Zetia: 7 things you should know

Medically reviewed by Carmen Pope, BPharm. Last updated on April 3, 2023.

1. How it works

• Zetia is a brand (trade) name for ezetimibe which may be used to lower high cholesterol.
• Zetia (ezetimibe) works by reducing the absorption of cholesterol from the brush border of the small intestine so that less cholesterol is delivered to the liver. This causes a reduction of hepatic cholesterol stores and an increase in the clearance of cholesterol from the blood. Zetia targets the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), which is involved in the intestinal uptake of cholesterol and phytosterols. Intestinal cholesterol is derived primarily from cholesterol secreted in the bile and from dietary cholesterol.
• Zetia belongs to the class of medicines known as cholesterol absorption inhibitors.

2. Upsides

• May be used alone or in combination with a statin to lower levels of total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), and non-high-density lipoprotein cholesterol (non-HDL-C) in patients with primary (heterozygous familial and non-familial) hyperlipidemia, in addition to diet, exercise, and other nonpharmacological interventions.
• May be used in combination with fenofibrate and lifestyle measures to reduce levels of elevated total-C, LDL-C, Apo B, and non-HDL-C in adult patients with mixed hyperlipidemia.
• May be used in combination with atorvastatin or simvastatin to reduce elevated total-C and LDL-C levels in patients with Homozygous Familial Hypercholesterolemia (HoFH), in addition to other lipid-lowering treatments. May also be used to reduce elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia.
• Zetia is an oral tablet that is taken once a day. The usual dosage is 10mg.
• Can be administered with or without food.
• Zetia can be taken alone or in combination with other medications that also lower cholesterol, such as statins or fenofibrate.
• Zetia does not cause weight loss or weight gain.
• The way Zetia works is different from other classes of cholesterol-reducing compounds such as statins, bile acid sequestrants, fibrates, or plant stanols. This means it has a complementary lipid-lowering effect when used in combination.
• Unlike statins, Zetia is unlikely to cause muscle aches and pains. Zetia may be prescribed to people who have had to discontinue statins because of intolerable muscle aches and pains.
• Zetia reduces the buildup of fats, cholesterol, and other substances on the artery walls (this process is known as atherosclerosis) and if taken long-term it may reduce the risk of heart disease.
• Zetia has a well-documented safety profile.
• Zetia does not cause an increase or a decrease in blood pressure.
• No dosage adjustments are necessary for people with liver or kidney disease; however, Zetia should not be given to people with moderate to severe liver disease. Studies have not shown an increase in liver enzymes when Zetia is used as sole therapy; however, an increase has been noted when Zetia is used in combination with a statin.
• Zetia is available as a cost-saving generic under the name ezetimibe.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• Upper respiratory tract infections, diarrhea, joint pain, sinusitis, tiredness, and pain in the extremities (2.7%) are the most common side effects reported, occurring in less than 5% of people. Overall, Zetia has few side effects. Rarely, dizziness and gamma-glutamyltransferase increases have been reported.
• Research has not yet determined if Zetia reduces the risk of hospitalization or death from cardiovascular disease.
• It is unknown if Zetia is effective for Fredrickson Type I, III, IV, and V dyslipidemias.
• Zetia may not be suitable for some people including pregnant women and should not be used in combination with a statin in people with active liver disease, with unexplained persistent elevations in hepatic transaminase levels, in women who are pregnant or intending to become pregnant, and in breastfeeding women.
• Zetia has not been studied in children under the age of 10.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

Zetia may be used to lower cholesterol alone or in combination with a statin or fibrate. It has few reported side effects and few drug interactions. It is effective at lowering intestinal absorption of cholesterol by approximately 54%; however, research has not yet determined if it reduces the risk of cardiovascular hospitalizations or death.

5. Tips

• Zetia can be taken at any time of the day, with or without food, as long as it is taken consistently and at the same time each day. Zetia works the same whether you take it in the morning, afternoon, or evening. If you forget to take Zetia, take it as soon as you remember. However, do not take more than one dose of Zetia a day.
• As with all other cholesterol-lowering medication, Zetia should be taken in conjunction with lifestyle changes including a cholesterol-lowering diet and a weight management plan.
• Regular exercise is also important as well as avoiding smoking.
• Zetia can be taken at the same time as the following cholesterol-lowering medications: fenofibrate, atorvastatin, lovastatin, simvastatin, pravastatin, and fluvastatin. Take Zetia at least 4 hours after cholestyramine, colestipol, and colesevelam; or 2 hours before.
• For Zetia to have cardiovascular benefits you need to take it regularly and long-term. If you stop taking it, within a few weeks when there is no Zetia left in the body, cholesterol absorption from the small intestine will return to normal and the rate of buildup of fats and cholesterol in the arteries will revert to what it was before you started taking Zetia.
• If you are pregnant or intend to become pregnant tell your doctor because Zetia may not be right for you. Combination therapy with a statin should not be taken by pregnant women.
• Regular blood tests may be needed to determine the effect of Zetia on lipids and liver function.
• Report to your doctor immediately if you experience any unexplained muscle pain, tenderness, or weakness, particularly if associated with tiredness or fever.

6. Response and effectiveness

• Zetia inhibited intestinal cholesterol absorption by 54%, compared with placebo in a 2-week clinical study in 18 hypercholesterolemic patients. In addition, Zetia had no clinically meaningful effect on the plasma concentrations of the fat-soluble vitamins A, D, and E (in a study of 113 patients), and did not impair adrenocortical steroid hormone production (in a study of 118 patients).
• Triglyceride levels were also reduced by 8% in an analysis of eight clinical trials comparing ezetimibe 10mg daily to a placebo. The results also showed an 18.5% reduction in LDL-C, a 3% increase in HDL-C ("good" cholesterol), and a 13% reduction in total cholesterol.
• For a more effective reduction in triglycerides levels, ezetimibe can be taken with a statin.
• In a review and analysis of 2722 people on ezetimibe, it was reported that the safety of ezetimibe was well documented. Side effects were at a similar rate for patients that took ezetimibe to those patients that took placebo tablets.

7. Interactions

Medicines that interact with Zetia may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with Zetia. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Common medications that may interact with Zetia include:

• anti-androgen medications such as darolutamide
• anti-cancer medications such as entrectinib
• HIV medications, such as fostemsavir
• flax
• statins, such as atorvastatin or simvastatin (increased risk of side effects)
• warfarin.

Note that this list is not all-inclusive and includes only common medications that may interact with Zetia. You should refer to the prescribing information for Zetia for a complete list of interactions.

References

• Zetia (ezetimide) [Package insert]. Updated 06/2022. Organon LLC. https://www.drugs.com/pro/zetia.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Zetia only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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