Author/Editor     Kohalmy, Krisztina; Rozman, Damjana; Pascussi, Jean-Marc; Sarvary, Eniko; Monostory, Katalin
Title     A koleszterinhomeosztazis es a gyogyszer-metabolizmus kapcsolata
Translated title     Crosstalk between cholesterol homeostasis and drug metabolism
Type     članek
Source     Orv Hetil
Vol. and No.     Letnik 149, št. 27
Publication year     2008
Volume     str. 1283-9
Language     hun
Abstract     Nowadays cardiovascular diseases are among the major causes of mortality in the developed world. High cholesterol level in blood and atherosclerosis play the main role in progression of cardiovascular diseases. Reducing serum cholesterol level has been shown to avoid deleterious effects, whereas in serious diseases it improves the outcome. A widely used, statin-based therapy induces a decrease in de novo cholesterol biosynthesis in the liver. Another possibility for lowering serum cholesterol level is to block the uptake of dietary cholesterol from intestine (e.g. ezetimibe). Coadministration of statins and cholesterol uptake inhibitors provides an efficient therapeutical strategy. Several therapeutic agents, reducing serum cholesterol level, are able to regulate the expression of not only cholesterogenic enzymes, but of the major drug metabolizing enzymes, cytochromes P450. The crosstalk between cholesterol homeostasis and drug metabolism is mediated by nuclear receptors, activating target genes in response of endogenous and exogenous ligands. Better understanding of the crosstalk between cholesterol homeostasis and drug metabolism is essential for developing an adequate strategy in therapy and in novel drug development.
Descriptors     CARDIOVASCULAR DISEASES
HYPERCHOLESTEROLEMIA
ANTILIPEMIC AGENTS
ATHEROSCLEROSIS
CHOLESTEROL