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PubMed1991

Randomized clinical trial of norfloxacin for shigellosis.

In a randomized clinical trial, norfloxacin was compared with nalidixic acid in the treatment of acute invasive diarrhea, with particular reference to shigellosis in adults. Of 104 patients studied, 40 were positive for Shigella in stool cultures, of which 22 received norfloxacin and 18 received nalidixic acid. The patients in these two groups were comparable on admission. In the treatment of culture-positive shigellosis cases, the responses to therapy with both drugs were similar, except that the duration of fever, anorexia, and abdominal pain were less in those who received norfloxacin. Norfloxacin appeared to be superior to nalidixic acid in the treatment of shigellosis cases caused by Shigella strains resistant to nalidixic acid.

Adult↗

PubMed1985

Inhibition of recovery from potentially lethal damage by chemicals in Chinese hamster V79 A cells.

The inhibition of recovery from potentially lethal damage and the influence of mutation induction by lactate, pyruvate, novobiocin, and nalidixic acid was studied in the stationary phase of Chinese hamster V79 A cells. Lactate and pyruvate were selected to elucidate their possible involvement in the inhibition of recovery from PLD since high levels of lactate and pyruvate accumulate due to increased aerobic and anaerobic glycolysis in tumours. Effects of novobiocin and nalidixic acid were also studied to elucidate the possible role of an enzyme similar to DNA gyrase in the potentially lethal damage recovery of V79 cells. The inhibition of recovery depends on drug concentration and is complete with 20 mM of lactate and pyruvate and 20 microM of nalidixic acid and novobiocin. The chemicals seem to interfere with an early step in the recovery process. Incubation with novobiocin in a post-irradiation period does not change the mutation frequency significantly whereas lactate and pyruvate demonstrate a slight increase. Cells incubated with nalidixic acid showed a significant increase in mutation frequency at 24 h post-irradiation recovery time.

Animals↗

PubMed1986

Quinolones and colonization resistance in human volunteers.

The suppression of alimentary canal flora by the three quinolones nalidixic acid, ciprofloxacin and pefloxacin was investigated in fifteen volunteers. They received the three quinolone compounds in tablet form both uncoated and colon-coated. Escherichia coli suppression was poor under nalidixic acid, but complete under ciprofloxacin and pefloxacin for both administration forms. The indigenous anaerobic flora contributing to the control of aerobic Streptococcus faecalis and Candida albicans in the intestines ('colonization resistance') was not affected by nalidixic acid and pefloxacin, and only slightly by ciprofloxacin. Out of the three quinolone compounds, only colon-coated pefloxacin was associated with a considerable absorption rate at colonic level. Using these criteria of successful Escherichia coli clearing from the intestinal canal--left the indigenous flora more or less intact (in a 'selective' way)--and a good absorption rate, pefloxacin is found to be superior to ciprofloxacin and nalidixic acid. These results suggest that a colon-coated tablet with a low dose of pefloxacin is a promising administration form in the therapy of recurrent urinary tract infections and diarrhoeal diseases and in the prevention of gut colonization in immunocompromised hosts.

Adult↗

PubMed2006

Multidrug resistance and distribution of Salmonella serovars in slaughtered pigs.

