摘要:

The concentrations of clarithromycin after a single oral dose of 500 mg were determined in serum and saliva of ten healthy adult volunteers. After 2 h, the levels were 4.04 ± 1.14 (SD) mg/l in serum and 2.72 ± 0.87 mg/l in saliva. After 7 h these values were 1.98 ± 0.65 and 1.21 ± 0.34 mg/l, respectively, and at the end of the dosing interval of 12 h, 0.95 ± 0.38 and 0.73 ± 0.35 mg/l, respectively. In comparison, amoxicillin (a 750-mg single dose) showed a much faster decline of serum levels and was virtually undetectable in s

ISSN:0009-3157    

DOI:10.1159/000239139

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

The pharmacokinetics of fosfomycin trometamol has been assessed in 12 healthy volunteers given oral doses of 2, 3, and 4 g of fosfomycin and 3 g intravenously of fosfomycin as fosfomycin sodium, all in the fasting state. The assay was microbiological (Proteus mirabilis ATCC 21100). There was a gradual rise in both peak serum concentrations and total area under the curve by rising oral doses, from 16.0 mg/l and 106.7 mg x h/1, after 2 g to 30.9 mg/l and 189.7 mg x h/1 after 4 g respectively. The serum half-life was 4 h after the oral doses and 2.1 h after the intravenous dose. After the oral doses, the amounts excreted in urine in the active form ranged from 36 to 40% compared to 93% after the intravenous dose. The bioavailability was slightly below 40%. Concentrations in urine covers the usual urinary tract pathogens after oral doses of 2, 3, and 4 g.

ISSN:0009-3157    

DOI:10.1159/000239140

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

The in vitro inhibitory and bactericidal activities of daptomycin and reference antibiotics were determined by serial macro-broth dilution for 23 gentamicin-susceptible (MIC: < 2,000 mg/l) and 21 high-level-gentamicin-resistant (HLGR) Enterococcus faecalis, Enterococcus faecium, and Enterococcus avium isolates. The activities of daptomycin, vancomycin, and teicoplanin were independent of the gentamicin susceptibility profile and species tested. For all the isolates, the inhibitory activity of daptomycin (MIC90:2 mg/l) was comparable to vancomycin (MIC90:2 mg/l), but less than that of teicoplanin (MIC90:0.5 mg/l). Daptomycin demonstrated excellent bactericidal activity against all enterococci tested (MBC90 64 mg/l. By time-kill curves, the combination of daptomycin plus ampicillin demonstrated synergistic bactericidal activity against gentamicin-susceptible and HLGR E. faecalis. Daptomycin, singly and in combination, may be useful in treating enterococcal infections, including those caused by HLGR microorganisms.

ISSN:0009-3157    

DOI:10.1159/000239141

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

The antimicrobial activity of the new fluoroquinolone rufloxacin (MF 934) was evaluated by a standardized agar dilution method against recent clinical isolates of Salmonella typhi (67 strains) and Brucella melitensis (108 isolates). The results were compared with 5 other commercially available or investigational fluoroquinolones. All the isolates of S. typhi were inhibited by 1.0 mg/l of rufloxacin as compared to 4-8 mg/l for B. melitensis. Minimum inhibitory concentrations of rufloxacin against both S. typhi and B. melitensis were 4-16 times higher than those of other fluoroquinolones.

ISSN:0009-3157    

DOI:10.1159/000239142

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

In this study, the antimicrobial activity of several new antibiotics was evaluated using microdilution antimicrobial susceptibility testing against 220 clinically significant isolates obtained from a community hospital. The following antibiotics were studied: loracarbef, cefixime, cefpirome, desacetylcefotaxime, cefpodoxime, cefmetazole, cefepime, cefprozil and fleroxacin. The synergy of two particular drug combinations was evaluated using cefpirome/desacetylcefotaxime and cefpodoxime/ desacetylcefotaxime. Cefpirome was clearly the most active antibiotic: 88% of the isolates tested were found to be susceptible. Specifically, this included 89% of enterococci, 84% of Pseudomonas aeruginosa, and 33% of Pseudomonas cepacia. All of the antibiotics tested demonstrated excellent activity against isolates of Escherichia coli and Klebsiella, Proteus and Salmonella species. For the other antimicrobials, 57, 50, 64, 65, 76, 74, and 64% of the isolates were sensitive to loracarbef, cefixime, cefmetazole, cefprozil, fleroxacin, desacetylcefotaxime, and cefpodoxime, respectively. Among the gram-positive species, 88 and 92.5% of the isolates were sensitive to cefprozil and cefpirome, respectively. Cefepime and fleroxacin demonstrated the highest gram-negative activity with 85 and 89%, respectively, of the isolates being sensitive. The results of this study highlighted cefepime and cefpirome, which showed high overall in vitro activity against 79 and 88%, respectively, of the isolates tested.

