One hundred and fifty strains of Gram negative bacilli isolated from urine of patients with urological disease were tested for resistance to antimicrobial drugs including quinolones. Escherichia coli (61 strains) was most frequently isolated, and followed by Klebsiella spp. (36), Pseudomonas aeruginosa (12). and Proteus spp. (6) in the decreasing order. New quinolone carboxylic acid compounds such as enoxacin (Ex). norfloxacin (Nf), ciprofloxacin (Cp), pefloxacin (Pf), and ofloxacin (Of) showed very high antimicrobial activities against the majority of organisms tested except P.aerogi. nose. In P.aeruginosa all strains were resistant to nalidixic acid, and 25-33% to Ex. Nf. Cp, Pf, and Or. The majority of strains tested were found to be resistant to beta-lactam antibiotics except moxalactam (Mr). aminoelycoside drugs except amikacin (Ak), and other drugs tested such as chloramphgnicol, tetracycline. rifampin and etc.. but in P.aeruginosa, 33-58% were resistant to Mx and Ak. Organisms multiplyine resistance to 5 or more druge were noted in almost all isolates tested The stain numbers of multiplying resistance to 5 or more drugs were 51 strains (83.6%) of E. Coli 24 strains (66.7%) of Klebsielle spp., 10 strains (83.3%) of P.aeruginosa, and 5 strains (83.3%) of Prorteus spp.
Amikacin ; Anti-Bacterial Agents ; Ciprofloxacin ; Drug Resistance, Microbial* ; Enoxacin ; Escherichia coli ; Humans ; Klebsiella ; Moxalactam ; Nalidixic Acid ; Norfloxacin ; Nose ; Ofloxacin ; Pefloxacin ; Proteus ; Pseudomonas aeruginosa ; Quinolones ; Rifampin ; Tetracycline ; Urologic Diseases

BACKGROUND: The photsensitizing effect of quinolones has been recognized since their introdulation as an antibacterial agents. Recently several new second eneration antibacterial agents of this pharmacological class have become available for therapy, and are gaining increasing impotance. OBJECTIVE: To reveal the phototoxic potentials of some new quinolones by photohemolysis test, estimation of fluorescenc spectra, and Candida albicans test. METHODS: Nalidixic acid and four second-generation quinolones(ciprofloxacin, enoxacini, norfloxacin, and ofloxacitid were examined by fluorescence spertra which measured t.he phototoxc potentials by photochemial instability, photohemolsis test for the phototoxic properties against cell membranes and Candida tlbicans test for phototoxic properties against DNA. RESULTS: All drugs showed a fluorescence spectra within 360 nm to 450 nm, and in the photohemolysis test, all studied drug except ofloxacin got above 5% hemolytic value, and all drugs showed clear zone. in Candida albicans test after 48hours. CONCLUSION: These results suggested that all tested drugs were photochemically unstable. According to the mechanisris of cellular phototoxicity, ciprofloxacin, enoxacin, and norfloxacin was phtototoxic to nucleus and cell membrane, whereas ofloxacin was phototoxic to nucleus only.
Anti-Bacterial Agents* ; Candida ; Candida albicans ; Cell Membrane ; Ciprofloxacin ; Dermatitis, Phototoxic ; DNA ; Enoxacin ; Fluorescence ; Nalidixic Acid ; Norfloxacin ; Ofloxacin ; Quinolones

A preparation of water soluble components(EA) was made from carpophores of Elfvingia applanata(Pers.) Karst and its in vitro antibacterial activity on a number of bacterial species was examined by macrobroth dilution assay. Among 16 species of bacteria tested, the most potent antibacterial activity was observed against Staphylococcus epiderrnidis and Proteus vulgaris, of which MICs were 1.25 mg/ml. To investigate the antibacterial effects in combinations of EA with quinolone antibiotics, such as ciprofloxacin, enoxacin, lomefloxacin, norfloxacin, and ofloxacin, the fractional inhibitory concentrations(FICs) and the fractional inhibitory concentration indices(FICIs) for four bacterial strains were determined by macrobroth dilution checkerboard assay. Combinations of EA and quinolones exhibited either additive or indifferent effects of antibacterial activity in most instances. However, both synergistic and antagonistic effects were not observed in any cases.
Anti-Bacterial Agents ; Bacteria ; Ciprofloxacin ; Enoxacin ; Norfloxacin ; Ofloxacin ; Proteus vulgaris ; Quinolones* ; Staphylococcus

