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PubMedDate not supplied

Experiences on the efficacy and safety of nalidixic acid, oxolinic acid, cinoxacin and norfloxacin in the treatment of urinary tract infections (UTI).

The purpose of this study was to determine the effectiveness and tolerability of norfloxacin, cinoxacin and oxolinic acid in the treatment of urinary tract infections (UTI) in comparison to nalidixic acid. 125 patients were given the drugs in the appropriate doses for 10-14 days and 30 patients were treated for six weeks. Clinical, bacteriological, hematological and chemical checks were made on all patients before and after treatment. It was found that norfloxacin, cinoxacin and oxolinic acid are safe and effective against Escherichia coli, Klebsiella and Proteus, the commonly encountered organisms in urinary tract infections. The cure rate for norfloxacin was 93%, for cinoxacin 83%, for oxolinic acid 80% and for nalidixic acid 70% in the short course. However, these differences were not statistically significant. Oxolinic acid, cinoxacin and norfloxacin have the advantage over nalidixic acid of being administered only twice daily.

Adolescent↗
PubMed1987

Simultaneous determination of nalidixic acid, oxolinic acid and piromidic acid in fish by high-performance liquid chromatography with fluorescence and UV detection.

A simple and rapid method for the simultaneous determination of nalidixic acid (NA), oxolinic acid (OXA) and piromidic acid (PMA) in cultured fish has been developed by high-performance liquid chromatography (HPLC). The drugs were extracted with 0.1% metaphosphoric acid-methanol (6:4), followed by a Sep-Pak C18 clean-up procedure. The HPLC separation was carried out on a Kaseisorb LC ODS 300-5 column (25 cm x 4.6 mm I.D.) using 5 mM phosphate buffer-acetonitrile (6:4) as a mobile phase. A fluorescence detector was used for NA and OXA at the excitation wavelength of 325 nm and the emission wavelength of 365 nm and an ultraviolet detector at 280 nm for PMA. The calibration graphs were rectilinear from 1 to 10 ng for OXA, from 2 to 20 ng for NA and PMA. The recoveries of NA, OXA and PMA added to fish were 81.5-85.3, 83.7-88.7 and 80.9-84.9%, respectively, with high accuracy. The limits of detection were 0.01 micrograms/g for each drug.

Animals↗
PubMedDate not supplied

Liquid chromatographic determination of flumequine, nalidixic acid, oxolinic acid, and piromidic acid residues in catfish (Ictalurus punctatus).

A peer-verified, liquid chromatographic (LC) method for simultaneous determination of residues of flumequine (FLU), nalidixic acid (NAL), oxolinic acid (OXO), and piromidic acid (PIR) in catfish muscle is presented. Sample workup involves homogenizing tissue with acetone, defatting with hexane, and extracting quinolones into chloroform. Sample is purified further by partitioning into base and then subsequently back-extracting into chloroform after acidifying the aqueous phase. After solvent is evaporated, the residue is diluted with mobile phase, and analytes are introduced into an LC system where separations are made with a 5 microns, reversed-phase polymer column and an isocratic, buffered acetonitrile-tetrahydrofuran mobile phase. Determinations are made by UV detection at 280 nm for PIR and by fluorescence detection (excitation at 325 excitation and emission at 365 nm) for the other 3 analytes. Each quinolone was used to fortify catfish muscle at 5, 10, 20, 40, and 80 ng/g. The following recoveries and relative standard deviation (RSD) values represent an average of the 5 levels for each analyte: FLU, 79.7% (RSD = 5.7%); OXO, 80.8% (RSD = 6.3%); PIR, 75.0% (RSD = 5.9%); and NAL, 87.1% (RSD = 10%). Assay of 5 levels (base incurred catfish, plus 4 dilutions with control catfish) of catfish muscle incurred with the 4 quinolones gave the following averages: FLU: base, 198 ng/g (RSD = 2.3%); dilutions, 98.0 ng/g (RSD = 4.2%), 61.6 ng/g (RSD = 4.4%), 21.6 ng/g (RSD = 2.8%), 9.24 ng/g (RSD = 8.7%); OXO, base, 257 ng/g (RSD = 6.9%); dilutions, 146 ng/g (RSD = 5.5%), 95.0 ng/g (RSD = 4.1%), 30.7 ng/g (RSD = 3.8%), 13.7 ng/g (RSD = 4.6%); PIR, base, 22.1 ng/g (RSD = 4.2%); dilutions, 13.7% ng/g (RSD = 6.7%), 6.49 ng/g (RSD = 15%), 2.65 ng/g (RSD = 15%); and NAL, base, 75.1 ng/g (RSD = 3.8%); dilutions, 42.3 ng/g (RSD = 5.1%), 24.1 ng/g (RSD = 6.3%), 8.59 ng/g (RSD = 4.8%). A second multiresidue analysis of the 4 quinolones was performed by an outside analyst. Average recoveries from catfish fortified at 5, 10, 20, and 40 ng/g were FLU, 75.9% (RSD = 4.0%); OXO, 84.0% (RSD = 5.5%); NAL, 85.6% (RSD = 8.9%); and PIR, 66.2% (RSD = 8.7%).

