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Therapie 1988
Topics: Acute Kidney Injury; Aged; Aged, 80 and over; Female; Humans; Male; Middle Aged; Nicotinic Acids; Piromidic Acid; Product Surveillance, Postmarketing
PubMed: 3227506
DOI: No ID Found -
Bollettino Chimico Farmaceutico Jul 1979
Topics: Bacteria; Humans; In Vitro Techniques; Microbial Sensitivity Tests; Nicotinic Acids; Oxolinic Acid; Piromidic Acid; Urinary Tract Infections
PubMed: 526354
DOI: No ID Found -
The Journal of Antimicrobial... May 1984In order to investigate the comparative activity of agents of the nalidixic acid series, cultures of nalidixic acid sensitive strains of E. coli were exposed to the...
In order to investigate the comparative activity of agents of the nalidixic acid series, cultures of nalidixic acid sensitive strains of E. coli were exposed to the drugs in an in-vitro model that simulates the hydrokinetic aspects of the treatment of bacterial cystitis. Intrinsic activity, as judged by the response to a single dose of drug and resistance as judged by response to a repeat dose, were investigated. All seven compounds tested in this way were able to inhibit bacterial growth for considerable periods of time even when the peak concentration achieved was as low as 10 mg/l. However, resistance emerged readily, particularly to nalidixic acid, pipemidic acid and piromidic acid. Norfloxacin was the most active of the seven compounds tested and was the only one to which resistance did not emerge at the concentrations tested. However, when two nalidixic acid resistant strains were tested in the bladder model, norfloxacin resistance was observed to emerge with one strain, but not with the other.
Topics: Anti-Infective Agents, Urinary; Cystitis; Drug Resistance, Microbial; Escherichia coli; Nalidixic Acid; Norfloxacin; Quinolines
PubMed: 6234274
DOI: 10.1093/jac/13.suppl_b.43 -
The Journal of Antimicrobial... Jun 1986Several new quinolone derivatives were investigated for their influence on human lymphocyte blastogenesis and gamma-interferon production following concanavalin A...
Several new quinolone derivatives were investigated for their influence on human lymphocyte blastogenesis and gamma-interferon production following concanavalin A stimulation. All the antimicrobials induced inhibition of lymphocyte DNA synthesis. The gamma-interferon measurements showed that nalidixic acid and norfloxacin have a negative influence on lymphokine production and release.
Topics: Adult; Anti-Infective Agents; DNA; Humans; In Vitro Techniques; Interferon-gamma; Lymphocyte Activation; Lymphocytes; Male; Middle Aged; Nalidixic Acid; Norfloxacin; Ofloxacin; Oxazines; Pipemidic Acid; Piromidic Acid
PubMed: 3090010
DOI: 10.1093/jac/17.6.811 -
Deutsche Medizinische Wochenschrift... Apr 1981
Topics: Acute Kidney Injury; Aged; Female; Humans; Nicotinic Acids; Piromidic Acid
PubMed: 7215176
DOI: No ID Found -
The Science of the Total Environment Jan 2013Laboratory-scale batch experiments were developed to investigate the main removal routes for 6 commonly found quinolones (ciprofloxacin, moxifloxacin, norfloxacin,...
