Skip to main content
NCBI home page
Applied Microbiology logoLink to Applied Microbiology
. 1968 Nov;16(11):1684–1694. doi: 10.1128/am.16.11.1684-1694.1968

Cephalexin and Cephaloglycin Activity In Vitro and Absorption and Urinary Excretion of Single Oral Doses in Normal Young Adults

Peter Braun 1,2, James R Tillotson 1,2,1, Clare Wilcox 1,2, Maxwell Finland 1,2
PMCID: PMC547740  PMID: 4387222

Abstract

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.

Full text

PDF
1684

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Abramowicz M., Klein J. O., Ingall D., Finland M. Levels of penicillin in serum of newborn infants. Am J Dis Child. 1966 Mar;111(3):267–271. doi: 10.1001/archpedi.1966.02090060077006. [DOI] [PubMed] [Google Scholar]
  2. Applestein J. M., Crosby E. B., Johnson W. D., Kaye D. In vitro antimicrobial activity and human pharmacology of cephaloglycin. Appl Microbiol. 1968 Jul;16(7):1006–1010. doi: 10.1128/am.16.7.1006-1010.1968. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Boyer J. L., Andriole V. T. Laboratory and clinical studies of a new antibiotic, cephaloglycin in the treatment of urinary tract infections. Yale J Biol Med. 1968 Feb;40(4):284–295. [PMC free article] [PubMed] [Google Scholar]
  4. Hoeprich P. D. Susceptibility of staphylococci to new antimicrobial agents. Antimicrob Agents Chemother (Bethesda) 1967;7:697–704. [PubMed] [Google Scholar]
  5. Hogan L. B., Jr, Holloway W. J., Jakubowitch R. A. Clinical experience with cephaloglycin. Antimicrob Agents Chemother (Bethesda) 1967;7:624–629. [PubMed] [Google Scholar]
  6. KLEIN J. O., EICKHOFF T. C., TILLES J. G., FINLAND M. CEPHALOTHIN: ACTIVITY IN VITRO, ABSORPTION AND EXCRETION IN NORMAL SUBJECTS AND CLINICAL OBSERVATIONS IN 40 PATIENTS. Am J Med Sci. 1964 Dec;248:640–656. [PubMed] [Google Scholar]
  7. Kislak J. W., Steinhauer B. W., Finland M. Cephaloridine activity in vitro and absorption and urinary excretion in normal young men. Am J Med Sci. 1966 Apr;251(4):433–448. [PubMed] [Google Scholar]
  8. Kunin C. M., Brandt D. Comparative studies of ampicillin, cephalothin and a new cephalosporin derivative, cephaloglycin. Am J Med Sci. 1968 Mar;255:196–201. doi: 10.1097/00000441-196803000-00006. [DOI] [PubMed] [Google Scholar]
  9. Ott J. L., Godzeski C. W. Resistance and cross-resistance of Staphylococcus aureus, Escherichia coli, and Aerobacter species to cephalosporins and semisynthetic penicillins. Antimicrob Agents Chemother (Bethesda) 1966;6:75–81. [PubMed] [Google Scholar]
  10. Pitt J., Siasoco R., Kaplan K., Weinstein L. Antimicrobial activity and pharmacological behavior of cephaloglycine. Antimicrob Agents Chemother (Bethesda) 1967;7:630–635. [PubMed] [Google Scholar]
  11. Ronald A. R., Turck M. Factors influencing in vitro susceptibility to the cephalosporins and clinical trial of an oral cephalosporin, cephaloglycin. Antimicrob Agents Chemother (Bethesda) 1966;6:82–87. [PubMed] [Google Scholar]
  12. Steigbigel N. H., Kislak J. W., Tilles J. G., Finland M. Clinical evaluation of cephaloridine. Arch Intern Med. 1968 Jan;121(1):24–38. [PubMed] [Google Scholar]
  13. WICK W. E., BONIECE W. S. IN VITRO AND IN VIVO LABORATORY EVALUATION OF CEPHALOGLYCIN AND CEPHALORIDINE. Appl Microbiol. 1965 Mar;13:248–253. doi: 10.1128/am.13.2.248-253.1965. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Wick W. E. Cephalexin, a new orally absorbed cephalosporin antibiotic. Appl Microbiol. 1967 Jul;15(4):765–769. doi: 10.1128/am.15.4.765-769.1967. [DOI] [PMC free article] [PubMed] [Google Scholar]

Articles from Applied Microbiology are provided here courtesy of American Society for Microbiology (ASM)

RESOURCES