The present study was undertaken to estimate the occurrence and distribution of multidrug resistance (MDR) among Salmonella serovars isolated from slaughtered pigs at Debre Zeit, Ethiopia. A total of 501 different samples were examined of which 42 (41.6%) of 101 mesenteric lymph nodes, 22 (21.8%) of 101 tongues, 17 (16.8%) of 101 caecal contents, 11 (11.1%) of 99 livers and two (2%) of 99 muscle (diaphragm and abdomen) samples were Salmonella positive. Of the 94 Salmonella isolates representing 15 different serovars, 69 (73.4%) were multidrug resistant (resistance to two or more antimicrobials). Among the Salmonella serovars a high level of MDR was observed in S. Hadar, S. Kentucky, S. Blockley and S. Enteritidis mainly to tetracycline (88.6%), streptomycin (82.9%), nitrofurantoin (74.3%), nalidixic acid and ciprofloxacin (42.9% each), sulfisoxazole (21.1%) and spectinomycin (20%). The pattern of MDR varied from two to eight antimicrobials among the resistant Salmonella serovars. The common profiles of resistance among the MDR serovars were the combined resistance to nitrofurantoin, streptomycin and tetracycline (R type NitStrTet, 51.4%), ciprofloxacin, nalidixic acid and nitrofurantoin (R type CipNalNit, 10%), ciprofloxacin, nalidixic acid, spectinomycin, streptomycin, sulfisoxazole and tetracycline (R type CipNalSptStrSulTet, 14.3%) and to ciprofloxacin, kanamycin, nalidixic acid, neomycin, nitrofurantoin, streptomycin and tetracycline (R type CipKanNalNeoNitStrTet, 10%). Results of the present study indicate the widespread occurrence and distribution of MDR Salmonella serovars in slaughtered pigs which could be a potential source of human MDR Salmonella infections.

Abattoirs↗

PubMed1998

Genotoxic activity of four inhibitors of DNA topoisomerases in larval cells of Drosophila melanogaster as measured in the wing spot assay.

Four inhibitors of DNA topoisomerases namely nalidixic acid, camptothecin, m-amsacrine and etoposide, have been evaluated for genotoxic effects in the wing spot test of Drosophila melanogaster. This assay assesses somatic recombination and mutational events. We studied nalidixic acid as an inhibitor of bacterial DNA gyrase, camptothecin as a topoisomerase I inhibitor, as well as m-amsacrine and etoposide as topoisomerse II inhibitors. The genotoxic effects were determined from the appearance of wing spots in flies trans-heterozygous for the recessive markers multiple wing hairs (mwh) and flare, as well as in flies heterozygous for mwh and the multiply inverted TM3 balancer chromosome. From our results it appears that whilst nalidixic acid and m-amsacrine were compounds that did not increase the incidence of mutant clones, camptothecin and etoposide proved to be significantly genotoxic in this test, being camptothecin more effective than etoposide. A significant proportion of the total spot induction was due to mitotic recombination, confirming previously reported data. On the other hand, the cotreatments of each topoisomerase inhibitor with the alkylating agent ethyl methanesulfonate (EMS) indicate that, while nalidixic acid, m-amsacrine and etoposide show a tendency to an antagonistic interaction, camptothecin shows an additive effect, suggesting mechanistic differences between the activity of the four inhibitors of DNA topoisomerases studied.

Amsacrine↗

PubMed1984

Genetic control of damage-inducible restriction alleviation in Escherichia coli K12: an SOS function not repressed by lexA.

The alleviation of K-specific DNA restriction after treatment of cells by UV or nalidixic acid has been studied in mutants with various alleles of recA and lexA and combinations of these alleles and with recB and recF mutations. The studies show that induction of restriction alleviation by UV or nalidixic acid is abolished in mutants in which the recA protein is defective (recA13, recA56), its protease activity is altered (recA430) or in which it cannot be efficiently activated (recA142). Thermoinduction of restriction alleviation was observed in tif mutant (recA441). In lexA amber mutants restriction alleviation is not constitutive but is still inducible. In a lexA3 mutant restriction alleviation is inducible by nalidixic acid provided that recA protein is overproduced as a result of a recA operator mutation. Induction by UV depends on the recF function and an unidentified function (Y) which is controlled by the lexA protein. The recBC enzyme is necessary for induction by UV or by nalidixic acid. Temperature shift experiments with a thermosensitive recB mutant indicate that the recBC enzyme functions in an early step during UV-induction. It is concluded that the damage-inducible function which alleviates restriction is similar to other damage inducible repair (SOS) functions in the dependence on activated recA protease for induction, but that it differs from these functions by the absence of a direct control through the lexA repressor.

