Ezetimibe

Hyperlipidemia, Mixed Hyperlipidemia, Diet + 4 more

Treatment

7 FDA approvals

6 Active Studies for Ezetimibe

What is Ezetimibe

Ezetimibe

The Generic name of this drug

Treatment Summary

Ezetimibe is a medication used to reduce cholesterol levels in the body. It works by blocking the absorption of cholesterol and phytosterols in the intestines. Ezetimibe has a unique mechanism of action that does not affect the absorption of other nutrients like fat-soluble vitamins or triglycerides. It targets the Niemann-Pick C1-Like 1 (NPC1L1) transporter in the intestines, which is essential for cholesterol absorption. By blocking this transporter, ezetimibe reduces the amount of cholesterol delivered to the liver.

Zetia

is the brand name

image of different drug pills on a surface

Ezetimibe Overview & Background

Brand Name

Generic Name

First FDA Approval

How many FDA approvals?

Zetia

Ezetimibe

2002

156

Approved as Treatment by the FDA

Ezetimibe, also called Zetia, is approved by the FDA for 7 uses which include Lipids and Homozygous Familial Hypercholesterolaemia (HoFH) .

Lipids

Used to treat Elevated Blood Lipids in combination with Simvastatin

Homozygous Familial Hypercholesterolaemia (HoFH)

Used to treat Homozygous Familial Hypercholesterolaemia (HoFH) in combination with Simvastatin

primary Hyperlipidemia

Used in combination with Pitavastatin to help manage primary Hyperlipidemia

Homozygous Familial Hypercholesterolemia

Used to treat Homozygous Familial Hypercholesterolaemia (HoFH) in combination with Simvastatin

Diet

Used to treat Diet in combination with Simvastatin

Hyperlipidemia

Used in combination with Pitavastatin to help manage primary Hyperlipidemia

Mixed Hyperlipidemia

Used to treat Mixed Hyperlipidemia in combination with Fenofibrate

Effectiveness

How Ezetimibe Affects Patients

Ezetimibe is a drug used to reduce levels of total cholesterol, low-density lipoprotein cholesterol, apoprotein B, non-high-density lipoprotein cholesterol, and triglycerides, while increasing high-density lipoprotein cholesterol in patients with hyperlipidemia. This drug is more effective when taken with a statin or fenofibrate. In clinical trials it was found to reduce LDL levels by 15-20% and increase HDL-C by 2.5-5%. Those with moderate-severe hepatic impairment should avoid taking ezetimibe as it can cause myopathy and r

How Ezetimibe works in the body

Ezetimibe helps lower cholesterol by blocking the absorption of cholesterol and phytosterols in the small intestine. It does this by targeting the Niemann-Pick C1-Like 1 (NPC1L1) protein, which helps move cholesterol into cells. Ezetimibe prevents the NPC1L1 protein from binding to cholesterol and other sterols, which stops the cholesterol from entering the cells. It also disrupts the function of other protein complexes involved in regulating cholesterol uptake, stopping them from doing their job. This leads to a decrease in the amount of cholesterol being delivered to the liver, and an increase in cholesterol

When to interrupt dosage

The recommended amount of Ezetimibe is contingent upon the diagnosed affliction, including Diet, Homozygous Familial Hypercholesterolemia and Hyperlipidemia. The dosage varies, depending on the technique of delivery (e.g. Oral or Tablet) described in the table below.

Condition

Dosage

Administration

Diet

10.0 mg,

Oral, Tablet, , Tablet - Oral, Tablet, film coated, Tablet, film coated - Oral

Lipids

10.0 mg,

Oral, Tablet, , Tablet - Oral, Tablet, film coated, Tablet, film coated - Oral

Mixed Hyperlipidemia

10.0 mg,

Oral, Tablet, , Tablet - Oral, Tablet, film coated, Tablet, film coated - Oral

Homozygous Sitosterolemia

10.0 mg,

Oral, Tablet, , Tablet - Oral, Tablet, film coated, Tablet, film coated - Oral

Hyperlipidemia

10.0 mg,

Oral, Tablet, , Tablet - Oral, Tablet, film coated, Tablet, film coated - Oral

sitosterols

10.0 mg,

Oral, Tablet, , Tablet - Oral, Tablet, film coated, Tablet, film coated - Oral

Homozygous Familial Hypercholesterolemia

10.0 mg,

Oral, Tablet, , Tablet - Oral, Tablet, film coated, Tablet, film coated - Oral

Warnings

Ezetimibe has three contraindications and should not be administered while having any of the conditions indicated in the below table.

