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Results for “NALIDIXIC ACID”

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At least 199 records · Page 11Linked to original sources

PubMed1987

Short-term nalidixic acid plus sodium citrate in acute lower urinary tract infection.

Low-dose nalidixic acid (0.66 g) in combination with 4 g of sodium citrate (NAC) was evaluated in acute lower UTI. In college-age females (n = 24) given NAC every 8 h for 3 days the nalidixic acid (NA) susceptible infecting strain was eradicated in 100% of the patients and recurrence during the 1 month follow-up period occurred in 1 case (5%) classified as relapse. In a following study the corresponding rates in general practice (GP) patients (n = 71) were 90% and 17%, respectively, irrespective of treatment with NAC every 12 h for 3 days or 5 days. The failures observed in GP were due to persistence of (or immediate reinfection by) the original infecting strain (4%) or its NA resistant mutant (6%). Emergence of NA resistance was associated with high age of the patient and a high incidence of NA resistant mutants in the infecting Escherichia coli strain. NA susceptible failure and recurrence during follow-up occurred primarily in younger GP patients. The recurrences were equally often classified as relapse (6 cases) as reinfection (5 cases). About 20% of the patients reported rather innocuous transient side effects of NAC and interruption of medication occurred in 1 case (0.6%).

Adolescent↗

PubMed1983

The effects of nalidixic acid on respiratory activity of asynchronous and synchronous cultures of Alcaligenes eutrophus.

Nalidixic acid inhibited DNA synthesis and cell division during asynchronous growth of Alcaligenes eutrophus but treated cells continued to grow as monitored by A550, respiratory activity and cell volume. Differential effects on cell division were seen when the antibiotic was added at different times during synchronous growth. The earlier in the cell cycle the time of addition the greater the inhibition of cell division. These results suggests that chromosome replication is confined to the first half of the cell cycle in A. eutrophus grown at 30 degrees C. Respiration rates of cells selected by continuous-flow centrifugation and immediately treated with nalidixic acid increased in a stepwise fashion. These steps were similar to those observed in untreated control cells and imply that the DNA-division cycle is not the causal factor for the periodicities in respiration rates and ATPase activity that have been previously reported in this bacterium.

Alcaligenes↗

PubMed1976

[Inhibition of Proteus sp. by Nalidixic acid].

The investigation comprised 192-positive and Gram-negative strains of bacteria, including 111 Proteus sp. The degree of resistance of these strains to nalidixic-acid was investigated on blood agar with 25 mug, 40 mug, and 50 mug nalidixin-acid per ml medium. None of the Proteus strains were able to grow on medium with 50 mug nalidixic-acid per ml, whereas Streptococcus sp., Corynebacterium pyogenes, Peptococcus indolicus, Pseudomonas aeruginosa, and beta-toxic staphylococci all were found resistant to this concentration (Tables I and II), and could be reisolated in pure culture after having grown together with a Proteus strain on such medium (Table III). Blood agar with 50 mug nalidixic-acid per ml is therefore suitable for isolation of the above mentioned Gram-positive bacteria and Pseudomonas aeruginosa from Proteus contaminated material.

Dose-Response Relationship, Drug↗

PubMed1976

Nalidixic acid inhibition of post-ultraviolet recovery in Escherichia coli K-12: requirement for recBC function.

Various repair-deficient mutants of Escherichia coli K-12 were tested for the impairment of post-ultraviolet survival by nalidixic acid. These studies have shown that the target of this nalidixic acid effect is dictated by the recB and recC genes and may be due to the binding of nalidixic acid to exonuclease V. Furthermore, this effect cannot be correlated with either recombination proficiency or excision repair alone.

Dose-Response Relationship, Radiation↗

PubMed1985

Evidence that novobiocin and nalidixic acid do not inhibit excision repair in u.v.-irradiated human skin fibroblasts at a pre-incision step.

