Zetia (Page 6 of 7)

14.2 Homozygous Familial Hypercholesterolemia (HoFH)

A study was conducted to assess the efficacy of ZETIA in the treatment of HoFH. This double-blind, randomized, 12-week study enrolled 50 patients with a clinical and/or genotypic diagnosis of HoFH, with or without concomitant LDL apheresis, already receiving atorvastatin or simvastatin (40 mg). Patients were randomized to one of three treatment groups, atorvastatin or simvastatin (80 mg), ZETIA administered with atorvastatin or simvastatin (40 mg), or ZETIA administered with atorvastatin or simvastatin (80 mg). Due to decreased bioavailability of ezetimibe in patients concomitantly receiving cholestyramine [see Drug Interactions (7.4)] , ezetimibe was dosed at least 4 hours before or after administration of resins. Mean baseline LDL-C was 341 mg/dL in those patients randomized to atorvastatin 80 mg or simvastatin 80 mg alone and 316 mg/dL in the group randomized to ZETIA plus atorvastatin 40 or 80 mg or simvastatin 40 or 80 mg. ZETIA, administered with atorvastatin or simvastatin (40- and 80-mg statin groups, pooled), significantly reduced LDL-C (21%) compared with increasing the dose of simvastatin or atorvastatin monotherapy from 40 to 80 mg (7%). In those treated with ZETIA plus 80-mg atorvastatin or with ZETIA plus 80-mg simvastatin, LDL-C was reduced by 27%.

14.3 Homozygous Sitosterolemia (Phytosterolemia)

A study was conducted to assess the efficacy of ZETIA in the treatment of homozygous sitosterolemia. In this multicenter, double-blind, placebo-controlled, 8-week trial, 37 patients with homozygous sitosterolemia with elevated plasma sitosterol levels (>5 mg/dL) on their current therapeutic regimen (diet, bile-acid-binding resins, statins, ileal bypass surgery and/or LDL apheresis), were randomized to receive ZETIA (n=30) or placebo (n=7). Due to decreased bioavailability of ezetimibe in patients concomitantly receiving cholestyramine [see Drug Interactions (7.4)] , ezetimibe was dosed at least 2 hours before or 4 hours after resins were administered. Excluding the one subject receiving LDL apheresis, ZETIA significantly lowered plasma sitosterol and campesterol, by 21% and 24% from baseline, respectively. In contrast, patients who received placebo had increases in sitosterol and campesterol of 4% and 3% from baseline, respectively. For patients treated with ZETIA, mean plasma levels of plant sterols were reduced progressively over the course of the study. The effects of reducing plasma sitosterol and campesterol on reducing the risks of cardiovascular morbidity and mortality have not been established.

Reductions in sitosterol and campesterol were consistent between patients taking ZETIA concomitantly with bile acid sequestrants (n=8) and patients not on concomitant bile acid sequestrant therapy (n=21).

Limitations of Use

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

16 HOW SUPPLIED/STORAGE AND HANDLING

ZETIA, 10 mg, are white to off-white, capsule-shaped tablets debossed with “414” on one side. They are supplied as follows:

NDC 78206-178-01 bottles of 30

Storage

Store at 25°C (77°F); excursions permitted to 15–30°C (59–86°F). [See USP Controlled Room Temperature.] Protect from moisture.

17 PATIENT COUNSELING INFORMATION

See FDA-Approved Patient Labeling (Patient Information).

Patients should be advised to adhere to their National Cholesterol Education Program (NCEP)-recommended diet, a regular exercise program, and periodic testing of a fasting lipid panel.

17.1 Muscle Pain

All patients starting therapy with ezetimibe should be advised of the risk of myopathy and told to report promptly any unexplained muscle pain, tenderness or weakness. The risk of this occurring is increased when taking certain types of medication. Patients should discuss all medication, both prescription and over-the-counter, with their physician.

17.2 Liver Enzymes

Liver tests should be performed when ZETIA is added to statin therapy and according to statin recommendations.

17.3 Pregnancy

Women of childbearing age should be advised to use an effective method of birth control to prevent pregnancy while using ZETIA added to statin therapy. Discuss future pregnancy plans with your patients, and discuss when to stop combination ZETIA and statin therapy if they are trying to conceive. Patients should be advised that if they become pregnant they should stop taking combination ZETIA and statin therapy and call their healthcare professional.

17.4 Breastfeeding

Women who are breastfeeding should be advised to not use ZETIA added to statin therapy. Patients who have a lipid disorder and are breastfeeding should be advised to discuss the options with their healthcare professionals.

Organon LLC, a subsidiary of
ORGANON & Co.,
Jersey City, NJ 07302, USA

For patent information: www.organon.com/our-solutions/patent/

Copyright © 2021 Organon Global Inc. All rights reserved.

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ZETIA® (ezetimibe) Tablets Patient Information about ZETIA (zĕt´-ē-ă) Generic name: ezetimibe (ĕ-zĕt´-ĕ-mīb)

Read this information carefully before you start taking ZETIA ^® and each time you get more ZETIA. There may be new information. This information does not take the place of talking with your doctor about your medical condition or your treatment. If you have any questions about ZETIA, ask your doctor. Only your doctor can determine if ZETIA is right for you.