Animals↗
PubMed1986

Penicillin-binding proteins of filaments of Escherichia coli induced by low concentrations of nalidixic acid, oxolinic acid, novobiocin or nitrofurantoin.

Nalidixic acid, novobiocin, oxolinic acid and nitrofurantoin, each at low concentrations, cause filamentation of Gram-negative bacilli. Filamentation induced by beta-lactam antibiotics has been correlated to the binding of these antibiotics to specific penicillin-binding proteins (PBPs) of the envelope of Gram-negative bacilli. The studies reported herein indicate that the former group of non-beta-lactam antibiotics do not bind to any of the PBPs of Escherichia coli. However, PBP 1a, PBP 4 and PBP 5/6 of the filaments induced by these agents are increased significantly.

Acyltransferases↗
PubMed1981

Nalidixic acid, oxolinic acid, and novobiocin inhibit yeast glycyl- and leucyl-transfer RNA synthetases.

Nalidixic acid and novobiocin inhibit the aminoacylation and pyrophosphate exchange activities of glycyl- and leucyl-transfer RNA synthetases from bakers' yeast. Similar types of inhibition are observed for both enzymes, suggesting similar mechanisms. The potency of these inhibitors is comparable to that observed for their inhibition of in vivo DNA synthesis in eukaryotic cells.

Amino Acyl-tRNA Synthetases↗
PubMed1995

A possible mechanism for the increase in serum luteinizing hormone levels in male rats by oxolinic acid.

Oxolinic acid (1-ethyl-1,4-dihydro-6,7-methylenedioxy-4-oxo-3- quinolinecarboxylic acid), an antimicrobial agent, raises the serum levels of luteinizing hormone (LH) and increases the incidence of testicular Leydig cell tumors in male rats. In the present study the mechanism by which serum LH levels are raised in male rats receiving oxolinic acid was investigated. Aged Wistar rats were fed a diet containing oxolinic acid at 0 or 3000 ppm for more than 4 weeks. There was no effect of oxolinic acid on either the maximal levels of serum LH after castration nor on the serum levels of LH stimulated with 1 microgram/rat of luteinizing hormone-releasing hormone (LHRH). The concentrations of testosterone in serum and testis were not changed by the treatment of oxolinic acid. In the in vitro organ culture, the testes of rats receiving oxolinic acid released testosterone in the same manner as the controls, in the presence or the absence of human chorionic gonadotropin (100 mIU/ml). The oxolinic acid-stimulated serum LH was not increased further by the daily administration of L-dopa (500 mg/kg/day, po, 7 days) and was blocked by the injection of a dopamine antagonist, haloperidol (2 mg/kg, ip). In a microdialysis study, oxolinic acid increased the extracellular concentration of dopamine in the preoptic area of hypothalamus. These findings suggest that a high dietary level of oxolinic acid elevates LH release from the anterior pituitary with an increase in LHRH, in part, by the excitatory input of a dopaminergic system in the preoptic area of rat hypothalamus.

Animals↗
PubMed1976

Replication of Escherichia coli DNA in vitro: inhibition by oxolinic acid.

Oxolinic acid, a quinolone antibacterial agent, inhibits reversibly the ATP-dependent replicative DNA synthesis in permeable cell systems as well as in cellophane disk lysates. It is about 10-fold more active than the structurally related nalidixic acid. Both drugs have no effect on the ATP-independent DNA repair, but interfere to some extent with RNA synthesis in permeable cells. They appear to interact with the same target since spontaneous nalidixic-acid-resistant mutants of nalA phenotype are also resistant to oxolinic acid. Full sensitivity to oxolinic acid can be conferred to lysates from resistant cells by addition of extracts from sensitive cells.

Adenosine Triphosphate↗
PubMedDate not supplied

[Radioprotective properties of oxolinic acid].

Oxolinic acid was shown to produce a radioprotective effect on mice and a therapeutic radioprotective action on rats and hamsters. As to radioprotective efficiency, oxolinic acid is inferior to such known sulfur-containing agents as indolylalkylamines and alpha-adrenomimetics. But oxolinic acid has an important advantage over them, that is, the increase in radioresistance it induces persists for several hours. The radioprotective effectiveness of oxolinic acid prompts that it is expedient to search for new radioprotective preparations among specific inhibitors of DNA polymerase of replicative synthesis.

