The in vitro inactivation of thirteen beta-lactam antibiotics by other mechanisms than adsorption to faecal substance

Infection. 1993 Mar-Apr;21(2):127-30. doi: 10.1007/BF01710750.

Abstract

We have investigated the antibiotic inactivating capacity of intestinal contents in vitro in faeces. In the presently reported study the influence of beta-lactamase catalyzed hydrolysis on the antimicrobial activity of 13 commonly used beta-lactam antibiotics was investigated, while the influence of non-specific adsorption of antibiotics to faecal compounds was also taken into account. The following antibiotics were tested: benzylpenicillin, amoxicillin, amoxicillin/clavulanate, cloxacillin, piperacillin, temocillin, cefuroxime, cefamandole, cephradine, cefotaxime, ceftazidime, aztreonam and imipenem. Faecal samples were obtained from 30 healthy volunteers. Six different concentrations of each antibiotic were added to 1 g of faeces. After 24 h of incubation at 37 degrees C the remaining amount of active antibiotic was determined by means of a "growth inhibition assay". The contribution to the test results of non-specific adsorption to macromolecules was calculated by means of a model and the inactivation data were subsequently corrected. The amount of antibiotic non-specifically bound to faecal macromolecules varied from 0% to 80% of the amount of antibiotic initially added to the faeces. A considerable difference was found in the degree of inactivation of several antibiotics. However, in contrast to earlier investigations, the results of this study show that in a normal population the influence of beta-lactamase catalyzed hydrolysis on the activity of beta-lactam antibiotics is apparently very small when compared to the influence of non-specific adsorption of beta-lactam antibiotics to faecal compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adsorption
  • Adult
  • Anti-Bacterial Agents / analysis
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology
  • Bacteria / drug effects
  • Drug Stability
  • Feces / chemistry*
  • Feces / enzymology
  • Female
  • Humans
  • In Vitro Techniques
  • Male
  • beta-Lactamases / metabolism
  • beta-Lactams

Substances

  • Anti-Bacterial Agents
  • beta-Lactams
  • beta-Lactamases