates were susceptible to kanamycin, spectinomycin, ceftiaxone, norfloxacin, ofloxacin and ciprofloxacin. However, a higher number of isolates recovered in 1989 showed decreased susceptibility to the quinolones. Treatment failure occurred more often in subjects with isolates having MIC values > or = 0.06 mg/L of norfloxacin (p = 0.006). Seven out of 13 patients who did not respond to therapy had no signs nor symptoms of urethritis., Conclusion: Quinolone antibiotics are now indicated as a first line treatment of gonorrhoea in countries with a problem of antimicrobial multiresistance. However, antimicrobial susceptibility to the quinolones may decrease rapidly, and close monitoring of the in vitro susceptibility of N gonorrhoeae and the clinical effectiveness of the antibiotics is imperative. more...

Patients were entered in a double-blind, placebo-controlled, multicenter study to compare low- and high-dose fleroxacin with norfloxacin for the treatment of complicated urinary tract infection (UTI). A total of 296 patients were enrolled; 102, 97, and 97 patients were randomized to receive 200 mg of fleroxacin (low-dose), 400 mg of fleroxacin (high-dose), both once daily, or 400 mg of norfloxacin twice daily, respectively, for 10 days. Of these patients, 101, 94, and 95 were included in the safety analysis, and 71, 61, and 58 in the efficacy analysis. The main reason for exclusion from the efficacy analysis was failure to isolate a pathogen at baseline. The groups were comparable with respect to demographics. In the low-dose fleroxacin group, 68 (96%) of 71 patients had bacteriologic cures (eight with superinfection), compared with 56 (92%) of 61 in the high-dose fleroxacin group (two with superinfection) and 52 (90%) of 58 in the norfloxacin group (four with superinfection). Escherichia coli was the most frequent isolate in all groups. In the low-dose fleroxacin group, clinical cure was recorded in 61 (86%) of 71, improvement in six, and failure in four. In the high-dose group, clinical cure was noted in 58 (95%) of 61 patients, improvement in two, and failure in one. In the norfloxacin group, 50 (86%) of 58 patients were clinically cured, four were improved, and four failed. Clinical adverse events were reported by 22 (22%) of 101, 36 (38%) of 94, and 19 (20%) of 95 patients in the low-dose fleroxacin, high-dose fleroxacin, and norfloxacin groups, respectively. Insomnia and nausea were reported most frequently in the fleroxacin groups, and nausea and headache were most common in the norfloxacin group. The efficacy and safety of low-dose fleroxacin are comparable to those of norfloxacin for treatment of complicated UTI. more...

Fleroxacin, 400 mg once daily, and norfloxacin, 400 mg twice daily, both administered orally, were compared for the treatment of serious urinary tract infections (UTIs). In total, 301 patients from multiple centers who had serious UTIs were randomized to receive fleroxacin or norfloxacin in a double-blind study. The demographic parameters of the two groups were similar. A total of 190 patients were evaluable for efficacy, 94 in the fleroxacin group and 96 in the norfloxacin group. The reasons for exclusion from the efficacy analysis were not significantly different in the two groups, but more patients receiving fleroxacin were prematurely withdrawn from the study. The majority (134) of the diagnoses were complicated UTI, and the pathogens were primarily Enterobacteriaceae. The clinical responses were cure or improvement in 98% of the fleroxacin group and 92% of the norfloxacin group and failure in 2% of the fleroxacin group and 7% of the norfloxacin group. The bacteriologic results by infection were cure in 98% of the fleroxacin group and 89% of the norfloxacin group (including cure with superinfection in 4% of the fleroxacin group and 5% of the norfloxacin group) and failure in 2% of the fleroxacin group and 11% of the norfloxacin group. Adverse events were more common in the fleroxacin group and were mostly nausea, insomnia, and headache. Fleroxacin, 400 mg once daily, was as effective as norfloxacin, 400 mg twice daily, in eradicating UTIs but was associated with more adverse events. more...

A randomized, controlled trial was carried out to compare two courses of treatment in women with acute urinary tract infection in general practice. The 3-day course of treatment was found to be as effective as, and cheaper than, the 7-day therapy. more...