What is ZETIA?

ZETIA is a medicine used to lower levels of total cholesterol and LDL (bad) cholesterol in the blood. ZETIA is for patients who cannot control their cholesterol levels by diet and exercise alone. It can be used by itself or with other medicines to treat high cholesterol. You should stay on a cholesterol-lowering diet while taking this medicine.

ZETIA works to reduce the amount of cholesterol your body absorbs. ZETIA does not help you lose weight. ZETIA has not been shown to prevent heart disease or heart attacks.

For more information about cholesterol, see the “What should I know about high cholesterol?” section that follows.

Who should not take ZETIA?

• Do not take ZETIA if you are allergic to ezetimibe, the active ingredient in ZETIA, or to the inactive ingredients. For a list of inactive ingredients, see the “Inactive ingredients” section that follows.
• If you have active liver disease, do not take ZETIA while taking cholesterol-lowering medicines called statins.
• If you are pregnant or breastfeeding, do not take ZETIA while taking a statin.
• If you are a woman of childbearing age, you should use an effective method of birth control to prevent pregnancy while using ZETIA added to statin therapy.

ZETIA has not been studied in children under age 10.

What should I tell my doctor before and while taking ZETIA?

Tell your doctor about any prescription and nonprescription medicines you are taking or plan to take, including natural or herbal remedies.

Tell your doctor about all your medical conditions including allergies.

Tell your doctor if you:

• ever had liver problems. ZETIA may not be right for you.
• are pregnant or plan to become pregnant. Your doctor will discuss with you whether ZETIA is right for you.
• are breastfeeding. We do not know if ZETIA can pass to your baby through your milk. Your doctor will discuss with you whether ZETIA is right for you.
• experience unexplained muscle pain, tenderness, or weakness.

How should I take ZETIA?

• Take ZETIA once a day, with or without food. It may be easier to remember to take your dose if you do it at the same time every day, such as with breakfast, dinner, or at bedtime. If you also take another medicine to reduce your cholesterol, ask your doctor if you can take them at the same time.
• If you forget to take ZETIA, take it as soon as you remember. However, do not take more than one dose of ZETIA a day.
• Continue to follow a cholesterol-lowering diet while taking ZETIA. Ask your doctor if you need diet information.
• Keep taking ZETIA unless your doctor tells you to stop. It is important that you keep taking ZETIA even if you do not feel sick.

See your doctor regularly to check your cholesterol level and to check for side effects. Your doctor may do blood tests to check your liver before you start taking ZETIA with a statin and during treatment.

What are the possible side effects of ZETIA?

In clinical studies patients reported few side effects while taking ZETIA. These included diarrhea, joint pains, and feeling tired.

Patients have experienced severe muscle problems while taking ZETIA, usually when ZETIA was added to a statin drug. If you experience unexplained muscle pain, tenderness, or weakness while taking ZETIA, contact your doctor immediately. You need to do this promptly, because on rare occasions, these muscle problems can be serious, with muscle breakdown resulting in kidney damage.

Additionally, the following side effects have been reported in general use: allergic reactions (which may require treatment right away) including swelling of the face, lips, tongue, and/or throat that may cause difficulty in breathing or swallowing, rash, and hives; raised red rash, sometimes with target-shaped lesions; joint pain; muscle aches; alterations in some laboratory blood tests; liver problems; stomach pain; inflammation of the pancreas; nausea; dizziness; tingling sensation; depression; headache; gallstones; inflammation of the gallbladder.

Tell your doctor if you are having these or any other medical problems while on ZETIA. For a complete list of side effects, ask your doctor or pharmacist.

What should I know about high cholesterol?

Cholesterol is a type of fat found in your blood. Your total cholesterol is made up of LDL and HDL cholesterol.

LDL cholesterol is called “bad” cholesterol because it can build up in the wall of your arteries and form plaque. Over time, plaque build-up can cause a narrowing of the arteries. This narrowing can slow or block blood flow to your heart, brain, and other organs. High LDL cholesterol is a major cause of heart disease and one of the causes for stroke.

HDL cholesterol is called “good” cholesterol because it keeps the bad cholesterol from building up in the arteries.

Triglycerides also are fats found in your blood.

General information about ZETIA

Medicines are sometimes prescribed for conditions that are not mentioned in patient information leaflets. Do not use ZETIA for a condition for which it was not prescribed. Do not give ZETIA to other people, even if they have the same condition you have. It may harm them.

This summarizes the most important information about ZETIA. If you would like more information, talk with your doctor. You can ask your pharmacist or doctor for information about ZETIA that is written for health professionals.

Inactive ingredients:

Croscarmellose sodium, lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone, and sodium lauryl sulfate.

Organon LLC, a subsidiary of
ORGANON & Co.,
Jersey City, NJ 07302, USA

For patent information: www.organon.com/our-solutions/patent/

Copyright © 2021 Organon Global Inc.
All rights reserved.

Revised: 6/2021

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