Showing papers on "Cefotaxime published in 1980"
TL;DR: MK0787 exhibits a broad spectrum of in vivo activity when evaluated parenterally for efficacy against systemic infections in mice and was at least 10-fold superior to reference beta-lactam antibiotics including two recently developed agents with antipseudomonal activity, cefotaxime and LY127935.
Abstract: The practical application of thienamycin, a novel beta-lactam antibiotic with a broad activity spectrum, was compromised by problems of instability. MK0787, N-formimidoyl thienamycin, does not have this liability. As reported, bacterial species resistant to most beta-lactam antibiotics, such as Pseudomonas aeurginosa, Serratis, Enterobacter, Enterococcus, and Bacteroides spp., are uniformly susceptible to MK0787, usually at one-half the inhibitory level of thienamycin. Bactericidal activity usually occurs at the minimal inhibitory concentration endpoint. Activity was reduced only at the highest inoculum densities tested and by a lessor factor than was observed with reference beta-lactam antibiotic active against P. aeruginosa and beta-lactamase-bearing strains. MK0787 exhibits a broad spectrum of in vivo activity when evaluated parenterally for efficacy against systemic infections in mice. The order of potency in vivo, 0.03 to 0.06 mg/kg for gram-positive species and 0.65 to 3.8 mg/kg for gram-negative infections including Pseudomonas, exceeded that of thienamycin and was at least 10-fold superior to reference beta-lactam antibiotics including two recently developed agents with antipseudomonal activity, cefotaxime and LY127935.
201 citations
TL;DR: GR 20263 is a new broad-spectrum injectable cephalosporin which is stable to most beta-lactamases, and produces high, long-lasting blood levels, with much of the antibiotic being recovered in the urine.
Abstract: GR 20263 is a new broad-spectrum injectable cephalosporin which is stable to most beta-lactamases. Its in vitro activities were of the same order as those of cefotaxime against most gram-negative bacteria, were clearly inferior to cefotaxime against Staphylococcus aureus, but were significantly more active against Pseudomonas aeruginosa. Against the 25 strains used, GR 20263 was significantly more active than any of the other agents tested: piperacillin, azlocillin, gentamicin, amikacin, and carbenicillin. GR 20263 protected mice against experimental infections with P. aeruginosa more effectively than other beta-lactam antibiotics; its general effectiveness in this test was comparable with gentamicin. Studies on human volunteers showed that it produces high, long-lasting blood levels, with much of the antibiotic being recovered in the urine. Intramuscular and intravenous injections were well tolerated by the volunteers, and there were no untoward side effects.
181 citations
TL;DR: The animal inhibitory concentrations of 32 antimicrobial agents for 322 strains of non-fermentative gram-negative bacilli, representing 30 species and unnamed groups other than Pseudomonas aeruginosa, were determined in cation-supplemented Mueller-Hinton broth with use of a microdilution method to indicate potential clinical usefulness of these agents.
Abstract: The minimal inhibitory concentrations of 32 antimicrobial agents for 322 strains of nonfermentative gram-negative bacilli, representing 30 species and unnamed groups other than Pseudomonas aeruginosa, were determined in cation-supplemented Mueller-Hinton broth with use of a microdilution method. The activities of 3-lactam antibiotics varied, but azlocillin, mezlocillin, piperacillin, cefotaxime, and moxalactam consistently were more active than were available penicillins and cephalosporins; the penicillin-like antibiotic mecillinam was less active. The activities of the aminoglycoside antibiotics were similar to each other although streptomycin and sometimes kanamycin were less active than the other aminoglycosides. Although minocycline and doxycycline usually were more active than tetracycline, the percentages of strains susceptible to the first two drugs at concentrations achievable in vivo were only occasionally higher than the percentage of strains susceptible to tetracycline. The activity of trimethoprim-sulfamethoxazole was variable. Chloramphenicol, erythromycin, clindamycin, and vancomycin were relatively inactive against most of the organisms tested, but the high degrees of activity of these drugs against specific species or strains, particularly those that were resistant to many drugs, indicated potential clinical usefulness of these agents. Nonfermentative gram-negative bacilli other than Pseudomonas aeruginosa generally are saprophytic in nature but are etiologic agents in a significant number of infections, particularly those acquired in the hospital or that occur in compromised hosts. Susceptibilities of these bacilli to antimicrobial agents often are different from those of Enterobacteriaceae and P. aeruginosa, and many of these organisms are multi-drug resistant [1-4]. A number of studies [3-9] have surveyed the patterns of susceptibility of nonfermenters to antimicrobial agents with use of the disk diffusion method [10]. The results of these susceptibility tests were used primarily for identification of the organisms, rather than for selection of therapeutic
112 citations
TL;DR: Thirteen children with meningitis due to Haemophilus influenzae, beta-haemolytic streptococcus group B, Streptococcas pneumoniae, Staphylococcus epidermidis, Neisseria meningitidis and Pseudomonas aeruginosa and who had been unsuccessfully treated with other antibiotics or had causative organisms which were resistant to available antibiotics were treated with intravenous cefotaxime.
