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, Volume 35, Supplement 2, pp 57–61 | Cite as

In Vitro Activity of Desacetylcefotaxime and the Interaction with its Parent Compound, Cefotaxime

  • Kohtaro Oizumi
  • I. Hayashi
  • S. Aonuma
  • K. Konno
Section 2: Desacetylcefotaxime and Cefotaxime: Implications of a Bactericidal Metabolites

Summary

Antibacterial activities of cefotaxime and its major metabolite, desacetylcefotaxime, against 178 strains (of 10 species) were assessed in terms of minimum inhibitory concentrations (MIC50 and MIC80), and were compared with those of cefoperazone and ceftazidime.

The activity of desacetylcefotaxime was several times less than that of cefotaxime against almost all of the species tested. Against Staphylococcus aureus, Morganella morganii, Enterobacter cloacae and Pseudomonas aeruginosa, the M1C8O values of desacetylcefotaxime were higher than those of cefoperazone and ceftazidime. The antibacterial potency of desacetylcefotaxime against Klebsiella pneumoniae and Pseudomonas cepacia was superior to that of cefoperazone and ceftazidime, and comparable with the activities of the latter compounds against the other 4 Gramnegative species.

Partial synergy was demonstrated in the activity of cefotaxime and desacetylcefotaxime against most of the strains examined. Antagonism was observed in activity against 2 of 18 strains of M. morganii. In general, desacetylcefotaxime enhances the potency of its parent compound, cefotaxime, when they coexist.

Intravenous infusion of cefotaxime Ig over a period of 1 hour resulted in mean peak serum concentrations of 48.5 mg/L of cefotaxime and 6.5 mg/L of desacetylcefotaxime at the end of the infusion. The mean elimination half life in β-phase of cefotaxime was 0.8 hour and that of desacetylcefotaxime was 2 hours.

Keywords

High Performance Liquid Chromatography Antibacterial Activity Cefotaxime Ceftazidime Klebsiella Pneumoniae 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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References

  1. Fu KP, Aswapokee P, Ho I, Mathijssen C, Neu HC. Pharmacokinetics of cefotaxime. Antimicrobial Agents and Chemotherapy 16: 592–597, 1980CrossRefGoogle Scholar
  2. Jones RN, Barry AL, Thornsberry C. Antimicrobial activity of desacetyl cefotaxime alone and in combination with cefotaxime: Evidence of synergy. Reviews of Infectious Diseases 4: S366–373, 1982PubMedCrossRefGoogle Scholar
  3. Kobayashi Y, Haruta T, Okura K, Kuroki S, et al. Evaluation of cefotaxime in treatment of infections in newborns. Japanese Journal of Antibiotics 35: 1801–1815, 1982PubMedGoogle Scholar
  4. Limbert M, Seibert G, Schrinner E. The cooperation of cefotaxime and desacetyl cefotaxime with respect to antibacterial activity and β-lactamase stability. Infection 10: 97–100, 1982PubMedCrossRefGoogle Scholar
  5. Neu HC. Antibacterial activity of desacetyl cefotaxime alone and in combination with cefotaxime. Reviews of Infectious Diseases 4: S374–378, 1982PubMedCrossRefGoogle Scholar
  6. Wise R, Willis PJ, Andrews JM, Bedford KA. Activity of the cefotaxime (HR756) desacetyl metabolite compared with those of cefotaxime and other cephalosporins. Antimicrobial Agents and Chemotherapy 17: 84–86, 1980PubMedCrossRefGoogle Scholar

Copyright information

© ADIS Press Limited 1988

Authors and Affiliations

  • Kohtaro Oizumi
    • 1
  • I. Hayashi
    • 2
  • S. Aonuma
    • 1
  • K. Konno
    • 1
  1. 1.Division of Medicine, The Research Institute for Chest Diseases and CancerTohoku UniversitySendaiJapan
  2. 2.Iwaki General HospitalIwakiJapan

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