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Applied Microbiology Nov 1968A large number of recently isolated bacterial pathogens were tested for susceptibility to cephalexin and cephaloglycin by the replica inoculating method. Strains of...
A large number of recently isolated bacterial pathogens were tested for susceptibility to cephalexin and cephaloglycin by the replica inoculating method. Strains of group A hemolytic streptococci, viridans (alpha and gamma) streptococci, pneumococci, gonococci, meningococci, and penicillin G-sensitive Staphylococcus aureus were all moderately to highly susceptible to both of these cephalosporin analogues, nearly all of the strains being two to eight (median four) times more susceptible to cephaloglycin than to cephalexin. The penicillin G-resistant, penicillinase-producing strains of S. aureus varied in their susceptibility; many were moderately resistant to both analogues, particularly to cephalexin. Strains of enterococci, Haemophilus influenzae, and most of the common gram-negative bacilli were moderately to highly resistant. Reducing the size of the inoculum had variable effects on inhibition by these drugs, depending on the species or strain. The activity of cephalexin was very little affected by pH of the medium within the clinical range or by incubation at 37 C in broth for up to 24 hr. In contrast, cephaloglycin in broth deteriorated rapidly at 37 C, and its activity was markedly reduced in alkaline medium. Both cephalexin and cephaloglycin were rapidly absorbed and excreted into the urine after single oral doses of 500 mg. Much higher levels were achieved and sustained with the former. Absorption of both analogues was delayed when taken with food, and the levels in the serum were significantly higher and better sustained when probenecid was also given. Very high concentrations of cephalexin were excreted into the urine during the first 4 hr, and the levels were still high in the 4- to 8-hr collection. The concentrations of cephaloglycin in the urine at these times were much lower. An average of 80 to 93% of the dose of cephalexin and 25 to 30% of the cephaloglycin were accounted for as active drug in the urine collected in 8 hr. Both analogues were well tolerated.
Topics: Adult; Cephalosporins; Enterobacteriaceae; Escherichia coli; Haemophilus influenzae; Humans; In Vitro Techniques; Klebsiella; Neisseria gonorrhoeae; Neisseria meningitidis; Penicillin Resistance; Proteus; Pseudomonas aeruginosa; Serratia marcescens; Staphylococcus; Streptococcus; Streptococcus pneumoniae
PubMed: 4387222
DOI: 10.1128/am.16.11.1684-1694.1968 -
Applied Microbiology Jul 1968Serum and urine concentrations of cephaloglycin (an orally absorbed derivative of cephalosporin C) were determined in normal volunteers and in patients. The in vitro...
Serum and urine concentrations of cephaloglycin (an orally absorbed derivative of cephalosporin C) were determined in normal volunteers and in patients. The in vitro activity of cephaloglycin was also studied. All strains of group A streptococci (Streptococcus pyogenes) and Diplococcus pneumoniae were inhibited by 0.4 mug of cephaloglycin per ml. Eighty per cent of the Staphylococcus aureus strains and about 50% of the Escherichia coli and Proteus mirabilis strains were inhibited by 1.6 mug of cephaloglycin per ml. Klebsiella-Aerobacter species were more resistant to cephaloglycin and 12.5 mug per ml was required to inhibit 70% of these strains. When single doses of 250, 500, or 1,000 mg of cephaloglycin were administered to fasting volunteers, a peak serum concentration of at least 0.5 mug per ml was achieved. A full breakfast did not interfere with absorption of cephaloglycin. Probenecid enhanced both the peak serum concentration and the duration of antibiotic activity in the serum. Serum concentrations of cephaloglycin were even higher in patients who were receiving repeated doses. The peak serum concentrations of cephaloglycin in all volunteers and patients were adequate to inhibit all strains of group A streptococci and D. pneumoniae. Many of the peak serum concentrations were adequate to inhibit some strains of S. aureus, E. coli, and P. mirabilis. Urine levels of cephaloglycin were high enough in all volunteers and patients to inhibit more than 90% of the E. coli and P. mirabilis strains and over 70% of the strains of Klebsiella-Aerobacter.