98 citations
TL;DR: Cftizoxime was the most active agent tested against Escherichia coli and Klebsiella, inhibiting 80% at 0.025 microgram/ml, and was more active than cefotaxime against Enterobacter cloacae and E. aerogenes.
Abstract: The in vitro activity of ceftizoxime was compared with that of other beta-lactam antibiotics against 538 isolates. Ceftizoxime was the most active agent tested against Escherichia coli and Klebsiella, inhibiting 80% at 0.025 microgram/ml. It was more active than cefotaxime against Enterobacter cloacae and E. aerogenes. Ceftizoxime was more active than cefoxitin, cefotaxime, cefoperazone, and carbenicillin against Proteus mirabilis and indole-positive Proteus. It inhibited 97% of multiresistant Serratia isolates at 12.5 microgram/ml, whereas cefotaxime inhibited only 19%. Ceftizoxime was less active than cefotaxime and cefoperazone against Pseudomonas aeruginosa, but was more active than carbenicillin. It was more active than cefotaxime and cefoxitin against Bacteroides. It was not appreciably destroyed by beta-lactamases of Staphylococcus aureus, Enterobacteriaceae, or Pseudomonas.
93 citations
TL;DR: A total of 91 multiply resistant bacterial strains, including Klebsiella pneumoniae and Serratia marcescens, were collected during hospital epidemics of nosocomial infection from 1975 to 1979, and were as susceptible to the three new broad-spectrum β-lactams as were non-multiply resistant strains.
Abstract: A total of 91 multiply resistant bacterial strains, including Klebsiella pneumoniae (32 strains), Pseudomonas aeruginosa (16 strains), and Serratia marcescens (43 strains), were collected during hospital epidemics of nosocomial infection from 1975 to 1979. These strains were resistant to gentamicin, tobramycin, cephalothin, chloramphenicol, and ampicillin. Their susceptibility to three new broad-spectrum β-lactams, LY127935 (a 1-oxa-β-lactam), cefotaxime (HR 756), and cefoperazone (T 1551), was compared with the susceptibility of random strains of nine species of aerobic gram-negative bacilli collected in the same hospital in 1979. Susceptibility to cefamandole and ticarcillin was also determined. Strains of staphylococci and streptococci from that hospital and two nearby city-county hospitals were also compared for the three new cephalosporins and other effective antibiotics. The agar dilution method was used to measure the minimum inhibitory concentration for each antibiotic. The multiply resistant strains (minimum inhibitory concentration for gentamicin ≥ 8 μg/ml) usually were as susceptible to the three new broad-spectrum β-lactams as were non-multiply resistant strains. Both Klebsiella pneumoniae and Serratia marcescens , including multiply resistant and non-multiply resistant strains, were most susceptible to the 1-oxa-β-lactam LY127935 and cefotaxime. P. aeruginosa (both multiply resistant and non-multiply resistant strains) were most susceptible to cefoperazone. All three new β-lactams were active against non-multiply resistant strains of Escherichia coli, Enterobacter spp., Proteus spp., and Citrobacter spp. Providencia stuartii were most susceptible to cefotaxime and the 1-oxa-β-lactam LY127935. The three new β-lactams were all less active against staphylococci (especially methicillin-resistant Staphylococcus aureus ) than cephalothin. Streptococcus pyogenes and S. pneumoniae were very susceptible to cefotaxime and cefoperazone, though less susceptible to LY127935. None of the three new β-lactams was active against S. faecalis . All were very active against both penicillinase-positive and -negative strains of Neisseria gonorrhoeae .