Animals↗
PubMed2003

A single-dose pharmacokinetic study of oxolinic acid and vetoquinol, an oxolinic acid ester, in cod, Gadus morhua L., held in sea water at 8 degrees C and in vitro antibacterial activity of oxolinic acid against Vibrio anguillarum strains isolated from diseased cod.

The pharmacokinetic properties of the antibacterial agent oxolinic acid and vetoquinol, the carbitol ester of oxolinic acid, were studied after intravenous (i.v.) and oral (p.o.) administration to 100-150 g cod, Gadus morhua L., held in sea water at 8 degrees C. Following i.v. injection, the plasma drug concentration-time profile showed two distinct phases. The distribution half-life (t1/2alpha) was estimated at 1.3 h, the elimination half-life (t1/2beta) as 84 h and the total body clearance (Cl(T)) as 0.047 L kg(-1) h(-1). The volume of distribution at steady state, Vd(ss) was calculated to be 5.5 L kg(-1), indicating good tissue penetration of oxolinic acid in cod. Following p.o. administration of oxolinic acid or vetoquinol, the peak plasma concentrations (C(max)) of oxolinic acid and the time to peak plasma concentrations (T(max) were estimated to be 1.2 and 2.5 microg mL(-1) and 24 and 12 h, respectively. The bioavailabilities of oxolinic acid following p.o. administration of oxolinic acid and vetoquinol were calculated to be 55 and 72%, respectively. The in vitro minimum inhibitory concentration (MIC) values of oxolinic acid against three strains of Vibrio anguillarum isolated from diseased cod were 0.016 microg mL(-1) (HI-610), 0.250 microg mL(-1) (HI-618) and 0.250 microg mL(-1) (HI-A21). Based on a MIC value of 0.016 microg mmL(-1) a single p.o. administration of 25 mg kg(-1) of oxolinic acid maintains plasma levels in excess of 0.064 microg mL(-1), corresponding to four times the MIC-value, for approximately 12 days. The analogous value for a single p.o. dose of 25 mg kg(-1) of oxolinic acid administered as vetoquinol was 13 days.

Administration, Oral↗
PubMed1976

Comparative in vitro studies of cinoxacin, nalidixic acid, and oxolinic acid.

Cinoxacin and nalidixic acid were found to be similar in in vitro activity against 138 Shigella isolates and somewhat less active than oxolinic acid on a weight basis. Cross-resistance developed when 10 shigellae were transferred on increasing amounts of the respective agent contained in Mueller-Hinton agar. Plate dilution studies of the effect of changes in agar pH on the minimum inhibitory concentration revealed that the antibacterial activity increased with decreasing pH. Protein binding investigations revealed a high degree of binding, with nalidixic acid > oxolinic acid > cinoxacin.

Culture Media↗
PubMed1988

The DNA gyrase inhibitors, nalidixic acid and oxolinic acid, prevent iron-mediated repression of catechol siderophore synthesis in Azotobacter vinelandii.

Low concentrations of nalidixic acid and oxolinic acid that were just inhibitory to Azotobacter vinelandii growth promoted the production of the catechol siderophores azotochelin and aminochelin, in the presence of normally repressive concentrations of Fe3+. There was a limited effect on the pyoverdin siderophore, azotobactin, where low concentrations of Fe3+ were rendered less repressive, but the repression by higher concentrations of Fe3+ was normal. These drugs did not induce high-molecular-mass iron-repressible outer-membrane proteins and similar effects on the regulation of catechol siderophore synthesis were not produced by novobiocin, coumermycin, or ethidium bromide. The timing of nalidixic acid and Fe3+ addition to iron-limited cells was critical. Nalidixic acid had to be added before iron-repression of catechol siderophore synthesis and before the onset of iron-sufficient growth. Continued production of the catechol siderophores, however, was not due to interference with normal iron uptake. These data indicated that nalidixic acid prevented normal iron-repression of catechol siderophore synthesis but could not reverse iron repression once it had occurred. The possible roles of DNA gyrase activity in the regulation of catechol siderophore synthesis is discussed.

Azotobacter↗
PubMed2002

Fast-scanning fluorescence spectroscopy as a detection system in liquid chromatography for confirmatory analysis of flumequine and oxolinic acid.

Oxolinic acid and flumequine were analysed by reversed-phase liquid chromatography after extraction from the sample matrix with dichloromethane and partitioning with NaOH. The detection system consisted of a fast-scanning fluorescence detector, which provides the full spectra of the eluting peaks and can thus be used to confirm the identity of analytes. Determination was performed by partial least squares (PLS) and three-way PLS over the three-dimensional data, i.e. fluorescence intensity versus retention time and excitation wavelength. In both cases, similar results, with prediction errors around 4%, were obtained. The method was successfully applied to the analysis of salmon, pork and chicken muscle spiked up to 300 ng g(-1).

