Ezetimibe is a useful cholesterol lowering drug. Ezetimibe is given orally. The half life of ezetimibe is around 22- 23 hours. Ezetimibe will be excreted in the forms of feces. Colestryamine will decrease the plasma concentration of ezetimibe while fibrates will increase the concentration of ezetimibe.
Ezetimibe is useful in treating hypercholesterolemia by decreasing the plasma concentration of LDL and inhibit the absorption of the cholesterol from the intestine. Ezetimibe will activated in the liver. Ezetimibe will inhibits and blocks a sterol carrier protein which present in the brush border of the enterocytes. This will lead to the reduction of the amount of cholesterol transfer through the liver via chylomicrons. These cholesterols may include biliary cholesterol and dietary cholesterol. As a consequences, there will be reduction in the cholesterol level in the liver and increase in the LDL hepatic absorption. There will also be an increase in the clearance of the LDL - cholesterol from the plasma.
Ezetimibe will achieved its maximum concentration 2 hours after ingestion where it undergoes enterohepatic cycling.The common side effects of ezetimibe may include myalgia, gastrointestinal discomfort ( constipation, diarrhea, bloating), rashes and headache.