In vitro activity of apalcillin compared with that of other new penicillins and anti-Pseudomonas cephalosporins.
Apalcillin, a naphthydridine derivative of ampicillin, was compared with ticarcillin, azlocillin, mezlocillin, piperacillin, cefotaxime, and cefoperazone against gram-negative and gram-positive bacterial isolates and with cefsulodin and tobramycin against Pseudomonas aeruginosa. The minimal concentrations of apalcillin at which 50 and 90% of hospital isolates of Escherichia coli were inhibited were similar to those of mezlocillin and piperacillin (1.6 and 100 micrograms/ml, respectively). Apalcillin had minimal inhibitory concentrations similar to those of piperacillin against Citrobacter freundii and Citrobacter diversus. Against Klebsiella, apalcillin inhibited 50% of organisms at a concentration of 6.3 micrograms/ml, similar to piperacillin. The activity of apalcillin against Enterobacter (E. aerogenes, E. cloacae, and E. agglomerans) was similar to that of mezlocillin and piperacillin and greater than that of ticarcillin. The activity of apalcillin against Proteus mirabilis was similar to that of the other agents, as was its activity against indole-positive Proteus and Providencia. Only 40% of Serratia were inhibited at an apalcillin concentration of 25 micrograms/ml. Apalcillin was as active as piperacillin but twofold less active than cefoxitin or moxalactam against Bacteroides fragilis. It was as active as piperacillin, cefoperazone, and cefsulodin against P. aeruginosa (apalcillin inhibited 90% of organisms at a concentration of 25 mg/ml). There was an inoculum effect and a difference in the minimal inhibitory concentration and minimal bactericidal concentration with beta-lactamase strains. Apalcillin was hydrolyzed by plasmid beta-lactamase but not as well by cephalosporinases.
D000667:Ampicillin / Q000031:analogs & derivatives* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D002511:Cephalosporins / Q000494:pharmacology*; D004355:Drug Stability; D004755:Enterobacteriaceae / Q000187:drug effects; D006190:Haemophilus / Q000187:drug effects; D009287:Naphthyridines; D009343:Neisseria / Q000187:drug effects; D010406:Penicillins / Q000494:pharmacology*; D011549:Pseudomonas / Q000187:drug effects; D001618:beta-Lactamases / Q000378:metabolism
D002511:Cephalosporins; D009287:Naphthyridines; D010406:Penicillins; C012122:apalcillin; D000667:Ampicillin; D001618:beta-Lactamases