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ZETIA (ezetimibe) is indicated as an adjunct to lifestyle changes, including diet, when the response to diet and other non-pharmacological measures alone has been inadequate.

ZETIA, administered alone or with an HMG-CoA reductase inhibitor (statin), is indicated for the reduction of elevated total cholesterol (total-C), low density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), and triglycerides (TG) and to increase high density lipoprotein cholesterol (HDL-C) in patients with primary (heterozygous familial and non-familial) hypercholesterolemia.

ZETIA, administered in combination with fenofibrate, is indicated for the reduction of elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia.

ZETIA, administered with a statin, is indicated for the reduction of elevated total-C and LDL-C levels in patients with HoFH as an adjunct to treatments such as LDL apheresis or if such treatments are not possible.

ZETIA is indicated for the reduction of elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia.

Hypersensitivity to any component of this medication.

When ZETIA is to be administered with a statin or with fenofibrate, the contraindications to that medication should be reviewed before starting concomitant therapy.

The combination of ZETIA with a statin is contraindicated in patients with active liver disease or unexplained persistent elevations in serum transaminases.

All statins and fenofibrate are contraindicated in pregnant and nursing women. When ZETIA is administered with a statin or with fenofibrate in a woman of childbearing potential, refer to the product labeling for that medication (see Warnings and Precautions, Special Populations, Pregnant Women).

When ZETIA is to be administered with a statin or with fenofibrate, please refer also to the Product Monograph for that medication. Note that all statins and fenofibrate are contraindicated in pregnant women (see the Product Monograph for the medication; see Warnings and Precautions, Special Populations, Pregnant Women).

When ZETIA is initiated in a patient already taking a statin or fenofibrate, liver function tests should be considered at initiation of ZETIA therapy, and then as indicated (see Adverse Reactions, Abnormal Hematologic and Clinical Chemistry Findings).

When ZETIA is initiated at the same time as a statin or fenofibrate, liver function tests should be performed at initiation of therapy and according to the recommendations of that medication (see Adverse Reactions, Abnormal Hematologic and Clinical Chemistry Findings).

In controlled monotherapy studies, the incidence of consecutive elevations (≥3 times the upper limit of normal [ULN]) in serum transaminases was similar between ZETIA (0.5%) and placebo (0.3%).

In controlled coadministration trials in patients receiving ZETIA with a statin, the incidence of consecutive transaminase elevations (≥3×ULN) was 1.3% compared to 0.4% in patients on a statin alone.

The pharmacokinetics of ezetimibe were examined in patients with impaired liver function as defined by the Child-Pugh scoring system.

• In patients with mild hepatic insufficiency (Child-Pugh score 5 or 6), the mean area under the curve (AUC) for total ezetimibe (after a single 10 mg dose of ZETIA) was increased approximately 1.7-fold compared to healthy subjects. No dosage adjustment is necessary for patients with mild hepatic insufficiency.

  
  

• In patients with moderate hepatic insufficiency (Child-Pugh score 7 to 9), the mean AUC for total ezetimibe (after multiple doses of 10 mg daily) was increased approximately 4-fold on Day 1 and Day 14 compared to healthy subjects. Due to the unknown effects of the increased exposure to ezetimibe in patients with moderate (Child-Pugh score 7 to 9) or severe (Child-Pugh score >9) hepatic insufficiency, ezetimibe is not recommended in these patients.

  
  

• No pharmacokinetic studies with ezetimibe have been carried out in patients with either active liver disease or unexplained and persistent elevations in serum transaminases. It is recommended that care be exercised in such patients.

  
  

The coadministration of ZETIA and a statin is contraindicated in patients with active liver disease or unexplained and persistent elevations in serum transaminases.

Post-marketing reports of adverse events have included rare cases of hepatitis in patients taking ZETIA, although causality has not been proven. If patients develop signs or symptoms of hepatitis, liver function should be evaluated.

The coadministration of ezetimibe with fibrates other than fenofibrate has not been studied. Therefore, coadministration of ZETIA and fibrates (other than fenofibrate) is not recommended (see Drug Interactions).

If cholelithiasis is suspected in a patient receiving ZETIA and fenofibrate, gallbladder studies are indicated and alternative lipid-lowering therapy should be considered (see Adverse Reactions and the Product Monograph for fenofibrate).