Bacterial Proteins↗

PubMed2005

Antibiotic resistance pattern among gram-negative bacteria isolated from raw milk in Multan.

The use of raw milk in Pakistan has led to the antibiotics resistance. This investigation has showed incidence and antibiotic resistance among Coliform and Klebsiella to nalidixic acid, urixin and little to chloramphenicol. Enterobacter was sensitive to nalidixic acid, tetracycline and showed little resistance to chloramphenicol. E. coli were very sensitive to nalidixic acid, tetracycline, chloramphenicol, urixin, amoxil and with no resistance to ceftriaxone.

Animals↗

PubMed1976

Pipemidic acid: its activities against various experimental infections.

Pipemidic acid, a structural relative of piromidic and nalidixic acids, exhibited substantial therapeutic activity when it was administered orally to mice bearing either widely disseminated or relatively localized infections with Staphylococcus aureus and a variety of gram-negative bacilli. The activity of pipemidic acid was always greater than that of piromidic and nalidixic acids; in infections with Pseudomonas aeruginosa and in bacilli resistant to the latter two drugs, pipemidic acid exhibited significant activity. In limited comparative studies, the activities of pipemidic acid were generally superior to the activities of cephalexin, ampicillin, and carbenicillin. Gentamicin, administered subcutaneously, was more active than pipemidic acid, given either orally or subcutaneously, against both systemic and localized infections with P. aeruginosa. The therapeutic accomplishments of pipemidic acid were attained with well-tolerated doses.

Ampicillin↗

PubMed1983

DNA gyrase (Topoisomerase II) from Pseudomonas aeruginosa.

DNA gyrase (Topoisomerase II) has been purified from Pseudomonas aeruginosa strain PAO. This enzyme is inhibited by novobiocin and nalidixic acid. DNA gyrase from P. aeruginosa is resistant to a much higher level of nalidixic acid than is Escherichia coli DNA gyrase. This increased level of resistance may explain, at least in part, the higher levels of natural resistance exhibited by P. aeruginosa toward nalidixic acid.

Bacterial Proteins↗

PubMed2005

Effects of pH and cationic and nonionic surfactants on the adsorption of pharmaceuticals to a natural aquifer material.

A wide range of pharmaceutical compounds have been identified in the environment, and their presence is a topic of growing concern, both for human and ecological health. Adsorption to aquifer materials and sediments is an important factor influencing the fate and transport of pharmaceutical compounds in the environment. Surfactants and other amphiphiles are known to influence the adsorption of many compounds and may be present in the environment from wastewaters or other sources. The work described here examines the adsorption of four pharmaceutical compounds, acetaminophen, carbamazepine, nalidixic acid, and norfloxacin, in the presence of a natural aquifer material. Adsorption was studied as a function of pH and in the presence and absence of two surfactants, cetylpyridinium chloride (CPC), a cationic surfactant, and Tergitol NP9, an ethoxylated nonionic surfactant. In the absence of surfactants, results indicate a 1-2 orders of magnitude variation in adsorption affinity with changing pH for each of the two quinolone pharmaceuticals (nalidixic acid and norfloxacin) but no measurable adsorption for carbamazepine or acetaminophen. In the presence of surfactants, adsorption of acetaminophen and carbamazepine was enhanced to extents consistent with compound hydrophobicity, while adsorption of nalidixic acid and norfloxacin was not. At high pH values, the anionic species of nalidixic acid exhibited enhanced adsorption in the presence of the cationic surfactant, CPC.

Acetaminophen↗

PubMed1981

Effect of DNA gyrase inhibitors on gene expression of the cysteine regulon.

Nalidixic acid inhibits the expression of those cysteine genes which are regulated by the cysB product, it has no affect, however, on the constitutively-expressed cysE gene. The expression of cysteine genes in a strain carrying a mutation in the nalA locus is resistant to this drug. Novobiocin affects the expression of cysteine genes similarly to nalidixic acid. The effect of nalidixic acid on the expression of genes in a cysteine constitutive mutant was studied.

