ZETIA (ezetimibe)

The information on this site is intended for healthcare professionals in the United States and is not intended for the general public.

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Important Information About ZETIA
ROSUVASTATIN – Stein 2003(3) A Titration Step Delivered LIMITED LDL-C Reduction

Examine Additional Statin Titration Studies

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Study Design3: An 18-week, weighted-randomization, double-blind, parallel-group, forced-titration study assessing LDL-C change from baseline in patients (N=623) with heterozygous familial hypercholesterolemia randomized to either rosuvastatin 20 mg or atorvastatin 20 mg. Patients were force-titrated every 6 weeks up to the 80-mg statin dose. The primary end point was the percent change in LDL-C from baseline to Week 18. Mean baseline LDL-C was 292 mg/dL and 288 mg/dL for the rosuvastatin and atorvastatin groups, respectively.
 
After 6 weeks, mean LDL-C reduction from baseline was 47% for rosuvastatin 20 mg vs 38% for atorvastatin 20 mg (P<0.001). After 12 weeks, mean LDL-C reduction from baseline was 54% for rosuvastatin 40 mg vs 46% for atorvastatin 40 mg (P<0.001). After 18 weeks, mean LDL-C reduction from baseline was 58% with rosuvastatin 80 mg vs 50% with atorvastatin 80 mg (P<0.001).
 
Additional LDL-C reduction provided by titration of rosuvastin 20 mg to 40 mg was 7% and from rosuvastatin 40 mg to 80 mg was 4%. Additional LDL-C reduction provided by titration of atorvastatin 20 mg to 40 mg was 8% and from atorvastatin 40 mg to 80 mg was 4%. Rosuvastatin 80 mg was included in this study but is not an approved dose.
 
The additional percent reductions in LDL-C with successive doses were obtained by subtraction from data presented.

Important Information About ZETIA

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

ZETIA, administered alone or in combination with an HMG-CoA reductase inhibitor (statin), is indicated as adjunctive therapy to diet for the reduction of elevated TOTAL-C, LDL-C, and Apo B in patients with primary (heterozygous familial and nonfamilial) hyperlipidemia when diet alone is not enough.

Contraindications: hypersensitivity to any component of this medication.
Statin contraindications apply when used with a statin: active liver disease; unexplained persistent elevations in hepatic transaminase levels. Statins are contraindicated in pregnant and nursing women. Refer to the statin label for details.

When using ZETIA with a statin, also follow the label recommendations for that specific statin.

Selected Cautionary Information: When ZETIA was coadministered with a statin, consecutive elevations in hepatic transaminase levels (>3 x ULN) were slightly higher (1.3%) than those of statins alone (0.4%). Liver function tests should be performed when ZETIA is added to statin therapy and according to statin recommendations. Should an increase in ALT or AST >3 x ULN persist, consider withdrawal of ZETIA and/or the statin.

Patients should be advised to promptly report muscle pain, tenderness, or weakness. Risk for skeletal muscle toxicity increases with higher statin doses, advanced age (>65), hypothyroidism, renal impairment, and depending on the statin used, concomitant use of other drugs. Discontinue drug if myopathy is diagnosed or suspected.

ZETIA is not recommended in patients with moderate to severe hepatic impairment.

The coadministration of ZETIA with fibrates other than fenofibrate is not recommended until use in patients is adequately studied.

Exercise caution when using ZETIA and cyclosporine concomitantly because exposure to both drugs is increased. Cyclosporine concentrations should be monitored in these patients.

ZETIA should be used in pregnant or nursing women only if the benefit outweighs the risk.

In clinical trials, regardless of causality assessment, the most frequent side effects for ZETIA coadministered with a statin vs statin alone included nasopharyngitis (3.7% vs 3.3%), myalgia (3.2% vs 2.7%), upper respiratory tract infection (2.9% vs 2.8%), arthralgia (2.6% vs 2.4%), and diarrhea (2.5% vs 2.2%); for ZETIA administered alone vs placebo: upper respiratory tract infection (4.3% vs 2.5%), diarrhea (4.1% vs 3.7%), arthralgia (3.0% vs 2.2%), sinusitis (2.8% vs 2.2%), and pain in extremity (2.7% vs 2.5%).

Before prescribing ZETIA, please read the Prescribing Information and Patient Product Information.

Reference: 3. Stein EA, Strutt K, Southworth H, Diggle PJ, Miller E, for the HeFH Study Group. Comparison of rosuvastatin versus atorvastatin in patients with heterozygous familial hypercholesterolemia. Am J Cardiol. 2003;91:1287–1293.

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