Metabolism of drugs and other xenobiotics in the gut lumen and wall

Pharmacol Ther. 1990;46(1):67-93. doi: 10.1016/0163-7258(90)90036-2.


Metabolism in the gut lumen and wall can decrease the bioavailability and the pharmacological effects of a wide variety of drugs. Bacterial flora in the gut, the environmental pH and oxidative or conjugative enzymes present in the intestinal epithelial cells can all contribute to the process. Bacterial biotransformation is greatest in the colon, while gut wall metabolism is generally highest in the jejunum and decreases distally. Gut wall metabolism may be induced or inhibited by dietary or environmental xenobiotics or by co-administered drugs. Recent evidence suggests that some drugs, food-derived mutagens and other xenobiotics can be metabolized by gut flora and/or gut wall enzymes to reactive species which may cause tumors.

Publication types

  • Review

MeSH terms

  • Animals
  • Digestive System / metabolism*
  • Gastric Mucosa / metabolism
  • Humans
  • Intestinal Mucosa / metabolism
  • Pharmaceutical Preparations / metabolism*
  • Xenobiotics / metabolism*


  • Pharmaceutical Preparations
  • Xenobiotics