Ezetimibe Contraindications

Condition

Risk Level

Notes

Transaminases

Do Not Combine

Liver Diseases

Do Not Combine

Severe Hypersensitivity Reactions

Do Not Combine

Ezetimibe may interact with Pulse Frequency

There are 20 known major drug interactions with Ezetimibe.

Common Ezetimibe Drug Interactions

Drug Name

Risk Level

Description

Atazanavir

Moderate

Ezetimibe may decrease the excretion rate of Atazanavir which could result in a higher serum level.

Belantamab mafodotin

Moderate

Ezetimibe may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.

Benzbromarone

Moderate

Ezetimibe may decrease the excretion rate of Benzbromarone which could result in a higher serum level.

Budesonide

Moderate

Ezetimibe may decrease the excretion rate of Budesonide which could result in a higher serum level.

Clarithromycin

Moderate

Ezetimibe may decrease the excretion rate of Clarithromycin which could result in a higher serum level.

Ezetimibe Toxicity & Overdose Risk

The lowest toxic dose in rats when taken orally or through the abdomen is greater than 2000 mg/kg. The lowest toxic dose in mice and dogs is greater than 5000 mg/kg and 3000 mg/kg respectively. In one case, a woman taking 120 mg/day for 28 days experienced no adverse effects due to an overdose. If someone does overdose, symptomatic treatments are recommended.

image of a doctor in a lab doing drug, clinical research

Ezetimibe Novel Uses: Which Conditions Have a Clinical Trial Featuring Ezetimibe?

8 active trials are presently investigating the potential of Ezetimibe to ameliorate sitosterols, Diet and Lipid levels.

Condition

Clinical Trials

Trial Phases

Mixed Hyperlipidemia

0 Actively Recruiting

sitosterols

0 Actively Recruiting

Hyperlipidemia

0 Actively Recruiting

Homozygous Sitosterolemia

0 Actively Recruiting

Lipids

0 Actively Recruiting

Homozygous Familial Hypercholesterolemia

2 Actively Recruiting

Phase 3

Diet

4 Actively Recruiting

Not Applicable, Phase 1

Ezetimibe Reviews: What are patients saying about Ezetimibe?

5

Patient Review

1/26/2022

Ezetimibe for High Cholesterol

My cholesterol was high before I started taking Accutane, so my NP prescribed this in addition to making lifestyle changes. So far it's working well with no noticeable side effects. My first blood test showed that my cholesterol was lower than before, even after just one month of Accutane.

5

Patient Review

5/23/2022

Ezetimibe for Heterozygous Inherited High Blood Cholesterol

I'm really pleased with this medication. After four months, my cholesterol dropped 60 points and triglycerides 50 points. I experienced zero negative side effects, which is more than I can say for statins (which made me feel like I was poisoned). So glad my GP suggested ezetimibe instead of pushing statins on me.

4.3

Patient Review

7/27/2022

Ezetimibe for Homozygous Inherited High Blood Cholesterol

This medication helped me to decrease my cholesterol levels by an additional 10%. I experienced no negative side effects.

3.7

Patient Review

7/22/2021

Ezetimibe for High Cholesterol

I've been taking this medication for a couple of years and it has helped lower my cholesterol. However, I stopped taking it a few months ago and have since been suffering from muscle weakness and pain.

2.7

Patient Review

3/9/2022

Ezetimibe for High Cholesterol

I experienced muscle aches, headaches, and a rash while taking Ezetimibe. I stopped after two months and went back to a vegan diet.

2.3

Patient Review

9/7/2022

Ezetimibe for High Cholesterol

I changed to ezetimibe after having issues with statins. I found that this new medication caused brain fog, weird dreams, and made me very sleepy. Additionally, it gave me diarrhea. I have decided that my quality of life is better without the medication and will take my chances until a better option is available.

