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PubMed2002

A multiresistant clone of Shiga toxin-producing Escherichia coli O118:[H16] is spread in cattle and humans over different European countries.

Multiresistant Shiga toxin-producing Escherichia coli (STEC) O118:H16 and O118 nonmotile strains (designated O118:[H16]) were detected by examination of 171 STEC isolates for their antimicrobial sensitivity. Of 48 STEC O118:[H16] strains, 98% were resistant to sulfonamide, 96% were resistant to streptomycin, 79% were resistant to kanamycin, 75% were resistant to tetracycline, 67% were resistant to ampicillin, 60% were resistant to chloramphenicol, 48% were resistant to trimethoprim, and 10% each were resistant to gentamicin and nalidixic acid. Nalidixic acid resistance and reduced susceptibility to ciprofloxacin were associated with the mutation gyrA(LEU-83). The STEC O118:[H16] strains were found to belong to a single genetic clone as investigated by multilocus enzyme electrophoresis and by multilocus sequence analysis of E. coli housekeeping genes. The STEC O118:[H16] strains originated from humans and cattle and were isolated in seven different countries of Europe between 1986 and 1999. Strains showing multiresistance to up to eight different antimicrobials predominated among the more recent STEC O118:[H16] strains. The genes in parentheses were associated with resistance to kanamycin (aphA1-Ia), chloramphenicol (catA1), tetracycline [tet(A)], and ampicillin (bla(TEM-1)). Class 1 integrons containing sulI (sulfonamide resistance), aadA1a (streptomycin resistance), or dfrA1 (trimethoprim resistance)-aadA1a gene cassettes were detected in 28 strains. The bla(TEM-1b) gene was present in 18 of 21 strains that were examined by nucleotide sequencing. Class 1 integrons and bla(TEM) genes were localized on plasmids and/or on the chromosome in different STEC O118:[H16] strains. Hybridization of XbaI-digested chromosomal DNA separated by pulsed-field gel electrophoresis revealed that bla(TEM) genes were integrated at different positions in the chromosome of STEC O118:[H16] strains that could have occurred by Tn2 insertion. Our data suggest that strains belonging to the STEC O118:[H16] clonal group have a characteristic propensity for acquisition and maintenance of resistance determinants, thus contrasting to STEC belonging to other serotypes.

Animals↗

PubMed2000

Quinolone resistance in enterotoxigenic Escherichia coli causing diarrhea in travelers to India in comparison with other geographical areas.

Enterotoxigenic Escherichia coli isolates were identified as a cause of traveler's diarrhea in 82 of 520 (16%) patients and tested for resistance to seven antimicrobial agents. Thirty patients (36%) needed antimicrobial therapy: 17 (56%) for persistence of symptoms and 13 (44%) for severity of symptoms. Ampicillin, tetracycline, and trimethoprim-sulfamethoxazole resistance was high. Chloramphenicol showed moderate activity, and amoxicillin plus clavulanic acid, nalidixic acid, and ciprofloxacin showed very good activity. Five nalidixic acid-resistant strains were isolated, four from patients visiting India.

Diarrhea↗

PubMed1989

Improvement of chemical analysis of antibiotics. XVI. Simple and rapid determination of residual pyridonecarboxylic acid antibacterials in fish using a prepacked amino cartridge.

A simple and rapid method for the determination of residual pyridonecarboxylic acid antibacterials (PCAs) (oxolinic acid, nalidixic acid and piromidic acid) in fish was developed using a combination of high-performance liquid chromatography (HPLC) and clean-up with an amino-type prepacked cartridge. PCAs were extracted with n-hexane-ethyl acetate (1:3) and the extract was applied to a Baker 10 amino cartridge. PCAs were eluted from the cartridge with acetonitrile-methanol-0.01 M aqueous oxalic acid solution (pH 3.0) (3:1:6) and were determined by HPLC. The separations were performed on Nucleosil 3C18 (3 microns, 75 x 4.6 mm I.D.) using a mobile phase containing oxalic acid. The recoveries of PCAs from various fishes fortified at the level of 1.0 ppm were 77.1-95.5%, and the detection limits were 0.05 ppm. The analytical time per sample was less than 30 min.

Animals↗

PubMed1998

Transferable trimethoprim resistance in Shigella strains.