Acetyltransferases↗

PubMed2006

Effect of anaerobic growth on quinolone lethality with Escherichia coli.

Quinolone activity against Escherichia coli was examined during aerobic growth, aerobic treatment with chloramphenicol, and anaerobic growth. Nalidixic acid, norfloxacin, ciprofloxacin, and PD161144 were lethal for cultures growing aerobically, and the bacteriostatic activity of each quinolone was unaffected by anaerobic growth. However, lethal activity was distinct for each quinolone with cells treated aerobically with chloramphenicol or grown anaerobically. Nalidixic acid failed to kill cells under both conditions; norfloxacin killed cells when they were grown anaerobically but not when they were treated with chloramphenicol; ciprofloxacin killed cells under both conditions but required higher concentrations than those required with cells grown aerobically; and PD161144, a C-8-methoxy fluoroquinolone, was equally lethal under all conditions. Following pretreatment with nalidixic acid, a shift to anaerobic conditions or the addition of chloramphenicol rapidly blocked further cell death. Formation of quinolone-gyrase-DNA complexes, observed as a sodium dodecyl sulfate (SDS)-dependent drop in cell lysate viscosity, occurred during aerobic and anaerobic growth and in the presence and in the absence of chloramphenicol. However, lethal chromosome fragmentation, detected as a drop in viscosity in the absence of SDS, occurred with nalidixic acid treatment only under aerobic conditions in the absence of chloramphenicol. With PD161144, chromosome fragmentation was detected when the cells were grown aerobically and anaerobically and in the presence and in the absence of chloramphenicol. Thus, all quinolones tested appear to form reversible bacteriostatic complexes containing broken DNA during aerobic growth, during anaerobic growth, and when protein synthesis is blocked; however, the ability to fragment chromosomes and to rapidly kill cells under these conditions depends on quinolone structure.

Aerobiosis↗

PubMed1973

Single-strand breaks in deoxyribonucleic acid and viability loss during deoxyribonucleic acid synthesis inhibition in Escherichia coli.

The effects of deoxyribonucleic acid (DNA) synthesis inhibition brought about in four different ways-thymidine starvation, nalidixic acid, hydroxyurea, and dnaB mutation-were examined in isogenic strains of Escherichia coli K-12. Three parameters were examined to determine whether there are strict correlations among them: (i) the extent of DNA synthesis inhibition; (ii) cell survival; and (iii) the rate of breakage of DNA molecules. There was no significant correlation between the extent of DNA synthesis inhibition and the rate of viability loss caused by the four DNA synthesis inhibitors, nor was there a strict correlation between the rate of occurrence of single-strand breaks in DNA and loss of viability. During treatment with hydroxyurea (0.1 M), no viability loss was observed and little, if any, single-strand breakage of DNA occurred. Both thymidine starvation and nalidixic-acid (20 mug/ml) treatment resulted in viability loss and breakage of DNA. For these latter two inhibitors, the two events appeared to be associated because greater rates of both viability loss and DNA breakage were observed for nalidixic acid compared with thymidine starvation. However, viability loss need not be associated with extensive breakage of DNA as demonstrated with a temperature-sensitive DNA synthesis mutant; at 39 C, viability loss occurred at a high rate without significant DNA breakage. With the other agents, the amount of DNA breakage accumulated when a cell population has sustained an average of one lethal hit was estimated to be about 30 single-strand breaks per genome. Differences in chromosomal and episomal breakage rates were observed.

Adenine↗

PubMed1999

Risk factors for death in hospitalized dysentery patients in Rwanda.

