Urinary excretion and bactericidal activities of a single oral dose of 400 milligrams of fleroxacin versus a single oral dose of 800 milligrams of pefloxacin in healthy volunteers.


:Twelve healthy volunteers participated in this randomized crossover study to compare the concentrations and recovery levels of fleroxacin and pefloxacin in urine and to assess their bactericidal activities against 12 strains of urinary pathogens with different susceptibilities over a wide range of MICs. The volunteers received a single oral dose of 400 mg of fleroxacin or 800 mg of pefloxacin. The mean cumulative renal excretion of unchanged fleroxacin, N-demethyl-fleroxacin, and N-oxide-fleroxacin accounted for 67, 7, and 6% of the total dose, respectively. The total urinary recovery of pefloxacin and the active metabolite norfloxacin was 34%. In the time-kill and the urinary bactericidal titer (UBT) studies, only the subjects' urine not supplemented with broth was used. With most tested organisms and both quinolones it took more than 8 h to achieve a reduction in CFU of 99.9% (3 log units). Overall, there was a good correlation between UBTs and MICs for the strains. Against Escherichia coli ATCC 25922 the median UBTs were similar for both antibiotics and at least 1:8 for 96 h; against the E. coli strain for which the MIC was 0.5 microgram/ml the UBT was at least 1:4 for 48 h. The UBTs of both drugs against Klebsiella pneumoniae were at least 1:16 for 72 h. The UBTs for Staphylococcus aureus (the MIC for which was 16 micrograms/ml) of both antibiotics were low, and in some of the samples, no bactericidal titers were observed. UBTs for Proteus mirabilis of pefloxacin are significantly higher than those of fleroxacin. For Pseudomonas aeruginosa the median UBTs were present for the 24-to-48-h interval. The same is true for Enterococcus faecalis. Against Staphylococcus saprophyticus, UBTs were present for at least 48 h with both quinolones. Overall, a single oral dose of 400 mg of fleroxacin exhibits UBTs comparable to those of 800 mg of pefloxacin. Therefore, it may be expected that half of the dose of fleroxacin gives comparable results in the treatment of urinary tract infections; this should be substantiated in comparative clinical trials.


Naber KG,Theuretzbacher U,Kinzig M,Savov O,Sörgel F




Has Abstract


1998-07-01 00:00:00












  • Distribution of tet(H) among Pasteurella isolates from the United States and Canada.

    abstract::Tetracycline-resistant isolates of Pasteurella multocida and Pasteurella haemolytica obtained from various locations in the United States and Canada were studied to determine the distribution of the tet(H) gene. Of the 31 isolates examined, 25 were found to contain the tet(H) gene. Chromosomal or plasmid DNA obtained ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Hansen LM,Blanchard PC,Hirsh DC

    更新日期:1996-06-01 00:00:00

  • SOS regulation of qnrB expression.

    abstract::In the sequence upstream from qnrB (but not qnrA or qnrS) is a LexA binding site. qnrB was shown to be under SOS control by demonstrating that quinolone susceptibility decreased with increasing temperature in a strain with a recA441(Ts) allele, whereas qnrB expression increased in response to ciprofloxacin or mitomyci...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Wang M,Jacoby GA,Mills DM,Hooper DC

    更新日期:2009-02-01 00:00:00

  • Fluoroquinolone and quinazolinedione activities against wild-type and gyrase mutant strains of Mycobacterium smegmatis.

    abstract::Quinazolinediones (diones) are fluoroquinolone-like inhibitors of bacterial gyrase and DNA topoisomerase IV. To assess activity against mycobacteria, C-8-methoxy dione derivatives were compared with cognate fluoroquinolones by using cultured Mycobacterium smegmatis. Diones exhibited higher MIC values than fluoroquinol...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Malik M,Marks KR,Mustaev A,Zhao X,Chavda K,Kerns RJ,Drlica K

    更新日期:2011-05-01 00:00:00

  • Drug susceptibility testing of anaerobic protozoa.

    abstract::A simple technique for routine, reproducible global surveillance of the drug susceptibility status of the anaerobic protozoa Trichomonas, Entamoeba, and Giardia is described. Data collected using this technique can be readily compared among different laboratories and with previously reported data. The technique employ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Upcroft JA,Upcroft P

    更新日期:2001-06-01 00:00:00

  • Nitric Oxide-Mediated Induction of Dispersal in Pseudomonas aeruginosa Biofilms Is Inhibited by Flavohemoglobin Production and Is Enhanced by Imidazole.

    abstract::The biological signal molecule nitric oxide (NO) was found to induce biofilm dispersal across a range of bacterial species, which led to its consideration for therapeutic strategies to treat biofilms and biofilm-related infections. However, biofilms are often not completely dispersed after exposure to NO. To better un...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Zhu X,Oh HS,Ng YCB,Tang PYP,Barraud N,Rice SA