93 citations
TL;DR: Although structurally related to cefotaxime and SCE-1365, Ro 13-9904 was found to differ from them in one important respect, namely, in having a long duration of action; this was observed with single-dose treatment given before bacterial challenge.
Abstract: Ro 13-9904, a new parenteral cephalosporin, was found to have high in vitro activity against Enterobacteriaceae and other gram-negative bacteria, including various isolates resistant to cefuroxime, cefamandole, cefoxitin, and cefazolin. It showed promising activity against Pseudomonas aeruginosa. Although inhibitory against Staphylococcus aureus at concentrations readily achievable in plasma, it was less potent against this pathogen than cefamandole, cefazolin, or cefuroxime. Isolates of Streptococcus faecalis were uniformly resistant to all the cephalosporins tested. Ro 13-9904 was more active than cefotaxime against Proteus mirabilis, Neisseria gonorrhoeae, Neisseria meningitidis, and Haemophilus influenzae, but less active against S. aureus. Ro 13-9904 was stable to various types of beta-lactamases. Its therapeutic efficacy against experimental septicemias in mice was equal to or slightly superior to that of cefotaxime and SCE-1365 when the antibiotics were administered in repeated subcutaneous doses after bacterial challenge. Cefoperazone, and particularly cefamandole nafate, cefazolin, and mezlocillin were less effective. Although structurally related to cefotaxime and SCE-1365, Ro 13-9904 was found to differ from them in one important respect, namely, in having a long duration of action; this was observed with single-dose treatment given before bacterial challenge. Its broad spectrum of activity coupled with favorable pharmacokinetic properties make Ro 13-9904 a promising compound for clinical studies.
92 citations
TL;DR: The drug most active against beta-lactamase-positive N. gonorrhoeae and H. influenzae was cefotaxime, followed closely by cefoperazone, moxalactam, piperacillin, and mezlocillin.
Abstract: Minimum inhibitory concentrations and agar disk diffusion tests were determined on clinical isolates of beta-lactamase-positive and beta-lactamase-negative Neisseria gonorrhoeae and Haemophilus influenzae with the newer beta-lactam antibiotics, cefoperazone, cefotaxime, moxalactam (LY127935), azlocillin, mezlocillin, and piperacillin, and with seven older beta-lactam antibiotics. All the drugs were active against beta-lactamase-negative strains of N. gonorrhoeae and H. influenzae. The drug most active against beta-lactamase-positive N. gonorrhoeae was cefotaxime, followed closely by cefoperazone, moxalactam, piperacillin, and mezlocillin. The drugs most active against beta-lactamase-positive strains of H. influenzae were cefotaxime, moxalactam, cefoperazone, and cefamandole.
92 citations
TL;DR: The desacetyl metabolite of cefotaxime (DES) is formed in vivo to a significant extent and may have considerable clinical significance, because it may accumulate in renal failure or be concentrated in the biliary tract.
Abstract: The desacetyl metabolite (DES) of cefotaxime (HR756) is formed in vivo to a significant extent. The in vitro activities of DES, the parent compound, and cefazolin, cefoxitin, and cefuroxime were compared against 70 bacterial isolates. DES was found to possess approximately 1/10th the activity of the parent compound against the common Enterobacteriaceae, but was somewhat more active than the other three compounds tested. DES had no useful activity against Pseudomonas aeruginosa and was less active than cefotaxime or cefoxitin against Staphylococcus aureus or Bacteroides fragilis. Because DES may accumulate in renal failure or be concentrated in the biliary tract, its antimicrobial activity may have considerable clinical significance.
