Skip to main content
SpringerLink
Log in

In vitro antibacterial properties of cefetamet and in vivo activity of its orally absorbable ester derivative, cefetamet pivoxil

  • New Antimicrobial Agents
  • Published:
European Journal of Clinical Microbiology and Infectious Diseases Aims and scope Submit manuscript

Abstract

The in vitro activity of cefetamet, the microbiologically active metabolite of the orally administered prodrug cefetamet pivoxil, was compared with that of cephalexin, cefaclor, cefuroxime and amoxicillin. Cefetamet was highly active againstEnterobacteriaceae, Neisseria spp.,Vibrio spp.,Haemophilus influenzae and streptococci other than enterococci. Cefetamet inhibited cefaclor-resistant species such asProteus vulgaris, Providencia stuartii, Providencia rettgeri andSerratia marcescens. Staphylococci,Pseudomonas aeruginosa and cephalosporinase-overproducing strains ofEnterobacter cloacae were resistant to cefetamet. The superior activity of cefetamet compared with older oral beta-lactam antibiotics against a large number of gram-negative pathogens correlated with enhanced stability towards betalactamases. In accordance with the in vitro findings, cefetamet pivoxil showed good activity in experimental infections in the mouse and rat, suggesting satisfactory bioavailability in these animals after oral administration.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  1. Heymès, R., Lutz, A., Schrinner, E.: Experimental evaluation of HR 756, a new cephalosporin derivative. Infection 1977, 5: 259–260.

    Article  PubMed  Google Scholar 

  2. Matsubara, N., Minami, S., Muraoka, T., Saikawa, I., Mitsuhashi, S.: In vitro antibacterial activity of cefoperazone (T-1551), a new semisynthetic cephalosporin. Antimicrobial Agents and Chemotherapy 1979, 16: 731–735.

    PubMed  Google Scholar 

  3. O'Callaghan, C. H., Acred, P., Harper, P. B., Ryan, D. M., Kirby, S. M., Harding, S. M.: GR 20263, a new broad-spectrum cephalosporin with anti-pseudomonal activity. Antimicrobial Agents and Chemotherapy 1980, 17: 876–883.

    PubMed  Google Scholar 

  4. Angehrn, P., Probst, P. J., Reiner, R., Then, R. L.: Ro 13-9904, a long-acting broad-spectrum cephalosporin: in vitro and in vivo studies. Antimicrobial Agents and Chemotherapy 1980, 18: 913–921.

    PubMed  Google Scholar 

  5. Harding, S. M., Williams, P. E. O., Ayrton, J.: Pharmacology of cefuroxime as the 1-acetoxyethyl ester in volunteers. Antimicrobial Agents and Chemotherapy 1984, 25: 78–82.

    PubMed  Google Scholar 

  6. Kamimura, T., Kojo, H., Matsumoto, Y., Mine, Y., Goto, S., Kuwahara, S.: In vitro and in vivo antibacterial properties of FK 027, a new orally active cephem antibiotic. Antimicrobial Agents and Chemotherapy 1984, 25: 98–104.

    PubMed  Google Scholar 

  7. Okamoto, S., Hamana, Y., Inoue, M., Mitsuhashi, S.: In vitro and in vivo antibacterial activities of T-2588, a new oral cephalosporin, compared with those of other oral beta-lactam antibiotics. Antimicrobial Agents and Chemotherapy, 1987, 31: 1111–1116.

    PubMed  Google Scholar 

  8. Hamashima, Y., Kubota, T., Minami, K., Ishikura, K., Konoike, T., Yoshioka, M.: Synthesis and biological properties of 7β-[(Z)-2-(2-amino-4-thiazolyl)-4-carboxy-2-butenoylamino]-3-cephem-4-carboxy-2-butenoylamino]-3-cephem-4-carboxylic acid (7432-S), a new oral cephem antibiotic. Journal of Antibiotics 1987, 40: 1468–1470.

    PubMed  Google Scholar 

  9. Utsui, Y., Inoue, M., Mitsuhashi, S.: In vitro and in vivo antibacterial activities of CS-807, a new oral cephalosporin. Antimicrobial Agents and Chemotherapy 1987, 31: 1085–1092.

    PubMed  Google Scholar 

  10. Koup, J. R., Dubach, U. C., Brandt, R., Wyss, R., Stoeckel, K.: Pharmacokinetics of cefetamet (Ro 15-8074) and cefetamet pivoxil (Ro 15-8075) after intravenous and oral doses in humans. Antimicrobial Agents and Chemotherapy 1988, 32: 573–579.