    更新日期:2018-02-23 00:00:00

  • Differential maintenance of the M184V substitution in the reverse transcriptase of human immunodeficiency virus type 1 by various nucleoside antiretroviral agents in tissue culture.

    abstract::The M184V substitution in human immunodeficiency virus type 1 reverse transcriptase (RT) is rapidly selected in tissue culture following serial passage of wild-type virus in the presence of increasing concentrations of lamivudine (3TC). M184V is also associated with several alterations of RT enzymatic function in vitr...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Petrella M,Oliveira M,Moisi D,Detorio M,Brenner BG,Wainberg MA

    更新日期:2004-11-01 00:00:00

  • Nonnucleoside inhibitors of norovirus RNA polymerase: scaffolds for rational drug design.

    abstract::Norovirus (NoV) is the leading cause of acute gastroenteritis worldwide, causing over 200,000 deaths a year. NoV is nonenveloped, with a single-stranded RNA genome, and is primarily transmitted person to person. The viral RNA-dependent RNA polymerase (RdRp) is critical for the production of genomic and subgenomic RNA ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Eltahla AA,Lim KL,Eden JS,Kelly AG,Mackenzie JM,White PA

    更新日期:2014-06-01 00:00:00

  • Clinical isolate of herpes simplex virus type 2 that induces a thymidine kinase with altered substrate specificity.

    abstract::In vitro and in vivo studies were done on a herpes simplex virus type 2 strain recovered from a patient on acyclovir (ACV) which was ACV resistant but expressed thymidine (dThd) kinase (EC activity. Plaque-purified clones derived from the original clinical sample were heterogeneous with respect to plaque siz...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Ellis MN,Keller PM,Fyfe JA,Martin JL,Rooney JF,Straus SE,Lehrman SN,Barry DW

    更新日期:1987-07-01 00:00:00

  • Therapy of murine aspergillosis with amphotericin B in combination with rifampin of 5-fluorocytosine.

    abstract::Suboptimal doses of amphotericin B in combination with either rifampin or 5-fluorocytosine were better than single-drug therapy in the treatment of disseminated Aspergillus fumigatus infection in mice. Despite the increased effectiveness of combination therapy, none of the therapeutic regimens we used completely eradi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Arroyo J,Medoff G,Kobayashi GS

    更新日期:1977-01-01 00:00:00

  • Synchrotron X-ray fluorescence microscopy of gallium in bladder tissue following gallium maltolate administration during urinary tract infection.

    abstract::A mouse model of cystitis caused by uropathogenic Escherichia coli was used to study the distribution of gallium in bladder tissue following oral administration of gallium maltolate during urinary tract infection. The median concentration of gallium in homogenized bladder tissue from infected mice was 1.93 μg/g after ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Ball KR,Sampieri F,Chirino M,Hamilton DL,Blyth RI,Sham TK,Dowling PM,Thompson J

    更新日期:2013-11-01 00:00:00

  • Reverse transsulfuration and its relationship to thienamycin biosynthesis in Streptomyces cattleya.

    abstract::Cystathionine gamma-lyase (EC was purified from Streptomyces cattleya, an actinomycete which produces the unusual beta-lactam antibiotic thienamycin. The enzyme displays broad substrate specificity and is similar to gamma-lyases purified from other microorganisms. That the gamma-lyase functions in vivo to pro...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Williamson JM,Meyer R,Inamine E

    更新日期:1985-10-01 00:00:00

  • Total extraction of aminoglycosides from guinea pig and bullfrog tissues with sodium hydroxide or trichloroacetic acid.

    abstract::In most experiments when aminoglycoside antibiotic (AG) tissue levels are measured, the AG is extracted into buffered media. The data from this study reveal that buffer extraction results in only partial recovery of AG from tissues and that total recovery can be obtained after NaOH or trichloroacetic acid treatment. T...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Fox KE

    更新日期:1989-04-01 00:00:00

  • Comparison of the in vitro activities of Bay 12-8039, a new quinolone, and other antimicrobials against clinically important anaerobes.

    abstract::Bay 12-8039, a new 8-methoxy quinolone, was compared with other agents for activity against clinically relevant anaerobes. Bay 12-8039 inhibited 91 and 96% of the 410 test isolates at 2 and 4 micrograms/ml, respectively. Bay 12-8039 had activity comparable to that metronidazole and overall was at least 16-fold more ac...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Aldridge KE,Ashcraft DS

    更新日期:1997-03-01 00:00:00

  • Lipid segregation explains selective toxicity of a series of fragments derived from the human cathelicidin LL-37.

