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To what class of drugs does ezetimibe belong?
Cholesterol absorption inhibitors / anticholesteremic agents
What are the indications associated with ezetimibe?
True or false?
Ezetimibe is insoluble in water.
What is ezetimibe's target MOA?
Ezetimibe binds to NPC1L1 (a transport protein) in GI epithelium and hepatocytes - inhibiting intestinal absorption of cholesterol and phytosterols.
As per ezetimibe's MOA, what happens to cholesterol delivery to the liver?
Cholesterol delivery decreases.
As per ezetimibe's MOA, describe cholesterol's incorporation into VLDL and LDL.
Incorporation of cholesterol into VLDL and LDL decreases.
As per ezetimibe's MOA, what happens to hepatic LDL receptors?
Receptors are up-regulated, leading to increased clearance of LDL from the blood.
What are some adverse effects associated with ezetimibe?
- Elevated serum transaminases (liver has to work harder)