Turtle-borne Salmonella enterica owns significance as a leading cause in human salmonellosis. The current study aimed to determine the quinolone susceptibility and the genetic characteristics of 21 strains of S. enterica subsp. enterica isolated from pet turtles. Susceptibility of four antimicrobials including nalidixic acid, ciprofloxacin, ofloxacin, and levofloxacin was examined in disk diffusion and MIC tests where the majority of the isolates were susceptible to all tested quinolones. In genetic characterization, none of the isolates were positive for qnr or aac(6')-Ib genes and no any target site mutations could be detected in gyrA, gyrB, and parC quinolone resistance determining regions (QRDR). In addition, neighbor-joining phylogenetic tree derived using gyrA gene sequences exhibited two distinct clads comprising; first, current study isolates, and second, quinolone-resistant isolates of human and animal origin. All results suggest that studied strains of S. enterica subsp. enterica isolated from pet turtles are susceptible to quinolones and genetically more conserved with regards to gyrA gene region.
Animals ; Ciprofloxacin ; Diffusion ; Humans ; Levofloxacin ; Nalidixic Acid ; Ofloxacin ; Quinolones ; Salmonella enterica* ; Salmonella Infections ; Salmonella* ; Trees ; Turtles*

The drug eruptions caused by quinolones are rarely reported. The patient took norfloxacin for several days prior to admission and was admitted due to systemic erythematous maculopapular eruptions. For the treatment of urinary tract infection, he was treated with pefloxacin via intravenous route, and then the symptom of drug eruption became aggravated. After termination of treatment, the symptom reduced. The causative agent was identified by intradermal test and confirmed by accidental rechallenge with levofloxacin which is an another quinolone. We report herein the case of drug eruption caused by several quinolones which was confirmed by intradermal test and incidental administration of the drug.
Drug Eruptions* ; Humans ; Intradermal Tests ; Levofloxacin ; Norfloxacin ; Pefloxacin ; Quinolones* ; Urinary Tract Infections

AIMTo analyze the response factors of different quinolone antibiotics detected by evaporative light-scattering detector (ELSD).

METHODSThe response factors of five different quinolones (enoxacin, levofloxacin, ciprofloxacin, lomefloxacin and gatifloxacin) detected by ELSD were determined by using a YMC-Pack ODS-AM cloumn (150 mm x 4.6 mm ID, 5 microns) as analytical column and 0.5% triethylamine (adjusting pH 2.5 with trifluoroacetic acid)-acetonitrile (48:12) as mobile phase at a flow rate of 0.6 mL.min-1, the temperature of the drift tube was set at 117 degrees C, and the flow of carrier gas at 3.0 L.min-1. Detector responses (A) and the amount of injection of each substance (m) were fitted to the logarithmic regression: log A = b log m + log a.

RESULTSThe linear regression equation obtained were: enoxacin: Y = 1.0799X + 2.7611, r2 = 0.9996; levofloxacin: Y = 1.0913X + 2.7235, r2 = 0.9997; ciprofloxacin: Y = 1.0828X + 2.7523, r2 = 0.9994; lomefloxacin: Y = 1.0891X + 2.7391, r2 = 0.9993; gatifloxacin: Y = 1.0878X + 2.7392, r2 = 0.9995. The differences between them were negligible.

CONCLUSIONDifferent quinolones can give the same responses with ELSD detection. So, the HPLC-ELSD methods can be applied to the determination of new substances by using another substance as reference.

