摘要:

Fleroxacin is a new oral and intravenous trifluorinated 4-quinolone, which acts by inhibiting the essential bacterial enzyme DNA gyrase. Fleroxacin exhibits a broad spectrum of action, characterized by pronounced activity against aerobic gram-negative bacteria, but also against gram-positive pathogens such as staphylococci. Fleroxacin is distinguished by its excellent bioavailability, high concentrations in the plasma and other body fluids, good tissue penetration, and a long half-life of 10-12 h, thus allowing once-a-day administration. A single oral dose of 400 mg fleroxacin is effective in uncomplicated cystitis in women, uncomplicated gonococcal infections, bacterial enteritis, and traveler’s diarrhea. A single daily dose of 200 mg administered for 3 days is effective in uncomplicated urinary tract infection (UTI), while longer treatment and higher doses may be required in acute uncomplicated pyelonephritis and complicated UTI. Skin, soft tissue, bone and joint infections, and lower respiratory tract infections including exacerbation of chronic bronchitis and non-pneumococcal pneumonia are further indications for fleroxaci

ISSN:0009-3157    

DOI:10.1159/000239485

出版商:S. Karger AG    

年代:1996

数据来源: Karger

摘要:

A single oral dose of an antimicrobial agent is as effective as a conventional 3-day course for the treatment of uncomplicated lower urinary tract infections. A case history of a young woman with recurrent cystitis is presented to demonstrate this approach to the management of a common clinical problem. The place of antimicrobial prophylaxis is also discussed.

ISSN:0009-3157    

DOI:10.1159/000239487

出版商:S. Karger AG    

年代:1996

数据来源: Karger

摘要:

In this multicenter study conducted in eight European countries, 13,173 pathogens – all isolated from community-acquired infections in 1992 and 1993 – were evaluated for their susceptibility to the following orally active antibiotics: penicillin G, ampicillin, amoxycillin plus clavulanic acid, cefaclor, cefuroxime, cefetamet, doxycycline and erythromycin. Ten centers in Italy, five in Germany, in the Netherlands and Switzerland, four in Greece and Spain, three in Hungary and one in Finland contributed to this study; ready-to-use standardized microtiter panels (Sceptor system, BBL, Heidelberg, Germany) were used throughout all assays. The most frequently encountered species were: Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae and non-typhoid Salmonella spp., Enterobacter cloacae, Streptococcus agalactiae, Haemophilus influenzae, Citrobacter freundii, Staphylococcus pyogenes, Streptococcus pneumoniae, Proteus vulgaris, Moraxella catarrhalis and Shigella spp. The percentage of susceptible isolates was assessed for each of the above-mentioned countries and European-wide with all the data available. For many species, the percentage of resistant isolates did not differ markedly between the countries considered. However, one of the most striking exceptions was the high prevalence of high-level penicillin-G-resistant S. pneumoniae isolates in Hungary and Spain; some of the low-level penicillin-G-resistant strains remained susceptible to cefuroxime, whereas complete cross-resistance occurred for all other β-lactams studied. The high frequency of ampicillin-resistant H. influenzae isolates in Spain deserves mentioning; this could be attributed mainly to the prevalence of a β-lactamase, as the addition of clavulanic acid rendered these strains susceptible to ampicillin. The penicillin compounds exhibited the greatest activity against Gram-positive pathogens, whereas cefetamet was the most active agent against Gram-negative pathogens with a well-balanced spectrum of activity.

ISSN:0009-3157    

DOI:10.1159/000239418

出版商:S. Karger AG    

年代:1996

数据来源: Karger

摘要:

The clinical evaluation of antimicrobial agents for the treatment of urinary tract infections (UTIs) requires clinically useful categorization of patients plus concurrent laboratory diagnosis. Appropriate diagnostics include (1) proper collection techniques, (2) quantitative urine culture, (3) urinalysis to determine pyuria, and (4) radiological, urological and gynecological evaluation. Categorization of patients suffering from UTIs should take into consideration (1)the site of infection, (2) the clinical presentation, (3) the frequency of infections, and (4) the coexistence of complicating factors. UTIs in men and older women are mostly complicated. The characterization of a UTI as complicated or uncomplicated is important since in the former condition, multiresistant nosocomial microorganisms are frequently encountered. Experience with fleroxacin 200 or 400 mg once daily (o.d.) in > 1,000 patients with complicated UTIs in noncomparative and comparative trials with other quinolones and cephalosporins has been very promising, with overall clinical and bacteriological cure rates of 86-95 and 89-95%, respectively. As with other qumolones, relapses and superinfections were mostly attributed to Enterococcus, Staphylococcus and Pseudomonas spp. The reported results make oral o.d. fleroxacin appropriate as an alternative to parenteral antimicrobials or for intravenous-to-oral switch therapy in complicated UTIs.

