Drug-induced effects on cholesterol catabolism and bile acids

Curr Opin Investig Drugs. 2006 Mar;7(3):214-8.

Abstract

Serum cholesterol level is a reflection of whole-body cholesterol metabolism, which is tightly regulated so that cholesterol absorption and synthesis are interrelated. The actions of serum cholesterol-lowering drugs are based primarily on influencing cholesterol synthesis (statins), cholesterol absorption (ezetimibe) or bile acid synthesis (resins). A great deal of research has been targeted at developing drugs that inhibit the metabolism of cholesterol in enterocytes, such as microsomal transfer protein inhibitors and acyl-cholesterol acyl transferase inhibitors, but there are little published data regarding their effect on whole-body cholesterol metabolism in humans. Cholesterol is catabolized and excreted as neutral sterols of cholesterol into feces, and by conversion to bile acids. This review examines lipid-lowering drugs and their effect on cholesterol metabolic pathways.

Publication types

  • Review

MeSH terms

  • Allylamine / analogs & derivatives*
  • Allylamine / therapeutic use
  • Anticholesteremic Agents / therapeutic use*
  • Azetidines / therapeutic use*
  • Bile Acids and Salts / metabolism*
  • Cholesterol / metabolism*
  • Colesevelam Hydrochloride
  • Epichlorohydrin / therapeutic use*
  • Ezetimibe
  • Humans
  • Imidazoles / therapeutic use*
  • Resins, Synthetic / therapeutic use*

Substances

  • Anticholesteremic Agents
  • Azetidines
  • Bile Acids and Salts
  • Imidazoles
  • Resins, Synthetic
  • colestimide
  • Epichlorohydrin
  • Allylamine
  • Cholesterol
  • Ezetimibe
  • Colesevelam Hydrochloride