cefpiramide and apalcillin

The therapeutic efficacy of cefpiramide and apalcillin was evaluated and compared with that of six other antipseudomonal beta-lactam antibiotics in an experimental mouse burn infection due to Pseudomonas aeruginosa. Both cefpiramide and apalcillin were as potent as cefsulodin and more potent than carbenicillin, cefotaxime, cefoperazone, piperacillin and gentamicin in protecting the infected mice from fatal bacteraemia and in eradicating Ps. aeruginosa from the infected site.

Topics: Ampicillin; Animals; Anti-Bacterial Agents; Burns; Cephalosporins; Female; Mice; Naphthyridines; Pseudomonas Infections; Wound Infection

The in vitro activities of cefpiramide and apalcillin were compared with those of other third-generation cephalosporins and extended-spectrum penicillins against over 1,000 clinical bacterial isolates. The activity of cefpiramide against Pseudomonas aeruginosa was comparable to those of piperacillin and cefoperazone, inhibiting 90% of strains at concentrations less than or equal to 16.0 micrograms/ml. This drug was also active against a broad range of gram-negative organisms but was generally less active than many of the other cephalosporins tested against members of the family Enterobacteriaceae. The activity of cefpiramide against gram-positive organisms was comparable to that of cefoperazone. Apalcillin, along with ceftazidime, was the most active agent tested against P. aeruginosa and Acinetobacter calcoaceticus subsp. anitratus, inhibiting 90% of these strains at concentrations less than or equal to 8 micrograms/ml. Against other gram-negative and gram-positive organisms, its activity was similar to that of piperacillin. The activities of both cefpiramide and apalcillin were significantly reduced by the presence of several plasmid-mediated beta-lactamases in a series of otherwise isogenic strains of P. aeruginosa in comparison with their activities against a parent strain which lacks these enzymes. Many strains of Enterobacter cloacae were synergistically inhibited by the combination of gentamicin with either cefpiramide (5 of 10 strains) or apalcillin (6 of 10 strains). Most strains of P. aeruginosa were synergistically inhibited by the combination of gentamicin with either cefpiramide (8 of 10 strains) or apalcillin (10 of 10 strains). However, cefoxitin antagonized the activity of both cefpiramide and apalcillin against most of these same strains.

Topics: Ampicillin; Anti-Bacterial Agents; Bacteria; Bacterial Infections; Cephalosporins; Drug Synergism; Enterobacteriaceae; Humans; Microbial Sensitivity Tests; Naphthyridines; Pseudomonas aeruginosa

Rabbits with experimentally induced pneumococcal meningitis were given single 25-mg/kg doses of apalcillin or cefpiramide. Mean percentages of the drug concentration in cerebrospinal fluid versus that in blood serum were 7.6% with apalcillin and 3.9% with cefpiramide. Bactericidal activity in cerebrospinal fluid resulted in mean reductions of from 4 to 5 log10 CFU/ml, and cerebrospinal fluid cultures became sterile for four of six animals treated with each drug.

Topics: Ampicillin; Animals; Cephalosporins; Kinetics; Male; Meningitis, Pneumococcal; Naphthyridines; Rabbits; Streptococcus pneumoniae

The in vitro activities of two new antimicrobial agents, apalcillin and cefpiramide (SM-1652), were evaluated against 324 strains of anaerobic bacteria. Apalcillin (a penicillin derivative) and cefpiramide (a semisynthetic cephalosporin) were compared with piperacillin, moxalactam, and cefoxitin. Organisms studied included the Bacteroides fragilis group, other Bacteroides species, fusobacteria, clostridia, nonsporeforming gram-positive rods, and anaerobic cocci. Piperacillin was found to be the most active overall, inhibiting 96% of the strains tested at its achievable level in serum (128 micrograms/ml). Apalcillin was comparable in activity to piperacillin, inhibiting 93% of anaerobes tested at this concentration. The other antibiotics inhibited ca. 80% of the strains at 32 micrograms/ml. In terms of activities against particular species, apalcillin was active against 75% of B. fragilis group strains and 97 to 100% of all other anaerobes. Cefpiramide inhibited 37% of B. fragilis group strains at 32 micrograms/ml and 68% at 64 micrograms/ml (a level that may be achievable with this drug). Cefpiramide inhibited 92% of all other anaerobes at 32 micrograms/ml and 95% at 64 micrograms/ml. The clostridia other than Clostridium perfringens were the most resistant (84% inhibited at 32 micrograms/ml and 95% inhibited at 64 micrograms/ml).

Topics: Ampicillin; Bacteria, Anaerobic; Cephalosporins; Microbial Sensitivity Tests; Naphthyridines