The susceptibility patterns of 35 Shigella isolates (16 S. flexneri, 14 S. dysenteriae and 5 S. sonnei) to trimethoprim (Tp) and various antibiotics including amoxycillin, amoxycillin-clavulanic acid, nalidixic acid, ciprofloxacin, ceftazidime and ceftriaxone, were investigated. Twenty-two (62.8%) strains were resistant to Tp with a minimal inhibitory concentration (MIC50) value of 512 mg/L. Only six isolates were amoxycillin resistant, to which clavulanic acid restored sensitivity in all of them. None of the isolates were resistant either to extended spectrum cephalosporins or to quinolones. Resistance to Tp was transferred from 7 of the 22 isolates (31.8%) to the recipient Escherichia coli K12. Tp MIC values of the transconjugants were 512 mg/L. In no strain could amoxycillin resistance be transferred. Our results indicate that as the prevalence of transferable Tp resistance in Shigella isolates in Izmir is substantially high, alternative antimicrobial agents should be considered for empirical antibiotic therapy.

Amoxicillin↗

PubMed1984

Comparative in vitro activity of five quinoline derivatives and five other antimicrobial agents used in oral therapy.

The antibacterial activity of ciprofloxacin was compared to those of norfloxacin, pefloxacin, pipemidic acid, nalidixic acid, nitrofurantoin, sulfamethoxazole, trimethoprim, cephradine and amoxycillin. Agar dilution tests were performed with 631 clinical isolates from urinary and respiratory tract infections. Ciprofloxacin was found to be the most active drug tested against all gram-negative organisms and streptococci, with the exception of Streptococcus faecalis and Streptococcus pneumoniae. MIC 90 values of ciprofloxacin were as follows: for Enterobacteriaceae, 0.03-0.23 mg/l, Pseudomonas aeruginosa, 0.37 mg/l, Haemophilus influenzae, less than 0.015 mg/l, Staphylococcus aureus, 0.75 mg/l, Streptococcus pneumoniae, 1.89 mg/l, and Streptococcus faecalis, 0.95 mg/l. The inhibitory quotients for urine, serum and bronchial secretion showed that ciprofloxacin had the broadest spectrum of all agents tested and covered and clinically significant bacteria.

Administration, Oral↗

PubMed1999

Enhanced susceptibility of pentylenetetrazole kindled mice to quinolone effects.

The present study was designed to examine the ability of different quinolones to affect the seizure severity and the latency of development of chemical kindling produced by repeated treatment using a subconvulsant dose of pentylenetetrazole (PTZ). A group of mice (kindled control) were treated subcutaneously (s.c.) with vehicle + PTZ (30 mg/kg, three times a week) for 6 consecutive weeks and the changes in excitability associated with the kindling state were observed over the following 2 h. A second group of mice were injected intraperitoneally (i.p.) with the following quinolone derivatives, ciprofloxacin (ciprox), pefloxacin (peflox), ofloxacin (oflox), cinoxacin (cinox), nalidixic acid (nalidixic), 1-cyclopropyl-6-amino-7-tetrahydroisoquinoline-8-methyl-4-oxo-1,4-dihydr oquinoline-3-carboxylic acid (M5) and 1-cyclopropyl-7-tetrahydro-isoquinoline-8-methyl-4-oxo-1,4-dihydroquinol ine-3-carboxylic acid (MH5) at a dose of 20 mg/kg 15 min before receiving a subconvulsant dose of PTZ (30 mg/kg, s.c.). The results showed that pretreatment with some of the quinolones tested facilitated the development of kindling to PTZ-induced seizures. In particular, ciprox, peflox, oflox, M5 and MH5 derivatives variously increased the development of kindling to PTZ induced seizures, whilst cinox and nalidix did not significantly affect it. Additionally we determined whether the enhanced susceptibility of kindled mice only occurred after relatively short intervals following the last seizure or whether it was a more permanent phenomenon. For the study of the persistence of kindling, the animals were rechallenged with the kindling stimulus (PTZ 25 mg/kg, s.c.) 15 and 30 days after the last injection of the chronic treatment with PTZ (30 mg/kg, s.c.) and the behavioural changes in the kindled mice were compared with the control ones (chronically treated with vehicle). The present data demonstrated that kindling produced long-lasting alterations, substantiating that epileptogenesis initiated by kindling renders the brain more susceptible to central nervous system (CNS) side effects of quinolones. An interaction between PTZ and quinolone derivatives which involves either an inhibition of gamma-aminobutyric acid (GABA) neurotransmission or/and an increase in the function of the excitatory amino acid (EAA) system is suggested.

