What is the generic name for Zetia (ezetimibe)?

Generic Name for Zetia

The generic name for Zetia is ezetimibe. 1

Medication Overview

Ezetimibe is a selective cholesterol absorption inhibitor that works by blocking the Niemann-Pick C1-Like 1 (NPC1L1) protein in the small intestine, thereby reducing intestinal cholesterol absorption. 2, 1

Key Prescribing Information

Standard Dosing:

• 10 mg orally once daily, with or without food 2, 1
• Can be taken in the morning or evening 3
• When combined with bile acid sequestrants, administer ezetimibe either ≥2 hours before or ≥4 hours after the bile acid sequestrant 2

Expected LDL-C Reduction:

• As monotherapy: approximately 18% reduction 2
• When added to statin therapy: additional 25% reduction 2
• Inhibits intestinal cholesterol absorption by approximately 54% 4

Clinical Indications

FDA-Approved Uses: 2, 1

• Primary hyperlipidemia (alone or with statins)
• Mixed hyperlipidemia (in combination with fenofibrate)
• Homozygous familial hypercholesterolemia (HoFH) when combined with atorvastatin or simvastatin
• Homozygous sitosterolemia (phytosterolemia)

Cardiovascular Outcomes Evidence

Ezetimibe has demonstrated cardiovascular benefit in major trials: 2

• IMPROVE-IT trial: When added to moderate-intensity statin therapy in post-acute coronary syndrome patients, ezetimibe reduced the composite endpoint of cardiovascular death, nonfatal MI, unstable angina requiring hospitalization, coronary revascularization, or nonfatal stroke over 6 years median follow-up
• SHARP trial: Simvastatin plus ezetimibe reduced major atherosclerotic cardiovascular disease events in patients with chronic kidney disease over 4.9 years median follow-up

Safety Profile

Adverse Effects: 2

• Monotherapy: upper respiratory tract infection, diarrhea, arthralgia, sinusitis, pain in extremities
• Combination with statin: nasopharyngitis, myalgia, upper respiratory tract infection, arthralgia, diarrhea
• Generally well tolerated with adverse event profile similar to placebo 5

Contraindications and Precautions: 2

• Contraindicated in patients with hypersensitivity to ezetimibe
• Not recommended in moderate to severe hepatic impairment (Child-Pugh B or C) 1
• Monitor hepatic transaminases when used with statins
• Myopathy and rhabdomyolysis reported when used alone or with statins

Drug Interactions

Significant Interactions: 2

• Cyclosporine: increases ezetimibe exposure; monitor cyclosporine levels carefully 3
• Fibrates (gemfibrozil, fenofibrate): increase ezetimibe bioavailability, though clinical significance is minor 3
• Bile acid sequestrants: significantly decrease ezetimibe bioavailability; separate administration by several hours 3

No Clinically Significant Interactions: 3

• Statins (atorvastatin, simvastatin, pravastatin, rosuvastatin, etc.)
• Digoxin, warfarin, glipizide, oral contraceptives
• Food, antacids, cimetidine

Generic Availability

Ezetimibe is available as a generic medication, making it a cost-effective option for LDL-cholesterol lowering. 2 This generic availability is specifically cited as a reason to favor ezetimibe as the first-line nonstatin agent before considering more expensive PCSK9 inhibitors in very high-risk patients. 2

Special Populations

No dosage adjustment required for: 1

• Renal impairment (any severity)
• Geriatric patients
• Mild hepatic impairment

Pregnancy and Lactation: 2

• No safety data in humans; avoid use during pregnancy