[Change in the cholesterol metabolism associated with the combined inhibition of synthesis and absorption].
Lowering lipid levels in the cardiovascular prevention we confine ourselves to measure the cholesterol level and care less for the background effects. Namely blood cholesterol level beyond the amount consumed with the diet highly depends on balance of intestinal absorption/secretion and synthesis. Studying the rate of absorption and synthesis has come only recently into the foreground of interest. Many observations proved that using even the strongest cholesterol lowering drug - beyond reducing the synthesis in the liver - may be associated with an up to 50 percent increase of the intestinal cholesterol absorption. When studying the effectiveness of statins in everyday practice we measure only the decrease of serum cholesterol level as the final result, and do not examine the changes in the synthesis and absorption. The amount of cholesterol synthesized or absorbed can be determined in an indirect way by measuring that of the non-cholesterol sterols (phytosterols). The absorption markers are campesterol, sitosterol, avenasterol as well as cholestanol. The biosynthesis of cholesterol correlates with the level of lathosterol, cholestanol, desmostenol. In practice the concentration of lathosterol or lathosterol/cholesterol can be considered the marker of synthesis and the campesterol or campesterol/cholesterol ratio the marker of absorption. So recent study results show that while inhibiting the cholesterol synthesis with statin the cholesterol absorption increases and the absorption inhibitor ezetimibe is associated with boost of synthesis. The increase in absorption caused by statins can be reduced or prevented by combining with ezetimibe. These data confirm that combination of statin and ezetimibe, inhibiting simultaneously both the synthesis and absorption provides the most effective cholesterol-level lowering with the least side-effects.
Márk
László
L
Békés Megyei Képviselo-testület Pándy Kálmán Kórháza II. Belgyógyászat-Kardiológia Gyula. mark@pandy.hu
Paragh
György
G
D000924:Anticholesteremic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D001384:Azetidines / Q000494:pharmacology* / Q000627:therapeutic use; D015415:Biomarkers / Q000097:blood; D004083:Cholestanol / Q000097:blood; D002784:Cholesterol / Q000031:analogs & derivatives / Q000096:biosynthesis* / Q000097:blood / Q000378:metabolism*; D002791:Cholesterol, Dietary / Q000008:administration & dosage / Q000378:metabolism*; D000069438:Ezetimibe; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D006937:Hypercholesterolemia / Q000097:blood / Q000188:drug therapy / Q000209:etiology / Q000378:metabolism*; D007408:Intestinal Absorption / Q000187:drug effects*; D010840:Phytosterols / Q000097:blood; D012855:Sitosterols / Q000097:blood
D000924:Anticholesteremic Agents; D001384:Azetidines; D015415:Biomarkers; D002791:Cholesterol, Dietary; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D010840:Phytosterols; D012855:Sitosterols; C021273:campesterol; C025473:gamma-sitosterol; C001521:lathosterol; D004083:Cholestanol; D002784:Cholesterol; D000069438:Ezetimibe