Ezetimibe

What it is and how it works

Mechanism of Action Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol by the small intestine. The molecular target of ezetimibe has been shown to be the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), which is involved in the intestinal uptake of cholesterol and phytosterols. Ezetimibe localizes at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in LDL receptors, resulting in clearance of cholesterol from the blood.

Indications

Ezetimibe tablets are indicated: • In combination with a statin, or alone when additional low-density lipoprotein cholesterol (LDL-C) lowering therapy is not possible, as an adjunct to diet to reduce elevated LDL-C in adults with primary hyperlipidemia, including heterozygous familial hypercholesterolemia (HeFH). • In combination with a statin as an adjunct to diet to reduce elevated LDL-C in pediatric patients 10 years of age and older with HeFH. • In combination with fenofibrate as an adjunct to diet to reduce elevated LDL-C in adults with mixed hyperlipidemia. • In combination with a statin, and other LDL-C lowering therapies, to reduce elevated LDL-C levels in adults and in pediatric patients 10 years of age and older with homozygous familial hypercholesterolemia (HoFH). • As an adjunct to diet for the reduction of elevated sitosterol and campesterol levels in adults and in pediatric patients 9 years of age and older with homozygous familial sitosterolemia.

Dosage and administration (summary)

• The recommended dose of ezetimibe tablets is 10 mg orally once daily, administered with or without food. • If as dose is missed, take the missed dose as soon as possible. Do not double the next dose. • Assess LDL-C when clinically appropriate, as early as 4 weeks after initiating ezetimibe tablets. • Administer ezetimibe tablets at least 2 hours before or 4 hours after administration of a bile acid sequestrant . • 10 mg orally once daily, with or without food • Administer ezetimibe tablets either ≥2 hours before or ≥4 hours after administration of a bile acid sequestrant. • Assess LDL-C when clinically appropriate, as early as 4 weeks after initiating ezetimibe tablets.

Contraindications

Ezetimibe tablets are contraindicated in patients with a known hypersensitivity to ezetimibe or any of the excipients in ezetimibe tablets. Hypersensitivity reactions including anaphylaxis, angioedema, rash, and urticaria have been reported . When used in combination with a statin, fenofibrate, or other LDL-C lowering therapy, ezetimibe tablets are contraindicated in patients for whom a statin, fenofibrate, or other LDL-C lowering therapy are contraindicated.

Warnings and precautions

• Risks Associated with Combination Treatment with a Statin, Fenofibrate, or Other LDL-C Lowering Therapies : Refer to the Prescribing Information of these products for a description of their risks including, but not limited to, the warnings and precautions. • Liver Enzyme Abnormalities and Monitoring : Increases in serum transaminases have been reported with use of ezetimibe. Perform liver enzyme testing as clinically indicated and consider withdrawal of ezetimibe if increases in ALT or AST ≥3 X ULN persist.

Pregnancy

Pregnancy Risk Summary There are insufficient data on ezetimibe use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes.

Storage and supply

Ezetimibe tablets USP, 10 mg are white to off-white, capsule shaped, flat faced bevel edged tablets debossed with ‘I’ on one side and ‘83’ on the other side. They are supplied as follows: NDC 71335-3092-1: 30 Tablets in a BOTTLE NDC 71335-3092-2: 90 Tablets in a BOTTLE NDC 71335-3092-3: 28 Tablets in a BOTTLE NDC 71335-3092-4: 18 Tablets in a BOTTL…

Source: Ezetimibe (Ezetimibe) — US FDA prescribing information, 2026-02-17, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.