Reference

In vitro activity and stability against novel beta-lactamases of investigational beta-lactams (cefepime, cefpirome, flomoxef, SCE 2787 and piperacillin plus tazobactam) in comparison with established compounds (cefotaxime, latamoxef and piperacillin)

In vitro activity and stability against novel beta-lactamases of investigational beta-lactams (cefepime, cefpirome, flomoxef, SCE 2787 and piperacillin plus tazobactam) in comparison with established compounds (cefotaxime, latamoxef and piperacillin). Bauernfeind, A.; Schweighart, S.; Eberlein, E.; Jungwirth, R. (Max von Pettenkofer-Inst., Munich W-8000, Germany). Infection (Munich), 19(Suppl. 5), S264-S275 (English) 1991. CODEN: IFTNAL. ISSN: 0300-8126. 113359-04-9 and 88040-23-7 are also occured in this study. DOCUMENT TYPE: Journal CA Section: 10 (Microbial, Algal, and Fungal Biochemistry) The therapeutic perspectives of flomoxef, SCE 2787, cefpirome, cefepime, latamoxef, cefotaxime and of piperacillin plus tazobactam were comparatively evaluated by their in vitro activity against 1119 clin. isolates of 83 bacterial species. Escherichia coli, Klebsiella spp., Enterobacter sakazakii, Proteus spp. and Shigella spp. were about equally susceptible to the cephalosporins (MIC90: 0.06 to 0.5 mg/L), while the MIC90 for piperacillin plus tazobactam was between 2 and 16 mg/L. Enterobacter cloacae, Enterobacter aerogenes and Serratia spp. were most susceptible to SCE 2787, cefpirome and cefepime (MIC90: 0.06 to 2 mg/L) followed by latamoxef, cefotaxime, flomoxef and piperacillin plus tazobactam. For Citrobacter spp., Providencia spp. and Yersinia enterocolitica, MIC90 were between 0.06 and 0.5 mg/L. Flomoxef was between 2 and 4 log2 less active against these species but more active than piperacillin plus tazobactam (MIC90: 2 and 8 mg/L). Morganella morganii and Hafnia alvei were most susceptible to cefepime, cefpirome and latamoxef (MIC90: 0.13 to 0.5 mg/L), while cefotaxime (MIC90: 8 mg/L) and piperacillin plus tazobactam (MIC90: 8 and >64 mg/L) were the least active compds. SCE 2787, cefepime and cefpirome were the most potent beta-lactams against the majority of the 13 species of non-fermentative bacilli (NFB) investigated (MIC90: 0.5 to 16 mg/L). The oxacephems were the least active compds. against NFB. Cefepime was the most active of the compds. included against Pseudomonas aeruginosa (MIC90: 16 mg/L). Haemophilus spp., Neisseria gonorrhoeae and Bordetella pertussis were most susceptible to cefotaxime (MIC90: 0.03 to 0.06 mg/L). Latamoxef had the lowest activity of all compds. against gram-pos. cocci. Flomoxef was the most active compd. against penicillinase producing Staphylococcus aureus and about equally active as the other betalactams against methicillin susceptible staphylococci of other staphylococcal species. Non-enterococcal streptococci had MIC90 between 0.03 and 0.5 mg/L for all. Streptococcus pneumoniae with MICs for penicillin equal to or above 1 mg/L were between 16 and 64 times less susceptible (MIC90: between 0.5 and 4 mg/L) than penicillin-susceptible organisms (MIC90: between 0.03 and 0.13 mg/L). Flomoxef and piperacillin plus tazobactam were the most active of the compds. against anaerobic organisms. The oxacephem flomoxef was the most stable of the compds. included against novel extended broad spectrum beta-lactamases (TEM-3 to TEM-7, SHV-2 to SHV-5, CMY-1, CTX-M-1) followed by latamoxef. However, both oxacephamycins are hydrolyzed by cephamycinases while SCE 2787, cefepime and cefpirome are stable against cephamycinases. Progress in antibacterial activity of parenteral cephalosporins was achieved both by structural modification (of latamoxef or cefotaxime) and combination of piperacillin with tazobactam. Flomoxef in comparison with latamoxef extended its spectrum to include staphylococci and increased activity against non-enterococcal streptococci 16 to 32 times. The various structural modifications of cefotaxime at position 3 of the cephalosporin ring improved the antibacterial profile of SCE 2787, cefepime and cefpirome in very much the same way (enhanced activity mainly against organisms producing chromosomal cephalosporinases, e.g. Enterobacter spp., Serratia spp., H. alvei, M. morganii and non-fermentative bacilli). Tazobactam protects piperacillin against plasmidic beta-lactamases; however, this was achieved to an even higher extent by the structural modifications of aminothiazole-methoximino cephalosporins (SCE 2787, cefepime and cefpirome) and in particular of flomoxef. .

Combination effect of SCE-2787 and cefepime with aminoglycosides on nosocomial gram-negative bacteria

Combination effect of SCE-2787 and cefepime with aminoglycosides on nosocomial gram-negative bacteria. Huebner, J.; Hartung, D.; Kropec, A.; Daschner, F. D. (Klinikhyg., Universitaetsklin.Chemicals with cas numbers 113359-04-9 and 88040-23-7 also play role., Freiburg W-7800, Germany). Infection (Munich), 19(3), 186-9 (English) 1991. CODEN: IFTNAL. ISSN: 0300-8126. DOCUMENT TYPE: Journal CA Section: 10 (Microbial, Algal, and Fungal Biochemistry) The in vitro activity of cefepime and SCE-2787, two new parenteral cephalosporins, and the combination effect with tobramycin and gentamicin against nosocomial gram-neg. rods were studied using checkerboard agar diln. technique. Cefepime showed excellent in-vitro activity against Klebsiella pneumoniae, Enterobacter cloacae, Serratia marcescens and Proteus vulgaris (MIC90 0.03-0.125 mg/L) and good to moderate activity against Acinetobacter anitratus, Pseudomonas aeruginosa and Pseudomonas cepacia (MIC90 4-16 mg/L). SCE-2787 had an excellent activity against Citrobacter spp. (MIC90 0.125 mg/L) and a very good activity against A. anitratus, P. aeruginosa and P. vulgaris (MIC90 1-2 mg/L). Pseudomonas maltophilia was not inhibited at therapeutically achievable concns. (MIC90 64 mg/L). On av., 14-28% of the strains were inhibited by synergistic SCE-2787 aminoglycoside-combinations, whereas only 8.6% were inhibited by a synergistic effect of the combination with cefepime and gentamicin. No antagonism occurred with any of the combinations. .