Ezetimibe
Hyperlipidemia, Mixed Hyperlipidemia, Diet + 4 more
Treatment
7 FDA approvals
6 Active Studies for Ezetimibe
Treatment for
Hyperlipidemia
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
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.
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
5
Patient Review
5/23/2022
Ezetimibe for Heterozygous Inherited High Blood Cholesterol
4.3
Patient Review
7/27/2022
Ezetimibe for Homozygous Inherited High Blood Cholesterol
3.7
Patient Review
7/22/2021
Ezetimibe for High Cholesterol
2.7
Patient Review
3/9/2022
Ezetimibe for High Cholesterol
2.3
Patient Review
9/7/2022
Ezetimibe for High Cholesterol
2.3
Patient Review
10/20/2021
Ezetimibe for High Cholesterol
2.3
Patient Review
11/5/2021
Ezetimibe for Homozygous Inherited High Blood Cholesterol
1
Patient Review
4/6/2022
Ezetimibe for Homozygous Inherited High Blood Cholesterol
1
Patient Review
4/10/2022
Ezetimibe for Combined High Blood Cholesterol and Triglyceride Level
1
Patient Review
6/8/2022
Ezetimibe for High Cholesterol
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