ISSN:0009-3157    

DOI:10.1159/000239143

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

Taurolidine at ≤1,250 ug/ml killed all 37 isolates of multiple-antibiotic-resistant Staphylococcus aureus (n = 9), Enterococcus faecium (n = 17), and Enterobacteriaceae (n = 11). Time-kill experiments disclosed that bovine serum (65% v/v) only marginally retarded the bactericidal activity of 2,000 and 1,000 μg/ml of taurolidine against the various strains. Taurolidine at 2,000 μg/ml did not antagonize the bactericidal activity of 50% (v/v) fresh human serum against promptly and delayed serum-sensitive test strains of Escherichia coli and Serratia marcescens. In the presence of 65% (v/v) of fresh defibrinated human blood from two donors, however, the bactericidal activity of this antimicrobial compound was delayed, i.e., manifested only following extended (overnight) incubation, against staphylococcal and enterococcal isolates, though less so in the case of Enterobacteriaceae. Taurolidine at 2,000 μg/ml killed ingested, i.e., intraphagocytic bacteria of human-serum-resistant S. marcescens strains CDC 06 :H3 and P 016

ISSN:0009-3157    

DOI:10.1159/000239144

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

While ceftizoxime given as a single intramuscular shot cures uncomplicated gonorrhoea in almost every case, its efficacy against Treponema pallidum in cases of concomitant incubating syphilis is less clear. To analyse this question, the rabbit orchitis model was used. After initial experiments defining appropriate inocula and doses, ceftizoxime was compared to penicillin G with its well-known activity against the organism in vitro and in vivo. According to the final experiment, ceftizoxime applied in doses corresponding to the ones used in humans for uncomplicated gonorrhoea cures rabbit orchitis due to T. pallidum about as effectively as penicillin. Hence there seems to be no need to refrain from using the third-generation cephalosporin ceftizoxime to cure gonorrhoea for fear of masking concomitant syphilis.

ISSN:0009-3157    

DOI:10.1159/000239145

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

Although many complications may arise with the use of central venous catheters, catheter-related bacteremia is considered to be the most serious complication. Microflora on the patient’s skin (coagulase-negative staphylococci, Staphylococcus aureus) is thought to represent the major source of microorganisms causing catheter-related infections. Gram-negative rods are increasingly observed as causative agents. We therefore performed an in vitro study to elucidate the pathogenesis of polymer-associated infections caused by enterobacteriaceae and nonfermenters and to study the resistance of polymer surface-grown gram-negative rods against antibiotics. Using a modification of the semiquantitative method for culturing vascular cannulas on solid media described by Maki et al., we studied the adherence of various gram-negative rods to 1-cm segments of silastic catheters, a material used for Port-A-Cath-systems. Organisms were obtained from the American Type Culture Collection (Escherichia coli, Klebsiella pneumoniae, Serratia marcescens, Pseudomonas aeruginosa, Enterobacter cloacae). All organisms but Klebsiella showed extensive irreversible adherence. Production of an extracellular slime substance was observed only with anti-microbially treated Pseudomonas. After ‘infection’, the silastic catheter segments were treated with various antimicrobial agents. The following antibiotics were used either individually or in combination: cefotaxime, ciprofloxacin, imipenem, fosfomycin and gentamicin. Despite the fact that the antibiotic concentrations used were many times greater than the respective MICs of the various antibiotics, none of the antibiotics tested succeeded in eliminating the organisms. E. coli was found to be the most susceptible organism. These in vitro data substantiate our clinical impression that it is hardly possible to successfully eliminate the colonization of central venous catheters with gram-negative rods by using the antimicrobial agents employed

ISSN:0009-3157    

DOI:10.1159/000239146

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

The in vivo activity of ceftriaxone was examined in an experimentally induced subcutaneous infection involving Bacteroides fragilis and Escherichia coli. Mice were challenged with 1 of 10 strains of B. fragilis or E. coli, or a dual combination of the two species. The efficacy was measured by a reduction in the count of viable organisms when antimicrobial treatment was initiated 1 h after challenge and continued for 5 days. Ceftriaxone exhibited impressive activity against E. coli but showed poor in vivo activity versus B. fragilis. The antimicrobial activity of ceftriaxone was influenced by the microbial interaction in our dual-isolate model. Pharmacokinetic studies showed that ceftriaxone penetrated into abscesses and achieved peak levels of about 40% of the peak serum levels. However, in abscesses infected with B. fragilis nearly all biological activity of ceftriaxone was lost.

ISSN:0009-3157    

DOI:10.1159/000239147

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

Forty-one patients with advanced renal cell cancer started treatment with recombinant alpha-interferon intramuscularly, beginning at a dose of 5 x 106 U x 3/week, progressively increasing doses every week, from 5 x 106 U x 3/week to 10 x 106 U x 3/ week, to the highest dose of 15 x 106 U x 3/week. No complete response was achieved, partial response was achieved in 6 (13%) patients with a median duration of 45.2 (13-134) weeks. The majority of side effects from interferon treatment evaluated according to WHO classification were seen during the first 2 months and they were fever (after interferon administration) in 95% patients, chills (51%), flu like syndrome (65%), fatigue (87%), anorexia (80%), worsening in performance status (56%), nausea and vomiting (19%), weight loss ( > 10% during therapy) (26%), leukopenia (14%), anemia (75%), neurological symptoms (43%), psychological symptoms (19%) and dyspnea (9%). The results are similar to other studies and toxicity was only moderate.

ISSN:0009-3157    

DOI:10.1159/000239148

出版商:S. Karger AG    

年代:1993

数据来源: Karger