What is the recommended dose of Ezetimibe (ezetimibe) for treating high cholesterol?

Ezetimibe Dosing for High Cholesterol

The recommended dose of ezetimibe for treating high cholesterol is 10 mg orally once daily, administered with or without food. 1

Dosing Guidelines and Administration

• Ezetimibe 10 mg daily is the standard FDA-approved dose for all approved indications, including primary hyperlipidemia, heterozygous familial hypercholesterolemia (HeFH), and homozygous familial hypercholesterolemia (HoFH) 1
• The medication can be taken at any time of day, with or without food 1
• If a dose is missed, take it as soon as possible, but do not double the next dose 1
• When used with bile acid sequestrants, administer ezetimibe at least 2 hours before or 4 hours after the bile acid sequestrant 1

Efficacy and LDL-C Reduction

• As monotherapy, ezetimibe 10 mg daily produces a consistent reduction in LDL-C by approximately 15-20% 2
• When combined with statin therapy, ezetimibe provides an additional 17-18% placebo-corrected incremental reduction in LDL-C 3
• The combination of ezetimibe with bempedoic acid (as a fixed-dose combination tablet) can achieve a 38% reduction in LDL-C when added to statin therapy 3

Special Populations and Considerations

• For pediatric patients with HeFH, the same 10 mg daily dose is recommended for those 10 years of age and older 1
• For pediatric patients with homozygous familial sitosterolemia, ezetimibe 10 mg daily is recommended for those 9 years of age and older 1
• No dose adjustment is necessary for elderly patients or those with mild hepatic impairment or renal insufficiency 1

Drug Interactions

• Avoid concomitant use of ezetimibe with simvastatin >20 mg daily or pravastatin >40 mg daily due to potential drug interactions 3
• Monitor for interactions with cyclosporine and fibrates 3
• When used with statins, be aware of the potential for increased risk of myopathy/rhabdomyolysis, although this is rare with ezetimibe monotherapy 1

Alternative Dosing Considerations

• While the standard dose is 10 mg daily, some research suggests that half-dose ezetimibe (5 mg) may be effective in Asian patients, showing a 24% reduction in LDL-C when added to statin therapy 4
• Conversely, limited research has explored ezetimibe 20 mg daily, which showed additional LDL-C reduction of 10.3% compared to the 10 mg dose in patients on concomitant statin therapy, but this is not an FDA-approved dosing regimen 5

Monitoring Recommendations

• Assess LDL-C when clinically appropriate, as early as 4 weeks after initiating ezetimibe 1
• Perform liver enzyme testing as clinically indicated, especially when used in combination with statins 1
• Consider withdrawal of ezetimibe if increases in ALT or AST ≥3 times the upper limit of normal persist 1

Clinical Use in Treatment Algorithms

• Ezetimibe is recommended as the initial non-statin agent for most patients when additional LDL-C lowering is desired beyond statin therapy 3
• It is preferred as the initial non-statin therapy due to its tolerability, convenience, and single-tablet daily dose 3
• For statin-intolerant patients, ezetimibe 10 mg is often the first-line therapy before considering PCSK9 inhibitors or bempedoic acid 6

Safety Profile

• Ezetimibe has an adverse event profile similar to placebo when used as monotherapy 2
• Common adverse effects include upper respiratory tract infection, muscle spasms, back pain, and abdominal pain 3
• Discontinue ezetimibe when pregnancy is recognized unless benefits outweigh potential risks 3

The 10 mg daily dose of ezetimibe has been extensively studied and has demonstrated a favorable efficacy and safety profile, making it the standard dose for clinical practice in the treatment of high cholesterol.