ISSN:0009-3157    

DOI:10.1159/000239488

出版商:S. Karger AG    

年代:1996

数据来源: Karger

摘要:

Nineteen representative isolates of gentamicin- and methicillin-resistant Staphylococcus aureus (MRSA) were found to comprise three phenotypes; these differed with regard to hydrolysis of nitrocefin and production of staphylococcal enterotoxin A or/and toxic shock syndrome toxin-1. All MRSA isolates produced a capsule and were susceptible to coumermycin, nitrofurantoin, novobiocin, trimethoprim, trimethoprim-sulfamethoxazole, teicoplanin and vancomycin. All MRSA isolates were resistant to co-amoxiclav, ciprofloxacin, clarithromycin, gentamicin, methicillin, norfloxacin, ofloxacin, oxacillin and polymyxin B. The isolates of the three putative phenotypes differed in susceptibility to ampicillin and sulbactam, ce-famandole, chloramphenicol, clindamycin, josamycin and piperacillin/tazobactam. Isolates of phenotype I varied in susceptibility to amikacin, fusidic acid, imipenem, meropenem and netilmicin. Isolates of phenotype II were inhibited, but not killed by doxycycline. Some isolates of phenotype II were resistant to mupirocin. Some recent isolates of phenotype I and the two isolates of phenotype III were resistant to rifampin. Pulsed-field gel electrophoresis of SmaI-restricted genomic DNA of the MRSA isolates revealed phenotype I to consist of three subpopulations, designated la, lb and Ic. The isolates comprising phenotypes II and III proved identical, respectively. Time-kill experiments with fresh defibrinated human blood/broth, using either 1 or 2 μg/ml of teicoplanin and vancomycin, respectively, combined with 1 μg/ml of fusidic acid, 1 μg/ml of netilmicin, 1 μg/ml of rifampin, 8 μg/ml of nitrofurantoin, 8/8 μg/ml of ampicillin and sulbactam, 8/4 μg/ml of co-amoxiclav, 16/2 μg/ml of piperacillin/tazobactam and 1/19 μg/ml of co-trimoxazole, respectively, yielded the following results. Human blood (65% v/v) from 4 donors failed to destroy bacterial inocula(1-2 × 104 CFU/ml, time 0). With few exceptions, the antimicrobial drugs were more active in Mueller-Hinton broth (MHB) than in the presence of blood. Overall, on a weight-for-weight basis, vancomycin was more active than teicoplanin in the presence of human blood, but not invariably so. Indifferent effects were obtained with teicoplanin/vancomycin combined with co-trimoxazole, fusidic acid, netilmicin and rifampin, respectively, against isolates comprising phenotypes II and III. Nitrofurantoin was bactericidal in MHB, but not in the presence of blood. Nitrofurantoin plus teicoplanin yielded an additive effect against 4 of 6 tested MRSA isolates in the presence of blood. Piperacillin/tazobac-tam plus teicoplanin resulted in an additive effect against 5 of 6 MRSA isolates examined in the presence of human blood; however, replacement of teicoplanin by vancomycin resulted in an additive effect against only 1 of the same 6 MRSA isolates tested although vancomycin alone killed 4 of the 6 isolates. Ampicillin plus sulbactam or co-amoxiclav combined with teicoplanin yielded an additive effect against 2 MRSA isolates of phenotype II which failed to hydrolyze nitrocefin.

ISSN:0009-3157    

DOI:10.1159/000239419

出版商:S. Karger AG    

年代:1996

数据来源: Karger

摘要:

In transurethral surgery, there is much controversy about the benefit of antimicrobial prophylaxis. Any urinary tract infection should be treated before proceeding with a transurethral operation. There is growing evidence that antimicrobial prophylaxis is also beneficial in cases with preoperatively sterile urine. A single dose or short-term prophylaxis appears to be sufficient. As newer fluoroquinolones reach very high tissue concentrations, have a suitable antimicrobial spectrum to cover most uropathogens and can be administered orally, these new drugs represent an attractive choice for prophylaxis in transurethral surgery.