Chromatography, High Pressure Liquid ; methods ; Ciprofloxacin ; analysis ; Enoxacin ; analysis ; Fluoroquinolones ; analysis ; Levofloxacin ; Light ; Linear Models ; Ofloxacin ; analysis ; Quinolones ; analysis

To study the gyrA mutations of E. coli from clinical specimens, 410 strains were isolated from 1994 to 1997 in Kyungpook National Vniversity hospital. Antimicrobial susceptibility tests, PCR and sequencing of gyrA, and in vitro induction of quinolone resistance were done. The frequency of quinolone resistant E. coli strains increased constantly during 1994 through 1996. Quinolone-resistant strains were more often resistant to unrelated antibiotics than quinolone-susceptible strains (chi-square test, p<0.05). All of the randomly selected 55 quinolone- resist#ant strains were highly resistant to nalidixic acid (NAL) but had low level resistance to fluoroquinolones. All of the 55 quinolone-resistant strains showed an amino acid substitution of Ser -> Leu (TCG -> TIG) at codon 83. In addition, four different types of amino acid substitution affecting codon 87 (Asp) were detected, 1) type I: Asn (GAC -> AAC); 2) type II: Tyr (GAC -> TAC); 3) type III: Oly (GAC -> GGC); 4) type IV: His (GAC -> CAC). The mutation of type IV has not been reported previously in quinolone-resistant E. coli strains. It is thought that the specific amino acid substitution probably affects minimum inhibitory concentrations (MIC) of quinolones because the MICs of ciprofloxacin, norfloxacin, and ofloxacin in type II were significantly higher than those of type I. By in vitro induction, MICs to quinolone-susceptible strains resulted in the increase in the MICs of all quinolones tested by 2- to 2048-fold. The induced mutants by quinolones had amino acid substitutions at codon 83, SerLeu or Asp87Asn, Gly or Tyr. Alteration of Ser83 results in the most effective increase in the MIC of quinolone such as NAL and alterations of Asp87 result in the effective increase of MIC of fluoroquinolone. These results suggest that the continuous use of quinolones might induce the specific amino acid substitution at gyrA.
Amino Acid Substitution ; Anti-Bacterial Agents ; Ciprofloxacin ; Codon ; Escherichia coli* ; Escherichia* ; Fluoroquinolones ; Gyeongsangbuk-do ; Microbial Sensitivity Tests ; Nalidixic Acid ; Norfloxacin ; Ofloxacin ; Polymerase Chain Reaction ; Quinolones

The susceptibilities of 45 clinical isolates of bacteroidis fragilis to cefaclor, ciproflxacin and imipenem were determined by new method, E-test (AB Bidisk, Solna, Sweden) and were compared with those from conventional agar dilution method by using brain heart infusion, Mueller-Hinton and Wilk:..s Chalgren agar plates. And the susceptibility of 60 clinical isolates of bacteroides fragilis group (B. fragilis 45 strains, B. distasonis 6 strains, B. ovatus 5 strains, B. thetaiotaomicron 4 strains) to 5 quinolones (ciprofloxacin, enoxacin, norfloxacin, ofloxacin, pefloxacin) were determined by in vitro agar dilution method. Compared with agar dilution MICs for B. fragilis 45 strains, 90.3% of E-test MICs were within +/- 1 dilution of the agar dilutions, and 98.4% were within 2 dilutions. And there were little effect of different medium bases to determine MICs except Mueller-Hinton agar. On Mueller-Hinton agar, B. fragilis showed have or no growth activity. In vitro susceptibility of B. fragilis group to quinolones, most of the test strains showed resistant patterns to quinolones except ofloxacin and there was little difference of susceptibility patterns between species of B. fragilis group.
Agar* ; Bacteroides fragilis* ; Bacteroides* ; Brain ; Cefaclor ; Enoxacin ; Heart ; Imipenem ; Norfloxacin ; Ofloxacin ; Quinolones