A total of 125 ambulatory women (85 premenopausal and 40 postmenopausal) who experienced 174 acute urinary tract infections with mainly gram-negative bacteria (99%) was randomized to receive a single dose, 2-tablet treatment with either ofloxacin (400 mg.), norfloxacin (800 mg.) or ciprofloxacin (500 mg.). Cure was achieved in 163 of the 174 acute episodes (94%). More specifically, the cure rates were 97% (57 of 59 infections) with ofloxacin, 96.5% (56 of 58) with ciprofloxacin and 88% (50 of 57) with norfloxacin. While the initial cure rate of the acute urinary tract infections was 96% (112 of 117) in the premenopausal group, it reached only 90% (51 of 57) in the postmenopausal group. The 17 urinary tract infections that followed the initial 2-tablet quinolone treatment were cured by either an additional single dose, 2-tablet treatment with a different quinolone in 6 cases, a 1-day treatment with other adequate antibacterials in 9 and a 7-day treatment in 2. The 2-tablet quinolone treatment proved to be an effective, easy and cost-effective treatment for acute urinary tract infections in premenopausal and postmenopausal women. more...

This multicentre, open, randomized trial, involving 482 patients and conducted by private practitioners, compared the effectiveness and safety of a single 800 mg dose of pefloxacin and of a 10 days' course of norfloxacin 400 mg bid. in the treatment of uncomplicated acute cystitis in women aged over 50 years. Clinical effectiveness was evaluated on days 17-19 and 28-32 respectively, and bacteriological effectiveness on days 15-17 and 26-28 respectively. The median time taken for the symptoms to disappear was 2 days with pefloxacin and 3 days with norfloxacin (P < 0.001). Irrespective of the nature of cystitis and the patients' age, no significant difference could be found in eradication of the pathogens. Undesirable side-effects were recorded in 7.8 percent of patients under pefloxacin and in 8.8 percent of those under norfloxacin (P = 0.68); gastrointestinal disorders were predominant. The acceptability of treatment, as judged by the patients themselves, was regarded as excellent by 55 percent of women treated with single dose pefloxacin and by 37.6 percent of those treated with norfloxacin (P = 0.001). more...

Objective: To make an assessment of the effectiveness and safety of a single oral dose compared with the conventional way of treating low-level Urinary Infections presenting no complications., Design: This was an investigative and prospective study, using a control, a simple blind and randomised sample. SITE. Health Centres in Oviedo and Zaragoza., Patients or Others Participants: We looked at 150 patients and included 106 females between the ages of 16 and 75 in the study. Their clinical symptoms were compatible with low-level urinary infections presenting no complications., Interventions: 49 patients were given Trometamol Phosphomicine (TP) in a single oral dose; 36 took Pipemidic Acid (PA) and 21 Norfloxacine (NFX), both of these in a dose of 400 mg twice a day for 5 to 7 days., Main Measurements and Results: Clinical and bacteriological assessments of the results were made 3, 7, and 28 days after treatment. A total of 75 gems were isolated: E. coli was the most common (68%). In all three groups, the main symptoms rapidly disappeared after the start of the treatment., Conclusions: Having considered the bacteriological and clinical findings, as well as tolerance levels, we are able to conclude that a single oral dose of Trometamol Phosphomicine is a good alternative to conventional therapy for the treatment of low-level Urinary Infections Which present no complications. more...

Optimal therapy for pyelonephritis requires the immediate administration of an effective broad-spectrum antibiotic. Because conventional oral antibiotics such as the sulfonamides and the aminopenicillins are limited by the development of resistant bacteria associated with this common disease, the therapeutic effectiveness of a new oral carbacephem antibiotic was investigated. Two double-blind, randomized clinical trials of loracarbef (LY163892) were conducted. A total of 245 patients (greater than or equal to 18 years old) with uncomplicated pyelonephritis were enrolled in parallel studies. One study compared loracarbef with cefaclor; the other compared loracarbef with norfloxacin. In the combined patient population, 119 patients were treated with loracarbef (400 mg twice daily), 43 with cefaclor (500 mg three times daily), and 83 with norfloxacin (400 mg twice daily). All treatment regimens continued for greater than or equal to 14 days. A total of 68 patients in the loracarbef group, 25 in the cefaclor group, and 43 in the norfloxacin group qualified for efficacy analysis. Escherichia coli was the causative pathogen in 85.0% of these patients. Successful posttherapy clinical and bacteriologic responses were similar for all three study drugs: 94.1 and 86.8%, 96.0 and 80.0%, 97.7 and 88.4% for loracarbef, cefaclor, and norfloxacin, respectively. Late posttherapy clinical responses were 87.4, 83.3, and 91.7% for the loracarbef, cefaclor, and norfloxacin groups, respectively. Bacteriologic responses for the three groups were 79.6, 60.0, and 88.9%. The most frequent adverse effects (headache, diarrhea, and nausea) were experienced by three patients (2.5%) in the loracarbef group; headaches were noted in two (4.7%) cefaclor patients, diarrhea was noted in three (7.0%) patients in the cefaclor group, and nausea was noted in four (9.3%). Gastrointestinal events were noted in four patients (4.8%) in the norfloxacin group. The data demonstrate that loracarbef is comparable in efficacy and safety to both cefaclor and norfloxacin as oral therapy for uncomplicated pyelonephritis. more...

