摘要:

To predict the clinical efficacy of a new antibiotic in uncomplicated gonorrhea, data pertinent to its pharmacokinetics in man are needed. Before starting clinical trials on cefotiam and cefmenoxime, 1 g of each antibiotic was administered intramuscularly as single dose to 5 healthy volunteers. Both blood and skin blister fluid samples (obtained by suction and cantharides blistering) were repeatedly taken. Peak plasma levels amounted on average to 24.8 and 48.2 μg/ml, respectively. 6 h after dose still average plasma concentrations of 3.4 and 6.52 μg/ml were found. Suction blister fluid levels essentially paralleled plasma levels, whereas cantharides blister fluid levels increased and decreased more slowly than plasma levels. Cefotiam penetrated more readily into suction blister fluid than cefmenoxime as obtained from area ratios. Thus, the chosen dosage regimens considered apt for gonorrhea led to high initial as well as long-standing drug levels. And this does not only hold true for the plasma. Facing their good in vitro activity on Neisseria gonorrhoeae, cefotiam and cefmenoxime well deserve further studies in this field including clinical trial

ISSN:0009-3157    

DOI:10.1159/000238281

出版商:S. Karger AG    

年代:1984

数据来源: Karger

摘要:

We used a new micromethod, an application of a previously published high-performance liquid chromatography assay, to investigate trimethoprim (TMP) pharmacokinetics in children. The subjects were 5 girls who were treated for urinary tract infection with a TMP suspension, 6 mg/kg/day, twice daily for 10 days. Elimination studies were done after the last dose. The girls were 1.08–9.71 years old. 3 healthy adult males, aged 26.35–37.31 served as controls. The half-life (t1/2) of TMP in the children was 3.0–5.5 versus 9.3–13.6 h in the adults. The volume of distribution (Vd) was 0.7–1.1 l/kg in the children and 0.5–0.9 l/kg in the adults. Plasma clearance (Clp) was 2.1–2.8 ml/min/kg for the children. The adults had a smaller Clp of 0.4–1.2 ml/min/kg. From this and previous studies we conclude that the t1/2 of TMP is much shorter in children

ISSN:0009-3157    

DOI:10.1159/000238282

出版商:S. Karger AG    

年代:1984

数据来源: Karger

摘要:

Pharmacokinetic studies were conducted with norfloxacin administered by the oral and subcutaneous routes to mice and rats, and by the oral route to rhesus monkeys. The compound was moderately well absorbed following oral dosing in these animal species. Serum levels in monkeys ranged from 1.0 to 2.35 μg/ml after an oral drug dose of 25 mg/kg of animal body weight and were similar to those in mice. Serum half-life of norfloxacin in rodents and monkeys was similar to that in humans. Concentrations of norfloxacin in tissues of mice, rats and monkeys were greater than those in serum suggesting a large volume of distribution for the drug

ISSN:0009-3157    

DOI:10.1159/000238283

出版商:S. Karger AG    

年代:1984

数据来源: Karger

摘要:

The diffusion of metioprim (MTP), tetroxoprim (TXP) and sulphadiazine (SDZ) in cerebrospinal fluid (CSF), following single intravenous doses and continuous infusions, was studied in dogs. The drugs penetrated well into the CSF of animals with and without experimental Staphylococcus aureus meningitis. In dogs with healthy meninges, the CSF bioavailability – expressed as the ratio of CSF/plasma area under the curve 0–5-hour values – following continuous infusion was determined to be 86.7% for MTP, 58.2% for TXP and 38.8% for SDZ. In infected animals, CSF availability following continuous infusion increases slightly to ratios of 96% (MTP), 70% (TXP) and 50% (SDZ). For all drugs, the concentrations reached in CSF were above the minimum inhibition concentrations for the majority of Enterobacteriaceae, indicating their potential value in the treatment of gram-negative bacillary menin

ISSN:0009-3157    

DOI:10.1159/000238284

出版商:S. Karger AG    

年代:1984

数据来源: Karger

摘要:

24 patients received an intravenous 5-min bolus injection of 2 g cefotetan at various times prior to abdominal or vaginal hysterectomy. Cefotetan concentrations in salpinges were significantly higher than in myometrium and endometrium. Tissue concentrations of 16 μg/g could be attained for at least 5 h. At this concentration, 90% of most aerobic and anaerobic bacteria causing genital tract infections are inhibited

ISSN:0009-3157    

DOI:10.1159/000238285

出版商:S. Karger AG    

年代:1984

数据来源: Karger

摘要:

