Relatively recently was developed a drug Zetia, which inhibits the absorption of cholesterol in the intestine. The mechanism of action of ezetimibe is not fully discovered yet, but however it is fundamentally different from the mechanism of ion exchange resins. It is known that ezetimibe in the villous epithelium of the small intestine is connected with glucuronyl acid and then a glucuronide of ezetimibe enteropechenochnom circulates in a cascade, providing the absorption of cholesterol from the intestinal lumen. Recycling process of Zetia has positive half-life of the drug is 22 hours, so it is administered one time per day.
Zetia (Ezetimibe) is not metabolized through the cytochrome P450 system, so it can be combined with many drugs without fear to get side effects. Monotherapy is ezetimibe decrease plasma cholesterol not more than 15-20%. Ezetimibe essentially has no effect on the other plasma lipid parameters. However, its combination with a statin cholesterol-lowering effect significantly increases the inhibition of two processes – the synthesis of cholesterol in the liver and absorption of cholesterol in the intestine. Results from clinical studies have shown that a combination therapy of simvastatin and ezetimibe (10 mg) decreased the LDL much more than monotherapy with simvastatin 40 mg.
Use of Zetia 10 mg in combination with atorvastatin 20 mg has the same effect on the reduction of LDL-C, and the application atorvvastatina 80 mg.
Advantages of combination therapy are obvious: it eliminates the need for a doctor prescribe maximum dose statin that reduces the incidence of side effects; a combination of a statin with ezetimibe enables more rapid achievement of the target level of LDL-C, again dispensing appointment of lower doses of statins. Already produced a combined preparation consisting of 10 mg of ezetimibe and simvastatin 10-20 mg.