In this double-masked study, we randomly assigned 488 patients with clinical signs of acute bacterial conjunctivitis or blepharitis, or both, to treatment with either norfloxacin ophthalmic solution 0.3% (245) or gentamicin ophthalmic solution 0.3% (243) for one week. Of the patients with positive cultures, 71% (85 of 120) of the norfloxacin-treated patients and 65% (86 of 133) of the gentamicin-treated patients were clinically cured. An additional 25% (30 of 120) of norfloxacin-treated patients and 32% (43 of 133) of gentamicin-treated patients were clinically improved. On the basis of posttreatment cultures, 89% of all cultured bacteria were eradicated (146 of 179 organisms) or suppressed (14 of 179 organisms) after treatment with norfloxacin. The condition of five norfloxacin-treated patients did not clinically improve, compared with the condition of eight gentamicin-treated patients. Both antibiotics had similar efficacy against gram-positive and against gram-negative organisms. One norfloxacin-treated patient and two gentamicin-treated patients withdrew from the study because of local intolerance. Norfloxacin appears to be an effective and relatively safe agent for the treatment of bacterial infections of the eyelids or conjunctiva, or both. In this study, norfloxacin was clinically and microbiologically similar in activity to gentamicin. more...

A novel approach using a self-setting hydroxyapatite (HAP) cement as a skeletal drug-delivery system has been proposed to solve the problem of delivering drugs to skeletal tissue at sufficiently high local concentrations for desirable therapeutic effects. HAP cements loaded with antibiotics can be formed in situ and can be used as bonding materials between bone and prostheses, as well as drug-release devices. The cement also possesses sufficient mechanical strength to be a potential bone grafting material. Using cephalexin and norfloxacin as model drugs, we observed continuous in vitro release profiles of these compounds from cement pellets loaded 0.9-4.8% by weight with one of the drugs. This drug-release pattern correlated well with the Higuchi model. This hydroxyapatite cement drug-delivery system can be applied in the treatment of osteomyelitis and infected compound fractures. more...

Seventy-three patients mainly receiving consolidation therapy for acute leukemia or autologous bone marrow transplantation were studied in a randomized trial comparing nystatin with norfloxacin (800 mg) given orally QID, for prevention of infection. Both groups were equally distributed in regard to age, disease, and duration of granulocytopenia, although far more patients entered the laminar air flow room in the norfloxacin group. Duration of more than a 39 degrees C fever was much longer in the nystatin group than in the norfloxacin group: Bacteremia, microbiologically documented infections, and fever of unknown origin were more frequently seen in the nystatin group, but there was no significant difference between the two groups. On the other hand, patients without fever during granulocytopenia were more numerous in the norfloxacin group than in the nystatin group (p less than 0.05). Furthermore, three deaths during granulocytopenia occurred in the nystatin group. In conclusion, prophylactic administration of norfloxacin during granulocytopenia showed a significant afebrile period. more...