Topics: Bacteria; Cephalosporins; Enterobacter; Escherichia coli; Humans; Klebsiella; Probenecid; Proteus; Staphylococcus; Streptococcus pneumoniae; Streptococcus pyogenes; Urinary Tract Infections
PubMed: 4385749
DOI: 10.1128/am.16.7.1006-1010.1968 -
The Journal of Antibiotics Feb 1980Metabolism and pharmacokinetics of cephaloglycin in man were investigated. High performance liquid chromatographic and gas chromatographic-mass spectrometric analyses of...
Metabolism and pharmacokinetics of cephaloglycin in man were investigated. High performance liquid chromatographic and gas chromatographic-mass spectrometric analyses of metabolites excreted in human urine following oral administration of cephaloglycin revealed that cephaloglycin was biotransformed in two pathways i.e. elimination of 3-acetyl group and hydrolysis of side chain amide linkage. The former yielded deacetylcephaloglycin, a part of which further underwent lactonization to deacetylcephaloglycin lactone, and the latter led to benzoyl formic acid via phenylglycine. The urinary excretion amounts of these metabolites and intact cephaloglycin were determined by a reversed phase ion pair high performance liquid chromatography. The average total excretion amounts at infinite time accounted for 0.50% of the administered dose for intact cephaloglycin, 17.09% for deacetylcephaloglycin, 0.35% for deacetylcephaloglycin lactone, and 0.86% for benzoyl formic acid. The excretion of phenylglycine was less than 0.2%, its chromatographic peak being too small to allow accurate determination. The rate constants for absorption, metabolism, and urinary excretion were estimated by the moment analysis of the excretion rate-time curves.
Topics: Adult; Biotransformation; Cephaloglycin; Chromatography, High Pressure Liquid; Gas Chromatography-Mass Spectrometry; Humans; Kinetics; Male
PubMed: 7380734
DOI: 10.7164/antibiotics.33.236 -
Applied Microbiology Mar 1965Two new antibiotics, structurally related to cephalothin, have been given the generic names cephaloglycin and cephaloridine. Cephaloglycin is the dipolar ion of...
Two new antibiotics, structurally related to cephalothin, have been given the generic names cephaloglycin and cephaloridine. Cephaloglycin is the dipolar ion of 7-(d-alpha-aminophenylacetamido)-cephalosporanic acid. Cephaloridine is 7-[alpha-(2-thiophene)acetamido]-3-(1-pyridylmethyl)-3-cephem-4-carboxylic acid betaine. These new compounds were evaluated simultaneously. The broad spectrum of activity observed in vitro and in vivo with both antibiotics, the good oral absorption obtained with cephaloglycin, and the stability of cephaloridine are emphasized. The data suggest that both antibiotics merit clinical trial in humans.
Topics: Alcaligenes; Anti-Bacterial Agents; Bacillus subtilis; Blood Chemical Analysis; Cephaloglycin; Cephaloridine; Cephalothin; Chemical Phenomena; Chemistry; Chromatography; Clostridium tetani; Corynebacterium diphtheriae; Drug Resistance; Drug Resistance, Microbial; Enterobacter; Enterobacteriaceae; Escherichia coli; Haemophilus; In Vitro Techniques; Klebsiella; Mice; Neisseria gonorrhoeae; Neisseria meningitidis; Pharmacology; Proteus; Pseudomonas; Pseudomonas aeruginosa; Research; Salmonella; Shigella; Staphylococcus; Streptococcus; Streptococcus pneumoniae; Toxicology
PubMed: 14325888
DOI: 10.1128/am.13.2.248-253.1965 -
The Journal of Antibiotics Jan 1969
Topics: Animals; Anti-Bacterial Agents; Bile; Carbon Isotopes; Chromatography, Paper; Feces; Formates; Injections, Intraperitoneal; Intestinal Absorption; Mandelic Acids; Rats
PubMed: 5768560
DOI: 10.7164/antibiotics.22.27 -
Applied Microbiology Mar 1971Chromatographic studies and microbiological assays show that, after oral administration, cephaloglycin is partially converted in man to a biologically active metabolite... (Comparative Study)
Comparative Study
Chromatographic studies and microbiological assays show that, after oral administration, cephaloglycin is partially converted in man to a biologically active metabolite desacetylcephaloglycin. The antibacterial activity of this metabolite compared to that of cephaloglycin is equivalent against gram-positive organisms but is lower against gram-negative bacilli. Successful therapy of urinary tract infections with cephaloglycin must be mainly attributed to the antibacterial activity of this metabolite. At the present time, it is not possible to assess what influence low amounts of unaltered cephaloglycin have on the outcome of therapy.
