BMY 28100, a new oral cephalosporin with a (Z)-propenyl side chain at the 3 position and a p-hydroxyphenylglycyl substituent at the 7 position, was evaluated in comparison with cefaclor and cephalexin and, when appropriate, ampicillin and vancomycin. In vitro, BMY 28100 was more active than the reference cephalosporins against streptococci, Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, Haemophilus influenzae, Propionibacterium acnes, Clostridium perfringens, and Clostridium difficile. BMY 28100 was comparable to cefaclor and more active than cephalexin against Staphylococcus saprophyticus and ampicillin-susceptible strains of Branhamella catarrhalis; but against ampicillin-resistant strains of B. catarrhalis, BMY 28100 was comparable to cephalexin and more active than cefaclor. Against Neisseria gonorrhoeae, BMY 28100 was comparable to cephalexin, but less active than cefaclor. Members of the family Enterobacteriaceae overall were equally susceptible to BMY 28100 and cefaclor but were less susceptible to cephalexin. In human serum, BMY 28100 was 45% protein bound. After an oral dose to mice, 82% of the drug was recovered in urine. The oral therapeutic efficacy of BMY 28100 in systemically infected mice reflected its activity in vitro.

BMY 28100, a new oral cephalosporin.

The susceptibility of 269 isolates of Haemophilus influenzae type b to cefatrizine (BL-S640), ampicillin, and chloramphenicol was evaluated by disk diffusion susceptibility tests, using a modified Bauer-Kirby method. Broth dilution susceptibility tests were performed on 88 of these isolates, including all isolates resistant by disk to cefatrizine or ampicillin. Six of the isolates were resistant by disk to cefatrizine (zone size, H. influenzae that were resistant to cefatrizine by disk were resistant to more than 4 μg of drug per ml. The four organisms resistant to ampicillin on disk were resistant, when tested by the broth method, to >128 μg/ml. These four ampicillin-resistant H. influenzae were susceptible to 4 μg of cefatrizine per ml were susceptible to 0.5 and 2 μg of ampicillin, respectively, per ml. The activity of cefatrizine appears to be comparable in vitro to ampicillin against H. influenzae .

Susceptibility of Haemophilus influenzae Type b to Cefatrizine, Ampicillin, and Chloramphenicol

Biological and physicochemical properties of BL-S786 were compared with those of cephalothin, cephaloridine, and cefazolin. With few exceptions, BL-S786 was more active than the reference compounds against major gram-negative pathogenic species and its antibacterial spectrum was broader than that of cephalosporins currently available for clinical use. Although BL-S786 was generally less active than the control cephalosporins against gram-positive pathogens, it inhibited their growth at concentrations that should readily be achieved in humans after standard parenteral dosage. Streptococcus faecalis , a species relatively unsusceptible to cephalosporins in general, was an exception. BL-S786 was an effective bactericidal agent for strains of various gram-negative organisms. After intramuscular administration to mice, BL-S786 achieved high concentrations in blood, and its biological half-life was longer than that of the other three cephalosporins.

Laboratory Evaluation of BL-S786, a Cephalosporin with Broad-Spectrum Antibacterial Activity

Comparative drug disposition studies in mice, rats, dogs, and humans indicate that cephapirin, a new semisynthetic cephalosporin antibiotic that exhibits broad-spectrum antimicrobial activity, is metabolized to desacetylcephapirin in these species. Pharmacokinetic analyses of the concentrations of cephapirin and desacetylcephapirin in plasma and urine reveal that the rate and extent of deacetylation decreases from rodents to dogs to humans. The kinetic analyses also suggest that the kidney performs a role not only in the excretion but also in the metabolism of cephapirin to desacetylcephapirin.

Comparative Pharmacokinetics and Metabolism of Cephapirin in Laboratory Animals and Humans

The in vitro inhibitory activities of cefaclor and cefatrizine, two new orally absorbed cephalosporin antibiotics, against 44 isolates of anaerobic pathogenic bacteria were measured using the agar dilution procedure of the World Health OrganizationInternational Collaborative Study. Tests also were performed with cephalexin, cephaloglycin, and cephadrine, as well as with the parenteral cephamycin antibiotic cefoxitin. Cefoxitin was the most active antibiotic and inhibited the majority of isolates at a concentration of '4 pg/ml. None of the oral cephalosporins was clearly superior against all of the anaerobic isolates; only cephadrine and cefatrizine appeared to have any potential clinical value. Cefaclor (3-chloro-7-D-[2-phenyl-glycemanido]-3cepham-4-carboxylic acid) is a semisynthetic broad-spectrum cephalosporin antibiotic active against both gram-negative and gram-positive bacteria [1]. Metabolic studies in animals have shown that this drug is readily absorbed intact from the gastrointestinal tract [2]. Cefatrizine (7-[D-a,-amino-a- (hydroxylphenyl)acetamido]-3- (1 H,2,3-triazol-5-yl) thio]methyl]-3-cephem-4-carboxylic acid) is another semisynthetic cephalosporin with a similar spectrum of activity and also is absorbed from the gastrointestinal tract of rodents [3, 4]. The purpose of this study was to compare the in vitro activities of these two new orally absorbed cephalosporins with those of other orally absorbed cephalosporins against clinical isolates of anaerobic pathogenic bacteria. The other oral cephalosporins studied, now in clinical use, included cephalexin, cephaloglycin, and cephadrine. Because of its previously demonstrated activity against certain anaerobes [5], cefoxitin, a parenteral cephamycin antibiotic, was included for comparison.

In vitro activities of five oral cephalosporins against aerobic pathogenic bacteria.

The bioavailability and therapeutic properties of BL-S 640 in rodents were compared with those of cephalothin, cephaloridine, and cefazolin after parenteral administration, and cephalexin after oral administration. When given intramuscularly in dosages of 5 to 40 mg/kg, peak concentrations of BL-S 640 in the blood of mice were proportional to dose, but when given orally, they were proportional only up to a dose of 25 mg/kg. After either route of administration, the concentration of BL-S 640 in the blood declined at a slower rate than that of the control compounds. Rats receiving BL-S 640 orally excreted an average of 39% of the drug in the urine. BL-S 640 was highly effective in the treatment of mice infected systemically with a variety of pathogenic bacteria, its therapeutic efficacy in comparison with that of other cephalosporins being frequently in excess of what would have been predicted on the basis of comparative activities in vitro.

BL-S640, a Cephalosporin with a Broad Spectrum of Antibacterial Activity: Bioavailability and Therapeutic Properties in Rodents

Laboratory studies with a new cephalosporanic acid derivative.

BL-S640, a Cephalosporin witha BroadSpectrum of Antibacterial Activity: Bioavailability andTherapeutic Properties inRodents

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BL-S640, a Cephalosporin with a Broad Spectrum of Antibacterial Activity: Bioavailability and Therapeutic Properties in Rodents

Laboratory studies with a new cephalosporanic acid derivative.

BL-S640, a Cephalosporin witha BroadSpectrum of Antibacterial Activity: Bioavailability andTherapeutic Properties inRodents