Indicated for:

Primary Hyperlipidemia:

Monotherapy:

• ZETIA, administered alone, is indicated as adjunctive therapy to diet for the reduction of elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), and non-high-density lipoprotein cholesterol (non-HDL-C) in patients with primary (heterozygous familial and nonfamilial) hyperlipidemia.

Combination Therapy with HMG-CoA Reductase Inhibitors (Statins):

• ZETIA, administered in combination with a 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor (statin), is indicated as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with primary (heterozygous familial and non-familial) hyperlipidemia.

Combination Therapy with Fenofibrate:

• ZETIA, administered in combination with fenofibrate, is indicated as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, Apo B, and non-HDL-C in adult patients with mixed hyperlipidemia.

Homozygous Familial Hypercholesterolemia (HoFH):

• The combination of ZETIA and atorvastatin or simvastatin is indicated for the reduction of elevated total-C and LDL-C levels in patients with HoFH, as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) or if such treatments are unavailable.

Homozygous Sitosterolemia:

• ZETIA is indicated as adjunctive therapy to diet for the reduction of elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia.

The effect of ZETIA on cardiovascular morbidity and mortality has not been determined.

ZETIA has not been studied in Fredrickson Type I, III, IV, and V dyslipidemias. 

The combination of ZETIA with a statin is contraindicated in patients with active liver disease or unexplained persistent elevations in hepatic transaminase levels.

In post-marketing experience with ZETIA, cases of myopathy and rhabdomyolysis have been reported. Risk for skeletal muscle toxicity increases with higher doses of statin, advanced age (>65), hypothyroidism, renal impairment, and depending on the statin used, concomitant use of other drugs.

ZETIA is contraindicated in the following conditions:

• The combination of ZETIA with a statin is contraindicated in patients with active liver disease or unexplained persistent elevations in hepatic transaminase levels
• Women who are pregnant or may become pregnant. Because statins decrease cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol, ZETIA in combination with a statin may cause fetal harm when administered to pregnant women. Additionally, there is no apparent benefit to therapy during pregnancy, and safety in pregnant women has not been established. If the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus and the lack of known clinical benefit with continued use during pregnancy
• Nursing mothers. Because statins may pass into breast milk, and because statins have the potential to cause serious adverse reactions in nursing infants, women who require ZETIA treatment in combination with a statin should be advised not to nurse their infants

Dosing of ZETIA should occur either ≥2 hours before or ≥4 hours after administration of a bile acid sequestrant.

When given with simvastatin in patients with moderate to severe renal impairment (estimated glomerular filtration rate <60 mL/min/1.73 m²), doses of simvastatin exceeding 20 mg should be used with caution and close monitoring.

Caution should be exercised when using ZETIA and cyclosporine concomitantly due to increased exposure to both ezetimibe and cyclosporine.

Concomitant cholestyramine administration decreased the mean area under the curve (AUC) of total ezetimibe approximately 55%.

Co-administration of ZETIA with fibrates other than fenofibrate is not recommended until use in patients is adequately studied.

If ezetimibe is added to warfarin, a coumarin anticoagulant, the International Normalized Ratio (INR) should be appropriately monitored.

ZETIA is contraindicated in women who are pregnant or may become pregnant.

It is not known whether ezetimibe is excreted into human breast milk.In rat studies, exposure to total ezetimibe in nursing pups was up to half of that observed in maternal plasma.

GoToSource

• Use in patients under the age of 10 or premenarchal girls. GoToSource 

• Nonalcoholic fatty liver disease. GoToSource

Rhabdomyolysis (breakdown of muscle tissue). GoToSource

Paradoxical progression of atherosclerosis. GoToSource

Impaired kidney allograft function. GoToSource

Prostate, gastrointestinal and skin cancers. GoToSource 

Toxic hepatitis (liver inflammation). GoToSource 

Liver failure when used with simvastatin. GoToSource 

Jaundice. GoToSource 

Immune thrombocytopenia (bleeding disorder). GoToSource 

Elevations of liver transaminases and myalgia. GoToSource

Pancreatitis. GoToSource

Lawsuits filed for rhabdomyolysis, liver damage, pancreatitis, thrombocytopenia, hepatitis and heart attacks.