Unlabelled: BACKGROUND--This study was undertaken to determine whether therapy for acute uncomplicated urinary tract infection in women with single-dose therapy with norfloxacin was superior to 3 days of norfloxacin therapy in efficacy or adverse effects. METHODS--The study was a multicenter, prospective, randomized, double-blind trial. Women with acute, uncomplicated urinary tract infection were randomized to receive norfloxacin, 800 mg as a single dose or 400 mg twice daily for 3 days. Clinical and laboratory evaluations were obtained before therapy and at days 3 and 7 and 4 to 6 weeks after initiation of therapy. RESULTS--The 83 subjects for whom data could be evaluated who received 3-day therapy had significantly improved outcome compared with the 73 subjects for whom data could be evaluated who received single-dose therapy at 3 days and 7 days after initiation of therapy. At 4 to 6 weeks, 88% of subjects who received 3 days of therapy remained cured, compared with 78% who received single-dose therapy. Three-day and single-dose therapy were equivalent for Escherichia coli infection, but single-dose therapy was significantly less effective for other organisms, primarily because of failure of treatment of Staphylococcus saprophyticus infection. Women older than 40 years were significantly less likely to be cured with either treatment regimen and with single-dose therapy. Adverse effects were similar for both treatment regimens., Conclusions: -Three days of norfloxacin therapy is more effective than single-dose therapy for women with acute, uncomplicated urinary tract infection. The two regimens are equally effective for E coli infection, but single-dose therapy is ineffective for S saprophyticus. more...

The aim of the study has been to assess if intermittent treatment with norfloxacin could be able to maintain selective intestinal decontamination in cirrhotic patients in order to prevent bacterial infections. Group I (n = 10, subgroup Ia, n = 5, hospitalized cirrhotics, subgroup Ib, n = 5, outpatient cirrhotics) received 400 mg/24 h norfloxacin 7 days. Group II (n = 5, outpatient cirrhotics) received 400 mg/12 h norfloxacin 7 days. Gram-negative aerobic bacilli of the fecal floral were strongly suppressed in all patients at the end of the treatment, and they totally (Group I) or partially (Group II) recovered the initial concentrations 7 days after the end of the treatment. There were not significant differences between subgroups Ia and Ib. These results suggest that prophylactic treatment with norfloxacin in cirrhotic patients at high risk of infection should be continuous during the period in whom patients must be submitted to selective intestinal decontamination. more...

A review of 115 cases of ulcerative keratitis that were diagnosed and treated at the specialized ambulatory care center for infectious eye diseases at the 2. Department of Ophthalmology over a period of eight years (January 1983-April 1991) is presented. In the analysis of the etiology nearly half (47.7%) were observed following a trauma to the epithelium, 38 (= 33.0%) were associated with contact lens wear and the third largest group (10.4%) was associated with lid problems. It is apparent that over the course of the last years the spectrum of microorganisms associated with this localized inflammation has shifted: the prevalence of Staphylococci (1983-1986 = 65%) has decreased, whereas the incidence of gram-negative rods increased (1987-1990 = 49%). In 19% Pseudomonas aeruginosa could be isolated, mostly associated with soft contact lens wear. A total of 37.5% of the staphylococci isolates were found to be resistant to gentamicin, most probably as a consequence of the widespread, indiscriminate use of this antibiotic. An updated treatment schedule is presented. more...

A series of 140 patients, undergoing various types of urological endoscopic procedures, was divided into 2 equal, parallel, randomised groups. The first group of 70 patients, undergoing lower urinary tract surgery, was randomised, half to receive norfloxacin prophylaxis and half no antibiotic cover; the other 70 patients, undergoing percutaneous renal surgery, were randomised, half to receive norfloxacin and half cefuroxime. It was found that 26% of patients not receiving antibiotic prophylaxis and 11% on cefuroxime prophylaxis developed post-operative bacteriuria, with a high incidence of urinary tract infection (UTI). Only 1 patient of 70 on norfloxacin prophylaxis developed post-operative bacteriuria, which quickly responded to prolongation of norfloxacin therapy. Prior to surgery, 10% of all patients were found to have previously undetected bacteriuria. This group was at high risk of developing post-operative infection. Norfloxacin effectively prevented post-operative bacteriuria and urinary tract infection in these patients. This study suggests that norfloxacin is a safe and effective prophylactic antibiotic in all forms of urological endoscopic procedures. more...

