Drug-induced effects on cholesterol catabolism and bile acids.
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.
Gylling
Helena
H
Department of Clinical Nutrition, University of Kuopio, Finland. helena.gylling@uku.fi
Miettinen
Tatu A
TA
D000499:Allylamine / Q000031:analogs & derivatives* / Q000627:therapeutic use; D000924:Anticholesteremic Agents / Q000627:therapeutic use*; D001384:Azetidines / Q000627:therapeutic use*; D001647:Bile Acids and Salts / Q000378:metabolism*; D002784:Cholesterol / Q000378:metabolism*; D000069472:Colesevelam Hydrochloride; D004811:Epichlorohydrin / Q000627:therapeutic use*; D000069438:Ezetimibe; D006801:Humans; D007093:Imidazoles / Q000627:therapeutic use*; D012117:Resins, Synthetic / Q000627:therapeutic use*
D000924:Anticholesteremic Agents; D001384:Azetidines; D001647:Bile Acids and Salts; D007093:Imidazoles; D012117:Resins, Synthetic; C417427:colestimide; D004811:Epichlorohydrin; D000499:Allylamine; D002784:Cholesterol; D000069438:Ezetimibe; D000069472:Colesevelam Hydrochloride