What is the use of Zetia (ezetimibe)?

From the Guidelines

Zetia (ezetimibe) should be considered as an adjunct to diet and statin therapy to lower LDL-C levels in patients with atherosclerotic cardiovascular disease (ASCVD) risk, with a recommended dose of 10 mg orally daily, as evidenced by the 2022 ACC expert consensus decision pathway 1. The mechanism of action of ezetimibe involves inhibiting the NPC1L1 protein, which reduces cholesterol absorption in the small intestine. According to the study, the mean percentage reduction in LDL-C with ezetimibe monotherapy is 18%, and 25% when used in combination with statin therapy 1. Key considerations for prescribing ezetimibe include:

• Contraindication in patients with a history of hypersensitivity to the medication
• Warnings and precautions, such as not recommending its use in patients with moderate to severe hepatic impairment, and monitoring hepatic transaminases before and during treatment
• Adverse effects, including upper respiratory tract infection, diarrhea, arthralgia, and sinusitis
• Drug-drug interactions with cyclosporine, fibrates, and bile acid sequestrants (BAS) The CV outcomes trials, such as IMPROVE-IT and SHARP, have demonstrated the efficacy of ezetimibe in reducing LDL-C levels and improving cardiovascular outcomes 1. In clinical practice, ezetimibe is generally well-tolerated, and a generic version is available. The use of ezetimibe as an adjunct to statin therapy can provide additional LDL-C reduction and improve cardiovascular outcomes in patients with ASCVD risk, as supported by the highest quality evidence from the 2022 ACC expert consensus decision pathway 1.

From the FDA Drug Label

Ezetimibe tablets is a medicine used with a cholesterol lowering diet: and with other cholesterol medicines called a statin, or alone (when additional cholesterol lowering treatments are not possible), to lower elevated low-density lipoprotein cholesterol (LDL-C) or bad cholesterol in adults with primary hyperlipidemia (too many fats in your blood), including heterozygous familial hypercholesterolemia (HeFH).

Ezetimibe tablets is also used: with a statin and other cholesterol lowering treatments to lower elevated LDL-C levels in adults and patients 10 years of age and older with homozygous familial hypercholesterolemia (HoFH).

The safety and effectiveness of ezetimibe tablets has not been established in children: younger than 10 years of age with HeFH or HoFH.

Do not take ezetimibe tablets: if you are allergic to ezetimibe or any of the ingredients in ezetimibe tablets

Zetia (Ezetimibe) Uses:

• Lowering elevated low-density lipoprotein cholesterol (LDL-C) or bad cholesterol in adults with primary hyperlipidemia
• Used with a statin to lower LDL-C in adults and children 10 years of age and older with heterozygous familial hypercholesterolemia (HeFH)
• Used with a statin and other cholesterol lowering treatments to lower elevated LDL-C levels in adults and patients 10 years of age and older with homozygous familial hypercholesterolemia (HoFH)
• Lowering elevated sitosterol and campesterol levels in adults and in children 9 years of age and older with homozygous familial sitosterolemia

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From the Research

Zetia Overview

• Zetia, also known as ezetimibe, is a cholesterol absorption inhibitor used to lower low-density lipoprotein (LDL) cholesterol levels 3, 4, 5, 6.
• It works by blocking the intestinal absorption of both biliary and dietary cholesterol, thereby inhibiting the intestinal absorption of cholesterol, phytosterols, and certain oxysterols 6.

Efficacy and Safety

• Ezetimibe has been shown to be effective in lowering LDL cholesterol levels when used as monotherapy or in combination with statins 3, 4, 5.
• The combination of ezetimibe and statin therapy has been found to be more effective than statin monotherapy in lowering LDL cholesterol levels and improving other lipid parameters 3, 4.
• Ezetimibe has a favorable safety profile, with a low risk of side effects, including myopathy and liver enzyme elevations 3, 4, 7.

Clinical Implications

• Ezetimibe is recommended for use in patients who do not achieve their LDL cholesterol goals with statin monotherapy 4, 5.
• It is also used in patients who experience statin-associated muscle symptoms or other adverse effects 4, 5.
• The combination of ezetimibe and statin therapy has been found to be effective in reducing the risk of major atherosclerotic events, including non-fatal myocardial infarction, non-haemorrhagic stroke, and arterial revascularisation procedures 7.

Patient Populations

• Ezetimibe has been studied in a wide range of patient populations, including those with chronic kidney disease 7.
• The SHARP trial found that the combination of simvastatin and ezetimibe safely reduced the incidence of major atherosclerotic events in patients with advanced chronic kidney disease 7.