89 citations
TL;DR: The in vitro activity of GR-20263, a new aminothiazolyl cephalosporin, was compared with the activities of other beta-lactam antibiotics by using 800 clinical bacterial isolates and found it to be highly active against the common Enterobacteriaceae and 5 to 20 times more active than cefuroxime, cefoxitin, and cEPhalothin.
Abstract: The in vitro activity of GR-20263, a new aminothiazolyl cephalosporin, was compared with the activities of other beta-lactam antibiotics by using 800 clinical bacterial isolates. GR-20263 was highly active (inhibition of 90% of the isolates between 0.03 and 1 microgram/ml) against the common Enterobacteriaceae and 5 to 20 times more active than cefuroxime, cefoxitin, and cephalothin. GR-20263 was three to six times less active than cefotaxime against Escherichia coli, Klebsiella pneumoniae, Salmonella, and Shigella, but three to four times more active than cefotaxime against Proteus vulgaris and Serratia marcescens. The activity of GR-20263 against Pseudomonas aeruginosa (with minimal inhibitory concentrations of 2 and 8 micrograms/ml for 90 and 100% of the isolates, respectively) was similar to that of tobramycin, 2 times that of cefsulodin, 5 times that of piperacillin, and 10 times that of cefotaxime. Against Haemophilus influenzae GR-20263 was three time more active than ampicillin. The beta-lactamase-producing strains were as susceptible to GR-20263 as the beta-lactamase-negative strains. GR-20263 was less active than cefotaxime and ampicillin against Staphylococcus aureus.
85 citations
TL;DR: In comparison with the other agents, GR 20263 was markedly more active against the Enterobacteriaceae than cefuroxime, cefoxitin, and cefazolin, but marginally less active than moxalactam or cofotaxime.
Abstract: The in vitro activity of GR 20263, a new cephalosporin, was compared primarily with the activities of moxalactam (LY 127935), cefotaxime, cefoxitin, cefuroxime, and cefazolin against 293 clinical isolates of a variety of gram-positive and -negative bacteria. The minimal inhibitory concentrations of GR 20263 for 90% of group isolates were between 0.06 and 0.5 microgram/ml for the Enterobacteriaceae, Haemophilus influenzae, Neisseria gonorrhoeae, and Lancefield group A beta-hemolytic streptococci; 2 micrograms/ml for Pseudomonas aeruginosa; 16 micrograms/ml for Staphylococcus aureus; and in excess of 128 micrograms/ml for Bacteroides fragilis and Lancefield group D streptococci. In comparison with the other agents, GR 20263 was markedly more active against the Enterobacteriaceae than cefuroxime, cefoxitin, and cefazolin, but marginally less active than moxalactam or cofotaxime. Aganist S. aureus, cefazolin was 16-fold and cefotaxime was 4-fold more active than GR 20263 and moxalactam. GR 20263 was eight-fold more active than cefotaxime and moxalactam against P. aeruginosa.
TL;DR: The bacteriostatic and bactericidal activities of 24 antimicrobial agents were tested with the Dynatech MIC 2000 system against 86 strains of Campylobacter fetus subsp.
Abstract: The bacteriostatic and bactericidal activities of 24 antimicrobial agents were tested with the Dynatech MIC 2000 system against 86 strains of Campylobacter fetus subsp. jejuni from human sources. The penicillins (penicillin G, ampicillin, amoxycillin, carbenicillin) had poor activity. Ampicillin and amoxycillin were equally active. Cefotaxime revealed a rather good activity. Erythromycin, gentamicin, tobramycin, amikacin, and furazolidone were the most active compounds. Two strains (2.3%) were resistant to erythromycin. One strain (1.2%) was completely resistant to tobramycin. The tetracyclines (tetracyline, doxycycline, minocycline) were generally effective, but 8% of the strains were totally resistant to them. Minocycline was the most active. Chloramphenicol, thiamphenicol, and clindamycin had good activity. The bacteriostatic and bactericidal distributions for colistin, nalidixic acid, and metronidazole were broad.