Laboratory-scale batch experiments were developed to investigate the main removal routes for 6 commonly found quinolones (ciprofloxacin, moxifloxacin, norfloxacin, ofloxacin, pipemidic acid, and piromidic acid), in wastewaters from a wastewater treatment plant, at μg L(-1) levels in an aerobic sludge system from a membrane bioreactor (MBR) pilot plant. It was demonstrated that sorption and biotransformation were the main removal routes for the target antibiotics over other possible pathways, as volatilization or hydrolysis, under the experimental conditions. Mass balances indicated that sorption on sludge played a dominant role in the elimination of antibiotics from waters. The sorption coefficient K(d) depended strongly on temperature and on the quinolone type and were higher at lower temperatures and for piperazinylic quinolones. K(d) values were between 516 and 3746 L kg(-1) in the temperature range of 9-38°C. Higher mixed liquor suspended solids (MLSS) increased quinolone removal efficiency mainly by sorption. Quinolone biodegradation constituted a secondary pathway, and could be described by first-order kinetics with degradation-rate constants ranging from 8.0 × 10(-4)h(-1) to 1.4 × 10(-2)h(-1) within the same temperature range and MLSS from 7000 to 15,000 mg L(-1). Biodegradation depended on the MLSS and temperature, but also on the initial chemical oxygen demand (COD). Higher biodegradation rates were observed at higher MLSS and temperature, as well as at low initial COD. Ciprofloxacin and moxifloxacin registered the highest biodegradation percentages (52.8% and 47.2%, respectively, at 38°C and 15,000 mg L(-1) MLSS), which is evidence that, despite the known persistence of this group of antibiotics and removal from waters mainly by sorption, it was possible to improve their removal by biodegradation, with an appropriate selection of conditions and control of process variables, as a preliminary step towards the elimination of these antibiotics from the environment. Further research is needed on the possibilities of removing sorbed antibiotics from sludge.
Topics: Adsorption; Aerobiosis; Anti-Bacterial Agents; Biodegradation, Environmental; Biomass; Bioreactors; Filtration; Kinetics; Molecular Structure; Pilot Projects; Quinolones; Sewage; Water Pollutants, Chemical; Water Purification
PubMed: 23178836
DOI: 10.1016/j.scitotenv.2012.10.026 -
Food Additives & Contaminants. Part A,... Jun 2018Seventeen quinolone antibiotics were determined in cows' milk. A method of high sensitivity, selectivity and accuracy was developed. Accuracy (trueness and precision),...
Seventeen quinolone antibiotics were determined in cows' milk. A method of high sensitivity, selectivity and accuracy was developed. Accuracy (trueness and precision), linearity, sensitivity, selectivity, decision limit and detection capability were established following the recommendations of the Commission Decision 2002/657/EC and the Food and Drug Administration (FDA) guideline. The use of polar stir-bar sorptive extraction (SBSE) prior to UHPLC-MS/MS analysis is proposed. The variables that affect SBSE were optimised using multivariate optimisation strategies. The ionic strength, the extraction time and the sample volume were studied. pH and stir-bar coating (polydimethylsiloxane, PDMS, and polyethyleneglycol modified silicone, PEG) were studied. PEG showed the best extraction yield at pH 6. For validation, a matrix-matched calibration and a recovery assay were carried out. Limits of quantification from 0.5 μg kg for nalidixic acid, flumequine and piromidic acid, to 4.0 μg kg for sarafloxacin were calculated. The precision (%, RSD) was lower than 15% for all antibiotics. Recoveries in fortified samples were between 88 and 114%.
Topics: Animals; Cattle; Chromatography, High Pressure Liquid; Drug Residues; Food Contamination; Milk; Quinolones; Solid Phase Extraction; Tandem Mass Spectrometry
PubMed: 29368583
DOI: 10.1080/19440049.2018.1430382 -
Hinyokika Kiyo. Acta Urologica Japonica Oct 1983The relationship between the concentrations of various antimicrobial agents in the genital organs of male rats, serum, liver and kidney after oral administration,... (Comparative Study)
Comparative Study
The relationship between the concentrations of various antimicrobial agents in the genital organs of male rats, serum, liver and kidney after oral administration, intramuscular infusion and i.v. infusion were systematically compared and studied. The concentration of Ampicillin in human prostatic tissues after intramuscular infusion was also measured. The drug concentration in the prostatic tissues after oral administration of nalidixic acid (20 mg/kg) was highest 21.5 micrograms/g (2-hour value) which was about 4 times the serum level, followed by chloramphenicol, Cefalexin, Ampicillin, piromidic acid and erythromycin. The concentration of Ampicillin and Cefaloridine in the prostatic tissues after intramuscular infusion was high, but the concentration of Cefazolin, was low after both intramuscular infusion and i.v. infusion. The drug concentration in the prostatic tissues after i.v. infusion of Cefaloridine, Erythromycin, and Ampicillin was high. The concentration of Erythromycin was high only after i.v. infusion. The concentration of both Chloramphenicol and Gentamicin in the blood, and in the prostatic tissues were low. Of the drugs tested, the concentration of Ampicillin in human prostatic tissues was the highest being about 8 micrograms/g at 60 minutes after intramuscular infusion, which was about 40% of its concentration in the blood. The concentrations of antimicrobial agents in the epididymis and testis of the rats were low. Even the relatively high values were only about 10% of the concentration in the blood. The concentration of nalidixic acid in the prostatic tissues was 4 times as high as that of Piromidic acid. In summary, the antimicrobial agents showing high concentrations in the prostatic tissues were nalidixic acid by oral administration, Ampicillin and Cefaloridine by intramuscular infusion, and i.v. infusion, which showed relatively high concentrations in the blood. Irrespective of the route of administration, the concentrations of Chloramphenicol and Gentamicin in the male genitals were low. The drug concentration in the testis was very low irrespective of the chemotherapeutic and administration form. This seems to signify the presence of the so-called blood-testis barrier to protect the important function of spermatogenesis.
