Multicenter comparison of in vitro activities of FK-037, cefepime, ceftriaxone, ceftazidime, and cefuroxime

Abstract

In a multicenter study, the MICs of FK-037 for 90%o of the strains tested (MIC90s) were <1 ,ug/ml for members of the family Enterobacteriaceae other than Citrobacter freundii, Enterobacter spp., and Serratia marcescens. Activity against Pseudomonas aeruginosa was variable, with a MIC50 and a MIC,0 of 4 and 32 ,ug/ml, respectively. Relative to cefepime, however, FK-037 was less active against ceftazidime-resistant isolates of Enterobacter cloacae. The MIC,0 of FK-037 for methicillin-resistant staphylococci was >16 ,ug/ml.FK-037 is a novel injectable oxime-type cephalosporin antibiotic with a 1-hydroxyethyl-5-aminopyrazole moiety at the three position (15). Data presented in abstracts in 1991 and 1992 suggested that FK-037 was more active than currently available extended-spectrum cephalosporins against staphylococci, including methicillin-resistant strains (5,12,15); however, at four times its MIC, FK-037 reduced the number of CFU of methicillin-resistant Staphylococcus aureus by only 1 order of magnitude while vancomycin reduced the number of CFU by over 3 orders of magnitude in killing curve studies (1). In studies by Neu et al. (14), 16 ,ug of FK-037 per ml inhibited 50% of the S. aureus isolates tested with oxacillin MICs of >16 ,ug/ml. FK-037 has also been reported to have a broad spectrum of activity against gram-negative bacilli, including members of the family Enterobacteriaceae and Pseudomonas aeruginosa, and to be active against many ceftazidime-resistant isolates of Citrobacter spp., Enterobacter spp., and P. aeruginosa (2, 4-7, 11, 13, 16

Effectiveness of short-course therapy (5 days) with cefuroxime axetil in treatment of secondary bacterial infections of acute bronchitis

“…The broad-spectrum antibacterial activity of cefuroxime axetil, including excellent activity against the major bacterial pathogens of the lower respiratory tract (17,23,24,39), as well as its high degree of stability to ␤-lactamases (12,40), supports its use in the treatment of this lower respiratory tract infection. In addition, the potential lower cost of a 5-day cefuroxime axetil regimen and the increased likelihood that patients will complete the entire prescribed therapy regimen of shorter duration make it a valuable therapeutic option in the treatment of acute bronchitis.…”

“…39,1995 SHORT-COURSE CEFUROXIME AXETIL IN ACUTE BRONCHITIS 2529 fection (no eradication of initial pathogen plus isolation of at least one new pathogen requiring additional or alternate therapy).…”

“…Cefuroxime is characterized by stability to ␤-lactamases (9) and demonstrates favorable in vitro activity against a wide range of gram-positive and gram-negative organisms (both ␤-lactamase producing and nonproducing), including the bacterial pathogens commonly associated with acute bronchitis (17,23,24,39). Amoxicillin, in combination with the ␤-lactamase inhibitor clavulanate potassium (Augmentin; SmithKline Beecham, Philadelphia, Pa.), is similarly active in vitro against both ␤-lactamase-producing and non-␤-lactamase-producing strains of common respiratory pathogens (37).…”

Laboratory assessment of antibacterial activity of zwitterionic 7-methoxyimino cephalosporins

“…The newer compounds have not yet been compared in the same study. Overall, cefpirome, cefepime and cefclidin seem to display similar activities against Enterobacteriacea which produce Class 1 /Mactamase, while FK037 and DQ2556 appear to be slightly less active than cefpirome or cefepime (Fujimoto etal., 1990;Jones et al, 1991 b;Tanaka et al, 1992;Fu et al, 1993;Washington et al, 1993).…”

“…The zwitterionic 7-methoxyimino cephalosporins are active against strains which synthesise the Bush type 2b /Mactamases (TEM-1, TEM-2, SHV-1), but, overall, resistance to cefepime, cefpirome, cefclidin and FKO37 is enhanced in strains which (Jones et al, 1991) (Fnetal., 1993) (Washington et al, 1993) 3.13 (Watanabe et al, 1988) produce extended spectrum /Mactamases; MIC<8 mg/L have been recorded in most cases, i.e. lower than those of ceftazidime (Jacoby & Can-eras, 1990;Jones et al, 1991a;Neu, Chin & Huang, 1993).…”