ISSN:0009-3157    

DOI:10.1159/000239489

出版商:S. Karger AG    

年代:1996

数据来源: Karger

摘要:

Currently available fluoroquinolones have established their value in the treatment of lower respiratory tract infections due to gram-negative rods and Staphylococcus aureus. The fact that these drugs are absorbed (and well tolerated) when given orally is a major positive feature. The once daily dosage of fleroxacin [400 mg once daily intravenously (i.v.) for 2-4 days followed by oral doses of 400 mg for up to 10 days] was compared with twice daily ciprofloxacin (400 mg twice daily i.v. for 2-4 days followed by oral doses of 2 x 500 mg for up to 10 days) for treatment of inpatients with pneumonia confirmed by clinical signs and chest X ray. To date, 93 evaluable patients have been enrolled in this study. Clinical cure and improvement rates were 73.3% in the fleroxacin group and 79.2% in the ciprofloxacin group. The rate of adverse clinical or laboratory events was similar in both study groups.

ISSN:0009-3157    

DOI:10.1159/000239490

出版商:S. Karger AG    

年代:1996

数据来源: Karger

摘要:

The ability of double and triple combinations of antimicrobials with different mechanisms of action, such as teicoplanin, meropenem, gentamicin and sparfloxacin, to achieve synergisms was investigated in vitro on some moderate-level gentamicin-resistant (MLGR: 8 ≤ MIC ≤ 256 mg/l) and high-level gentamicin-resistant (HLGR: MIC > 500 mg/l) enterococci. On MLGR strains, a constant synergistic effect was achieved by a combination of teicoplanin with gentamicin or with meropenem, while generally addition, sometimes close to synergism, was exhibited by gentamicin-meropenem, gentamicin-sparfloxacin and teicoplanin-sparfloxacin associations. Triple combinations of teicoplanin, meropenem and gentamicin, or teicoplanin, sparfloxacin and gentamicin, always showed a remarkable advantage in terms of synergism over double combinations. On HLGR enterococci, the only double association showing an additive effect, sometimes close to synergism, was teicoplanin plus meropenem, while the triple combination of teicoplanin with gentamicin and meropenem always showed a marked synergistic effect. An effect very close to synergism was also shown by the combination of teicoplanin with sparfloxacin and gentamicin.

ISSN:0009-3157    

DOI:10.1159/000239420

出版商:S. Karger AG    

年代:1996

数据来源: Karger

摘要:

Fluoroquinolones are efficient antimicrobial drugs for the treatment of enteric fever, shigellosis, Escherichia coli diarrhea, cholera, and traveler’s diarrhea. They also play a role in the therapy of yersiniosis, campylobacteriosis, and intestinal salmonellosis. A single dose of quinolones has been effective in the treatment of traveler’s diarrhea and cholera. Uncomplicated typhoid fever was cured by norfloxacin, pefloxacin, and ofloxacin 400 mg twice daily (b.i.d.) for 7-14 days or ciprofloxacin 500 mg b.i.d. for 10 days. A single daily dose of 400 mg fleroxacin for 3 days has been shown to be effective in this indication. A few reports suggest that the newer quinolones can eliminate the carrier state. The efficacy of quinolones in the prophylaxis and treatment of intra-abdominal infections following abdominal surgery requires further investigat

ISSN:0009-3157    

DOI:10.1159/000239491

出版商:S. Karger AG    

年代:1996

数据来源: Karger

摘要:

Two genetically distinct classes of meropenem-low-susceptibility Pseudomonas oaeruginosa PA02152 mutants, which arose spontaneously, were isolated. Two meropenem resistance genes, mpmA and mpmB, were mapped near ilvB/C and proC, respectively, on the P. aeruginosa PAO chromosome. The mpmA was thought to be identical to oprD2 because of the cross-resistance to carbapenems and the association with the loss of the outer membrane protein D2 (OprD2). The mpmB mutation conferred a 4-fold increase in resistance to meropenem, and cross-resistance to various types of antimicrobial agents, e.g. carbenicillin, norfloxacin and chloramphenicol. However, the mpmB mutant was susceptible to imipenem. This mutant still possessed OprD2 and showed increased expression of a 48-kD outer membrane protein, although its profiles of β-lactamase activity and affinities of penicillin-binding proteins for β-lactams were indistinguishable from those of the parent strain. The resistance gene mpmB was considered to be an allele of nalB (or cfxB or oprK) from the results of the transductional analysis. The mutation frequency of mpmA:mpmB was in the ratio of 4:1. The same results were obtained in another clinically isolated P. aeruginosa strain. Meropenem resistance caused by both mpmA and mpmB mutations seemed to be due to the reduction in permeability of antibiotics through the outer membrane. These findings suggest a new pathway for the translocation of meropenem other than that mediated by OprD2 across the outer membrane. Thus, meropenem showed about 4- to 8-fold higher activity than imipenem against OprD2-deficient P. aeruginosa.

ISSN:0009-3157    

DOI:10.1159/000239421

出版商:S. Karger AG    

年代:1996

数据来源: Karger