TL;DR: The in vitro activity of Ro 13-9904 was assessed against clinical isolated of common bacteria and was resistant to most beta-lactamases but was attacked by enzymes from B. fragilis, isolates of indole-positive Proteus species, and also by a cefoxitin-hydrolyzing enzyme from an isolate of Enterobacter cloacae.
Abstract: The in vitro activity of Ro 13-9904 was assessed against clinical isolated of common bacteria. Its activity against most enterobacteria was similar to that of cefotaxime and moxalactam, but it was even more active than these compounds against all Proteus species. It was also highly active against Haemophilus influenzae and Neisseria gonorrhoeae, including beta-lactamase producers. Like cefotaxime and moxalactam, Or 13-9904 was approximately eightfold more active than carbenicillin against most isolates of Pseudomonas aeruginosa and also active against highly carbenicillin-resistant isolates, but it was relatively inactive against moderately carbenicillin-resistant isolates. Ro 13-9904 also resembled cefotaxime and moxalactam in that it was active, though less so than cephaloridine, against staphylococci and streptococci, except for methicillin-resistant staphylococci and Streptococcus faecalis, which were resistant to it. It was less active than cefoxitin but slightly more active than ampicillin against both Bacteroides fragilis and other Bacteroides spp. Ro 13-9904 was resistant to most beta-lactamases but was attacked by enzymes from B. fragilis, isolates of indole-positive Proteus species, and also by a cefoxitin-hydrolyzing enzyme from an isolate of Enterobacter cloacae.
TL;DR: This study compares the minimum inhibitory concentrations of cefoperazone, cefotaxime, and moxalactam for 446 aerobic gram-negative bacillary isolates with those of thienamycin for Pseudomonas aeruginosa to show each antibiotic at low concentrations inhibited nearly all Enterobacteriaceae tested.
Abstract: This study compares the minimum inhibitory concentrations of cefoperazone, cefotaxime, and moxalactam (LY127935) for 446 aerobic gram-negative bacillary isolates and further compares the minimum inhibitory concentrations of LY127935 and these third-generation cephalosporins with those of thienamycin for Pseudomonas aeruginosa. Each antibiotic at low concentrations inhibited nearly all Enterobacteriaceae tested. Minimum inhibitory concentrations for P. aeruginosa were higher, but for a majority of strains they fell below achievable serum levels. Thienamycin and cefoperazone showed significantly greater antipseudomonal activity than did cefotaxime or LY127935. Cefoxitin-inducible resistance to LY127935 and the two cephalosporins was demonstrated among Enterobacter species but did not occur with thienamycin.
TL;DR: N-Formimidoyl thienamycin was the only drug tested for which an MIC100 and MBC100 (MIC and M BC for 100% of isolates) could be determined, and these were not significantly different from the MIC90 and MCB90.
Abstract: Forty clinical isolates of Pseudomonas aeruginosa were tested for their susceptibility to cefoperazone, cefotaxime, moxalactam, piperacillin, N-formimidoyl thienamycin (MK0787), and gentamicin at three different inocula. At an inoculum of 5 x 10(3) colony-forming units (CFU) per ml, the minimum inhibitory concentrations (in micrograms per milliliter) for 90% of isolates (MIC90) were as follows: gentamicin, 1; N-formimidoyl thienamycin, 2; cefoperazone, 4; piperacillin, 8; moxalactam, 16; and cefotaxime, 16. When the inoculum was increased to 5 x 10(5) CFU/ml, the MIC90 for all drugs tested increased. Among the beta-lactam antibiotics, N-formimidoyl thienamycin and cefoperazone had the lowest MIC90 (8 micrograms/ml) at this inoculum. When the inoculum was increased further to 5 x 10(7) CFU/ml, an MIC90 could be determined only for gentamicin and N-formimidoyl thienamycin (4 and 8 micrograms/ml, respectively). Indeed, the MIC50 for moxalactam, cefotaxime, cefoperazone, and piperacillin was 128 micrograms/ml or more at this inoculum. The minimum bactericidal concentration for 90% of isolates (MBC90) at an inoculum of 5 x 10(5) CFU/ml ranged from 8 micrograms/ml for gentamicin and N-formimidoyl thienamycin to 128 micrograms/ml for cefotaxime. At the highest inoculum, however, whereas the MBC90 for gentamicin and N-formimidoyl thienamycin remained at 8 micrograms/ml, the MBC90 for each of the other drugs was greater than 128 micrograms/ml. N-Formimidoyl thienamycin was the only drug tested for which an MIC100 and MBC100 (MIC and MBC for 100% of isolates) could be determined, and these were not significantly different from the MIC90 and MCB90.
