Ezetimibe: A Selective Cholesterol Absorption Inhibitor

Edith A. Nutescu, Pharm.D.; Nancy L. Shapiro, Pharm.D.


Pharmacotherapy. 2003;23(11) 

In This Article

Role in Therapy

Ezetimibe was approved in the United States and Germany in October 2002 as adjunctive therapy to diet, alone or combined with statins, for reduction of elevated levels of total cholesterol, LDL, and apolipoprotein B in patients with primary (heterozygous familial and nonfamilial) hypercholesterolemia. The combination of ezetimibe with atorvastatin or simvastatin is indicated for reduction of elevated total cholesterol and LDL levels in patients with HoFH, as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis), or if such treatments are unavailable. In addition, ezetimibe is indicated as adjunctive therapy to diet for reduction of elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia.[17]

Ezetimibe 10 mg/day is the recommended dosage for all indications. For convenience and to enhance compliance in patients receiving combination therapy with a statin, the daily doses may be taken at the same time. No additional laboratory monitoring is necessary when ezetimibe is given as monotherapy. When administering ezetimibe in combination with a statin, liver function should be monitored according to the recommendations for the specific statin.

In clinical practice, ezetimibe's role as monotherapy is for patients who require modest reductions in their LDL level or who cannot tolerate other lipid-lowering agents. Ezetimibe's major benefit is seen when administered in combination with a statin in patients who cannot tolerate high statin dosages or who need further LDL reductions despite treatment with maximum statin dosages.[57] Due to its additive effect, ezetimibe is beneficial for attaining large LDL reductions when given in combination with low-dose statin therapy. Addition of ezetimibe 10 mg to the starting dose of a statin is equivalent to doubling the statin dose 2-3 times (Figure 5).[57]

Effect of ezetimibe plus statin combination therapy on reducing statin dosage. LDL = low-density lipoprotein cholesterol. (From reference 57 with permission.)

Ezetimibe offers several advantages over the intestinally acting lipid-lowering agents that are available (e.g., bile acid sequestrants, plant stanol and sterol esters). It is more selective and does not affect absorption of lipid-soluble vitamins; lowers triglyceride levels; has an excellent side-effect profile, which enhances patient tolerability; and offers convenient, once-daily dosing, which improves compliance ( Table 2 ).


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