Anti-Infective Agents↗
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↗
PubMed1988

Nalidixic acid and oxolinic acid reversibly suppress 3-methylcholanthrene-induced cell transformation of BALB/3T3 mouse cells.

The effects of nalidixic acid (Nal) and oxolinic acid (Oxl), synthetic antibacterial compounds that inhibit bacterial DNA gyrase, on 3-methylcholanthrene (MC)-induced transformation of BALB/3T3 mouse cells were investigated. Exposure of the cells to Nal or Oxl for 2 weeks at any time during 4 weeks of incubation following MC treatment suppressed MC-induced transformation. Nal and Oxl also suppressed the enhancement of transformation by 12-O-tetradecanoylphorbol-13-acetate (TPA) initiated by MC. The suppression of transformation by Nal was released by exposure of the cells to TPA after removal of Nal. Since the suppressive effects of Nal and Oxl on transformation were time-related, they may be due to epigenetic changes.

Animals↗
PubMed1976

Pharmacokinetics of nalidixinic acid and oxolinic acid in healthy women.

The pharmacokinetics of oral nalidixic acid (NA, 1 gm 4 times a day) and oxolinic acid (OA, 750 mg 2 times a day) administered for 7 days were studied in the same 10 healthy women on the first, third, and seventh days of the treatment. The peak concentrations of NA + OH-NA (hydroxynalidixinic acid) in serum at 2 to 3 hr were 34 mug/ml (total) and 23 mug/ml (unconjugated) on the first day and nearly two times higher on the third and seventh days; 82% to 85% of these amounts were NA. The protein-free fraction of NA + OH-NA was 8.8% to 18.3%. The total concentration of NA + OH-NA in urine was 1,220 to 2,700 mug/ml, the unconjugated concentration, 250 to 350 mug/ml, and the chemotherapeutically active concentration, 55 to 75 mug/ml. In steady state the 24-hr recovery of the total drug was 79% of the daily dose. The excretion rate in urine was 591 to 853 mg/6 hr. The OA concentration in serum was very low on the first day of the treatment, but increased to 4- to 5-fold on the third and seventh days: 6.2 to 6.4 mug/ml (total) and 3.3 to 3.6 mug/ml (unconjugated). The protein-free OA represented 19% to 23% of the total amount. The modest initial serum concentrations of OA were confirmed by the low urine concentrations on the first day. In steady state the OA concentration in urine was 570 mug/ml (total) and 35 mug/ml (unconjugated), and the 24-hr recovery, 49% and 3%, respectively. The microbiologic assay gave somewhat higher concentrations of the active drug than did the chemical assay. When taken with food, the excretion of OA in urine was retarded by 6 hr but the 48-hr recovery was not decreased.

Administration, Oral↗
PubMed1999

Efficacy of orally administered oxolinic acid and Vetoquinol, an oxolinic acid ester, for the treatment of furunculosis in Atlantic salmon Salmo salar held in seawater.

This study was performed to determine the efficacy of orally administered oxolinic acid and Vetoquinol, an oxolinic acid ester, in the treatment of experimental induced furunculosis in Atlantic salmon Salmo salar held in seawater. Two strains of the causative bacterium Aeromonas salmonicida subsp. salmonicida, 1 sensitive (VI-88/09/03175) and 1 resistant (3475/90) to oxolinic acid, were used. In 2 trials, cohabitational challenges were performed by introducing 8 fish challenged in advance by an intraperitoneal injection of 2.2 x 10(4) colony forming units of strain 3475/90 (Trial 1) or strain VI-88/09/03175 (Trial 2) to 10 aquaria each containing 40 healthy fish. The treatment groups in both trials consisted of 4 groups receiving either oxolinic acid (2 groups) or Vetoquinol (2 groups) and 1 control group. An unchallenged, unmedicated group was used to determine the natural mortality in the population. The recommended therapeutic dose of 25 mg oxolinic acid kg-1 fish at Days 1, 2, 4, 6, 8 and 10 following initiation of treatment was used. Oral medication initiated at Day 10 (Trial 1) or Day 11 (Trial 2) following challenge significantly (p < 0.05) lowered the specific mortality in all drug-treated groups compared to the untreated control groups. Mortality in Vetoquinol-treated groups was significantly (p < 0.05) lower than in oxolinic acid-treated groups in Trial 1 whereas no significant (p < 0.05) difference in survival rate was found between the medicated groups in Trial 2.

Administration, Oral↗