Ezetimibe

Template:HVLP 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

Links

References

• JAN, Švihovec and Kolektiv KOLEKTIV. Pharmacology. - release. Grada Publishing a.s., 2018. 1008 p. ISBN 9788024755588.

• JIŘINA, Martínková and Kolektiv KOLEKTIV. Pharmacology: for medical students, 2nd, completely revised and supplemented edition. - release. Grada Publishing a.s., 2018. 520 p. ISBN 9788024741574.

• Study materials from the teaching of pharmacology at the Institute of Pharmacology of the 1st Faculty of Medicine, UK and VFN