Ezetimibe

Hyperlipidemia, Mixed Hyperlipidemia, Diet + 4 more
Treatment
5 FDA approvals
9 Active Studies for Ezetimibe

What is Ezetimibe

EzetimibeThe Generic name of this drug
Treatment SummaryEzetimibe 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.
Zetiais 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 5 uses which include Lipids and Diet .
Lipids
Used to treat Elevated Blood Lipids in combination with Simvastatin
Diet
Used to treat Diet in combination with Simvastatin
Mixed Hyperlipidemia
Used to treat Mixed Hyperlipidemia in combination with Fenofibrate
Homozygous Familial Hypercholesterolemia
Used to treat Homozygous Familial Hypercholesterolaemia (HoFH) in combination with Simvastatin
Hyperlipidemia
Used in combination with Pitavastatin to help manage primary Hyperlipidemia

Effectiveness

How Ezetimibe Affects PatientsEzetimibe 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 bodyEzetimibe 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
Hyperlipidemia
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
Lipids
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
sitosterols
10.0 mg,
, Oral, Tablet, Tablet - Oral, Tablet, film coated, Tablet, film coated - Oral
Diet
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

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
active liver disease
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 RiskThe 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
Diet
5 Actively Recruiting
Not Applicable
Homozygous Sitosterolemia
0 Actively Recruiting
Homozygous Familial Hypercholesterolemia
4 Actively Recruiting
Phase 3, Phase 2
Hyperlipidemia
0 Actively Recruiting
Lipids
0 Actively Recruiting
sitosterols
0 Actively Recruiting
Mixed Hyperlipidemia
0 Actively Recruiting

Ezetimibe Reviews: What are patients saying about Ezetimibe?

5Patient 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.
5Patient 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.
4.3Patient 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.
3.7Patient 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.
2.7Patient 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.
2.3Patient 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.
2.3Patient 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.
2.3Patient 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.
1Patient 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.
1Patient 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.
1Patient 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.