To evaluate the management of severe dysentery cases in in-patient facilities during an epidemic of Shigella dysenteriae type 1 (Sd1), and to identify the factors associated with the risk of death, we conducted a prospective cohort study in 10 Rwandese hospitals between September and December 1994. Data were obtained from 849 cases admitted to hospitals with diarrhoea and visible blood in stools. The proportion of patients with persistent bloody diarrhoea was 51.0% at treatment day 3 and 27.9% at treatment day 5. At discharge, 79.9% had improved or were cured. The case fatality ratio was 13.2%, higher for patients treated with nalidixic acid than for those treated with ciprofloxacin (12.2% vs. 2.2%, RR = 5.80, 95% CI = 0.83-40.72). In a logistic regression model three risk factors were significantly associated with an increased risk of death during hospitalization: severe dehydration on admission (adjusted OR = 2.79, 95% CI = 1.46-5.33), age over 50 (adjusted OR vs. 5-49 age group = 3.22, 95% CI = 1.70-6.11) and prescription of nalidixic acid (adjusted OR vs. ciprofloxacin = 8.66, 95% CI = 1.08-69.67). Those results were consistent with reported high levels of resistance of Sd1 to the commonest antibiotics, including nalidixic acid. Patients belonging to groups with a higher risk of dying should be given special medical attention and supportive care. In areas of high resistance to nalidixic acid, severe cases of dysentery should be treated with fluoroquinolones in order to reduce the mortality associated with these epidemics.

Adolescent↗

PubMed1973

Compound 64716, a new synthetic antibacterial agent.

Compound 64716, 1-ethyl-4 (1H)-oxo-[1,3]dioxolo[4,5-g]cinnoline-3-carboxylic acid, is a new synthetic antibacterial agent. The antibacterial spectrum of this compound includes gram-negative bacteria that are most frequently isolated from urinary tract infections. Minimal inhibitory concentration values of 64716 for isolates of Escherichia coli and Proteus sp. ranged from 2 to 4 and 2 to 8 mug/ml, respectively, and the compound was bactericidal at concentrations close to the minimal inhibitory concentration values. In vivo, doses required for successful therapy of experimental mouse infections were comparable to those for nalidixic acid. After oral administration of 40 mg/kg, peak concentrations of this compound in mouse blood reached 19.2 mug/ml. Within 30 min after doses of 20 mg/kg, bacteriologically active drug concentrations of 64716, nalidixic acid, and oxolinic acid in mouse urine were >1,000, 170, and <1.5 mug/ml, respectively. Resistant bacteria were not selected when bacteria were exposed to 500 mug/ml of 64716. Compound 64716 was less bound by human serum proteins than was nalidixic acid. Equivalent antibacterial activity along with superior pharmacological properties of 64716 when compared with nalidixic acid lead to the conclusion that this new compound is a promising antibacterial agent.

Animals↗

PubMed1993

Determination of MICs for staphylococci using the API ATB quinolone and API ATB macrolide systems.

The determination of minimal inhibitory concentrations (MICs) is cumbersome, but remains necessary in certain cases. We tested the two ATB MIC experimental strips (Biomérieux SA), of which each contains 4 antimicrobials of the same class. These strips can be read automatically. The MIC quinolone strip contains nalidixic acid, pefloxacin, ofloxacin and ciprofloxacin, whereas the MIC macrolide (lincosamide-streptogramin) strip contains erythromycin, clindamycin, lincomycin, and pristinamycin. In order to evaluate these strips, 102 S. aureus and 63 coagulase negative staphylococci were used. Correlation coefficients for these MICs (micrograms/ml) and disk diffusion inhibition zone diameters (mm) were nalidixic acid -0.59, pefloxacin -0.95, ofloxacin -0.95, ciprofloxacin -0.91, erythromycin -0.98, clindamycin -0.96, lincomycin -0.96, and pristinamycin -0.64. Using the Biomic system (Giles Scientific USA), the same zone diameters were converted to MICs (micrograms/ml). Rates of agreement (+/- 1 dilution) between ATB MICs and Biomic MICs were nalidixic acid 96 p. cent, ciprofloxacin 98 p. cent, erythromycin 99 p. cent and clindamycin 98 p. cent. Rates of agreement between MICs for the same strains determined using agar dilution and ATB MICs were nalidixic acid 93 p. cent, pefloxacin 100 p. cent, ciprofloxacin 99 p. cent, ofloxacin 94 p. cent and erythromycin 96 p. cent. The ATB MIC strips are an easy-to-use tool for MIC determination and their composition is well-suited to the study of phenotypic resistance and detection of low-level resistance.

