Ezetimibe (oral)

Ezetimibe is a cholesterol-lowering medicine often prescribed alongside lifestyle changes to treat high cholesterol levels.

Overview

Ezetimibe works to reduce the amount of cholesterol and other fatty substances in the blood. Cholesterol is a fat-like substance which can build up in the blood vessels and, over time, reduce blood flow. When blood flow is reduced, the heart, brain and other organs are less likely to receive enough oxygen from the blood, which can lead to a variety of serious conditions such as heart attack, stroke and angina. Ezetimibe blocks the absorption of cholesterol into the body in order to minimize further buildup of the substance in the blood vessels.

Most patients who take ezetimibe are told to make lifestyle changes to further reduce cholesterol levels, as the drug alone may not reduce the risk of heart attack, stroke or other complications adequately. Lifestyle changes usually include changes to diet, weight loss, and increased exercise.

Sometimes ezetimibe is also prescribed at the same time as other medicines called statins (known professionally as HMG-CoA reductase inhibitors), which help to reduce cholesterol production in the liver. It is thought that in combination statins and ezetimibe may be more effective than if used alone. However, there is evidence to suggest that some statins may be just as effective when used alone as they are when used with ezetimibe. Talk to your doctor if you have questions about the risks and benefits of ezetimibe when used in addition to statins.

In the US, ezetimibe is only available with a doctor's prescription. It is known under the brand name Zetia and is administered orally in the form of tablets.

Conditions Treated?

Type Of Medicine?

  • Cholesterol absorption inhibitor

Side Effects

Along with its needed effects, ezetimibe can cause unwanted side effects, some of which are serious and require medical attention. Although not all of these side effects may occur, it is important to familiarize yourself with all of them in order that you can recognize when to seek medical care.

The following side effects, although rare, are serious and should be reported to a doctor immediately:

  • Abdominal fullness
  • Bloating
  • Gaseous abdominal pain
  • Upper right abdominal pain
  • Pain in stomach, side, or abdomen, possible radiating to back
  • Indigestion
  • Severe nausea
  • Vomiting
  • Loss of appetite
  • Light-colored stools
  • Black, tarry stools
  • Blood in stools
  • Constipation
  • Blood in urine
  • Dark urine
  • Fast heartbeat
  • Recurrent fever
  • Muscle cramps or spasms
  • Muscle tenderness, weakness or wasting
  • Abnormal bleeding or bruising
  • Bleeding gums
  • General abnormal tiredness or weakness
  • Skin rash
  • Large, hive-like swellings on face, lips, tongue, throat, hands, feet, legs or genitals
  • Pinpoint red spots on skin
  • Yellow skin or eyes

The following side effects are usually minor and don't require medical attention unless they become very severe or prolonged. They may dissipate once your body adjusts to the medicine. Discuss them with your doctor if you have questions about them.

  • More common
  •  Headache
  •  Fever
  • Sore throat
  • Runny nose
  • Muscle pain
  • Less common
  • Stomach pain
  • Body aches or pain
  • Joint pain
  • Pain or tenderness around eyes or cheekbones
  • Muscle stiffness
  • Back pain
  • Chest pain
  • Chills
  • Cold, flu-like symptoms
  • Congestion
  • Stuffy nose
  • Coughing
  • Dry or sore throat
  • Hoarseness
  • Tender, swollen glands in neck
  • Trouble swallowing
  • Voice change
  • Tightness in chest or wheezing
  • Dizziness
  • Diarrhea

This may not be an exhaustive list of all side effects associated with ezetimibe. If you notice others not listed here, report them to your doctor. You could also report side effects to the FDA.

Dosage

The recommended dose of ezetimibe for treating high cholesterol in adults in 10 mg taken once each day. Children aged 10 years and older may also take the same dose. The drug is not recommended for children under 10 years.

Your doctor may prescribe different doses to those recommended here based on your medical history and other factors personal to you. Always follow your doctor's instructions, and never take more or less ezetimibe than what is prescribed.

Ezetimibe tablets should be swallowed whole without breaking, crushing or chewing. They can be taken either with or without food. If you miss a dose, take it as soon as you remember unless it is almost time for your next dose, in which case simply skip the missed dose and continue with your usual dosing schedule. Never double doses of ezetimibe to make up for a missed dose as doing so could increase the risk of unwanted side effects.

Interactions

Ezetimibe can interact with a variety of different medicines. It is very important that you know about all the medicines you take in order to avoid harmful interactions. This includes prescribed medicines, those purchased over the counter, and herbal supplements or multivitamins. It can be helpful to keep a list of all medicines you take which you can then present to each doctor, nurse or pharmacist.

If you do take medicines which are known to interact with ezetimibe, your doctor may change some of the current medicines you take in order for you to safely consume ezetimibe. If both medicines are necessary, your doctor may adjust the dosages of your medicines or instruct you to take them at different times. It is very important to follow your doctor's instructions.

