cefetamet and cefteram

In vitro Ro 15-8074 and Ro 19-5247 (T2525), two new oral cephalosporins, were active against 410 penicillin-susceptible and -resistant isolates of Neisseria gonorrhoeae. Two new macrolides, A-56268 and to a lesser extent roxithromycin (RU 28965), were active against Chlamydia trachomatis. A-56268 had activity against N. gonorrhoeae similar to that of erythromycin.

Topics: Anti-Bacterial Agents; Cefmenoxime; Ceftizoxime; Cephalosporins; Chlamydia trachomatis; Clarithromycin; Erythromycin; Leucomycins; Microbial Sensitivity Tests; Neisseria gonorrhoeae

We examined 300 strains of Neisseria gonorrhoeae and 100 strains of Haemophilus ducreyi to determine their in vitro susceptibility to two new cephalosporins, cefetamet (Ro 15-8074) and ceftetrame (Ro 19-5247; T-2588), and a new fluroquinolone, fleroxacin (Ro 23-6240; AM-833). Their activity was compared with that of ceftriaxone, penicillin, spectinomycin, tetracycline, and erythromycin. Cefetamet, ceftetrame, and fleroxacin had excellent in vitro activity against both groups of microorganisms. beta-Lactamase production did not significantly affect the MICs of these agents. The Mtr phenotype of N. gonorrhoeae raised the MICs two- to fourfold, but the MICs remained within the range of achievable levels in serum. These newer compounds have a distinct advantage over existing therapeutic agents in that they can be administered orally. Clinical trials are warranted to assess their usefulness in the therapy of gonorrhea and chancroid.

Topics: Cefmenoxime; Ceftizoxime; Ceftriaxone; Cephalosporins; Ciprofloxacin; Erythromycin; Fleroxacin; Haemophilus ducreyi; Humans; Neisseria gonorrhoeae; Penicillins; Spectinomycin; Tetracycline

The in vitro activity of RO 15-8074 (cefetamet) and RO 19-5247, new oral cephalosporins, was compared with that of amoxicillin, cephalexin, cefaclor, cefuroxime and erythromycin against 292 clinical isolates using the agar dilution method. Both RO 15-8074 and RO 19-5247 were very active against Proteus mirabilis, Neisseria gonorrhoeae, Haemophilus influenzae and Streptococcus pyogenes, but less active against Staphylococcus saprophyticus and Enterobacter cloacae. RO 19-5247 was more active than RO 15-8074 against Haemophilus influenzae and Streptococcus viridans.

Topics: Amoxicillin; Bacteria; Cefmenoxime; Ceftizoxime; Cephalosporins; Enterobacteriaceae; Erythromycin; Haemophilus influenzae; Microbial Sensitivity Tests; Neisseria gonorrhoeae; Staphylococcus; Streptococcus

We have compared the in-vitro activity of the 4-quinolone Ro 23 6240 and the oral cephalosporins Ro 15 8074 and Ro 19 5247 with that of penicillin, spectinomycin, cefuroxime, ceftriaxone, ciprofloxacin, ofloxacin and norfloxacin against 60 strains of Neisseria gonorrhoeae. MICs 90 against penicillinase producing N. gonorrhoeae (PPNG) and chromosomally-mediated resistant N. gonorrhoeae (CMRNG) respectively were: spectinomycin 16 and 16 mg/l, cefuroxime 0.12 and 1.0 mg/l, ceftriaxone 0.008 and 0.03 mg/l, Ro 15 8074 0.015 and 0.12 mg/l, Ro 19 5247 0.015 and 0.12 mg/l, Ro 23 6240 0.06 and 0.06 mg/l, ciprofloxacin 0.008 and 0.015 mg/l, ofloxacin 0.03 and 0.06 mg/l, norfloxacin 0.06 and 0.12 mg/l. The spectinomycin resistant and spectinomycin-sensitive strains did not differ. All three new agents show good activity against gonococci and warrant further clinical investigation. Ro 23 6240 in common with the other 4-quinolones appears to be as active against gonococcal strains exhibiting non-enzymic chromosomal resistance to penicillin as against PPNG and penicillin-sensitive isolates.