Two hundred and eighty-four patients with acute conjunctivitis were enrolled in a double-masked study comparing norfloxacin ophthalmic solution with placebo. The proportion of patients who were clinically improved after 5 days treatment was 88.1% in the norfloxacin group and 71.6% in the placebo group (p less than 0.01). The proportion of patients who had all organisms eradicated, including the coagulase-negative staphylococci, after two to three days treatment was 52.7% for norfloxacin and 23.9% for placebo (p less than 0.01) and 64.7% and 26.3% (p less than 0.01) respectively when the coagulase-negative staphylococci were not included. Adverse experiences occurred in 4.2% of the patients receiving norfloxacin compared to 7.1% of the placebo patients. None of the adverse experiences was serious. more...

15/60 subjects from one center, who all took part in a multicenter double-blind, placebo-controlled study to evaluate the effect of norfloxacin on acute enteritis, had norfloxacin sensitive strains of Campylobacter jejuni in pre-study stool specimens. Eight of the 15 subjects received active drug. In 3 of these 8, high-level quinolone resistant Campylobacter strains of the same serotype as in pre-treatment samples were isolated 4-90 days after the initiation of treatment. more...

Two hundred and forty-six patients with signs of acute bacterial conjunctivitis and/or blepharitis were randomised to receive either norfloxacin or chloramphenicol for one week in this double-masked parallel group study. Ninety-two per cent of the norfloxacin-treated patients and 93% of the chloramphenicol-treated patients were rated as either clinically improved or cured at the end of the treatment period. Based upon pre-treatment bacteriological cultures, 31.3% of the patients had significant bacterial infection of the lids and/or conjunctiva. All of these culture-positive patients were rated as either clinically improved or cured. Based upon post-treatment cultures, 72 of 82 strains of Gram-positive and Gram-negative bacteria were eradicated or suppressed following treatment with either norfloxacin or chloramphenicol. However six of 41 strains persisted for norfloxacin and four of 41 for chloramphenicol. Two norfloxacin-treated patients and three chloramphenicol-treated patients had adverse experiences, predominantly ocular discomfort, which required cessation of drug therapy. Norfloxacin appears to be an effective and relatively safe agent for the treatment of bacterial infections of the lids and/or conjunctiva. In this study, norfloxacin was clinically and microbiologically similar in activity to chloramphenicol. more...

The in vitro activities of enoxacin, lomefloxacin, norfloxacin, ofloxacin, and pefloxacin against 274 strains of Salmonella typhi isolated from suspected typhoid fever patients (137 multi-resistant strains and 137 strains sensitive to chloramphenicol, ampicillin and/or co-trimoxazole) were determined using disk diffusion and agar dilution techniques. In vitro, enoxacin was active against all tested strains with a MIC90 and inhibition zone size against multi-resistant strains of 0.12 mg/l and 34 mm diameter, respectively. Similar results were found with the other fluoroquinolones. Enoxacin and other fluoroquinolones may be the therapy of choice in cases of typhoid fever caused by organisms resistant to the standard therapy, chloramphenicol. more...

Temafloxacin is a new oral fluoroquinolone with broad-spectrum antimicrobial activity against gram-negative and gram-positive pathogens. The safety and efficacy of temafloxacin were evaluated in a multicenter, double-blind study of patients with complicated urinary tract infections. Patients were randomized to receive temafloxacin 400 mg (n = 138) or norfloxacin 400 mg (n = 141). Treatment was given orally twice daily for 10-14 days. Clinical response (cure or improvement) occurred in 75 of 78 patients (96%) in the temafloxacin group and in 89 of 91 patients (98%) in the norfloxacin group. Bacteriologic eradication rates in both treatment groups exceeded 95%. Adverse events occurred in a similar, low percentage of patients in both treatment groups and consisted primarily of nausea and dizziness. Temafloxacin appears to be as safe and effective as norfloxacin in the treatment of complicated urinary tract infections. more...

