摘要:

A total of 5 healthy volunteers were enrolled in a crossover study on the dose dependency and the effect of probenecid on pharmacokinetics of DQ-2556. They were administered intravenously 0.5 and 1.0 g of DQ-2556 , and 1.0 g of DQ-2556 with oral administration of probenecid. The linearity in pharmacokinetics of DQ-2556 was confirmed up to the dose of 1.0 g. In the case of 1.0 g of DQ-2556 with probenecid treatment, the area under the serum concentration-time curve was larger, and total and renal clearances were less than those in the case of 1.0 g of DQ-2556 alone (by approximately 15% for each parameter, p < 0.01). These results demonstrated that DQ-2556 is secreted in the renal tubule, although it is excreted mainly by the glomerular filtration.

ISSN:0009-3157    

DOI:10.1159/000239029

出版商:S. Karger AG    

年代:1992

数据来源: Karger

摘要:

BAY Y3118, 1-cyclopropyl-7-(2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-8-chloro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid hydrochloride, is a new fluoroquinolone with antibacterial activity against an expanded spectrum of species including Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis, Enterococcus faecium, Streptococcus pneumoniae, Streptococcus pyogenes, and also anaerobes such as Bacteroides fragilis and Clostridium perfringens. MIC90s for S. aureus, S. epidermidis, E. faecalis, and S. pneumoniae clinical isolates were 0.125, 0.25, 0.125 and 0.25 μg/ml, respectively. Against methicillin- and/or quinolone-resistant S. aureus, MIC50 levels of BAY Y3118 were 10- to 100-fold lower than those of tosufloxacin, sparfloxacin, or ciprofloxacin. The potency of BAY Y3118 against all members of the Enterobacteriaceae generally was equal to or 2-fold greater than that of ciprofloxacin or tosufloxacin. BAY Y3118 was also highly active against Haemophilus influenzae, Moraxella catarrhalis, Acinetobacter spp. and Pseudomonas aeruginosa. Increasing inoculum concentrations had a minimal effect on MIC determinations. The drug was determined to be bactericidal based upon reference MBCs and time-kill curves. From the results presented here, it was concluded that this new compound surpasses other known 4-qui-nolones both in spectrum and activity and that its further evaluation by in vitro, in vivo, and clinical studies seems warranted

ISSN:0009-3157    

DOI:10.1159/000239031

出版商:S. Karger AG    

年代:1992

数据来源: Karger

摘要:

This investigation used the postantibiotic effect (PAE) and killing curves to examine the antimicrobial activity of subinhibitory (1/8 ×, 1/4 × and 1/2 × MIC) and inhibitory (1 × MIC) concentrations of ciprofloxacin against mucoid (M) and non-mucoid (NM) urinary isolates of Pseudomonas aeruginosa. Subinhibitory concentrations (1/8 ×, 1/4 × and 1/2 × MIC) of ciprofloxacin produced PAEs with no difference between M and NM strains. For NM strains, those with low MICs (≤1.0 mg/l) to ciprofloxacin produced significantly longer PAEs than isolates with high MICs ( > 1 mg/l). Killing curve studies demonstrated that subinhibitory concentrations of ciprofloxacin produce little effect (1/8 × MIC) or stasis (1/4 × and 1/2 × MIC) of growth for several hours. Only 1 × MIC was bactericidal for several strains. At 1/2 × and 1 × MIC, bacterial inhibition was greater against NM versus M isolates. The M phenotype of P. aeruginosa reduces killling by ciprofloxacin but not the PAE.

ISSN:0009-3157    

DOI:10.1159/000239032

出版商:S. Karger AG    

年代:1992

数据来源: Karger

摘要:

In vitro antibacterial activity of 429 clinical isolates of gram-positive cocci was tested against citreamicin-alpha (LL-E 19085-alpha) by the agar dilution method. The microorganisms consisted of 313 isolates of staphylococci and 116 strains of streptococci. In vitro activity of citreamicin-alpha was compared with ampicillin, augmentin, cephalothin, erythromycin and vancomycin. MICs of citreamicin-alpha for staphylococci ranged between 0.12-4.0 μg/ml and 0.03-0.12 μg/ml for Streptococcus pyogenes. Enterococci, however, were relatively more resistant, requiring 2.0 μg/ml of this drug to inhibit 64% of the 62 isolates tested. In vitro activity of this antibacterial agent was far superior to that of ampicillin, augmentin, cephalothin and erythromycin, but equal to or slightly inferior to that of vancomyc

ISSN:0009-3157    

DOI:10.1159/000239033

出版商:S. Karger AG    

年代:1992

数据来源: Karger

摘要:

Escherichia coli strains resistant to ampicillin/sulbactam from hospitals in 4 different geographic locations were examined with respect to type and amount of β-lactamase produced. A total of 5 strains was examined from each region. The isoelectric points of all of the involved β-lactamases were 5.4, corresponding to TEM-1. Km and Vmax 6,500 bp) as the susceptible isolates. In transformation experiments, both the resistance and the degree of resistance appeared to have been transferable by plasmids. The mechanism for resistance is likely to be a baseline overproduction of TEM-1 β-lactamase due to either an alteration in the control of gene expression or simply to an increase in the number of copies of the β-lactamase gene in the pla

ISSN:0009-3157    

DOI:10.1159/000239034

出版商:S. Karger AG    

年代:1992

数据来源: Karger

摘要:

The effects of netilmicin exposure on two aminoglycoside (AMG)-resistant and two AMG-susceptible Enterobacter cloacae isolates were studied. It was found that 1 h incubation of bacterial suspensions with netilmicin at 16 mg/l reduces the amounts of lipopolysaccharides present on the bacterial surface. Also, netilmicin pretreatment increased both the susceptibility to normal human serum and the adhesion to human epithelial cells of all four E. cloacae strains examined.

ISSN:0009-3157    

DOI:10.1159/000239035

出版商:S. Karger AG    

年代:1992

数据来源: Karger

摘要:

Chlorpromazine (CPZ) is one of several phenothiazines known to have antimicrobial properties. It can inhibit mycobacteria, and was reported in the early literature to improve tuberculosis clinically. CPZ was tested here for its ability to inhibit the replication of Mycobacterium tuberculosis and Mycobacterium avium in cultured normal human macrophages, as determined by counts of viable bacteria at 0,4, and 7 days after bacterial infection of the macrophages. CPZ inhibited the intracellular bacteria at a concentration range of 0.23-3.6 μg/ml, and was more effective intracellularly than extracellularly. It was further tested for its ability to cooperate with isoniazid, streptomycin, pyrazinamide, rifampin, rifabutin, penicillin and ethambutol (EMB) against intramacrophage M. tuberculosis and M. avium. CPZ enhanced the effectiveness of most of the drugs tested against intracellular mycobacteria. However, the combination of CPZ and EMB did not result in augmented antimycobacterial activity

ISSN:0009-3157    

DOI:10.1159/000239036

出版商:S. Karger AG    

年代:1992

数据来源: Karger

摘要:

Two hundred and eighty-four febrile episodes in immunocompromised patients were treated with ceftriaxone alone or in combination with amikacin. In the ceftriaxone-treated group, 60 out of 143 febrile episodes were microbiologically documented, while in the group receiving the combination therapy, there were 32 out of 140 (p = 0.0007). Gram-positive microorganisms were more common than gram-negative ones, accounting for 59 of the 101 isolated bacteria. The ceftriaxone regimen appeared to have a response rate comparable to the combination regimen (73.91 vs. 78.88%). Superinfections occurred under both regimens.

ISSN:0009-3157    

DOI:10.1159/000239037

出版商:S. Karger AG    

年代:1992

数据来源: Karger

摘要:

We studied the effect of subinhibitory concentrations of cefuroxime on the capacity of Haemophilus influenzae to adhere to buccal epithelial cells (BEC). Two encapsulated strains (serotype b) and two nonencapsulated, nontypable strains were studied. All four strains adhered strongly to BEC, with indices (mean number of bacteria adhering to a single BEC) ranging from 19 to 48. Subinhibitory concentrations of cefuroxime (serial dilutions from MIC/2 to MIC/32) were added to cultures in tryptic soy broth and their effect on adherence was tested after 18 h incubation at 37°C. Adherence was diminished by more than 50% by concentrations of cefuroxime ranging from MIC/2 to MIC/8 and varied according to the strain studied. These results show that the adherence of H. influenzae to BEC is inhibited by subinhibitory concentrations of cefuroxime

ISSN:0009-3157    

DOI:10.1159/000239038

出版商:S. Karger AG    

年代:1992

数据来源: Karger

摘要:

The ability of flurithromycin and erythromycin to enter human polymorphonuclear phagocytes were studied and compared by a velocity centrifugation gradient technique. Both macrolides were markedly concentrated by human cells and attained cellular to extracellular concentration ratios (C/E) ≥ 10. The incorporation was rapid and essentially complete after 60 min incubation. When PMNs were pretreated with formaldehyde, or incubated at low temperatures (4-25°C) or at low pH, the transport ratios of both molecules were reduced. Sodium fluoride and 2,4-dinitrophenol, which decreased erythromycin uptake, did not affect flurithromycin penetration. Perturbation of cell membrane by phorbol myristate acetate, but not by formyl methionyl leucyl peptide, affected C/E ratios of both antibiotics. The addition of amino acids or nucleosides did not influence their transfer into PM

ISSN:0009-3157    

DOI:10.1159/000239039

出版商:S. Karger AG    

年代:1992

数据来源: Karger