Topics: Anti-Bacterial Agents; Cefmenoxime; Ceftizoxime; Cephalosporins; Ciprofloxacin; Fleroxacin; Neisseria gonorrhoeae; Penicillin Resistance

Topics: Amikacin; Anti-Bacterial Agents; Cefmenoxime; Ceftizoxime; Cephalosporins; Ciprofloxacin; Drug Combinations; Fleroxacin; Mycobacterium; Nontuberculous Mycobacteria; Sulfamethoxazole; Trimethoprim; Trimethoprim, Sulfamethoxazole Drug Combination

Topics: Anti-Bacterial Agents; Cefmenoxime; Ceftizoxime; Ciprofloxacin; Drug Resistance, Microbial; Fleroxacin; Humans; Microbial Sensitivity Tests; Neisseria gonorrhoeae

A total of 629 clinical strains of gram positive and gram negative bacteria were tested for their susceptibility to RO 19-5247, RO 15-8074, and other antimicrobial agents. Both RO 19-5247 and RO 15-8074 had good activity against strains of Enterobacteriaceae; however, resistance was found among some strains of Enterobacter, Citrobacter, Klebsiella and Morganella spp. Both compounds showed moderate to poor active against Acinetobacter spp., Pseudomonas aeruginosa, staphylococci and Streptococcus faecalis. Against strains of Haemophilus influenzae, Neisseria gonorrhoeae, Gardnerella vaginalis, Streptococcus pneumoniae and streptococci (not enterococci), each compound was highly active in vitro. RO 19-5247 and RO 15-8074 had comparable activity to cotrimoxazole, ceftazidime and ceftizoxime. Each new compound had considerably better activity then did cefaclor and amoxicillin/potassium clavulanate.

Topics: Cefmenoxime; Ceftizoxime; Cephalosporins; Drug Resistance, Microbial; Enterobacteriaceae; Gram-Negative Bacteria; Gram-Positive Bacteria; Microbial Sensitivity Tests; Staphylococcus; Streptococcus

The in vitro activities of two new oral cephalosporins, ceftetrame (Ro 19-5247) and cefetamet (Ro 15-8074), were tested against 990 clinical bacterial isolates in comparison with that of cephalexin. Both compounds were more active than cephalexin against gram-negative bacteria, inhibiting most isolates of the family Enterobacteriaceae at concentrations of less than or equal to 4 micrograms/ml, but were not active against Acinetobacter species, most Pseudomonas species, Campylobacter jejuni, and Flavobacterium meningosepticum. Ceftetrame was also more active than cephalexin against most streptococcal isolates and as active as cephalexin against methicillin-susceptible Staphylococcus aureus; against the latter cefetamet was ineffective.

Topics: Bacteria; Cefmenoxime; Ceftizoxime; Cephalexin; Cephalosporins; Microbial Sensitivity Tests

Preliminary interpretive zone criteria were calculated for cefetamet (Ro 15-8074) and cefteram (Ro 19-5247) by using 10- and 30-micrograms disks and three possible MIC susceptibility breakpoints. Absolute interpretive agreement between MICs and zone size criteria ranged from 91.8 to 97.2%. Very major errors (false susceptibility) were less than or equal to 1.2% for both cephalosporin disk tests. Morganella morganii strains appeared to produce the highest rates of very major interpretive errors with cefetamet disks.

Topics: Bacteria; Cefmenoxime; Ceftizoxime; Cephalosporins; Computers; Microbial Sensitivity Tests; Predictive Value of Tests; Regression Analysis

Topics: Aztreonam; Cefmenoxime; Ceftizoxime; Cephalexin; Cephalosporins; Cephradine; Enterobacteriaceae; Pseudomonas

