Gut Microbiota-Mediated Drug-Antibiotic Interactions

Drug Metab Dispos. 2015 Oct;43(10):1581-9. doi: 10.1124/dmd.115.063867. Epub 2015 Apr 29.


Xenobiotic metabolism involves the biochemical modification of drugs and phytochemicals in living organisms, including humans and other animals. In the intestine, the gut microbiota catalyzes the conversion of hydrophilic drugs into absorbable, hydrophobic compounds through hydroxyzation and reduction. Drugs and phytochemicals are transformed into bioactive (sulfasalazine, lovastatin, and ginsenoside Rb1), bioinactive (chloramphenicol, ranitidine, and metronidazole), and toxic metabolites (nitrazepam), thus affecting the pharmacokinetics of the original compounds. Antibiotics suppress the activities of drug-metabolizing enzymes by inhibiting the proliferation of gut microbiota. Antibiotic treatment might influence xenobiotic metabolisms more extensively and potently than previously recognized and reduce gut microbiota-mediated transformation of orally administered drugs, thereby altering the systemic concentrations of intact drugs, their metabolites, or both. This review describes the effects of antibiotics on the metabolism of drugs and phytochemicals by the gut microbiota.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / metabolism*
  • Drug Interactions / physiology*
  • Gastrointestinal Microbiome / drug effects*
  • Gastrointestinal Microbiome / physiology*
  • Gastrointestinal Tract / drug effects
  • Gastrointestinal Tract / metabolism
  • Gastrointestinal Tract / microbiology
  • Humans
  • Pharmaceutical Preparations / administration & dosage
  • Pharmaceutical Preparations / metabolism


  • Anti-Bacterial Agents
  • Pharmaceutical Preparations