PURPOSE: Reports evaluating diagnosis and cross reactivity of quinolone hypersensitivity have revealed contradictory results. Furthermore, there are no reports investigating the cross-reactivity between gemifloxacin (GFX) and the others. We aimed to detect the usefulness of diagnostic tests of hypersensitivity reactions to quinolones and to evaluate the cross reactivity between different quinolones including the latest quinolone GFX. METHODS: We studied 54 patients (mean age 42.31±10.39 years; 47 female) with 57 hypersensitivity reactions due to different quinolones and 10 nonatopic quinolone tolerable control subjects. A detailed clinical history, skin test (ST), and single-blind placebo-controlled drug provocation test (SBPCDPT), as well as basophil activation test (BAT) and lymphocyte transformation test (LTT) were performed with the culprit and alternative quinolones including ciprofloxacin (CFX), moxifloxacin (MFX), levofloxacin (LFX), ofloxacin (OFX), and GFX. RESULTS: The majority (75.9%) of the patients reported immediate type reactions to various quinolones. The most common culprit drug was CFX (52.6%) and the most common reaction type was urticaria (26.3%). A quarter of the patients (24.1%) reacted to SBPCDPTs, although their STs were negative; while false ST positivity was 3.5% and ST/SBPCDPTs concordance was only 1.8%. Both BAT and LTT were not found useful in quinolone hypersensitivity. Cross-reactivity was primarily observed between LFX and OFX (50.0%), whereas it was the least between MFX and the others, and in GFX hypersensitive patients the degree of cross-reactivity to the other quinolones was 16.7%. CONCLUSIONS: These results suggest that STs, BAT, and LTT are not supportive in the diagnosis of a hypersensitivity reaction to quinolone as well as in the prediction of cross-reactivity. Drug provocation tests (DPTs) are necessary to identify both culprit and alternative quinolones.
Basophils ; Ciprofloxacin ; Diagnosis* ; Diagnostic Tests, Routine* ; Humans ; Hypersensitivity* ; In Vitro Techniques* ; Levofloxacin ; Lymphocyte Activation ; Ofloxacin ; Quinolones* ; Skin Tests ; Urticaria

BACKGROUND: The actual trends in antibiotic use in Korea are difficult to determine because antibiotic usage, which is not covered by insurance or not consumed in all hospitals in Korea, cannot be calculated accurately. Therefore, this study estimated the antibiotic usage indirectly from the data available in the 'Annual Products of Medicine,' which is published by the Korean Pharmaceutical Manufacturers Association. MATERIALS AND METHODS: The data from 'Annual Products of Medicine in 2008' was analyzed. The cost and amounts of antibiotics produced were calculated and compared with previous data. RESULTS: In 2008, the total cost of antibiotics was $ 1.6 billion, and the total amount was 1,140 tons. Since 1993, there has been an upward trend in the total amount of antibiotics produced. In contrast, there has been a downward trend in the proportion of antibiotics among all pharmacological agents produced. In terms of the amount, the production of cephalosporins was highest since 2003, whereas the production of penicillins was highest before 2003. The production of third and fourth generation cephalosporins is increasing, whereas that of first generation cephalosporins is decreasing gradually. Regarding the class of penicillins, the production of beta-lactam/beta-lactamase inhibitor combinations was the highest after 2003, whereas the production of aminopenicillin was the highest before 2003. Compared to 2003, although the amount of quinolones produced in 2008 has decreased by 52.9%, the cost increased by 41.7%. This was attributed to an increase in the production of ciprofloxacin and levofloxacin instead of older quinolones. Since 1993, aminoglycoside, tetracycline, lincosamide and chloramphenicol have been decreasing in both amount and cost. The increase in carbapenems (241.9%), antifungals (128.4%) and antiviral agents (193.2%) in 2008 is remarkable compared to that in 2003. CONCLUSIONS: The production and cost of broader spectrum and more expensive antibiotics are increasing, and is believed to be responsible for the emergence of resistance. Therefore, restriction of these broader spectrum antibiotics, such as carbapenems, is recommended.
Anti-Bacterial Agents ; Antiviral Agents ; Carbapenems ; Cephalosporins ; Chloramphenicol ; Ciprofloxacin ; Insurance ; Korea ; Ofloxacin ; Penicillins ; Quinolones ; Tetracycline