Animals↗

PubMed1992

Lomefloxacin: microbiologic assessment and unique properties.

In comparative studies, lomefloxacin, a new difluorinated quinolone, exhibits broad antibacterial activity in vitro, similar or superior to that of other quinolones (enoxacin, ofloxacin, pipemidic acid, nalidixic acid, and norfloxacin) but less than that of ciprofloxacin. Lomefloxacin inhibited Neisseria gonorrhoeae, Moraxella (Branhamella) catarrhalis, Haemophilus influenzae, Pseudomonas aeruginosa, Staphylococcus aureus, and the majority of aerobic gram-negative rods, including nosocomial isolates, at concentrations readily achievable in biologic fluids and tissues. Lomefloxacin was less active against obligate anaerobes and streptococci. Organisms resistant to methicillin, penicillin, or the aminoglycosides were susceptible to lomefloxacin. No significant lomefloxacin resistance was identified in 18 countries in which in vitro studies were conducted, with the exception of a small number of strains tested in France. The frequency with which spontaneous single-step resistance to lomefloxacin develops in vitro is low.

Anti-Infective Agents↗

PubMed2005

Antibiotic susceptibility profiles of new probiotic Lactobacillus and Bifidobacterium strains.

The antimicrobial susceptibilities and presence of plasmids in four new probiotic lactic acid bacteria (LAB) strains, Lactobacillus rhamnosus HN001 (DR20) HN067, Lactobacillus acidophilus HN017 and Bifidobacterium lactis HN019 (DR10), were determined. Resistance to 18 commonly used antibiotics was assessed by disk diffusion. The three Lactobacillus strains had similar antibiotic susceptibility profiles to those of Lactobacillus plantarum strain HN045 and two commercial probiotic Lactobacillus strains, GG and LA-1. The B. lactis strain HN019 had a similar profile to three commercial probiotic B. lactis strains (Bb12, HN049 and HN098). All 10 strains were sensitive to the Gram-positive spectrum antibiotics erythromycin and novobiocin, the broad-spectrum antibiotics rifampicin, spectinomycin, tetracycline and chloramphenicol and the beta-lactam antibiotics penicillin, ampicillin and cephalothin. By contrast, most strains were resistant to the Gram-negative spectrum antibiotics fusidic acid, nalidixic acid and polymyxin B and the aminoglycosides neomycin, gentamicin, kanamycin and streptomycin. All three L. rhamnosus strains (HN001, HN067 and GG) were resistant to vancomycin and several strains were also resistant to cloxacillin. Of the four new probiotic strains, only L. rhamnosus HN001 contained plasmids; however, a plasmid-free derivative of HN001 had the same antibiotic susceptibility profile as the parent strain.

Anti-Bacterial Agents↗

PubMed2002

Multiresidue determination of (fluoro)quinolone antibiotics in swine kidney using liquid chromatography-tandem mass spectrometry.

New antibiotics were recently developed, among which are the (fluoro)quinolones. This paper presents an analytical method which allows the determination of 11 (fluoro)quinolones in swine kidneys: norfloxacin, ofloxacin, cinoxacin, oxolinic acid, nalidixic acid, flumequine, enrofloxacin, enoxacin, ciprofloxacin, danofloxacin and marbofloxacin. The procedure involves a rapid and efficient pre-treatment by solid-phase extraction (recoveries 83-98%), followed by the sensitive and selective determination of all compounds in a single run using LC-ESI-MS-MS. Multiple reaction monitoring (MRM) was used for selective detection of each (fluoro)quinolone. Quinine was selected as internal standard. The accuracy of the method, expressed as recovery, was between 89 and 109%; the repeatability had a maximum RSD lower than 15%. The limits of detection (LOD) were much lower than the respective Maximum Residue Limits (MRL)/4.

Animals↗

PubMed2003

Increasing prevalence of antimicrobial resistance among Enterobacteriaceae uropathogens in Dakar, Senegal: a multicenter study.

