Cholesterol Absorption Inhibitors: Ezetimibe

Question 1

Ezetimibe
MOA

Answer 1

Inhibits the absorption of dietary cholesterol from the intestine by blocking a transport protein in the brush border of enterocytes.
This results in a decrease in liver C store, an increase in hepatic LDL absorption and increase clearance of LDL-C from plasma

Question 2

Ezetimibe
Abs/Distrb/Elim

Answer 2

Given orally, activated in the liver
Maximum concentration in 2h
Undergoes enterohepatic cycling
Gradually excreted in the faeces.
Plasma half-life: 22h.

Question 3

Ezetimibe
Clinical use

Answer 3

Hypercholesterolaemia

Question 4

Ezetimibe
Adverse effects

Answer 4

Generally well tolerated, without affecting the absorption of vitamins, TGs or bile acids
Can cause diarrhoea, abdominal pain