Zetia (Ezetimibe) - Summary

ZETIA SUMMARY

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

ZETIA is indicated for the following:

Primary Hypercholesterolemia

Monotherapy

ZETIA, administered alone, 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 non-familial) hypercholesterolemia.

Combination therapy with HMG-CoA reductase inhibitors

ZETIA, administered in combination with an HMG-CoA reductase inhibitor, 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 non-familial) hypercholesterolemia.

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.

Therapy with lipid-altering agents should be a component of multiple risk-factor intervention in individuals at increased risk for atherosclerotic vascular disease due to hypercholesterolemia. Lipid-altering agents should be used in addition to an appropriate diet (including restriction of saturated fat and cholesterol) and when the response to diet and other non-pharmacological measures has been inadequate.

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NEWS HIGHLIGHTS

Media Articles Related to Zetia (Ezetimibe)

Liptruzet Approved By FDA To Cut Cholesterol, Despite Criticism By Cardiologists
Source: Cholesterol News From Medical News Today [2013.05.05]
Liptruzet, a cholesterol-lowering drug that combines Merck's Zetia (ezetimibe) with atorvastatin (generic version of Pfizer's Lipitor) has been approved by the US FDA (Food and Drug Administration)...

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Published Studies Related to Zetia (Ezetimibe)

Effect of a monoclonal antibody to PCSK9, REGN727/SAR236553, to reduce low-density lipoprotein cholesterol in patients with heterozygous familial hypercholesterolaemia on stable statin dose with or without ezetimibe therapy: a phase 2 randomised controlled trial. [2012]
hypercholesterolaemia... INTERPRETATION: REGN727 was well tolerated and achieved substantial further LDL-C

The effect of ezetimibe and simvastatin on hemostasis in patients with isolated hypercholesterolemia. [2012]
The aim of this study was to assess the strength of hemostatic effects of ezetimibe, administered alone or in combination with simvastatin, in patients with isolated hypercholesterolemia. One hundred and four patients with isolated primary hypercholesterolemia were randomized to one of four treatment groups, simultaneously treated for 90 days with ezetimibe (10 mg daily), simvastatin (40 mg daily), ezetimibe (10 mg daily) plus simvastatin (40 mg daily), or placebo.

Safety and efficacy of ezetimibe added on to rosuvastatin 5 or 10 mg versus up-titration of rosuvastatin in patients with hypercholesterolemia (the ACTE Study). [2011.08.15]
The present multicenter, 6-week, randomized, double-blind, parallel-group, clinical trial evaluated the safety and efficacy of ezetimibe (10 mg) added to stable rosuvastatin therapy versus up-titration of rosuvastatin from 5 to 10 mg or from 10 to 20 mg... In conclusion, compared to up-titration doubling of the rosuvastatin dose, ezetimibe 10 mg added to stable rosuvastatin 5 mg or 10 mg produced greater improvements in many lipid parameters and achieved greater attainment of the National Cholesterol Education Program Adult Treatment Panel III recommended LDL cholesterol targets in subjects with elevated LDL cholesterol and at moderately high/high coronary heart disease risk.

Combined effects of ezetimibe and phytosterols on cholesterol metabolism: a randomized, controlled feeding study in humans. [2011.08.02]
CONCLUSION: The addition of phytosterols to ezetimibe significantly enhanced the effects of ezetimibe on whole-body cholesterol metabolism and plasma low-density lipoprotein cholesterol. The large cumulative action of combined dietary and pharmacological treatment on cholesterol metabolism emphasizes the potential importance of dietary phytosterols as adjunctive therapy for the treatment of hypercholesterolemia. CLINICAL TRIAL REGISTRATION: URL: http://www.clinicaltrials.gov. Unique identifier: NCT00863265.

The ezetimibe controversy: implications for clinical practice. [2011.08]
Low-density lipoprotein cholesterol (LDL-C) remains the primary target of lipid-lowering therapy. Achieving LDL-C goals as outlined by the National Cholesterol Education Program Adult Treatment Panel III can be difficult with statins alone; therefore, adjunctive therapy is often indicated to reduce cardiovascular risk...

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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 >>

PATIENT REVIEWS / RATINGS / COMMENTS

Zetia review by 60 year old male patient
		Rating
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.