When to initiate ezetimibe (Zetia) therapy?

From the Guidelines

Ezetimibe should be started in patients with clinical ASCVD who are on maximally tolerated statin therapy and are judged to be at very high risk and have an LDL-C level of 70 mg/dL or higher, as recommended by the 2018 AHA/ACC/AACVPR/AAPA/ABC/ACPM/ADA/AGS/APhA/ASPC/NLA/PCNA guideline on the management of blood cholesterol 1. This guideline suggests that ezetimibe therapy is reasonable in patients who have not achieved their LDL-C targets with statin therapy alone. The typical starting dose of ezetimibe is 10 mg once daily, taken with or without food, and it can be administered at any time of day. Some key points to consider when starting ezetimibe include:

• Ezetimibe works by inhibiting cholesterol absorption in the small intestine, complementing statins' mechanism of reducing cholesterol synthesis in the liver 1.
• This medication is particularly useful for patients who experience muscle pain, weakness, or elevated liver enzymes with statins.
• Ezetimibe may also be initiated as monotherapy in patients with mild to moderate hypercholesterolemia who are statin-intolerant, though combination therapy with statins is generally more effective for LDL reduction.
• When adding ezetimibe to statin therapy, no dose adjustment is typically needed for either medication.
• Patients should be monitored with lipid panels 4-12 weeks after starting treatment to assess efficacy.
• Common side effects of ezetimibe include diarrhea, joint pain, and fatigue, though it is generally well-tolerated with fewer adverse effects than statins. In patients 20 to 75 years of age with an LDL-C level of 190 mg/dL or higher, maximally tolerated statin therapy is recommended, and ezetimibe therapy is reasonable if the patient achieves less than a 50% reduction in LDL-C while receiving maximally tolerated statin therapy and/or has an LDL-C level of 100 mg/dL or higher 1.

From the FDA Drug Label

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 The recommended dose of ezetimibe tablets is 10 mg orally once daily, administered with or without food

• Ezetimibe Initiation: Ezetimibe can be started at any time, but it is recommended to assess LDL-C levels when clinically appropriate, as early as 4 weeks after initiating ezetimibe tablets 2.
• Dosing: The recommended dose of ezetimibe is 10 mg orally once daily, administered with or without food 2.
• Administration with Other Medications: Ezetimibe tablets should be administered at least 2 hours before or 4 hours after administration of a bile acid sequestrant 2 2.

From the Research

When to Start Ezetimibe

• Ezetimibe can be started when patients are unable to achieve their LDL cholesterol goals with statin monotherapy 3, 4, 5.
• It can be used as monotherapy for patients who are intolerant to statins 6, 7.
• Ezetimibe can also be added to statin therapy to further reduce LDL cholesterol levels in high-risk patients 6, 4, 5.
• The decision to start ezetimibe should be based on the patient's individual risk factors and response to other lipid-lowering therapies 3, 4, 5.

Patient Selection

• High-risk patients with hypercholesterolemia who are unable to achieve their LDL cholesterol goals with statin monotherapy may benefit from ezetimibe therapy 6, 4, 5.
• Patients who are intolerant to statins may also be considered for ezetimibe monotherapy 6, 7.
• The presence of other cardiovascular risk factors, such as diabetes or hypertension, may also influence the decision to start ezetimibe 3, 4.

Timing of Initiation

• Ezetimibe can be initiated at any time, depending on the patient's individual needs and response to other therapies 3, 4, 5.
• It is essential to monitor the patient's LDL cholesterol levels and adjust the treatment plan as needed to ensure that the patient is achieving their lipid goals 6, 4, 5.