    PubMed  Google Scholar 

  11. Peeters, M., Piot, P.: In vitro activity of Ro 15-8074, a new oral cephalosporin. Journal of Antimicrobial Chemotherapy 1985, 16: 469–473.

    PubMed  Google Scholar 

  12. Neu, H. C., Chin, N.-X., Labthavikul, P.: In vitro activity and β-lactamase stability of two oral cephalosporins, cefetrame (Ro 19-5247) and cefetamet (Ro 15-8074). Antimicrobial Agents and Chemotherapy 1986, 30: 423–428.

    PubMed  Google Scholar 

  13. Then, R. L., Kohl, I.: Affinity of carumonam for penicillin-binding proteins. Chemotherapy 1985, 31: 246–254.

    PubMed  Google Scholar 

  14. Then, R. L.: Interaction of two new cephalosporins, cefetamet and cefteram, with beta-lactamases and penicillin binding proteins. In: Berkarda, B., Kuermmerle, H. P. (ed.): Progress in Antimicrobial and Anticancer Chemotherapy I. Ecomed, Landsberg, 1987, p. 185–187.

    Google Scholar 

  15. Then, R. L.: Ability of newer beta-lactam antibiotics to induce beta-lactamase production inEnterobacter cloacae. European Journal of Clinical Microbiology 1987, 6: 451–455.

    PubMed  Google Scholar 

  16. Then, R. L.: Interaction of Ro 17-2301 (AMA-1080) with β-lactamases. Chemotherapy 1984, 30: 398–407.

    PubMed  Google Scholar 

  17. Stobberingh, E. E., Wundernik, M., Philips, M., Houben, A.:Branhamella catarrhalis: beta-lactamase production and sensitivity to oral antibiotics, including new cephalosporins. Journal of Antimicrobial Chemotherapy 1987, 20: 765–770.

    PubMed  Google Scholar 

  18. Wise, R., Andrews, M. J., Piddock, L. J. V.: In vitro activity of Ro 15-8074 and Ro 19-5247, two orally administered cephalosporin metabolites. Antimicrobial Agents and Chemotherapy 1986, 29: 1067–1072.

    PubMed  Google Scholar 

  19. Fass, R. J., Helsel, V. L.: In vitro activities of Ro 19-5247 and Ro 15-8074, new oral cephalosporins. Antimicrobial Agents and Chemotherapy 1986, 30: 429–434.

    PubMed  Google Scholar 

  20. Jones, R. N., Fuchs, P. C., Barry, L., Ayers, L. W., Gerlach, E. H., Gavan, T. L.: Antimicrobial activity of Ro 15-8074, active metabolite of a new oral cephalosporin (Ro 15-8075), against 7,775 recent clinical isolates. Antimicrobial Agents and Chemotherapy 1986, 30: 961–963.

    PubMed  Google Scholar 

  21. Sykes, R. B., Matthew, M.: Detection assay and immunology of beta-lactamases. In: Hamilton-Miller, J. M. T., Smith, J. T. (ed.): Beta-lactamases. Academic Press, London, 1979, p. 17–49.

    Google Scholar 

  22. Petit, A., Sirot, D. L., Chanal, C. M., Sirot, J. L., Labia, R., Gerbaud, A., Cluzel, R. A.: Novel plasmid-mediated beta-lactamase in clinical isolates ofKlebsiella pneumoniae more resistant to ceftazidime than to other broad-spectrum cephalosporins. Antimicrobial Agents and Chemotherapy 1988, 32: 626–630.

    PubMed  Google Scholar 

  23. Richmond, M. H., Sykes, R. B.: The beta-lactamases of gram-negative bacteria and their possible physiological role. In: Rose, A. H., Tempest, D. W. (ed.): Advances in microbial physiology. Volume 9. Academic Press, New York, 1973, p. 31–88.

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Pharmaceutical Research, F. Hoffmann-La Roche & Co., 4002, Basel, Switzerland

    P. Angehrn, P. Hohl & R. L. Then

Authors
  1. P. Angehrn
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. P. Hohl
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. R. L. Then
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Angehrn, P., Hohl, P. & Then, R.L. In vitro antibacterial properties of cefetamet and in vivo activity of its orally absorbable ester derivative, cefetamet pivoxil. Eur. J. Clin. Microbiol. Infect. Dis. 8, 536–543 (1989). https://doi.org/10.1007/BF01967476

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF01967476

Keywords

Search

Navigation