2.3

Patient Review

10/20/2021

Ezetimibe for High Cholesterol

I took this medication for three weeks and unfortunately experienced a lot of negative side effects, like dizziness and intense back pain.

2.3

Patient Review

11/5/2021

Ezetimibe for Homozygous Inherited High Blood Cholesterol

I unfortunately had to discontinue use of this medication because I was in so much pain that I could hardly move. Every part of my body hurt, from my joints to my muscles.

1

Patient Review

4/6/2022

Ezetimibe for Homozygous Inherited High Blood Cholesterol

After just three months of taking this medication, I stopped due to the host of negative side effects. These included confusion, skin rashes, nightmares, abdominal pain, shoulder pain, and a cough that was both painful and productive.

1

Patient Review

4/10/2022

Ezetimibe for Combined High Blood Cholesterol and Triglyceride Level

I have been disappointed with this medication. I took it as prescribed for 60 days and saw a significant deterioration in my lab results across the board.

1

Patient Review

6/8/2022

Ezetimibe for High Cholesterol

I had awful muscle and joint pain after taking just one pill. By day three, I was experiencing stomach ache as well. This stuff is garbage and going straight in the trash.
image of drug pills surrounding a glass of water symbolizing drug consumption

Patient Q&A Section about ezetimibe

These questions and answers are submitted by anonymous patients, and have not been verified by our internal team.

Is ezetimibe considered a statin?

"Ezetimibe is a non-statin lipid-lowering medication that inhibits the absorption of dietary cholesterol by blocking the Niemann-Pick C1-Like 1 protein (NPC1L1)."

Answered by AI

Should ezetimibe be taken at night?

"There's no best time of day to take ezetimibe – it works just as well whether you take it in the morning, afternoon or evening. You should take it once a day, at the same time each day. You can take it with or without food."

Answered by AI

What are the side effects of taking ezetimibe?

"You may have ALS if you're experiencing unexplained muscle pain in your shoulders, thighs, or lower back, and having trouble moving your arms and legs because of weakness. Other symptoms include dark-colored urine, producing less urine than normal, nausea and vomiting, fever, and confusion."

Answered by AI

What is the difference between statin and ezetimibe?

"Ezetimibe works by preventing cholesterol absorption in the intestine, while statins work primarily by inhibiting cholesterol production in the liver. These two drugs therefore have complementary effects."

Answered by AI

Clinical Trials for Ezetimibe

Have you considered Ezetimibe clinical trials?

We made a collection of clinical trials featuring Ezetimibe, we think they might fit your search criteria.
Go to Trials
Image of National Institutes of Health Clinical Center in Bethesda, United States.

Cooking Intervention for Heart Disease

18 - 99
All Sexes
Bethesda, MD

Background: The risk of heart disease among African Americans is still common despite a greater understanding of the disease and better approaches to managing it. Healthy cooking and eating patterns can help reduce the risk of heart disease. But things like access to grocery stores and knowledge of good nutrition can affect these healthy patterns. Researchers want to see if community-based programs can help. Objective: To learn about the cooking behaviors of African American adults at risk for heart disease. Also, to see if a community-based cooking intervention will affect home-cooking behaviors. Eligibility: African American adults 18 and older who live in Wards 7 and 8 of Washington, D.C., and have at least one self-reported risk factor for heart disease Design: Phase I participants will complete a survey. It asks about their medical history, lifestyle, stress level, and eating habits. They will take part in a focus group. During this, they will talk about what they eat and what foods are available to them. Participation lasts 1 day for 3 hours at Pennsylvania Avenue Baptist Church in Washington, D.C. Phase II participants will go to shared cooking events at Pennsylvania Avenue Baptist Church. These will be held once a week for 6 weeks. They will be led by a trained chef. Participants will visit the NIH Clinical Center 3 times. Transportation will be provided if they need it. They will have physical exams and have blood drawn. They will be interviewed and complete questionnaires. A dietician will review the food they eat. An occupational therapist will assess their cooking skills. They will keep a daily cooking journal. Participation lasts 18 weeks.

Recruiting
Has No Placebo

National Institutes of Health Clinical Center

Nicole M Farmer, M.D.