[In vitro and in vivo antibacterial activities of sulopenem, a new penem antibiotic].
The in vitro and in vivo antibacterial activities of sulopenem, a new penem, were evaluated in comparison with imipenem (IPM), meropenem (MEPM), ceftazidime (CAZ) and flomoxef (FMOX). Sulopenem had broad and potent antibacterial spectra against Gram-positive and Gram-negative bacteria, including Enterococcus faecalis, Proteus vulgaris, Morganella morganii, Enterobacter spp. and Citrobacter freundii. Sulopenem showed concentration-dependent bactericidal activities against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae and Acinetobacter calcoaceticus. Morphological observation using phase-contrast microscope revealed that sulopenem induced spherical cell formation with E. coli and K. pneumoniae at lower concentrations and bacteriolysis at higher concentrations. Therapeutic efficacies of sulopenem against systemic infections in mice were almost equal to those of imipenem against Streptococcus pneumoniae. While its therapeutic efficacies were superior to those of meropenem, ceftazidime and flomoxef against S. aureus and S. pneumoniae, they were inferior to those of imipenem/cilastatin against S. aureus, K. pneumoniae and A. calcoaceticus.
Komoto
A
A
Department of Microbiology, Kyoto Pharmaceutical University, Japan.
Otsuki
M
M
Nishino
T
T
D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001424:Bacterial Infections / Q000188:drug therapy; D002442:Ceftazidime / Q000494:pharmacology; D002511:Cephalosporins / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D015378:Imipenem / Q000494:pharmacology; D007769:Lactams; D008297:Male; D000077731:Meropenem; D051379:Mice; D013845:Thienamycins / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D002511:Cephalosporins; D007769:Lactams; D013845:Thienamycins; C082897:sulopenem; D015378:Imipenem; D002442:Ceftazidime; D000077731:Meropenem; C045693:flomoxef