The effects of novobiocin and nalidixic acid on the specific toxicity of aphidicolin towards u.v. irradiated arrested (nondividing) human skin fibroblasts have been determined. Contrary to the result expected if either drug were causing inhibition of excision repair at a pre-incision step the sector of toxicity due to a combined treatment of 300 micrograms ml-1 nalidixic acid and 1.0 micrograms ml-1 aphidicolin is unchanged when compared with that due to treatment with 1.0 micrograms ml-1 aphidicolin alone, while that for 150 micrograms ml-1 novobiocin + 1.0 micrograms ml-1 aphidicolin was slightly increased. In parallel measurements of the inhibition of u.v.-induced DNA repair synthesis in arrested fibroblasts by these drugs, 150 micrograms ml-1 novobiocin inhibited repair synthesis by approximately 60% over the fluence range employed. Nalidixic acid at a concentration of 300 micrograms ml-1 caused no detectable inhibition of repair synthesis. We conclude that the mode of action of novobiocin in the inhibition of DNA excision repair is not via the inhibition of a pre-incision step and the data do not support the hypothesis that a type II topoisomerase mediated change in DNA supercoiling is an essential early step in excision repair of u.v.-induced damage.

Aphidicolin↗

PubMed1975

[The effect of puromycin, nalidixic acid, and cycloheximide acetylcholinesterase purified from Electrophorus electricus L].

The action of puromycin, nalidixic acid and cycloheximide on acetylcholinesterase has been studied using an "electrophoretically pure" preparation. Results obtained show that these well known inhibitors of protein synthesis have an inhibitory effect on acetylcholinesterase activity. The inhibitory action exercised by puromycin and nalidixic acid is of a mixed inhibition type, similar to the one seen when decamethonium and d-tubocurarine are used as inhibitory agents. Cycloheximide acts in a non competitive way on the enzyme activity.

Cycloheximide↗

PubMed1984

Bioavailability of nalidixic acid from uncoated tablets in humans--Part I: Correlation with the dissolution rates of the tablets.

Bioavailabilities of three commercially available tablets and two trial tablets of nalidixic acid were determined. The correlation between in vivo bioavailability parameters and in vitro dissolution rates derived by eight methods (oscillating basket I and II, beaker I, II, and III, rotating basket, paddle and rotating flask) is discussed. Nalidixic acid and its metabolite, 7-hydroxynalidixic acid, were determined in serum by HPLC with a strong anion-exchange resin column. All parameters for nalidixic acid bioavailability showed significant differences among the tablets tested. The relationship between Cmax and AUC was not linear but concave. However, Cmax decreased linearly in proportion to the delay of Tmax. The rank order of tablets according to bioavailabilities was just the same as the rank order obtained when comparing dissolution rates determined by any of the above methods, with the exception of one tablet which had a poor disintegrating ability. The parameters for the rate of bioavailability (Cmax and Tmax) showed good linearity with 1/T50 determined by all of the methods. However, AUC showed significant correlation with neither T50 nor 1/T50.

Adult↗

PubMed1985

Influence of penicillin and nalidixic acid on growth and cell division of Escherichia coli K-12.

Ultrastructure of E. coli K-12 cells and the synthesis of DNA in bacteria treated with low concentration of nalidixic acid and penicillin was investigated. In E. coli both drugs caused inhibition of cell division in period D of the life cycle although nalidixic acid inhibits division at an earlier stage of septum formation. The ability of cells to form filaments in the presence of nalidixic acid depends on their age, i.e. time at which cells are taken from synchronous culture.

Cell Division↗

PubMed1982

[A comparison of cinoxacin and nalidixic acid in the treatment of chronic urinary tract infections].