TL;DR: The major in vitro difference of these newer beta-lactam compounds appeared to be their antipseudomonal activity; cefoperazone was the most active, whereas cefotaxime had the least potency.
Abstract: The in vitro activities of four new beta-lactam antimicrobial agents (moxalactam, cefotaxime, cefoperazone, and piperacillin) and the aminoglycosides against 744 recent clinical isolates of facultative gram-negative bacilli were compared simultaneously by the agar dilution method. The major in vitro difference of these newer beta-lactam compounds appeared to be their antipseudomonal activity; cefoperazone was the most active, whereas cefotaxime had the least potency. The aminoglycosides, however, had the most effective in vitro activity on a weight basis against Pseudomonas aeruginosa.
TL;DR: The new drugs were uniformly active against coliform bacilli obtained from patients with meningitis and against aminoglycoside-resistant coliformbacilli.
Abstract: Moxalactam, Ro 13-9904, cefotaxime, cefoperazone, older cephalosporins, and four aminoglycosides were tested in vitro against 432 strains of gram-negative bacteria isolated from pediatric patients. The new drugs were uniformly active against coliform bacilli obtained from patients with meningitis and against aminoglycoside-resistant coliform bacilli.
TL;DR: LY127935 was the most active of the antibiotics tested against Bacteroides, showing good activity against Clostridia and poor activity on Peptococcaceae, whereas T-1551 was more active against Peptococccaceae and had similar activity againstclostridium andpoor activity on Bactroides.
Abstract: The in vitro activity of 1-oxa-beta-lactam (LY127935), cefoperazone (T-1551), cefuroxime, cefsulodin, cefaclor, cefotaxime, and cefoxitin on 85 anaerobic clinical isolates (30 Bacteroides, 30 Clostridium, 25 Peptococcaceae) was simultaneously determined by the agar dilution test in two different media, Brucella Agar (Difco Laboratories) and Wilkins-Chalgren agar. In Wilkins-Chalgren agar, 90% of Bacteroides were inhibited by (micrograms per milliliter): LY127935, 0.5; T-1551, 64; cefoxitin or cefuroxime, 8; cefsulodin or cefotaxime, 32; and cefaclor, 128. All Clostridia were inhibited in Wilkins-Chalgren by (micrograms per milliliter): LY127935, 4; T-1551, 2; cefoxitin, 6; cefuroxime, 0.12; cefsulodin, 0.5; cefaclor, 1; and cefotaxime, 8. All Peptococccaceae were inhibited by T-1551, cefsulodin or cefotaxime at 4 microgram/ml and by cefoxitin or cefuroxime at 1 to 2 microgram/ml. With cefaclor at 8 microgram/ml, 92% of strains were inhibited, and LY127935 at 16 microgram/ml only inhibited 64% of strains. LY127935 was the most active of the antibiotics tested against Bacteroides, showing good activity against Clostridia and poor activity on Peptococcaceae, whereas T-1551 was more active against Peptococccaceae and had similar activity against Clostridia and poor activity on Bacteroides. There are no significant differences between minimal inhibitory concentrations obtained in Brucella Agar and those obtained in Wilkins-Chalgren.
TL;DR: Moxalactam exhibited greater in vitro activity than cefamandole and tobramycin against clinical isolates of Enterobacteriaceae, Aeromonas hydrophila, and Pseudomonas maltophilia and demonstrated significant activity against the Bacteroides fragilis group and other anaerobes.
