Reduced duodenal cytochrome P450 3A protein expression and catalytic activity in patients with cirrhosis

Clin Pharmacol Ther. 2009 Apr;85(4):387-93. doi: 10.1038/clpt.2008.292. Epub 2009 Feb 11.

Abstract

The small intestine and liver express high levels of cytochrome P450 3A (CYP3A), an enzyme subfamily that contributes significantly to drug metabolism. In patients with cirrhosis, reduced metabolism of drugs is typically attributed to decreased liver function, but it is unclear whether drug metabolism in the intestine is also compromised. In this study, we compared CYP3A protein expression and in vitro midazolam hydroxylation in duodenal mucosal biopsies from subjects with normal liver function (controls; n = 20) and subjects with various levels of severity of cirrhosis (n = 23). In samples from subjects with cirrhosis, duodenal CYP3A expression and total midazolam hydroxylation were lower by 47 and 34%, respectively, as compared with samples from controls. Greater decreases in CYP3A expression were seen in subjects with more severe cirrhosis. Therefore, patients with advanced cirrhosis may have greater drug exposure following oral dosing as a result of both impaired liver function and decreased intestinal CYP3A expression and activity.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural

MeSH terms

  • Adult
  • Aged
  • Catalysis / drug effects
  • Cytochrome P-450 CYP3A / analysis
  • Cytochrome P-450 CYP3A / biosynthesis*
  • Duodenum / drug effects
  • Duodenum / enzymology*
  • Enzyme Activation / genetics
  • Female
  • Gene Expression Regulation, Enzymologic / drug effects
  • Gene Expression Regulation, Enzymologic / physiology*
  • Humans
  • Intestinal Mucosa / drug effects
  • Intestinal Mucosa / enzymology
  • Liver Cirrhosis / drug therapy
  • Liver Cirrhosis / enzymology*
  • Male
  • Midazolam / pharmacokinetics
  • Midazolam / therapeutic use
  • Middle Aged

Substances

  • Cytochrome P-450 CYP3A
  • Midazolam