    abstract::The only human cathelicidin, the 37-residue peptide LL-37, exhibits antimicrobial activity against both gram-positive and gram-negative bacteria. We studied the ability of several fragments of LL-37, exhibiting different antimicrobial activities, to interact with membranes whose compositions mimic the cytoplasmic memb...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Epand RF,Wang G,Berno B,Epand RM

    更新日期:2009-09-01 00:00:00

  • High-level tetracycline resistance in Neisseria gonorrhoeae is result of acquisition of streptococcal tetM determinant.

    abstract::Recently, strains of Neisseria gonorrhoeae have been isolated which are highly resistant to tetracycline (MICs of 16 to 64 micrograms/ml). This resistance was due to the acquisition of the resistance determinant tetM, a transposon-borne determinant initially found in the genus Streptococcus and more recently in Mycopl...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Morse SA,Johnson SR,Biddle JW,Roberts MC

    更新日期:1986-11-01 00:00:00

  • Effect of amphotericin B and rifampin against Coccidioides immitis in vitro and in vivo.

    abstract::Amphotericin B, the principal drug used for treating systemic mycoses, possesses undesirable toxic properties. The ability of this antibiotic to potentiate antifungal activity of other compounds suggests that lower doses of amphotericin B could be used in combination with a second drug without loss of therapeutic effi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Huppert M,Pappagianis D,Sun SH,Gleason-Jordan I,Collins MS,Vukovich KR

    更新日期:1976-03-01 00:00:00

  • Pharmacokinetics and safety of a new parenteral carbapenem antibiotic, biapenem (L-627), in elderly subjects.

    abstract::The pharmacokinetics and tolerability of a new parenteral carbapenem antibiotic, biapenem (L-627), were studied in healthy elderly volunteers aged 65 to 74 years (71.6 +/- 2.7 years [mean +/- standard deviation], n = 5; group B) and > or = 75 years (77.8 +/- 1.9 years, n = 5; group C), following single intravenous dos...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Kozawa O,Uematsu T,Matsuno H,Niwa M,Takiguchi Y,Matsumoto S,Minamoto M,Niida Y,Yokokawa M,Nagashima S,Kanamaru M

    更新日期:1998-06-01 00:00:00

  • Susceptibility of gram-positive cocci to various antibiotics, including cefotaxime, moxalactam, and N-formimidoyl thienamycin.

    abstract::The activities of cefotaxime, moxalactam, MK 0787 (N-formimidoyl thienamycin), ampicillin, oxacillin, vancomycin, and clindamycin were compared against gram-positive cocci. MK 0787 was the most active and moxalactam was the least active of these drugs, except against methicillin-resistant Staphylococcus aureus, where ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Cherubin CE,Corrado ML,Sierra MF,Gombert ME,Shulman M

    更新日期:1981-10-01 00:00:00

  • Antimicrobial susceptibility patterns of Streptococcus pneumoniae.

    abstract::Fifty clinical isolates of Streptococcus pneumoniae received by the Streptococcus Laboratory of the Center for Disease Control from August 1976 through March 1977 and 50 pneumococcal strains retrieved from 13- to 16-year storage (originally isolated October 1961 through December 1964) were tested for susceptibility to...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Cooksey RC,Facklam RR,Thornsberry C

    更新日期:1978-04-01 00:00:00

  • Targeting the parasite's DNA with methyltriazenyl purine analogs is a safe, selective, and efficacious antitrypanosomal strategy.

    abstract::The human and veterinary disease complex known as African trypanosomiasis continues to inflict significant global morbidity, mortality, and economic hardship. Drug resistance and toxic side effects of old drugs call for novel and unorthodox strategies for new and safe treatment options. We designed methyltriazenyl pur...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Rodenko B,Wanner MJ,Alkhaldi AA,Ebiloma GU,Barnes RL,Kaiser M,Brun R,McCulloch R,Koomen GJ,de Koning HP

    更新日期:2015-11-01 00:00:00

  • Mutations in ponA, the gene encoding penicillin-binding protein 1, and a novel locus, penC, are required for high-level chromosomally mediated penicillin resistance in Neisseria gonorrhoeae.

    abstract::Chromosomally mediated penicillin resistance in Neisseria gonorrhoeae occurs in part through alterations in penicillin-binding proteins (PBPs) and a decrease in outer membrane permeability. However, the genetic and molecular mechanisms of transformation of a penicillin-susceptible strain of N. gonorrhoeae to high-leve...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Ropp PA,Hu M,Olesky M,Nicholas RA

    更新日期:2002-03-01 00:00:00

  • Identification of the coumermycin A(1) biosynthetic gene cluster of Streptomyces rishiriensis DSM 40489.