Topics: Administration, Oral; Animals; Anti-Bacterial Agents; Epididymis; Humans; Injections, Intramuscular; Injections, Intravenous; Kidney; Liver; Male; Prostate; Rats; Rats, Inbred Strains; Testis
PubMed: 6681499
DOI: No ID Found -
The Journal of Antimicrobial... Sep 1976
Topics: Animals; Cytochrome c Group; Electron Transport; Gram-Negative Aerobic Bacteria; Horses; Kinetics; Myocardium; Nalidixic Acid; Nicotinic Acids; Oxidation-Reduction; Phenanthrolines; Pyrrolidines
PubMed: 185191
DOI: 10.1093/jac/2.3.299 -
Journal of Neurophysiology Aug 19911. Interaction of quinolone antibiotics and the anti-inflammatory agent fenbufen with the gamma-aminobutyric acid-A (GABAA) receptor-chloride channel complex in...
1. Interaction of quinolone antibiotics and the anti-inflammatory agent fenbufen with the gamma-aminobutyric acid-A (GABAA) receptor-chloride channel complex in pyramidal neurons freshly dissociated from the hippocampal CA1 region of the rats was investigated in whole-cell mode, using the patch-clamp technique under voltage-clamp conditions. 2. Quinolones in clinical doses had no effects on the GABA-gated Cl- current (ICl) but slightly suppressed the response at concentrations greater than 10(-5) M. A metabolite of fenbufen, 4-biphenylacetic acid (BPA), also had little effect on the GABA response at therapeutic concentrations. 3. Coadministration of one of quinolones and BPA suppressed the GABA-gated ICl with increase in each of them in a concentration-dependent manner, and there was a parallel shift of the concentration-response curve for GABA to the right but with no effect on the maximum response, thereby indicating a competitive antagonism. The inhibitory potency of antibiotics in combination with BPA was in the order of norfloxacin much greater than enoxacin greater than cyprofloxacin greater than pipemidic acid much greater than ofloxacin greater than cinoxacin = piromidic acid = nalidixic acid = 0. 4. Norfloxacin and BPA, administered simultaneously, also strongly suppressed pentobarbital sodium (PB)-gated ICl, but they did not act on benzodiazepine (BZP) receptors. 5. Both GABA- and PB-induced ICls reversed at the Cl- equilibrium potential (ECl). In the presence of BPA, the quinolone-induced inhibition of GABA-gated ICls showed no voltage dependence. 6. It was concluded that, in the presence of an anti-inflammatory agent, the quinolone antibiotics decrease the affinity of GABAA receptors, the result being induction of epileptogenic neurotoxicities.
Topics: 4-Quinolones; Animals; Anti-Infective Agents; Anti-Inflammatory Agents, Non-Steroidal; Chloride Channels; Drug Interactions; Electrophysiology; Hippocampus; In Vitro Techniques; Ion Channels; Membrane Proteins; Muscimol; Neurons; Pentobarbital; Phenylbutyrates; Pyramidal Tracts; Rats; Rats, Inbred Strains; Receptors, GABA-A; Structure-Activity Relationship; gamma-Aminobutyric Acid
PubMed: 1723095
DOI: 10.1152/jn.1991.66.2.497