Antibacterial activity of cefotaxime and other newer cephalosporins (in vitro and in vivo)

Schrinner, E; Limbert, M.; Penasse, L.; Lutz, A

doi:10.1093/jac/6.suppl_a.25

Cited by 54 publications

(16 citation statements)

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“…Cefoperazone, cefotaxime, ceftizoxime, and ceftazidime are recently introduced cephalosporins which differ from their predecessors, such as cefoxitin, by alterations of the basic cephalosporin nucleus and its substituent groups. These new cephalosporins have been reported to have broader spectrum of activity than older agents and relative resistance to hydrolysis by beta-lactamases (10,16,20,26). In this investigation, cefoxitin, a beta-lactamase-resistant cephamycin, was level.…”

Section: Resultsmentioning

confidence: 90%

Comparative In Vitro Activity of New Beta-Lactam Antibiotics Against Anaerobic Bacteria

Rolfe

Finegold

1981

Antimicrob Agents Chemother

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Several new beta-lactam antimicrobial agents have been introduced in the last few years. In this investigation, the in vitro activities of several recently introduced cephalosporins (cefoperazone, cefotaxime, ceftazidime, and ceftizoxime), moxalactam, and N-formimidoyl thienamycin were compared with those of cefoxitin, clindamycin, and metronidazole against 203 strains of anaerobic bacteria. At achievable serum levels, all of the antimicrobial agents were active against essentially 100% of the strains of anaerobic gram-positive cocci, Clostridium perfringens, Leptotrichia buccalis, and species of Selenomonas, Veillonella, and Eubacterium. Clindamycin, metronidazole, and N-formimidoyl thienamycin were the most active agents against the Bacteroides fragilis group, inhibiting all strains at concentrations which can be achieved in serum. Of the remaining agents tested against the B. fragilis group, cefoxitin (which required 64 ,tg/ml to inhibit 90% of the strains) was the most active, followed by cefoperazone (128 ,ug/ml), cefotaxime (128 ,tg/ml), moxalactam (128 ,ug/ml), ceftizoxime (256 ,ug/mi), and ceftazidime (>256 pg/ml). Important differences in cephalosporin susceptibility among species of the B. fragilis group were observed. Metronidazole and N-formimidoyl thienamycin were the most active drugs against species of clostridia other than C. perfringens; the other antibiotics displayed poor activity, although this is partly due to inclusion of a relatively large number of strains of Clostridium difficile which were very resistant to several of the cephalosporins. Only metronidazole was active against all species of Fusobacterium. Clindamycin and N-formimidoyl thienamycin displayed excellent activity against gram-positive, non-spore-forming bacilli, requiring c8 ytg/ml to inhibit 100% of the strains. Ceftazidime, cefoperazone, and moxalactam were bactericidal for 25 strains of B. fragilis at concentrations equal or close to those required for inhibition. On the basis of its activity in vitro, N-formimidoyl thienamycin appears to be the most promising of the new beta-lactam antibiotics for the treatment of infections involving anaerobic bacteria.Several new beta-lactam antibiotics have been introduced in the last few years. Several recently introduced cephalosporins, including ceftizoxime, cefoperazone, cefotaxime, and ceftazidime, are distinguished from earlier cephalosporins by increased resistance to beta-lactamase degradation and extended antibacterial spectrum. N-formimidoyl thienamycin, a stable derivative of thienamycin, and moxalactam are beta-lactam antibiotics with potent and broad-spectrum activities.The purpose of the present study was to examine the in vitro activity of these new compounds against various strains of anaerobic bacteria. Using an agar dilution technique, the act Present address:

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Section: Resultsmentioning

confidence: 90%

Comparative In Vitro Activity of New Beta-Lactam Antibiotics Against Anaerobic Bacteria

Rolfe

Finegold

1981

Antimicrob Agents Chemother

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“…The antimicrobial activity [11] of CT and DACT is of the same order against gram-positive microbes, whereas the mini mum inhibitory concentrations of DACT against enterobacteria ranges from 0.05 to 0.8 of CT. The CT is some 10-30 times more active than DACT against Pseudo monas aeruginosa.…”

Section: Discussionmentioning

confidence: 97%

Assay of Cefotaxime by High-Pressure-Liquid Chromatography

Bergan

Solberg

1981

Chemotherapy

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A high-pressure-liquid chromatographic (HPLC) procedure for quantitative assay of cefotaxime (CT) and its major metabolite in serum of normal individuals, desacetyl cefotaxime (DACT), is described. It employs Lichrosorb RP-8, elution with phosphoric-acid-methanol and UV absorption at 310 nm. The method is optimized for cefotaxime and allows differentiation between the parent compound and the biotransformation product DACT. The lower assay sensitivity level of CT and DACT is 0.3 μg/ml. Correlation between HPLC and microbiological assay with Escherichia coli or Proteus rettgeri of pooled serum with CT added is r = 0.99. The method is rapid; processing of one sample takes 17 min. Use of HPLC avoids the errors of microbiological assays which derive from the presence in patient sera of different ratios of CT and DACT. The apparent rate of serum elimination is linearly related to the sensitivity of the microbial assay indicator strain to DACT. There is synergistic antibacterial activity between CT and DACT regardless of relative minimum inhibitory concentrations of the agents.

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“…The aminothiazolyl cephalosporins are particularly important because they possess favorable chemotherapeutic properties and are associated with low rates of adverse effects (1,8). Cefotaxime was the first representative of this group of cephalosporins (11). During our efforts to find new derivatives with even broader antibacterial spectra or better pharmacokinetics, a series of polar cephalosporins was synthesized (3).…”

mentioning

confidence: 99%

Antibacterial activities in vitro and in vivo and pharmacokinetics of cefquinome (HR 111V), a new broad-spectrum cephalosporin

Limbert¹,

Isert²,

Klesel³

et al. 1991

Antimicrob Agents Chemother

107

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Cefquinome is a new injectable aminothiazolyl cephalosporin derivative. It is stable against chromosomally and plasmid-encoded I8-lactamases and has a broad antibacterial spectrum. Staphylococcus aureus, streptococci, Pseudomonas aeruginosa, and members of the family Enterobacteriaceae (Escherichia coli, Salmonella spp., Klebsiella spp., Enterobacter spp., Citrobacter spp., and Serratia marcescens) are inhibited at low concentrations. Cefquinome is also active against many strains of methicillin-resistant staphylococci and enterococci. Its in vitro activity against gram-negative anaerobes is very limited. The high in vitro activity of cefquinome is reflected by its high in vivo efficacy against experimental septicemia due to different gram-positive and gram-negative bacteria. We studied the pharmacokinetic properties of cefquinome in mice, dogs, pigs, and calves. After single parenteral administrations, cefquinome displayed high peak levels, declining with half-lives of about 0.5, 0.9, 1.2, and 1.3 h, respectively. The areas under the concentration-time curve determined for dogs and mice showed linear correlations to the given doses. In dogs the urinary recovery was more than 70% within 24 h of dosing.

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Antibacterial activity of cefotaxime and other newer cephalosporins (in vitro and in vivo)

Cited by 54 publications

References 0 publications

Comparative In Vitro Activity of New Beta-Lactam Antibiotics Against Anaerobic Bacteria

Comparative In Vitro Activity of New Beta-Lactam Antibiotics Against Anaerobic Bacteria

Assay of Cefotaxime by High-Pressure-Liquid Chromatography

Antibacterial activities in vitro and in vivo and pharmacokinetics of cefquinome (HR 111V), a new broad-spectrum cephalosporin

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