A total of 60 patients with chronic urinary tract infections were included in this comparative study. 29 patients received cinoxacin and 31 nalidixic acid for a period of ten days. There were five therapy failures in the cinoxacin group and nine in the nalidixic acid group. Drug-related side-effects were reported by 11 patients in the cinoxacin group and by 13 patients in the nalidixic acid group. Gastrointestinal and central nervous disturbances were the adverse reactions which occurred most frequently. In all cases side-effects disappeared quickly after therapy was discontinued.

Bacteriuria↗

PubMed1981

A clinical comparison of cinoxacin and nalidixic acid in the treatment of urinary tract infection.

In a single blind clinical study of 50 patients with urinary tract infections 250 mg. cinoxacin were compared to 1 g. nalidixic acid 4 times daily. Both drugs produced similar improvement in symptomatic response during therapy and were equally effective in eradicating the causative pathogens. In the 5 of 9-day post-therapy followup 4 patients from the cinoxacin group became reinfected compared to 1 from the nalidixic acid group. Side effects were reported by twice as many patients in the nalidixic acid group. It is concluded that cinoxacin is an effective drug for the treatment of uncomplicated urinary tract infections.

Adult↗

PubMed1992

Role of nalidixic acid in isolation of Salmonella typhimurium strains capable of growth at 48 degrees C.

Salmonella typhimurium thermotolerant mutants dependent on the presence of nalidixic acid for growth at 48 degrees C were isolated and designated nalidixic acid-dependent, thermotolerant mutants, naldttl. Genetic mapping revealed that naldttl alleles map within the gyrA gene. When S. typhimurium strain Q was plated in the dark on nutrient agar containing nalidixic acid (20 micrograms/ml) as a photosensitizer and briefly exposed to white light or near VU light prior to incubation at 42 degrees C, nalidixic acid-resistant mutants arose in about 16 h at frequencies of 5 x 10(-8) for white light and 1 x 10(-6) for near UV light. About 10% of these nalidixic acid-resistant mutants derived from photodynamic mutagenesis exhibited the thermotolerant characteristic.

Culture Media↗

PubMed1986

Effect of the bacterial DNA gyrase inhibitors, novobiocin, nalidixic acid, and oxolinic acid, on oxidative phosphorylation.

When incubated with isolated intact rat liver mitochondria, novobiocin and nalidixic acid act as uncouplers of oxidative phosphorylation; they stimulate oxygen uptake and inhibit ATP synthesis. Novobiocin is about as powerful an uncoupler as is 2,4-dinitrophenol, nalidixic acid is somewhat less powerful, and oxolinic acid exerts no inhibition whatsoever at the concentrations used. The three inhibitors are without effect on oxidative phosphorylation in Escherichia coli nor does novobiocin affect this process in a novobiocin-permeable mutant of yeast. While it would appear that oxolinic acid may be a relatively specific tool for the manipulation of the superhelicity of DNA in complex systems such as mammalian mitochondria and intact mammalian cells, the specificity of each of these inhibitors may depend upon the particular conditions and species used and such experiments require adequate controls on oxidative phosphorylation.

Animals↗

PubMed1984

Effect of food on bioavailability of nalidixic acid from uncoated tablets having different dissolution rates.

The effect of food on the bioavailability of two single lots of commercial tablets and one trial tablet of nalidixic acid, varying widely in drug dissolution characteristics, was determined in healthy male subjects after oral administration. Four subjects received, in a crossover fashion, a single 250 mg dose in an uncoated tablet during periods of fasting and non-fasting. Significant differences in Cmax, Tmax and AUC0-8 were observed between the tablet having the fastest dissolution rate and the other tablets tested, when administered postprandially. Both Cmax and AUC0-8 were significantly increased after administration of the two tablets exhibiting the poorer dissolution characteristics to the non-fasting subjects. However, food was not observed to affect any of the bioavailability parameters after postprandial administration of the tablet exhibiting the fastest dissolution rate. The improvement of bioavailability of the two tablets exhibiting the poorer dissolution by food intake was ascribable to enhanced dissolution of nalidixic acid resulting from vigorous mixing and agitation in the digestive tract. It was concluded that the effect of food on the bioavailability of nalidixic acid from uncoated tablets varies with formulation factors, especially with dissolution characteristics.