Abstract: Moxalactam (LY127935) exhibited greater in vitro activity than cefamandole and tobramycin against clinical isolates of Enterobacteriaceae, Aeromonas hydrophila, and Pseudomonas maltophilia. The activities of the three drugs against other microorganisms were as follows: for staphylococci, cefamandole = tobramycin greater than moxalactam; for streptococci, cefamandole greater than moxalactam greater than tobramycin; and for Pseudomonas aeruginosa, tobramycin greater than moxalactam greater than cefamandole. Moxalactam also demonstrated significant activity against the Bacteroides fragilis group and other anaerobes. Moxalactam was comparable to cefotaxime (HR756) in its inhibition of cephalothin-resistant and aminoglycoside-resistant clinical isolates.
TL;DR: In vitro susceptibilities of 53 clinical isolates of Pseudomonas aeruginosa to nine antipseudomonal antibiotics were determined and synergy was not demonstrated consistently in vitro with 1-oxace-phalosporin combined with either carbenicillin, ticarcillin, gentamicin, or tobramycin.
Abstract: In vitro susceptibilities of 53 clinical isolates of Pseudomonas aeruginosa to nine antipseudomonal antibiotics were determined. From 96 to 100% of the isolates were susceptible to piperacillin, ticarcillin, and 1-oxacephalosporin (LY 127935). Of the aminoglycosides, 89, 82, 79, and 29% were susceptible to amikacin, tobramycin, gentamicin, and netilmicin, respectively. A total of 96% and 78% of the isolates were susceptible to 1-oxacephalosporin (LY127935) and cefotaxime, respectively, at concentrations of 62.5 micrograms/l. Supplementation of testing media by calcium and magnesium not only markedly increased the minimal inhibitory concentrations of the aminoglycosides, but also raised those of cefotaxime and the penicillins; no significant effect was noted with 1-oxace-phalosporin. Synergy was not demonstrated consistently in vitro with 1-oxace-phalosporin combined with either carbenicillin, ticarcillin, gentamicin, or tobramycin.
TL;DR: Agar dilution antimicrobial susceptibility testing showed that Campylobacter jejuni was significantly more resistant to cephalosporin C than fetus subsp.
Abstract: Agar dilution antimicrobial susceptibility testing showed that Campylobacter jejuni was significantly more resistant than Campylobacter fetus subsp. fetus (intestinalis) to cephalosporin C, cephaloridine, cephalothin, cefazolin, and cefamandole. No species differences in susceptibility were noted with cephalexin, cefotaxime, and cefoxitin. Rapid species differentiation on the basis of an antibiogram could be achieved with the disk diffusion method. C jejuni failed to produce a zone of inhibition around a 30-microgram cephalothin disk but produced a significant zone around a 30-microgram nalidixic acid disk. C. fetus subsp. fetus (intestinalis) produced exactly the reverse pattern.
TL;DR: Comparative turbidimetric and morphological studies revealed that ceftizoxime was able to induce spheroplast formation and rapid lysis in Escherichia coli strains at lower concentrations than cefotaxime.
Abstract: Cefotaxime and its desacetoxymethyl derivative, ceftizoxime (previously known as FK749), are both extremely active against a wide spectrum of bacteria. In the present comparative study, the activity of ceftizoxime exceeded that of cefotaxime by a factor of four or more for strains of Klebsiella, Enterobacter, Providencia, Serratia, and Bacteroides; the only species for which the activity of cefotaxime exceeded that of ceftizoxime by a factor of four was Vibrio cholerae. Against other species, the activity of the two drugs was roughly comparable. Both showed outstanding activity against Haemophilus influenzae and Neisseria gonorrhoeae. Comparative turbidimetric and morphological studies revealed that ceftizoxime was able to induce spheroplast formation and rapid lysis in Escherichia coli strains at lower concentrations than cefotaxime. This difference was not found, however, when E. coli strains resistant to ampicillin by an intrinsic (nonenzymic) mechanism were tested.
TL;DR: Cefotaxime MIC susceptible and resistant breakpoints of less than or equal to 8 and greater than 32 micrograms/ml are tentatively proposed, based on the MIC breakpoints, which showed the best discrimination among the three susceptibility categories (susceptible, indeterminate, and resistant) when the 30-micrograms cefotAXime disk was used.