We studied the efficacy of a fourteen-day course of the fluoroquinolone, norfloxacin, in a group of 69 catheter-free spinal cord injury (SCI) outpatients who experienced a total of seventy-nine urinary tract infection (UTI) episodes. A total of 114 bacterial strains representing twenty species, including sixteen Pseudomonas aeruginosa, all susceptible to norfloxacin, were isolated from initial urine cultures. Mid-treatment cultures in 58/79 (73%) cases were negative. Cultures taken five to seven days after completing treatment in 42 cases (53%) were negative. In the remaining 37 there was persistence of initial or superinfecting pathogen(s), or early reinfection with new organisms. Cultures eight to twelve weeks later in 32 cases with initial eradication showed that 27 (84%) had either relapsed and/or become reinfected. Clinical cure occurred in 4/6 (67%) symptomatic episodes. Side effects occurred in 6 of 73 (8%) patients who received norfloxacin, 4 of whom required withdrawal from the study. Twenty of one hundred twenty-two (16%) bacterial strains isolated during or after treatment were resistant to norfloxacin. Given the limited oral treatment options and the constant risk of reinfection in the SCI population, norfloxacin appears to be a reasonable choice in many patients. However, as with other antimicrobials, when using norfloxacin in SCI patients, the emergence of resistant bacteria must be carefully monitored. more...

The efficacy of norfloxacin 400 mg every 12 hours for 7 days was prospectively and openly studied among patients with urinary tract infection. Enrolled were 30 patients based on inclusion and exclusion criteria. 23 patients completed the study and were evaluated for efficacy and tolerability with urinary infections defined as a bacterial count of at least 10(5) bacterial per ml of urine. Follow-up urine cultures at 14-21 days and 4-6 weeks post-treatment were done. 21 of 23 were cured and this was a cure rate of 91%. There were no clinical adverse effects which necessitated cessation of treatment. In vitro test studies were carried out to compare the activity of norfloxacin with commonly used antimicrobials as well as to observe its activity against other organisms which are not normally urinary pathogens. In this aspect of the study, norfloxacin was found to be superior to eleven other antimicrobials with which it was compared. This study showed that drug is very active against urinary and enteric pathogens. more...

At the Eastern Section Meeting of the Triological Society January 26, 1990, Levinson et al reported outstanding success with ciprofloxacin in the treatment of malignant otitis externa. Moreover, several of the individuals so managed had been refractory to conventional therapy with semisynthetic penicillin and aminoglycoside protocols. This new class of antibiotics may result in a profound change in our management of patients with otologic, neurotologic, and skull base infections. more...

A novel approach using a self-setting hydroxyapatite (HAP) cement as a skeletal drug delivery system has been proposed to solve the problem of delivering drugs to skeletal tissue at high local concentrations for desirable therapeutic effects. Hydroxyapatite cements loaded with antibiotics can be formed in situ and can be used as bonding materials between bone and prostheses as well as for drug release devices. The cement also possesses sufficient mechanical strength to be a potential bone grafting material. Using cephalexin and norfloxacin as model drugs, the continuous in vitro release profiles of these compounds from 0.9-4.8% by weight loaded cement pellets were observed. These drug release patterns correlated well with the Higuchi model. This hydroxyapatite cement drug delivery system can be applied in the treatment of osteomyelitis and infected compound fractures. more...

Two hundred patients that underwent ESWL were randomized into 4 groups in order to determine the benefits of antibiotic prophylaxis. All comparisons among groups were not statistically significant. Neither cephalosporin nor quinolone prophylaxis impacted significantly on bacteriuria rate after ESWL. Thus, in patients without infected stones, urinary tract obstruction and ancillary procedures ESWL could be performed without prophylactic antibiotic regimes. more...

To evaluate the efficacy of the single dose chemoprophylaxis of recurrent urinary tract infection (UTI) in the elderly, 20 female inpatients (mean age 81.4) who had one or more culture documented UTIs in the past 12 months were studied. They were randomly assigned to be treated for 6 months either with chemoprophylaxis (200 mg of norfloxacin) or conventional therapy (without any antimicrobials except when overt UTI occurred). After a 4 months of washout period, the protocols were exchanged with each other and next 6 months of trial was carried out. All cases were followed at least 4 months after the discontinuance of the chemoprophylaxis. The difference of efficacy between the two modalities was evaluated by periodical examinations of urine cultures, urinalysis and inflammatory markers. During chemo-prophylaxis, the frequency of the symptomatic UTI (bacteriuria greater than 10(4)/ml, pyuria greater than 5/HPF, CRP greater than +) was 0.267/patient.year which was significantly lower than during conventional therapy (2.97/patient.year, p less than 0.01). This prophylactic effect remained 4 months after the discontinuance of the drug. On the other hand, bacteriuria was persistent in more than half of patients with chemoprophylaxis. Minimal inhibitory concentration of norfloxacin for separated bacteria revealed that the resistant species steeply increased from 4 to 6 months after the beginning of chemoprophylaxia. These species disappeared 4 months after the drug was discontinued. Optimal durations of chemoprophylaxis and drug-holidays were discussed. more...