Ceftetrame (Ro 19-5247) and cefetamet (Ro 15-8074), two new orally administered aminothiazolyl imimomethoxy cephalosporins, inhibited hemolytic streptococci and Streptococcus pneumoniae at less than or equal to 0.5 micrograms/ml but were less active against staphylococci than were cephalexin and cefaclor. They did not inhibit S. faecalis, S. faecium, Listeria monocytogenes, Corynebacterium JK species, or Pseudomonas aeruginosa. Haemophilus influenzae, Branhamella catarrhalis, and Neisseria gonorrhoeae, including ampicillin-resistant isolates, were inhibited at less than 0.25 micrograms/ml. Both agents inhibited Escherichia coli, Klebsiella pneumoniae, K. oxytoca, Proteus mirabilis, Salmonella species, Shigella species, Citrobacter diversus, and Aeromonas hydrophila resistant to ampicillin, cephalexin, and cefaclor at less than or equal to 2 micrograms/ml, although many isolates of Enterobacter cloacae, Citrobacter freundii, and Serratia marcescens resistant to cefotaxime were not inhibited by these agents. A marked inoculum effect was noted for Enterobacteriaceae carrying the Richmond-Sykes type 1A chromosomally mediated beta-lactamases, but plasmid-mediated beta-lactamases did not hydrolyze the compounds. Both drugs inhibited the chromosomally mediated beta-lactamase of E. cloacae, P99.

Topics: Bacteria; beta-Lactamases; Cefmenoxime; Ceftizoxime; Cephalosporins; Enzyme Stability; Microbial Sensitivity Tests

The activity of two iminomethoxy aminothiazoly cephalosporins, Ro 15-8074 and Ro 19-5247, was compared with that of other beta-lactams against a total of 491 bacterial strains. Both were highly active (MIC for 90% of the strains tested [MIC 90], less than or equal to 2 micrograms/ml) against the majority of the members of the family Enterobacteriaceae, Haemophilus influenzae, Neisseria spp., and Streptococcus pneumoniae, being at least 16-fold more active than cephalexin and 8-fold more active than cefuroxime. There was no activity against Pseudomonas aeruginosa and poor activity against Morganella morganii (in the case of Ro 15-8074), Enterobacter sp., and Citrobacter sp. Staphylococcus aureus was moderately susceptible to Ro 19-5247 (MIC90, 8 micrograms/ml), but Ro 15-8074 was eightfold less active. The protein binding of the two compounds at 5 micrograms/ml was 9.1% for Ro 15-8074 and 69.9% for Ro 19-5247. The major target site for the two cephalosporins was PBP 3.

Topics: Bacteria; Blood Proteins; Cefmenoxime; Ceftizoxime; Cephalosporins; Culture Media; Microbial Sensitivity Tests; Protein Binding

The in vitro activities of two new oral cephalosporins, Ro 19-5247 and Ro 15-8074, were compared with the in vitro activities of cefuroxime, cefaclor, amoxicillin-clavulanate, trimethoprim-sulfamethoxazole (TMP-SMZ), and doxycycline against a variety of bacterial species. MIC50s (MICs required to inhibit 50% of strains) of Ro 19-5247 were less than or equal to 0.13 micrograms/ml for streptococci (except Streptococcus faecalis) and Haemophilus influenzae; 0.25 to 2 micrograms/ml for most strains of Enterobacteriaceae, Aeromonas hydrophila, Branhamella catarrhalis, and gram-positive anaerobic bacteria; and 1 to 8 micrograms/ml for methicillin-susceptible staphylococci. MIC50s of Ro 15-8074 were similar to those of Ro 19-5247, except that gram-positive aerobes and anaerobes were less susceptible. Both Ro 19-5247 and Ro 15-8074 had greater in vitro activity against strains of Enterobacteriaceae than did comparative beta-lactams and doxycycline; TMP-SMZ had the broadest spectrum of activity against these organisms. None of the cephalosporins were active against methicillin-resistant staphylococci, S. faecalis, most nonfermenters, or Bacteroides sp. Inoculum size variations affected MICs in a species-dependent manner for beta-lactams and unpredictably for TMP-SMZ but had little effect for doxycycline. Bactericidal activity was consistent with beta-lactams, inconsistent with TMP-SMZ, and uncommon with doxycycline.

Topics: Anti-Bacterial Agents; Bacteria; Cefmenoxime; Ceftizoxime; Cephalosporins; Microbial Sensitivity Tests