Ezetimibe
- Atc Codes:C10AX09
- CAS Codes:163222-33-1
- PHARMGKB ID:163222-33-1
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Ezetrol; Belgium: Ezetrol; Bulgaria: Ezetrol; Cyprus: Ezetrol; Czech Republic: Ezetrol, Zient; Denmark: Ezetrol; Estonia: Ezetrol; Finland: Ezetrol; France: Ezetrol; Germany: Ezetimibe, Ezetrol, Viemm; Greece: Ezetimibe, Ezetrol; Hungary: Ezetrol; Ireland: Ezetrol; Italy: Ezetrol, Zetia; Latvia: Ezetrol; Lithuania: Ezetrol; Malta: Ezetrol; Netherlands: Ezetrol; Poland: Ezetrol; Portugal: Adacai, Ezetrol; Romania: Ezetrol; Slovakia: Ezetrol; Slovenia: Ezetrol, Ezoleta; Sweden: Ezetrol; UK: Ezetrol.
North America
Canada: Ezetrol; USA: Zetia.
Latin America
Argentina: Acotral, Alin, Alipas, Cerclerol, Cetrakam, Coracil, Enediex, Ezetrol, Ixacor, Nalecol, Sinterol, Trilip, Vadel, Zetia; Brazil: Zetia; Mexico: Ezetrol, Zient.
Asia
Japan: Zetia.
Drug combinations
Ezetimibe and Atorvastatin
Ezetimibe and Fenofibrate
Ezetimibe and Simvastatin
Chemistry
Ezetimibe: C~24~H~21~F~2~NO~3~. Mw: 409.43. (1) 2-Azetidinone, 1-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)-, [3R-[3α(S*),4β]]-; (2)(3R,4S)-1-(p-Fluorophenyl)-3-[(3S)-3-(p-fluorophenyl)-3-hydroxypropyl]-4-(p-hydroxyphenyl)-2-azetidinone. CAS-163222-33-1. (1999).
Pharmacologic Category
Antilipemic Agents; Cholesterol Absorption Inhibitors; 2-Azetidinone. (ATC-Code: C10AX09).
Mechanism of action
Inhibits absorption of cholesterol at the brush border of the small intestine via the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1). This leads to a decreased delivery of cholesterol to the liver, reduction of hepatic cholesterol stores and increased clearance of cholesterol from the blood. Decreases total cholesterol, LDL-C, APOB, and triglycerides while increasing HDL-C.
Therapeutic use
Used in combination with dietary therapy for treatment of primary hypercholesterolemia (as monotherapy or in combination with HMG-CoA reductase inhibitors). Homozygous sitosterolemia. Homozygous familial hypercholesterolemia (in combination with atorvastatin or simvastatin). Mixed hyperlipidemia (in combination with fenofibrate).
Pregnancy and lactiation implications
Use during pregnancy only if potential benefit to mother outweighs possible risk to fetus. Use not recommended during lactation.
Unlabeled use
Contraindications
Hypersensitivity to ezetimibe or any component of the formulation. Concomitant use with an HMG-CoA reductase inhibitor in active hepatic disease or unexplained persistent elevations in serum transaminases.
Warnings and precautions
Use with caution in mild hepatic impairment. Not recommended for use with moderate or severe hepatic impairment. Use with caution in severe renal impairment (CrCl <30 mL/minute). Concurrent use of fibric acid derivatives (e.g. fenofibrate, gemfibrozil) may increase the risk of cholelithiasis. Secondary causes of hyperlipidemia should be ruled out prior to therapy. Hypersensitivity reactions might occur. Transient elevations in serum aminotransferase (transaminase) concentrations reported (more frequently with ezetimibe-statin combination). Use not recommended in children <10 years of age.