Abstract: Tested against 9,412 recent clinical isolates, cefotaxime exhibited 8 to 64 times greater activity against the Enterobacteriaceae than did cephalothin and two to four times greater activity against Pseudomonas aeruginosa, but only one-half to one-eighth the activity of cephalothin against staphylococci. Using 420 different clinical isolates, but with comparable minimal inhibitory concentration (MIC) distributions, disk diffusion-MIC regression analyses were performed, using 5- and 30-micrograms cefotaxime disks. Cefotaxime MIC susceptible and resistant breakpoints of less than or equal to 8 and greater than 32 micrograms/ml are tentatively proposed. Based on the MIC breakpoints, the data showed the best discrimination among the three susceptibility categories (susceptible, indeterminate, and resistant) when the 30-micrograms cefotaxime disk was used. The zone diameter breakpoints as determined by the error rate-bounded method and regression analysis were greater than or equal to 23 mm for susceptible, 15 to 22 mm for indeterminate, and less than or equal to 14 mm for resistant.
TL;DR: Both moxalactam and cefotaxime demonstrated impressive in vitro activities against both groups of microorganisms, clearly more active than any of the other beta-lactam antibiotics against species of Escherichia, Citrobacter, Enterobacter, Klebsiella, Proteus, Providencia, Pseudomonas and Serratia.
Abstract: The in vitro activities of two new beta-lactam antibiotics, moxalactam disodium (LY 127935) and cefotaxime (HR-756), were compared with cefoxitin, cefamandole, cefuroxime, cephalothin, and, in some instances, carbenicillin, gentamicin, and amikacin against aerobic gram-negative bacilli. Test isolates included normally cephalosporin-resistant members of the Enterobacteriaceae and Pseudomonas spp. and a variety of nonfermentative or oxidase-positive bacteria. Both moxalactam and cefotaxime demonstrated impressive in vitro activities against both groups of microorganisms. The two new drugs were clearly more active than any of the other beta-lactam antibiotics against species of Escherichia, Citrobacter, Enterobacter, Klebsiella, Proteus, Providencia, Pseudomonas, and Serratia. An additive or synergistic effect could also be demonstrated with the majority of Pseudomonas and Serratia isolates when either moxalactam or defotaxime was combined with amikacin.
TL;DR: The pharmacokinetics of cefotaxime and moxalactam were compared in six healthy male volunteers aftr the administration of 1-g doses intravenously and Penetration of the compounds into tissue fluid was studied in cantharides-induced blisters.
Abstract: The pharmacokinetics of cefotaxime and moxalactam were compared in six healthy male volunteers aftr the administration of 1-g doses intravenously. Penetration of the compounds into tissue fluid was studied in cantharides-induced blisters. Both serum and tissue fluid levels of moxalactam were higher than those of cefotaxime. The elimination half-life of cefotaxime was 1.2 h, and that of moxalactam was 2.85 h. On the average, 50.5% of cefotaxime and 87.5% of moxalactam were recovered in the urine in 24 h.
TL;DR: Moxalactam proved to be the most active agent tested against Bacteroides Fragilis and other species of the B. fragilis group and penicillin was the most effective drug tested against most species of Clostridium, the anaerobic gram-positive cocci, and Eubacterium lentum.
Abstract: The in vitro activities of moxalactam (LY127935 [6059S]) and cefotaxime were compared with those of cefoxitin, cefamandole, cefuroxime, carbenicillin, and penicillin by agar dilution susceptibility testing of a variety of anaerobic bacteria. Moxalactam proved to be the most active agent tested against Bacteroides fragilis and other species of the B. fragilis group. Moxalactam and cefotaxime showed activity similar to the other drugs against the remaining species of Bacteroides, Fusobacterium, Actinomyces, Propionibacterium, and Veillonella. Penicillin was the most effective drug tested against most species of Clostridium, the anaerobic gram-positive cocci, and Eubacterium lentum.