To assess antibiotic susceptibility among Enterobacteriaceae isolated in urine from outpatients in Dakar, Senegal, a prospective multicenter study involving 3 laboratories had been conducted between June and October 2001. During this period, 300 strains were isolated and susceptibility testing was performed against antibiotics commonly used in treatment of community-acquired urinary tract infections (UTI). E. coli and K. pneumoniae represented 89% of isolates. The overall resistance rates of ampicillin, amoxicillin-clavulanic acid, nalidixic acid, fluoroquinolones and cotrimoxazole were respectively 77.3%, 34.7%, 14.7%, 13.3%, and 55%. In the light of these results, a re-evaluation of first line therapies and prudent use of fluoroquinolones is advised. At the same time a continued surveillance of antimicrobial resistance should be developed in Senegal in order to control the emergence of multidrug resistant strains and to establish a national therapeutic guideline for treatment of UTI.

Adolescent↗

PubMed1999

Is monochromatic irradiation testing useful in the differentiation of drug-induced photosensitivity from chronic actinic dermatitis?

Chronic actinic dermatitis (CAD) is an uncommon, eczematous photosensitive eruption affecting predominantly elderly men and to which drug-induced photosensitivity may sometimes appear clinically identical. This retrospective study compares the monochromatic irradiation results in 11 patients with CAD and 14 patients with drug-induced photosensitivity, to assess whether such testing is useful in the differentiation of these two conditions. Thus, the action spectra of the drug photosensitivity patients were plotted and compared with those of 12 nonphotosensitive control patients: 10 patients were found to be photosensitive in the UVA range; the implicated drugs included quinine, sparfloxacin, amiodarone, doxycycline, mefenamic acid, nalidixic acid, fenbrufen, diclofenac, enalapril, diltiazem and prochlorperazine maleate. One patient on doxycycline was photosensitive in both the UVA and UVB ranges. The remaining three patients were not tested until after discontinuation of their drug and their light tests were then normal. In the CAD group, five patients were photosensitive in the UVA, UVB and visible light ranges and six were photosensitive in the UVA and UVB ranges. Comparison of the mean minimal erythema dose responses then demonstrated dissociation of the drug-induced from the CAD group in the UVB region; the result was statistically significant. This suggests that UVA-sensitivity dissociated from UVB-sensitivity is a relative indicator of drug-induced photosensitivity and monochromatic irradiation testing may therefore be helpful in the differentiation of these two disorders.

Adult↗

PubMed1979

Antimicrobial susceptibility of clinical isolates of Serratia marcescens.

The in vitro susceptibilities of 242 isolates of Serratia marcescens to 17 antibacterial drugs have been determined. Oxolinic acid, nalidixic acid, cefoxitin, and amikacin were the most active drugs. Ampicillin, kanamycin, and cephalothin were among the least active. A 4-year study showed that resistance of S. marcescens to dibekacin, tobramycin, sisomycin, and gentamicin has increased at least one order of magnitude in that period, whereas resistance to amikacin showed but a twofold increase.

Aminoglycosides↗

PubMed1986

Multiple low-level antibiotic resistance in Aeromonas salmonicida.

Mutants with multiple low-level antibiotic resistance were isolated from virulent wild-type Aeromonas salmonicida strains exposed to a low concentration of any one of several low-molecular-mass (approximately 635 daltons or less) antibiotics. Multiple resistance was toward beta-lactam compounds (penicillin G, ampicillin, cloxacillin), quinolones (flumequine, oxolinic acid, nalidixic acid), tetracyclines, chloramphenicol, and novobiocin. Susceptibilities of the mutants toward several higher-molecular-mass (greater than 700 daltons) hydrophobic or polycationic antibiotics such as rifampin, erythromycin, polymyxin B, and streptomycin sulfate were not affected. The mutants were obtained at frequencies suggesting point mutations. Outer membrane protein profiles, examined by sodium dodecyl sulfate-polyacrylamide gel electrophoresis, revealed that all multiple low-level resistant mutants were deficient in a major protein of approximately 38.5 kilodaltons and contained a major protein of approximately 37 kilodaltons which was not present in significant amounts in the wild-type strains. In addition, these mutants lacked exoprotease activity. Furthermore, mutants isolated as deficient in exoprotease were found, with the exception of one avirulent strain, to exhibit multiple low-level antibiotic resistance and the outer membrane protein changes.

Aeromonas↗

PubMed1985

Incidence of penicillinase producing Neisseria gonorrhoeae (PPNG) strains and susceptibility of gonococcal isolates to antibiotics in Benin City, Nigeria.

