ISSN:0009-3157    

DOI:10.1159/000238020

出版商:S. Karger AG    

年代:1981

数据来源: Karger

摘要:

The antibacterial properties of the new cephalosporin Ro 13-9904 were investigated in vitro and in vivo. The compound showed good activity against Enterobacteriaceae and gram-positive cocci, except Streptococcus faecalis. Haemophilus influenzae, Neisseria gonorrhoeae and Neisseria meningitidis were extremely susceptible to Ro 13-9904. The bactericidal activity of Ro 13-9904 was comparable to that of cefotaxime. The new cephalosporin showed better therapeutic efficacy in mice against Pseudomonas aemginosa than cefotaxime, cefoperazone, azlocillin, and piperacillin. Ro 13-9904 was highly effective in prophylactic studies, in contrast to cefotaxime, SCE-1365, cefoperazone and piperacillin. This indicates that Ro 13-9904 essentially differs from other β-lactam compounds in showing unusually prolonged in vivo efficacy

ISSN:0009-3157    

DOI:10.1159/000238021

出版商:S. Karger AG    

年代:1981

数据来源: Karger

摘要:

The levels of ribavirin or its antivirally active metabolic products were determined in the serum and urine of rats treated with single oral doses of 1,000 or 100 mg/kg of the compound, using a newly developed micromethod in which measles virus inhibition was assayed in BS-C-1 cells. At the high dosage level, maximum ribavirin serum levels of 24 μg/ml were observed 2 h postribavirin administration. Approximately 10-fold less active material was seen in the rats receiving the lower ribavirin dosage; this peak effect was seen 1 h after treatment. Urine excretion was maximal between 4 and 20 h after treatment in both dosage groups

ISSN:0009-3157    

DOI:10.1159/000237949

出版商:S. Karger AG    

年代:1981

数据来源: Karger

摘要:

The study was carried out with 50 strains of gonococci. Susceptibility to the antibiotics was determined by standard sensitivity test, by systematic test for β-lactamase and by measurement of the MICs. The cephalosporins tested were: moxalactam, cefotaxime, ceftriaxone, cefotiam, cefoxitin, cefazolin and cephalothin. Their activities were also compared with other β-lactams, namely penicillin and ampicillin. The efficacy in vitro of the cephalosporins: in the lead, ceftriaxone, remarkably active, with cefotaxime following very close, and then moxalactam with cefotiam a little behind, and finally all the other β-lactams tested. The median MICs of the new cephalosporins (moxalactam, cefotaxime, ceftriaxone and cefotiam) were at least 10 times greater than those of the other β-lactams tested. The MIC values observed with a resistant strain (penicillin, ampicillin; MIC 256 μg/ml) never exceed the maximum values found with the 50 susceptible str

ISSN:0009-3157    

DOI:10.1159/000238023

出版商:S. Karger AG    

年代:1981

数据来源: Karger

摘要:

The biliary excretion of cefuroxime was studied experimentally, using a preparation of isolated rabbit liver (n = 5) perfused in vitro during 3 h; 0.92% of the cefuroxime (10 mg) added to the circulating blood was found in the bile, while peak antibiotic activity reached a mean value of 8.0 ± 1.1 μg/ml. In man, 1 h after a single intravenous injection of cefuroxime (0.5 g), a maximum concentration of 4.0 ± 1.6 μg/ml was found in the duodenal aspiration fluid collected from 5 healthy subjects. In 10 patients with T-tube drainage, a mean biliary peak of 10.3 ± 2.4 μg/ml was observed 2 h after intravenous injection of the same dose; the biliary excretion of cefuroxime during the 12-hour experiment corresponded to 0.13% of the administered dose. Assays performed during cholecystectomy in 10 patients 1 h after cefuroxime intravenous injection of 0.5 g showed concentrations of 11.9 ± 0.8 μg/ml in the serum, 12.0 ± 1.5 μg/ml in the common duct bile and 7.4 ± 1.1 μg/ml in the gallbladder bile. These results were compared with those observed after administration of 11 other β-lactam antibiotics in identical experimental and clinica

ISSN:0009-3157    

DOI:10.1159/000237950

出版商:S. Karger AG    

年代:1981

数据来源: Karger

摘要:

The in vitro activity of 8 cephalosporins – cephalothin, cefamandole, cefoxitin, cefuroxime, cefotaxime, cefoperazone, moxalactam and ceftriaxone (Rocephin®) was studied on 109 strains of Neisseria gonorrhoeae and 60 strains of Neisseria meningitidis, isolated from pathological material. Determination of the MICs of these antibiotics by an agar dilution method shows that on N. gonorrhoeae ceftriaxone (geometric mean of the MICs: 0.0008 μg/ml) is the most active, followed by cefotaxime (0.001 μg/ml); cefoperazone (0.008 μg/ml) and moxalactam (0.01 μg/ml) are one-tenth as active; then come cefuroxime (0.05 μg/ml), cefamandole (0.10 μg/ml) and finally cephalothin (0.26 μg/ml) and cefoxitin (0.26 μg/ml). The least susceptibility to penicillin and, to a greater degree, the production of β-lactamase (8 strains) affect the level of susceptibility to these cephalosporins, but the MICs always remain rel

ISSN:0009-3157    

DOI:10.1159/000238024

出版商:S. Karger AG    

年代:1981

数据来源: Karger

摘要:

Ro 13-9904 is a novel semisynthetic and highly active parenteral cephalosporin. Its stability against hydrolysis by several β-lactamases was studied. The enzymes were isolated from various Enterobacteriaceae or Staphylococcus aureus and several commercially available enzyme preparations were also included. Most of the penicillinases, cephalosporinases or the TEM-type β-lactamase studied were unable to hydrolyze this novel cephalosporin. The cephalosporinases from Bacillus cereus 569/H9 and Proteus vulgaris 1028, however, were found to readily cleave all new cephalosporins like cefuroxime, cefotaxime and Ro 13-9904, but not cefoxitin. Ro 13-9904 was seen to be a potent inhibitor of several cephalosporinases, but had little or no affinity for penicillinases or the TEM lactamas

ISSN:0009-3157    

DOI:10.1159/000238025

出版商:S. Karger AG    

年代:1981

数据来源: Karger

摘要:

A gentamicin radioimmunoassay is described for microliter and nanoliter samples. The assay was performed in the inner ears’ fluids (perilymph and endolymph) of rats. Endolymph and perilymph samples were collected under oil with a glass capillary micropipette. The absolute threshold of sensitivity was 20 · 10––12 g. Considering the maximum sampling volume, 15–400 · 10––9 and 10 · 16––6 l for endolymph and perilymph respectively, the limit of detection is 4.19 · 10––4μM · ml––1 in endolymph, 1.26 · 10––4μM · ml––1 in perilymph. Clinical a

ISSN:0009-3157    

DOI:10.1159/000237951

出版商:S. Karger AG    

年代:1981

数据来源: Karger

摘要:

The pharmacokinetics of Ro 13-9904/001 following i.v. injection of 40 mg/kg was studied in a tissue cage model in rabbits. Binding to rabbit serum proteins was determined by ultrafiltration and found to be 98% at a concentration of 100 μg/ml. In the early post-injection period concentrations of the drug in rabbit serum reached 500–900 μg/ml, the antibiotic binding capacity of serum proteins was exceeded and the outflow of drug into the tissues was high. Tissue cage fluid (TCF) concentrations increased during 4 h, such as to reach a maximum level of about 30 μg/ml. After 8 h a t½ of 15 h was calculated both in serum and TCF. From 36 h onwards the t½ was 75 h. After a single injection of 14C-Ro 13-9904/001 radiological activity could be followed in serum and TCF for 7–10 days and in urine for more than 2 weeks. The results are discussed and compared to those from similar experiments with benzylpenicillin and fluclo

ISSN:0009-3157    

DOI:10.1159/000238026

出版商:S. Karger AG    

年代:1981

数据来源: Karger

摘要:

The comparative in vitro activity of three new cephalosporin antibiotics LY-127935 (LY), cefotaxime (CTX) and cefoperazone (CFP) was examined. LY, CTX and CFP had similar activity against Staphylococcus aureus, Escherichia coli and Proteus mirabilis while CFP was less inhibitory than LY or CTX against Klebsiella spp.; indole + Proteus and gentamicin (GM)-susceptible Serratia. LY and CTX were effective while CFP was inactive against Enterobacter spp. and GM-resistant Serratia. CFP was more active than LY or CTX against GM-susceptible Pseudomonas aeruginosa but was the least active agent against GM-resistant isolates. Bacteroides fragilis were more susceptible to LY than CTX or CFP. Combination studies against P. aeruginosa with cephalosporin-GM pairs demonstrated synergy.

ISSN:0009-3157    

DOI:10.1159/000237952

出版商:S. Karger AG    

年代:1981

数据来源: Karger