Hyzetimibe

A cholesterol absorption inhibitor

Hyzetimibe
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Hyzetimibe is a pharmaceutical compound used primarily to lower cholesterol levels in the blood. It functions as a cholesterol absorption inhibitor, which helps reduce the amount of cholesterol absorbed by the intestines. This medication is often prescribed to patients who have high cholesterol levels that cannot be controlled by diet and exercise alone.

Mechanism of Action

Hyzetimibe works by selectively inhibiting the absorption of cholesterol in the small intestine. It targets the Niemann-Pick C1-Like 1 (NPC1L1) protein, which is responsible for the uptake of cholesterol into the enterocytes. By blocking this protein, Hyzetimibe reduces the amount of cholesterol that enters the bloodstream, thereby lowering total cholesterol levels, including low-density lipoprotein (LDL) cholesterol, which is often referred to as "bad" cholesterol.

Clinical Use

Hyzetimibe is typically used in conjunction with statins, a class of drugs that reduce cholesterol production in the liver, to achieve a more significant reduction in cholesterol levels. It is particularly beneficial for patients who are unable to tolerate high doses of statins or who have a genetic predisposition to high cholesterol, such as those with familial hypercholesterolemia.

Dosage and Administration

Hyzetimibe is usually administered orally in the form of a tablet. The standard dosage is 10 mg once daily, with or without food. It is important for patients to adhere to their prescribed dosage and to continue following a cholesterol-lowering diet while taking this medication.

Side Effects

Common side effects of Hyzetimibe include headache, diarrhea, and fatigue. Some patients may experience muscle pain or liver enzyme abnormalities, especially when Hyzetimibe is used in combination with statins. Patients are advised to report any unusual symptoms to their healthcare provider.

Contraindications

Hyzetimibe is contraindicated in patients with active liver disease or unexplained persistent elevations in hepatic transaminase levels. It should be used with caution in patients with moderate to severe hepatic impairment.

Related Pages

• Cholesterol
• Statin
• Familial hypercholesterolemia
• Niemann-Pick C1-Like 1