The objective of this study was to assess the effect of a novel regimen of antibiotic prophylaxis on the incidence of lower respiratory tract infection in patients requiring prolonged (at least five days) mechanical ventilation. The design was a controlled, prospective, randomized trial, with blinded comparison of the groups regarding the incidence of respiratory tract infection in an intensive care unit of a university hospital. After determination of the APACHE II score for severity of disease, 88 patients were randomly divided in three groups. Twenty-four of these patients did not complete five days of mechanical ventilation, and eight were withdrawn for other reasons. Fifty-six patients (18 in group 1, 21 in group 2, 17 in group 3) completed the study. Patients in both control groups 1 and 2 did not receive antibiotic prophylaxis, but the two groups differed in the antibiotic policy in case of infection. Patients in group 3 received antibiotic prophylaxis consisting of norfloxacin, polymyxin E, and amphotericin B, applied topically in oropharynx and stomach from time of ICU admission until extubation, and intravenous cefotaxime 500 mg three times a day during the first five days of admission. In both control groups, about 90 percent of the patients acquired microbial colonization of oropharynx or stomach. In group 3, only 12 percent and 24 percent of the patients acquired colonization of oropharynx and stomach, respectively (p less than 0.001). This resulted in a reduction of the incidence of lower respiratory tract infection (78 percent in group 1, 62 percent in group 2, 6 percent in group 3 [p = 0.0001]). The regimen of antibiotic prophylaxis studied prevented respiratory tract infection in mechanically ventilated patients. Antibiotic prophylaxis should be considered in all patients expected to require prolonged mechanical ventilation. more...

The present study investigates the effects of some quinolone carboxylic acid derivatives on GABAA receptor-mediated excitatory responses in gastrointestinal preparations in vivo and in vitro. In stomach-perfused rats, norfloxacin, nalidixic and pipemidic acid dose dependently antagonized acid hypersecretion induced by muscimol. Under the same conditions, the quinolone derivatives failed to modify acid hypersecretion evoked by 2-deoxy-D-glucose. In the isolated guinea-pig ileum, norfloxacin, nalidixic and pipemidic acid antagonized muscimol-elicited contractions in a non-competitive manner. In contrast, these drugs did not influence ileal cholinergic contractions evoked by transmural electrical stimulation or by exogenous acetylcholine. Taken together, these results suggest that the quinolone derivatives tested act as antagonists at both central and peripheral GABAA receptors. In addition, GABAA-mediated gastrointestinal responses might represent a simple and reliable method to assay the GABAA receptor antagonist properties of new quinolone derivatives. more...

The results of an open, randomized study comparing the efficacy and safety of Fosfomycin trometamol (Monuril), 3-gram single dose, and Norfloxacin (Noroxine 400), 400 mg twice daily for 5 days, are reported. Clinical and bacteriological assessments were performed before and 3-4 (short-term) and 25-30 days (long-term) after treatment. Only female patients with uncomplicated lower urinary tract infection were eligible for inclusion in the study: 33 cases were given Fosfomycin trometamol and 30 cases Norfloxacin. In the overall etiology, Escherichia coli (74% of the strains found), Proteus mirabilis (6%) and Klebsiella pneumoniae (6%) are highly predominant. With regard to bacteriological efficacy, the percentages of eradication in the two groups were similar: after the short-term test, 93.9% (31 of 33 patients) in the Fosfomycin trometamol group and 86.6% (26 of 30) in the Norfloxacin group, and after the long-term tests, 73.3% (22 of 30) in the Fosfomycin trometamol group and 77.89% (21 of 27) in the Norfloxacin group. There are no statistically significant differences. The duration of the reported side effects was significantly lower in the Fosfomycin trometamol group. The simplified dosage regimen (single dose) and its favorable benefit/risk ratio justifies the use of Fosfomycin trometamol as a treatment for uncomplicated urinary tract infections in female patients. more...