Ciprofloxacin↗

PubMed1983

Antibacterial activity of norfloxacin.

Norfloxacin, a new quinoline derivative, was studied in vitro, and determinations of agar dilution minimal inhibitory concentrations (MICs) and broth dilution MICs and MBCs were made. Nalidixic acid and cinoxacin were used as comparative agents. Norfloxacin was found to be extremely active against all strains tested of Escherichia coli, Klebsiella spp., Proteus mirabilis, indole-positive Proteus spp. Serratia spp., Citrobacter spp., and Enterobacter spp., with MICs normally below 1 microgram/ml. It also was found to be highly active against Pseudomonas aeruginosa, Staphylococcus saprophyticus, and enterococci, which are all resistant to nalidixic acid and cinoxacin. The MICs for norfloxacin obtained by broth dilution were slightly higher than those obtained by agar dilution, whereas the reverse was true for nalidixic acid and cinoxacin. The MBCs of norfloxacin were only slightly higher than the MICs, even at high inocula. The in vitro activity of norfloxacin was not dependent on the inoculum size, whereas both the MICs and the MBCs of nalidixic acid increased markedly for many of the strains tested when the inoculum was increased in broth dilution from 10(3) to 10(6) colony-forming units per ml. Norfloxacin seems to be a promising antibacterial agent for the treatment of urinary tract infections, especially those caused by Pseudomonas spp. and other species today requiring the use of injectable antibiotics.

Anti-Bacterial Agents↗

PubMed1998

Quinolone resistance from a transferable plasmid.

BACKGROUND: Bacteria can mutate to acquire quinolone resistance by target alterations or diminished drug accumulation. Plasmid-mediated resistance to quinolones in clinical isolates has been claimed but not confirmed. We investigated whether a multiresistance plasmid could transfer resistance to quinolones between bacteria. METHODS: We transferred resistance between strains by conjugation. The resistance plasmid was visualised in different hosts by agarose-gel electrophoresis. We determined the frequency of spontaneous mutations to ciprofloxacin or nalidixic-acid resistance in Escherichia coli strains, with or without the quinolone resistance plasmid. FINDINGS: A multiresistance plasmid (pMG252) from a clinical isolate of Klebsiella pneumoniae was found to increase quinolone resistance to minimum inhibitory concentrations (MICs) as high as 32 microg/mL for ciprofloxacin when transferred to strains of K pneumoniae deficient in outer-membrane porins. Much lower resistance was seen when pMG252 was introduced into K pneumoniae or E coli strains with normal porins. The plasmid had a wide host range and expressed quinolone resistance in other enterobacteriaceae and in Pseudomonas aeruginosa. From a plasmid-containing E coli strain with ciprofloxacin MIC of 0.25 microg/mL and nalidixic-acid MIC of 32 microg/mL, quinolone-resistant mutants could be obtained at more than 100 times the frequency of a plasmid-free strain, reaching MICs for ciprofloxacin of 4 microg/mL and for nalidixic acid of 256 microg/mL. INTERPRETATION: Transferable resistance to fluoroquinines and nalidixic acid has been found in a clinical isolate of K pneumoniae on a broad host range plasmid. Although resistance was low in wild-type strains, higher levels of quinolone resistance arose readily by mutation. Such a plasmid can speed the development and spread of resistance to these valuable antimicrobial agents.

Anti-Infective Agents↗