Topics: Administration, Oral; Animals; Bacillus subtilis; Bacteria; Biological Assay; Cephalosporins; Chromatography, Paper; Disease Models, Animal; Drug Resistance, Microbial; Drug Stability; Human Experimentation; Humans; Male; Mice; Microbial Sensitivity Tests; Sarcina; Species Specificity; Temperature; Urinary Tract Infections
PubMed: 4994901
DOI: 10.1128/am.21.3.426-434.1971 -
Applied Microbiology Aug 1968Thin-layer and paper chromatographic systems were used to detect and determine the concentration of cephaloglycin and its biologically active metabolites in serum and...
Thin-layer and paper chromatographic systems were used to detect and determine the concentration of cephaloglycin and its biologically active metabolites in serum and urine. Data are presented on the procedures, solvent systems, and specific techniques used in this evaluation.
Topics: Biological Assay; Cephalosporins; Chromatography, Paper; Chromatography, Thin Layer; Sarcina
PubMed: 5675503
DOI: 10.1128/am.16.8.1132-1133.1968 -
Applied Microbiology Jul 1967A new antibiotic, structurally related to cephaloglycin, has been assigned the generic name cephalexin,...
A new antibiotic, structurally related to cephaloglycin, has been assigned the generic name cephalexin, 7-(D-alpha-amino-alpha-phenylacetamido)-3-methyl-3-cephem-5-carboxylic acid. In vitro antimicrobial activity of cephalexin does not equal that of cephaloglycin. However, excellent oral absorption and lack of serum binding of cephalexin compensates significantly for the lower in vitro activity. Exceptional efficacy against experimental bacterial infections in mice was obtained with cephalexin therapy as compared with cephaloglycin, tetracycline, and chloramphenicol. The data suggest that cephalexin merits clinical trial.
Topics: Alcaligenes; Animals; Cephalosporins; Chloramphenicol; Clostridium; Corynebacterium; Enterobacteriaceae; Mice; Neisseria; Pseudomonas; Staphylococcus; Streptococcus; Streptococcus pneumoniae; Tetracycline
PubMed: 4383049
DOI: 10.1128/am.15.4.765-769.1967 -
Antimicrobial Agents and Chemotherapy Jan 1977The antibiotic activity of cephalothin, cephaloridine, cephalexin, cephaloglycin, cefazolin, and cefamandole was determined after storage for up to 30 days in horse...
The antibiotic activity of cephalothin, cephaloridine, cephalexin, cephaloglycin, cefazolin, and cefamandole was determined after storage for up to 30 days in horse serum at -10 and 4 degrees C. Cephalothin, cefamandole, cefazolin, and cephalexin were stable for at least 30 days at -10 degrees C, whereas cephaloridine lost 29% of its initial activity and cephaloglycin lost more than 50%. Cefamandole, cefazolin, and cephalexin could only be stored for 3 days at 4 degrees C without significant loss in activity, whereas cephalothin, cephaloridine, and cephaloglycin could be stored for only 1 day. Repeated freezing and thawing had a detrimental effect on the stability of cephaloridine.
Topics: Animals; Bacillus subtilis; Blood; Cephalosporins; Culture Media; Drug Stability; Horses; Sarcina; Temperature
PubMed: 402105
DOI: 10.1128/AAC.11.1.174 -
Kidney International Nov 1980
Comparative Study
Topics: Animals; Biological Transport, Active; Cefazolin; Cephaloglycin; Cephaloridine; Dose-Response Relationship, Drug; Guinea Pigs; Humans; Kidney Cortex; Kidney Diseases; Kidney Tubules; Mitochondria; Rabbits; Rats
PubMed: 7463955
DOI: 10.1038/ki.1980.177