Ezetimibe (Zetia) is a selective cholesterol absorption inhibitor that specifically inhibits the absorption of dietary and biliary cholesterol by acting on the brush border of the small intestine. Approved by the U.S. FDA in 2002, this medication provides an innovative treatment option for various lipid metabolism disorders, including primary hyperlipidemia and heterozygous familial hypercholesterolemia.

What is Ezetimibe (Zetia)?

Pharmacological Actions

Ezetimibe is a unique lipid-lowering drug acting on the small intestine. Its molecular target is Niemann-Pick C1-Like 1 (NPC1L1), a sterol transporter involved in the uptake of intestinal cholesterol and phytosterols.

Mechanism of action includes:Specific localization: Ezetimibe localizes to the brush border of the small intestine to inhibit cholesterol absorption.

Dual effect: Simultaneously inhibits the absorption of both dietary and biliary cholesterol.

Metabolic regulation: Reduces the transport of intestinal cholesterol to the liver, leading to decreased hepatic cholesterol storage.

Receptor upregulation: Increases the expression of low-density lipoprotein (LDL) receptors, promoting the clearance of cholesterol from the bloodstream.

Specifications and Properties of Ezetimibe (Zetia)

Dosage Form and Specifications

Tablet: 10 mg, white to off-white, capsule-shaped.

Marking feature: The imprint "414" is embossed on one side.

Packaging specification: 30 tablets per bottle (NDC 78206-178-01).

Physicochemical Properties

Appearance: White crystalline powder.

Solubility: Freely to very freely soluble in ethanol, methanol, and acetone; practically insoluble in water.

Melting point: Approximately 163°C.

Molecular formula: C₂₄H₂₁F₂NO₃.

Molecular weight: 409.4.

Excipient Composition

Croscarmellose sodium.

Lactose monohydrate.

Magnesium stearate.

Microcrystalline cellulose.

Povidone.

Sodium lauryl sulfate.

Storage Conditions for Ezetimibe (Zetia)

Storage Environment Requirements

Temperature: Store at room temperature between 68°F and 77°F (20°C and 25°C).

Moisture protection: Protect from moisture.

Contraindications: Avoid exposure to high temperature and humid environments.

Usage Precautions

Administer orally once daily, with or without food.

If coadministered with bile acid sequestrants, take ezetimibe either 2 hours before or 4 hours after the sequestrant.

Missed dose handling: Take the missed dose as soon as remembered. Do not double the dose at the next scheduled time.