Of 53 strains of Neisseria gonorrhoeae isolated in Benin City, Nigeria, in February 1983 to October 1984, 46 (87%) produced penicillinase. The minimum inhibitory concentrations (MICs) of penicillin G and ampicillin for these isolates were between 1 mg/l and and 50 mg/l. About 48% (22/46) of the penicillinase producing strains were also resistant to streptomycin, cotrimoxazole, and ampicillin and cloxacillin. All 53 isolates were sensitive to tetracycline, erythromycin, amoxycillin and clavulanic acid, nalidixic acid, spectinomycin, and the penicillinase stable cephalosporins. The high incidence of resistance may have been the result of indiscriminate and unsupervised use of antibiotics before patients presented for proper treatment in clinics and hospitals.

Ampicillin↗

PubMed1991

Quinolones and fenbufen interact with GABAA receptor in dissociated hippocampal cells of rat.

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.

4-Quinolones↗

PubMed1987

In vitro activity and concentrations in serum, urine, prostatic secretion and adenoma tissue of ofloxacin in urological patients.

Studies in vitro showed that at concentrations of 1 and 4 mg/L ofloxacin inhibited 94 and 99% of the Gram-negative pathogens in isolates cultured from the urine of patients with complicated urinary tract infections (UTI). Against Gram-positive bacteria, 60 and 100% were inhibited at the corresponding concentrations. Comparisons of the MIC90 values of 8 quinolones showed the decreasing order of in vitro antibacterial activity to be ciprofloxacin, ofloxacin, norfloxacin, pefloxacin, enoxacin, pipemidic acid, nalidixic acid and cinoxacin. After an oral dose of ofloxacin 400mg, the mean peak serum concentration in 10 elderly patients was 5.5 mg/L and mean renal excretion during 24 hours was 41%. In 17 patients undergoing transurethral resection of the prostate, ofloxacin 400mg was given for perioperative prophylaxis. Two to 4.5 hours after administration, the median concentrations in prostatic secretion (5 patients) and prostatic adenoma tissue were 4.0 mg/L and 4.1 mg/kg, respectively. The corresponding serum concentrations of ofloxacin were 3.4 and 3.9 mg/L, respectively. In a group of 10 patients, 14.5 to 19.5 hours after oral administration of ofloxacin 400mg the median serum and prostatic adenoma tissue concentrations of ofloxacin were 1.9 mg/L and 1.2 mg/kg, respectively. The in vitro activity of ofloxacin concentrations attained in serum, urine, prostatic secretion and adenoma tissue show that it appears to be well suited for the treatment of complicated UTI.

Adenoma↗

PubMedDate not supplied

Comparison of aztreonam against other antibiotics used in urinary tract infections.

BACKGROUND: Urinary tract infection is a very common problem in adults as well as in children. There is always need for the right antibiotic to be chosen for treatment. METHODS: This study was conducted at Microbiology section in Pathology department of Ayub Medical College, Abbottabad, Pakistan. In this study the aztronam which is only effective against gram negative bacilli has been compared with other conventionally used antibiotics, ampicillin, cotrimoxazole, minocyclin, pipemedic acid, nalidixic acid, norfloxacin, ciprofloxacin, gentamicin and ceftriaxon. RESULTS: Total gram negative isolates were 342. Out of this 76.6% (262) were E. coli, klebsiella pneumoniae 14.3% (49), proteus species 5.2%(18) and pseudomonas aeruginosa were 3.8% (13). The aztreonam showed 78% sensitivity against gram negative bacilli which is better than norfloxacin which showed 62.2% sensitivity.

Anti-Infective Agents, Urinary↗

PubMed1980

Antibacterial activity of miloxacin.

The chemotherapeutic properties of miloxacin (5,8-dihydro-5-methoxy-8-oxo-2H-1,3-dioxolo-[4,5-g]quinoline-7-carboxylic acid) have been compared with those of oxolinic acid and nalidixic acid. The in vitro activities of miloxacin (minimum inhibitory concentrations) against a variety of gram-negative bacteria, especially Enterobacteriaceae and Haemophilus, were comparable to those of oxolinic acid and 8 to 16 times greater than those of nalidixic acid. Miloxacin was more active than oxolinic acid against some anaerobes and less active against staphylococci. Miloxacin exhibited significant activities when administered orally to mice infected with Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Proteus vulgaris, or Serratia marcescens. Its efficacy was comparable to that of oxolinic acid and two to four times greater than that of nalidixic acid. Miloxacin was less active against a Pseudomonas aeruginosa infection and inactive at the maximum test doses against a Streptococcus pyogenes infection.

4-Quinolones↗