    abstract::The biosynthetic gene cluster of the aminocoumarin antibiotic coumermycin A(1) was cloned by screening of a cosmid library of Streptomyces rishiriensis DSM 40489 with heterologous probes from a dTDP-glucose 4,6-dehydratase gene, involved in deoxysugar biosynthesis, and from the aminocoumarin resistance gyrase gene gyr...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Wang ZX,Li SM,Heide L

    更新日期:2000-11-01 00:00:00

  • Synergistic antiviral activities of oligonucleoside methylphosphonates complementary to herpes simplex virus type 1 immediate-early mRNAs 4, 5, and 1.

    abstract::An oligonucleoside methylphosphonate (ONMP) complementary to the splice acceptor site of immediate-early (IE) pre-mRNAs 4 and 5 (IE4,5SA) inhibits herpes simplex virus type 1 (HSV-1) growth in vitro and in infected animals. The antiviral effect appears to be due to inhibition of IE pre-mRNA 4 and 5 splicing and/or IE4...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Kulka M,Smith CC,Levis J,Fishelevich R,Hunter JC,Cushman CD,Miller PS,Ts'o PO,Aurelian L

    更新日期:1994-04-01 00:00:00

  • Pharmacodynamics of Ceftazidime and Avibactam in Neutropenic Mice with Thigh or Lung Infection.

    abstract::Avibactam is a new non-β-lactam β-lactamase inhibitor that shows promising restoration of ceftazidime activity against microorganisms producing Ambler class A extended-spectrum β-lactamases (ESBLs) and carbapenemases such as KPCs, class C β-lactamases (AmpC), and some class D enzymes. To determine optimal dosing combi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Berkhout J,Melchers MJ,van Mil AC,Seyedmousavi S,Lagarde CM,Schuck VJ,Nichols WW,Mouton JW

    更新日期:2015-11-02 00:00:00

  • Serum aminoglycoside assay by enzyme-mediated immunoassay (EMIT): correlation with radioimmunoassay, microbiological assays.

    abstract::Enzyme-mediated immunoassay (EMIT) serum aminoglycoside assay results were accurate and precise and correlated well with radioimmunoassay, fluoroimmunoassay, and acetyltransferase and microbiological assay determinations. ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: White LO,Scammell LM,Reeves DS

    更新日期:1981-06-01 00:00:00

  • Characterization of Tn6238 with a new allele of aac(6')-Ib-cr.

    abstract::Here, we report that the genetic structure of Tn1331 remained conserved in Argentina from 1989 to 2013 (72 of 73 isolates), with the exception being the plasmid-borne Tn1331-like transposon Tn6238 containing a new aac(6')-Ib-cr allele recovered from a colistin-resistant Klebsiella pneumoniae clinical isolate. A bioinf...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Quiroga MP,Orman B,Errecalde L,Kaufman S,Centrón D

    更新日期:2015-05-01 00:00:00

  • Rapid, modified Kirby-Bauer susceptibility test with single, high-concentration antimicrobial disks.

    abstract::A rapid (6-7 hr), modified Kirby-Bauer disk-susceptibility method, by which derivatives of tetrazolium dyes are used to enhance delineation between areas of growth and zones of inhibition, has been developed. Inoculated petri plates, prepared by the Kirby-Bauer method, were sprayed, after 6 to 7 hr of incubation (37 C...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Boyle VJ,Fancher ME,Ross RW Jr

    更新日期:1973-03-01 00:00:00

  • Susceptibility of Plasmodium falciparum to a combination of thymidine and ICI D1694, a quinazoline antifolate directed at thymidylate synthase.

    abstract::Unlike mammalian cells, malarial parasites lack the enzymes to salvage preformed pyrimidines. For this reason, a combination of a thymidylate synthase inhibitor and the nucleoside thymidine should provide selective antimalarial activity even in the absence of any known active site differences between malarial and mamm...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Rathod PK,Reshmi S

    更新日期:1994-03-01 00:00:00

  • Colicinogeny of Escherichia coli MRE 600.

    abstract::Escherichia coli MRE 600 is a colicinogenic bacterium. Its colicinogenic activity may be ascribed mostly to colicin E1, although it produces a small amount of another, as yet unidentified, colicin. ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Salaj-Smic E

    更新日期:1978-11-01 00:00:00

  • In vivo pharmacodynamic profile of tigecycline against phenotypically diverse Escherichia coli and Klebsiella pneumoniae isolates.

    abstract::Tigecycline is a glycylcycline with activity against Enterobacteriaceae, including multidrug-resistant isolates of Klebsiella pneumoniae and Escherichia coli producing extended-spectrum beta-lactamase (ESBL) and carbapenemases. Herein, we used an in vivo murine thigh model to characterize the pharmacodynamic profile o...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章


    authors: Nicasio AM,Crandon JL,Nicolau DP

    更新日期:2009-07-01 00:00:00