Adult↗

PubMed2006

Efficient approach to acyloxymethyl esters of nalidixic acid and in vitro evaluation as intra-ocular prodrugs.

Various alkylcarbonyloxymethyl esters of nalidixic acid ranging from 3 to 15 carbon units in the pro-moiety have been prepared and assessed as potential prodrugs. Their chromatographic retention factors k', silicone oil solubilities and in vitro conversion to nalidixic acid by a commercial esterase were determined together with their in vitro antimicrobial activity and cytotoxicity. The preliminary results suggest that silicone oil may have potential for the intra-ocular delivery of antibacterial compounds. Moreover, the in vitro release rate can be controlled by the lipophilicity of the prodrug.

Anti-Bacterial Agents↗

PubMed1995

Bioactive polymers 53: synthesis of poly(vinyl alcohol) and nalidixic acid based pro-drugs.

The present paper studies the process of esterification of nalidixic acid on poly(vinyl alcohol). The influence of time, dilution and concentration of the reactants on the efficiency of esterification with dicyclohexylcarbodiimide has been followed. By experiment scheduling according to a centered, rotatory, compound, second order program, optimum conditions for the system under study have been found. On the other hand, the evolution of reaction of esterification of the nalidixic acid on poly(vinyl alcohol) was followed by using the activator-catalyst (4-pirolidinopyridine) system. An increase of the esterification yield up to 37% has been observed.

Biocompatible Materials↗

PubMed1977

Factors governing the emergence of resistance to nalidixic acid in treatment of urinary tract infection.

Cultures of Escherichia coli were exposed to nalidixic acid in an in vitro model in which the conditions of drug-organism interaction resembled those of bacterial cystitis treatment. Results obtained in this way suggested that emergence of bacterial resistance should not be a major problem in treatment of uncomplicated urinary infection; such cases might indeed respond to a less intensive course of treatment than is usual. More prolonged, high-dosage therapy with nalidixic acid may be required for patients with more complicated infections if the risk of failure from the emergence of bacterial resistance is to be minimized.

Cystitis↗

PubMed1984

Inhibition of beta-lactamase production in gram-positive and gram-negative strains by sub-inhibitory concentrations of nalidixic acid.

We found it of interest to try to determine a microbiological parameter for the effects that sub-inhibitory doses of a chemotherapeutic agent may have on bacteria. To this end, the antibacterial activity of nalidixic acid was analyzed and our attention was directed to evidence of the production of beta-lactamase by 60 strains. The tests carried out showed that sub-inhibitory concentrations of nalidixic acid, from 2 to 64 times lower than the MIC (minimum inhibitory concentrations), were able to inhibit production of penicillinases in the 14 strains of Staphylococcus spp. tested, while only in 7 of the 21 strains of Gram-negative bacteria. Strains from our collection of beta-lactamase producing bacteria were analyzed, and our results confirmed that nalidixic acid inhibits plasmidic and chromosomic beta-lactamases.

Gram-Negative Bacteria↗

PubMed1986

The effect of nalidixic acid on expression from related E. coli promoters.

The effect of the DNA gyrase inhibitor, nalidixic acid, on expression from E. coli promoters was studied using the pKO-1, galactokinase expression vector system. Expression from a series of related hybrid promoters, tet promoter variants and the trp promoter flanked by oligonucleotide blocks was measured after incubation with nalidixic acid. Expression from the pBR322 tet promoter and tet promoter mutants within the -10 region was reduced after the drug treatment. The lacUV5, trp, and tettrp promoters were essentially unaffected while the trplac and the trptet promoters were stimulated. Studies of the trp promoter flanked by upstream or downstream oligonucleotide blocks revealed similar responses to the trp promoter parent control plasmids.

Base Sequence↗