Ezetimibe

 is a sterol absorption inhibitor'. It is used to treat hypercholesterolemia, usually in combination with statins, if statin therapy alone is not effective enough.

Mechanism of action
Ezetimibe belongs to the group hypolipidemic. It blocks the sterol transporter, protein Niemann-Pick C1-Like 1 (NPC1L1) in the brush lining of enterocytes (and bile duct epithelium), which is necessary for the absorption of cholesterol and phytosterols in the intestine (also within the enterohepatic circulation of cholesterol).

Pharmacokinetics
After administration, it is rapidly absorbed and glucuronidated to an active metabolite. It has a significant enterohepatic circulation and a biological half-life of 22 hours. More than 90% is bound to plasma proteins.

Indication
Ezetimibe is given with a statin':
 * in primary hypercholesterolemia (non-familial or heterozygous familial) as a dietary supplement, if statin treatment alone is insufficient;
 * in homozygousfamilial hypercholesterolemia;

In monotherapy it is used:
 * in primary hypercholesterolemia (non-familial or heterozygous familial) as a dietary supplement, if statin treatment is contraindicated or not tolerated;
 * in case of homozygous familial sitosterolemia as a dietary supplement.

Side effects
They are practically not. If they do occur, they are usually only headaches and GIT problems. In combination with fibrates there is a higher risk of cholelithiasis