It is particularly important that your doctor knows if you are taking the following medicines:

  • Cyclosporine (Neoral, Sandimmune)
  • Fenofibrate (TriCor)
  • Gemfibrozal (Lopid)
  • Warfarin (Coumadin)
  • Other anticoagulant medicines (also known as 'œblood thinners')

The following medicines must be taken either four hours before or two hours after taking ezetimibe:

  • Cholestyramine (Questran)
  • Colesevelam (WellChol)
  • Colestipol (Colestid)

Warnings

Lifestyle changes to reduce cholesterol

Your doctor will probably try to control your cholesterol levels by recommending lifestyle changes, such as:

  • Following a low-fat, low-sugar or low-cholesterol diet
  • Increasing the amount of exercise you do
  • Losing weight

It is very important to follow your doctor's advice, as ezetimibe alone may not be enough to reduce your cholesterol to a healthy level. Your doctor may be able to refer you to a dietitian if you need help in formulating a low-fat diet. Always check with your doctor or another healthcare professional before adopting dramatic diet changes. You should also check with your doctor before starting a new exercise regime to ensure the activity is safe for you. Generally, it is safer to gradually build up the rate of exercise you do as your fitness levels improve.

Less effective for overweight patients

Ezetimibe can be less effective in patients who are very overweight. Your doctor may recommend that you lose weight before they prescribe ezetimibe. Check with your doctor before changing your diet and ask your healthcare provider for advice if you think you may need help in losing weight.

Risk of worsened liver problems

People with liver disease (or a history of) or persistently high levels of liver hormones may not be able to take ezetimibe. This is because the medicine could worsen these liver problems. Make sure your doctor knows your full medical history in order that they can assess whether ezetimibe is a safe medicine for you.

Pediatric use

Ezetimibe is not suitable for children under the age of 10 years. In children over 10, the drug appears to be just as effective as it is for adults, and does not seem to cause different side effects to those found in adults.

Geriatric use

Although ezetimibe has not been studied in older adults, there is no evidence to suggest that it would be any less safe or effective in geriatric patients than it is in younger adult patients.

Pregnancy and breastfeeding

Ezetimibe is a pregnancy category C drug, which means it is not recommended for pregnant women unless the potential benefits of the drug justify potential risks to the fetus. Animal studies have demonstrated potential harm to the fetus, and there are not enough well-controlled studies in humans to determine the risk. You should use contraception while take ezetimibe to prevent pregnancy, and tell your doctor straight away if you become pregnant or plan to become pregnant.

It is not known whether ezetimibe is excreted in human breast milk, but it is excreted in animal milk. Experts believe that if it is excreted in breast milk, it could harm infant lipid metabolism. For this reason, the drug is not recommended for use during breastfeeding, particularly if breastfeeding a newborn or preterm infant. Ask your doctor for advice if you are recommended ezetimibe while breastfeeding.

Storage

Ezetimibe should be stored in the container it is provided in with the lid tightly closed when not in use. Store the container at room temperature, away from heat, direct light or moisture, and keep the medicine from freezing. Do not store it in the bathroom.

Keep ezetimibe away from children and pets. Store it up and away from the ground so that it is not in sight or within easy reach. Avoid using weekly pill minders which do not have child-resistant lids.

If you have unused or expired medicine, ask your healthcare provider how to dispose it. There may be a local medicine take-back program available to allow you to safely dispose of it. Do not flush ezetimibe down the toilet.

Summary

Ezetimibe is a cholesterol absorption inhibitor which helps to reduce cholesterol levels when used in conjunction with diet and lifestyle changes. High cholesterol can increase the risk of stroke, heart attack and angina, and since ezetimibe inhibits the absorption of cholesterol, it can help to prevent these conditions. Sometimes it prescribed at the same time as statins, which prevent cholesterol production in the liver.

The more common side effects associated with ezetimibe are headache, fever, sore throat, runny nose and muscle pain. Unless these effects become severe or prolonged, they do not require medical attention. If patients notice unexplained muscle pain and tenderness, recurrent fever, unusual tiredness or dark colored urine, they should consult a doctor immediately.

The average dose of ezetimibe for adults and children aged ten years or older is 10 mg, taken once each day. The drug is not suitable for children under 10 years old. Ezetimibe should be taken orally and is administered in tablet form. Tablets can be taken either with or without food. A low-fat diet is usually recommended to patients with high cholesterol levels.

Ezetimibe should not be taken at the same time of cyclosporine, fenofibrate, gemfibrozil and warfarin. If patients also take cholestyramine, colesevelam or colestipol, they should take these either four hours before or two hours after taking ezetimibe.

Ezetimibe may not be suitable for patients with liver disease, thyroid disease or liver enzyme problems. It is also unsuitable for pregnant women, unless the benefits of the drug justify potential risks to the fetus. The drug is also not recommended for use while breastfeeding, particularly when nursing newborn or preterm infants.