[The role of intestinal absorption blockade in hypercholesterolemia treatment]

Mechanisms of biliary and diet cholesterol absorption are reviewed, and the characteristics of a new specific intestinal cholesterol absorption inhibitor (ezetimibe) are discussed. Ezetimibe is absorbed well by oral route, shows glucuronization in the liver and enters in enterohepatic circulation; thus, half-life is long, around 22 hours. Dose is 10 mg administered once a day. Ezetimibe works through both cholesterol sources: the production of cholesterol by hepatocytes and the absorption of cholesterol by enterocytes, giving rise in this way to an additive hypolipemic effect. The administration of lower dose of statin besides 10 mg of ezetimibe amounts to the administration of highest dose of statin. In patients who take statins whose LDL cholesterol levels are higher than normal, adding ezetimibe increase from 27% to 75% the percentage of those who reach the therapeutic objective. In addition to increasing the effectiveness, side effects are also avoided since the tolerability to ezetimibe is similar to placebo. The average maximum reduction of the plasma level of cholesterol with 10 mg of ezetimibe and 80 mg of simvastatin or atorvastatin is higher 60%.