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Zetia (Ezetimibe) - Summary



ZETIA (ezetimibe) is in a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol and related phytosterols.

Therapy with lipid-altering agents should be only one component of multiple risk factor intervention in individuals at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia. Drug therapy is indicated as an adjunct to diet when the response to a diet restricted in saturated fat and cholesterol and other nonpharmacologic measures alone has been inadequate.



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 non-familial) 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.


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.


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.


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Published Studies Related to Zetia (Ezetimibe)

Rationale and design of LAPLACE-2: a phase 3, randomized, double-blind, placebo- and ezetimibe-controlled trial evaluating the efficacy and safety of evolocumab in subjects with hypercholesterolemia on background statin therapy. [2014]
Low-density lipoprotein cholesterol (LDL-C) levels are significantly associated with atherosclerotic cardiovascular disease (ASCVD) risk, and studies using interventions that lower LDL-C levels have been shown to reduce the risk of ASCVD events and mortality... This study will also provide comparative efficacy, safety, and tolerability data between evolocumab and ezetimibe when added to background atorvastatin therapy.

Simvastatin but not ezetimibe reduces sympathetic activity despite similar reductions in cholesterol levels. [2014]
The relationship between the sympatholytic effects of statins and their lipid-lowering activity remains unclear. Ezetimibe lowers cholesterol, but its sympatholytic activity is unknown...

Changes in lipoprotein particle number with ezetimibe/simvastatin coadministered with extended-release niacin in hyperlipidemic patients. [2013]
CONCLUSIONS: These results suggest that E/S+N improves lipoprotein particle

The effects of ezetimibe/simvastatin versus simvastatin monotherapy on platelet and inflammatory biomarkers in patients with metabolic syndrome. [2013]
In a randomized, double-blind, crossover study of 15 aspirin-naive patients (mean age 48.8 ± 10.2 years) with the metabolic syndrome, statin monotherapy (simvastatin 40 mg daily) was compared to combination therapy (simvastatin 40 mg and ezetimibe 10 mg daily) on biomarkers of inflammation and platelet activity...

A comparison of efficacy and safety of an ezetimibe/simvastatin combination compared with other intensified lipid-lowering treatment strategies in diabetic patients with symptomatic cardiovascular disease. [2013]
The low-density lipoprotein cholesterol (LDL-C) lowering efficacy of switching to ezetimibe/simvastatin (EZ/S) 10/20 mg versus doubling the run-in statin dose (to simvastatin 40 mg or atorvastatin 20 mg) or switching to rosuvastatin 10 mg in subjects with cardiovascular disease (CVD) and diabetes was assessed...

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Clinical Trials Related to Zetia (Ezetimibe)

Pharmacokinetic Drug Interaction Between Ezetimibe and Tacrolimus After Single Dose Administration in Healthy Subjects [Completed]

Pharmacokinetic Drug Interaction Between Ezetimibe and Sirolimus After Single Dose Administration in Healthy Subjects [Completed]

Comparison of Ezetimibe Plus Simvastatin Versus Ezetimibe or Simvastatin Alone in Subjects With Primary Hypercholesterolemia (Study P03757)(COMPLETED) [Completed]
This is a multicenter, randomized, double blind; active-controlled parallel groups study enrolling subjects with primary hypercholesterolemia. Subjects receive ezetimibe, simvastatin, or the combination once daily for 8 weeks to determine the effect on LDL-cholesterol.

Assessment of Potential Interaction Between Ezetimibe and Rosuvastatin in Healthy Subjects With High Cholesterol (P03317)(COMPLETED) [Completed]
The purpose of this study is to obtain data of the coadministration of ezetimibe and rosuvastatin to support the concomitant use of these two drugs in patients requiring additional cholesterol-lowering management. Treatment is administered for 14 days.

Evaluation of Potential for Drug Interaction Between SCH 58235 (Ezetimibe) and Pitavastatin (Study P03962)(COMPLETED) [Completed]
This study was designed to evaluate the pharmacokinetic interaction and safety of coadministration of SCH 58235 (ezetimibe) and pitavastatin in healthy Japanese adult male subjects or adult male subjects having no obvious disease other than high cholesterol levels.

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Reports of Suspected Zetia (Ezetimibe) Side Effects

Myalgia (38)Pain in Extremity (31)Fatigue (27)Arthralgia (25)Asthenia (24)Dyspnoea (22)Constipation (21)Nausea (21)Drug Ineffective (20)Back Pain (20)more >>


Based on a total of 1 ratings/reviews, Zetia has an overall score of 9. The effectiveness score is 8 and the side effect score is 10. The scores are on ten point scale: 10 - best, 1 - worst.

Zetia review by 60 year old male patient

Overall rating:  
Effectiveness:   Considerably Effective
Side effects:   No Side Effects
Treatment Info
Condition / reason:   high cholestrol
Dosage & duration:   10mg/day taken ongoing for the period of ongoing
Other conditions:   knee osteoartritis
Other drugs taken:   glucosamine, multivitamins
Reported Results
Benefits:   My target was to have the a cholestrol reduction from 240 to under 200. I did not want want to take statins because I am not comfortable with drugs that inhibit normal metabolic processes. Evolution is parsimonius, and inhibition of any enzyme is likely to be reflected as an adverse effect in a seemingly unrelated area. Also, I did not want to take red yeast rice, which basically is a non-phrmaceutical grade of a statin. I liked the physical mode of action of Zetia. Within 6 months of starting treatment, my total cholesterol was down from to 200 and my HDL went up from 45 to 58.
Side effects:   I did not experience any perceptible side effects.
Comments:   See treatment benefits above. I take my daily dose of Zetia shortly after having my breakfast.

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Page last updated: 2015-08-10

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