Ezetimibe (brand name Zetia) for high cholesterol

Zetia, also sold under the generic name ezetimibe, is a type of drug called a cholesterol absorption inhibitor. It reduces the amount of cholesterol absorbed by the digestive system. It is rarely prescribed on its own. If a patient isn’t meeting their cholesterol target with diet, exercise, and other cholesterol-lowering drugs (such as statins or fibrates), ezetimibe may help. 

Clinical trials showed an average 18% reduction in low-density lipoprotein (LDL, or “bad”) cholesterol versus placebo with Zetia taken alone. When combined with statins, it performed slightly better, with an average 21.4% reduction over and above statins alone. Trials also showed patients taking ezetimibe with statins had better high-density lipoprotein (HDL, or “good”) cholesterol levels versus those only taking statins (Ballantyne, 2002).

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We’ve spoken about “good” and “bad” cholesterols. What’s the difference?

Cholesterol in and of itself isn’t a bad thing. We need cholesterol to survive. It helps our bodies make hormones and vitamin D. It helps the digestive system absorb other nutrients. Our bodies synthesize most of the cholesterol that we need (Huff, 2020).

Cholesterol is a lipid—a fatty acid that doesn’t dissolve in water, like oil or wax. Having too many lipids in the blood is called hyperlipidemia. 

Cholesterol doesn’t dissolve in blood, so it gets around your body inside what are called lipoproteins. Low-density lipoprotein (LDL) cholesterol is the “bad” kind. It can hang around the circulatory system and take up residence in the arterial walls in deposits called plaque. This can lead to a medical condition called atherosclerosis, also known as hardened arteries.

Plaque buildup can reduce blood flow, depriving your organs of oxygen, causing organ failure. Plaque can also cause blood clots, which can result in a heart attack or stroke.

Having high cholesterol on its own can lead to heart disease. However, even having lower levels combined with other risk factors such as high blood pressure, smoking, or diabetes mellitus can be enough. For patients with genetic hyperlipidemia, this can happen even with a healthy diet and lifestyle (Bentzon, 2014).

High-density lipoprotein (HDL) is the “good” kind. It carries unneeded cholesterol to the liver, where it’s broken down and eventually expelled from the body. HDL cholesterol also has antioxidant and anti-inflammatory properties, which may help prevent atherosclerosis (Feingold, 2018). 

Keeping LDL cholesterol low and HDL cholesterol high is vital to maintaining good health. 

High LDL cholesterol can result from several causes, including poor diet, an unhealthy lifestyle, and genetics. 

Ezetimibe is a type of drug called a cholesterol absorption inhibitor. It works by blocking cholesterol from crossing the intestinal walls and getting into the circulatory system (Gagné, 2002).

Statins are another type of drug. They work by inhibiting the production of cholesterol in the liver. Statins, a low cholesterol diet, and regular exercise are the standard first-line therapy for most patients. These will often bring LDL cholesterol down to a safe level. For others, such as patients with genetic conditions like familial hypercholesterolemia, it may take more to lower cholesterol. They need additional medical help. Some patients don’t respond enough to statins alone or have side effects they can’t tolerate when taking higher statin doses. For those patients, a lower statin dose combined with ezetimibe can help achieve the desired result. 

Ezetimibe is generally well tolerated, with few patients encountering side effects. The most common adverse effects reported in clinical trials by patients taking ezetimibe alone were (DailyMed, n.d.):

• Diarrhea

• Fatigue

• Nasal inflammation

• Flu-like symptoms

• Upper respiratory infection

• Joint pain

• Pain in extremities (arms, legs)

Fewer than 5% of participants reported experiencing any given adverse effect. These percentages were only marginally higher than for those taking a placebo (DailyMed, n.d.). Side effects when taking ezetimibe in combination with a statin were also very close to those taking statins alone.

There have been reported cases of patients taking ezetimibe suffering rhabdomyolysis, an extremely rare condition that, left untreated, can lead to kidney failure. Whether ezetimibe played a role in the condition is not known, but data suggests there is no significant increase in risk when adding ezetimibe to statins versus taking statins alone (Kashani, 2008).

Talk to a healthcare professional and follow their medical advice if any of the above symptoms are extreme or don’t go away independently.

Some serious side effects could be signs of something more severe, such as an allergic reaction. Contact your healthcare provider immediately if you experience any of the following (MedLine Plus, n.d.):

• Hives, rash, or itching

• Trouble breathing or swallowing

• Swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs

• Hoarseness

• Pain in the upper right part of the stomach

• Upset stomach, abdominal pain

• Extreme tiredness, fatigue

• Odd bleeding or bruising

• Loss of appetite

• Yellowing of the skin or eyes

• Flu-like symptoms

• Unexplained muscle pain or weakness

• Fever

• Chills

• Pale or fatty stools

• Chest pain

Your healthcare provider will have questions about your medical history and will want to do blood tests to check your blood cholesterol levels before prescribing ezetimibe. Be sure to tell them (MedLine Plus, n.d.):

• If you are allergic to ezetimibe or any other medications.

• If you have or have ever had liver disease, liver damage, or impaired liver function.

• If you are pregnant, plan to become pregnant, or are breastfeeding. There have been no relevant studies regarding ezetimibe in breast milk to date, so it is recommended to seek alternate treatment while nursing (LactMed, 2020).

Always tell your healthcare provider about all medications, both prescription and non-prescription, and any vitamins or herbal supplements you are taking. Be sure to mention any of the following (MedLine Plus, 2018):

• Blood thinners, such as warfarin (brand name Coumadin)

• Cyclosporine (brand names Neoral, Sandimmune)

• Fenofibrate (brand names Triglide, Antara, Fibricor, Trilipix, Lipofen, and Fenoglide)

• Gemfibrozil (brand name Lopid)

You may need to be monitored for specific medical conditions when taking these drugs with ezetimibe.

Bile acid sequestrants should be taken four hours before or two hours after ezetimibe. Do not take these medications close to your ezetimibe dose. Bile acid sequestrants include cholestyramine (brand name Questran), colesevelam (brand name WelChol), and colestipol (brand name Colestid) (MedLine Plus, n.d.).

Zetia comes in 10 mg tablets, to be taken once per day with or without food. If you miss a dose, take it when you realize it, unless it is close to the time for your next dose. Don’t double-dose.

If not covered by your insurance, generic ezetimibe tablets are inexpensive. The lowest prices on generic Zetia are currently $10–$15 for a thirty-day supply (GoodRx, n.d.).

Ezetimibe also comes in combined doses with other drugs: 

• With atorvastatin under the brand name Liptruzet

• With simvastatin under the brand name Vytorin

• With rosuvastatin under the brand name Ridutrin

• With bempedoic acid under the brand name Nexlizet

Store Zetia at room temperature in a dry area out of sight and reach of children (MedLine Plus, 2018). Do not store Zetia in the bathroom, refrigerator, or anywhere that can become humid or develop condensation.

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How we reviewed this article

Every article on Health Guide goes through rigorous fact-checking by our team of medical reviewers. Our reviewers are trained medical professionals who ensure each article contains the most up-to-date information, and that medical details have been correctly interpreted by the writer.

Editorial Guidelines | Medical Review Process

Current version

November 25, 2020

Written by

Seth Gordon

Fact checked by

Mike Bohl, MD, MPH, ALM

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About the medical reviewer

Mike Bohl, MD, MPH, ALM

Dr. Mike is a licensed physician and a former Director, Medical Content & Education at Ro.