Two multiple drug resistant Enterobacter cloacae isolates (Nos. 460 and 493) varied phenotypically in bacteriocin susceptibility in the absence of significant·antigen variation. Both isolates were susceptible to chloramphenicol, nitrofurantoin, polymyxin B, nalidixic acid, norfloxacin, and enoxacin only. One isolate carried a non-conjugative resistance (R) plasmid, whereas the other isolate contained a conjugative, ‘curable’ R plasmid and a cryptic plasmid. Both wild-type isolates constitutively produced a chromosomal cephalosporinase (nitrocefin hydrolysis); ‘cured’ variants of E. cloacae isolate No. 493, which had become susceptible for lamoxactam, produced a cefazolin-inducible β-lactamase. The two E. cloacae isolates, including their ‘cured’ variants, were of low-grade virulence for outbred NMRI mice. Both isolates differed somewhat in susceptibility to defibrinated human blood. Inhibitory (0.25 μg/ml), but not subinhibitory (0.125 μg/ml) concentrations of norfloxacin and enoxacin combined with human blood yielded additive effects against both E. cloac

ISSN:0009-3157    

DOI:10.1159/000238286

出版商:S. Karger AG    

年代:1984

数据来源: Karger

摘要:

Ceftizoxime – a new β-lactamase-resistant cephalosporin – was tested for its potential efficacy in the cure of uncomplicated gonorrhea. While more than a half of the 102 freshly isolated Neisseria gonorrhoeae strains examined was partially or totally resistant to penicillin (MIC ≥0.06 μg/ml), most of these strains proved highly susceptible to ceftizoxime (as well as cefotaxime). The MIC90% amounted to 0.004 μg/ml,while serum levels after the intramuscular application of as little as 0.5 g exceed 1 μg/ml for more than 6 h. The clinical results were excellent. 105 male or female patients suffering from uncomplicated gonorrhea were treated with a single intramuscular application of 1 g of ceftizoxime. 61 of them reattended our clinic twice for follow-up. All of them were cured. Anaphylactic shock or rashes were not observed. Thus, we consider the intramuscular application of 1 g of ceftizoxime as a reliable and safe treatment for uncomplicated gonococcal urethritis and c

ISSN:0009-3157    

DOI:10.1159/000238287

出版商:S. Karger AG    

年代:1984

数据来源: Karger

摘要:

Antistaphylococcal activity of newer β-lactam antibiotics, cefmenoxime, cefotaxime and latamoxef was compared with that of the more conventional antistaphylococcal agents, nafcillin, cefazolin and vancomycin. 53 strains of Staphylococcus aureus, 40 from patients with endocarditis and 13 from patients with bacteremia from other causes were tested in vitro against each antibiotic using agar dilution methods. Minimal concentration of antibiotic to inhibit 90% of strains tested was 2 μg/ml for cefmenoxime and cefotaxime, 8 μg/ml for latamoxef and only 0.5 μg/ml for nafcillin, cefazolin and vancomycin. The newer β-lactam antibiotics may not be preferred to nafcillin, cefazolin or vancomycin in the treatment of serious staphylococcal infect

ISSN:0009-3157    

DOI:10.1159/000238288

出版商:S. Karger AG    

年代:1984

数据来源: Karger

摘要:

The efficacy of cefoxitin, mezlocillin, latamoxef and metronidazole in anaerobic lung infection was studied using a rabbit model. A mixture of Bacteroides fragilis, Peptococcus morbillorum, Eubacterium lentum and Fusobacterium nucleatum was inoculated transtracheally to produce infection within the lung. Mezlocillin was most effective, achieving bacteriologic cure in 5 out of 8 animals. With cefoxitin therapy, 4 out of 8 became bacteriologically sterile. Severe diarrhea with elevated titers of Clostridium difficile toxin was noted in most cefoxitin-treated animals. Latamoxef- and metronidazole-treated animals had apparently healed lesions, but cultures were positive in 6 and 7 out of 8 in each group, respectively. The commonest pathogen isolated in the last two groups was P. morbillorum. The therapeutic superiority of mezlocillin over metronidazole and latamoxef was statistically significant (p ≤ 0.05

ISSN:0009-3157    

DOI:10.1159/000238289

出版商:S. Karger AG    

年代:1984

数据来源: Karger

摘要:

The efficacy and pharmacokinetics of latamoxef were evaluated during initial therapy of bacteriologically proven bone and joint infections in children. Pharmacokinetic evaluation revealed no significant difference in latamoxef biodisposition after the first dose or at steady state. Peak serum concentrations exceeded 140 mg/l and 8-hour trough concentrations averaged 6.5 mg/l. The patients were infected with a variety of gram-positive and gram-negative pathogens. All were sensitive to readily achievable serum concentrations of latamoxef; moreover, the serum concentration remained above the MIC of the most resistant organism for at least 7 h after each dose. All patients responded favorably to initial therapy and there have been no relapses in more than 2 years of clinical follow-up.

ISSN:0009-3157    

DOI:10.1159/000238290

出版商:S. Karger AG    

年代:1984

数据来源: Karger