The Aqueous humor concentration of norfloxacin was measured following topical administration in 20 eyes. The substance was applied at different time intervals. Nineteen samples obtained prior to cataract extraction had mean concentrations between 0.014 and 0.105 microgram/ml. These concentrations are under the MIC90 of most germs. One eye with minimal congestion due to a neovascular glaucoma, however, had a concentration of 0.206 microgram/ml. more...

An aminoglycoside-resistant strain of Pseudomonas aeruginosa was injected intrastromally into the corneas of rabbits, and keratitis was allowed to develop over a 22-h period. Rabbits were treated with either 0.75% ciprofloxacin, 1% norfloxacin, or 1.36% tobramycin administered topically every 15 min for 1 h and then every 30 min for the following 3 h. All therapy ceased 26 h postinoculation. Rabbits were killed 1 h after the treatment, and the number of bacteria per cornea were quantified in terms of bacterial colony-forming units. Aqueous humor specimens were obtained from rabbits receiving norfloxacin and ciprofloxacin, and bioassays were performed to determine drug concentration. Ciprofloxacin caused a 5 log reduction in the number of bacterial colony-forming units, as compared with untreated controls (p less than 0.0001); it also produced a significantly greater reduction in bacterial colony-forming units than either norfloxacin or fortified tobramycin drops (p less than 0.0001). Norfloxacin produced a 2 log reduction in bacterial colony-forming units, as compared with untreated controls (p less than 0.0001). The mean aqueous concentration of norfloxacin (7.5 micrograms/ml) was substantially less than that achieved by ciprofloxacin (30.5 micrograms/ml). We conclude that ciprofloxacin may be a useful broad spectrum, topical chemotherapeutic agent in the therapy of aminoglycoside-resistant P. aeruginosa keratitis. more...

The antimicrobial activity of intravenously given quinolones on the intestinal microflora was unknown and therefore studied in dogs with a surgically isolated loop of the jejunum. Ciprofloxacin, enoxacin and norfloxacin were actively excreted by the intestinal mucosa and achieved therapeutic levels within the lumen of this isolated jejunal loop. Also the total counts of enterococci and Escherichia coli decreased in this loop of the jejunum as well as in the stool. All three quinolones, when given intravenously, decreased the total counts of anaerobic bacteria including Bacteroides fragilis. more...

Rabbit corneas were infected with a tobramycin-resistant (minimum inhibitory concentration, 31.25 micrograms/ml) strain of Pseudomonas aeruginosa 27853 (10(3) colony-forming units) and were treated 22 hours later with collagen corneal shields hydrated in either 25 mg/ml ciprofloxacin, 40 mg/ml norfloxacin, 40 mg/ml tobramycin, or deionized water. Shields were removed at 26 hours postinfection, and 1 hour later, corneas were harvested for bacterial enumeration. Application of shields hydrated in ciprofloxacin reduced the number of viable bacteria per cornea approximately 4 log units compared with the application of shields containing tobramycin or deionized water (P less than 0.0001). Use of shields hydrated in norfloxacin reduced the number of P. aeruginosa organisms by greater than 2 log units compared with shields containing tobramycin or deionized water (P less than 0.0001). Ciprofloxacin was significantly more effective than norfloxacin in reducing the number of bacteria per cornea (P less than 0.0001). There was no significant difference in the number of bacteria recovered from corneas treated with tobramycin or deionized water (P less than 0.56). more...

Ciprofloxacin, pefloxacin, norfloxacin, and ofloxacin were investigated for immunomodulatory activity on humoral and cell-mediated immune responses. Ciprofloxacin and pefloxacin altered the humoral immune responses of mice to sheep red blood cells. This effect was not exhibited by norfloxacin or ofloxacin. All four quinolones did not alter cell-mediated responses. When these antimicrobial agents were tested for their interaction with human polymorphonuclear phagocytic activity, all agents suppressed this activity. In addition, all except norfloxacin showed anti-inflammatory activity. more...

The pharmacokinetic properties of the new fluoroquinolones are characterized by a high volume of distribution, long biological half-life, low serum protein binding, elimination by renal and extrarenal mechanisms with high total and renal clearances, limited biotransformation and moderate to excellent bioavailability after oral administration. However, each quinolone derivative (ciprofloxacin, enoxacin, fleroxacin, norfloxacin, ofloxacin and pefloxacin) possesses individual pharmacokinetic parameters, which should be considered in the treatment of patients, especially when liver or renal dysfunction exists. more...