Post-marketing reports of adverse events have included rare cases of acute pancreatitis occurring in patients taking ZETIA, although causality has not been proven. The diagnosis of acute pancreatitis should be considered in patients taking ZETIA who develop sudden acute abdominal pain.

Myopathy and rhabdomyolysis are known adverse effects of statins and fibrates. Post-marketing reports of adverse events have included rare cases of myopathy/rhabdomyolysis occurring in patients taking ZETIA with or without a statin, regardless of causality. Myopathy/Rhabdomyolysis should be considered in patients presenting with muscle pain during treatment with ZETIA with or without a statin or fenofibrate, and consideration given to discontinuation of the drugs. Most cases of myopathy/rhabdomyolysis resolved when drugs were discontinued.

In controlled clinical trials, the incidence of myalgia was 5.0% for ZETIA vs 4.6% for placebo (see Adverse Reactions, Table 2). Post-marketing reports of adverse events have included myalgia in patients taking ZETIA with or without a statin, regardless of causality. Patients should be instructed to contact their physician if they experience persistent and severe muscle pains with no obvious cause.

A number of patients treated with ZETIA, in whom myalgia occurred had previously experienced myalgia (with or without elevated CK levels) with statin therapy. Patients with a history of statin intolerance (myalgia with or without elevated CK levels) should be closely monitored for adverse muscle events during treatment with ZETIA.

After a single 10 mg dose of ZETIA in patients with severe renal disease, the mean AUC for total ezetimibe was increased approximately 1.5 fold, compared to healthy subjects. Accordingly, no dosage adjustment is necessary for renal impaired patients.

No clinical data on exposed pregnancies are available for ZETIA. The effects of ezetimibe on labour and delivery in pregnant women are unknown. Note that all statins and fenofibrate are contraindicated in pregnant women (see the Product Monograph for the medication). Caution should be exercised when prescribing to pregnant women.

Studies in rats have shown that ezetimibe is excreted in milk. It is not known whether ezetimibe is excreted into human breast milk, therefore, ZETIA should not be used in nursing mothers unless the potential benefit justifies the potential risk to the infant. Note that all statins and fenofibrate are contraindicated in nursing women (see the Product Monograph for the medication).

The pharmacokinetics of ZETIA in adolescents (10 to 18 years) have been shown to be similar to that in adults. Treatment experience with ZETIA in the pediatric population is limited to 4 patients (9 to 17 years) in the sitosterolemia study and 5 patients (11 to 17 years) in the HoFH study. Treatment with ZETIA in children (<10 years) is not recommended.

Plasma concentrations for total ezetimibe are about 2-fold higher in the elderly (≥65 years) than in the young (18 to 45 years). LDL-C reduction and safety profile are comparable between elderly and young subjects treated with ZETIA. Therefore, no dosage adjustment is necessary in the elderly.

Plasma concentrations for total ezetimibe are slightly higher (<20%) in women than in men. LDL-C reduction and safety profile are comparable between men and women treated with ezetimibe. Therefore, no dosage adjustment is necessary on the basis of sex.

Based on a meta-analysis of pharmacokinetic studies, there were no pharmacokinetic differences between Blacks and Caucasians.

The most commonly reported adverse events in clinical studies were upper respiratory tract infection, headache, myalgia and back pain. In post-marketing use, serious adverse events reported rarely or very rarely, regardless of causality, included hepatitis, hypersensitivity reactions, pancreatitis and myopathy/rhabdomyolysis.

When ZETIA is to be administered with a statin or fenofibrate, please refer also to the Product Monograph for that medication.

ZETIA clinical trial experience involved 2486 patients in placebo-controlled monotherapy trials (1691 treated with ZETIA) and 4547 patients in active controlled trials (449 of whom were treated with ZETIA alone and 1708 treated with ZETIA plus a statin and 185 patients treated with ZETIA and fenofibrate). The studies were of 8 to 14 weeks duration. The overall incidence of adverse events reported with ZETIA was similar to that reported with placebo and the discontinuation rates due to treatment related adverse events was similar between ZETIA (2.3%) and placebo (2.1%).