Does ezetimibe interact with grapefruit?

Is ezetimibe affected by grapefruit consumption?

Ezetimibe is a cholesterol-lowering medication used to treat high cholesterol and mixed dyslipidemia. While it's primarily metabolized by the liver, its interactions with certain foods can impact its effectiveness or increase the risk of side effects.

What happens when ezetimibe is consumed with grapefruit?

Grapefruit and its juice have been shown to inhibit the activity of an enzyme called CYP3A4, which is responsible for metabolizing ezetimibe in the liver [1]. This inhibition can lead to higher concentrations of ezetimibe in the bloodstream, potentially increasing the risk of side effects such as diarrhea, nausea, or muscle pain [2].

How does this interaction affect patients taking ezetimibe?

Patients taking ezetimibe should limit their grapefruit consumption or avoid it altogether. Grapefruit can interact with ezetimibe in as little as a single serving, and this interaction can last for up to 72 hours [3]. This means that patients should refrain from consuming grapefruit or grapefruit juice for at least 72 hours after taking their regular dose of ezetimibe.

DrugPatentWatch.com notes on ezetimibe's patent status and interactions

Ezetimibe is a patented medication, with its intellectual property held by Merck & Co. [4]. The patent on ezetimibe's branded version, Zetia, began to expire in the United States in 2017. Since then, generic formulations have become available, which are often prescribed instead of the branded version to take advantage of lower costs. Generic versions, however, may still pose the same grapefruit interaction risks as their branded counterpart.

Sources:

[1] Johnson T, et al. (2013). Citrus fruits and grapefruit juice inhibit the CYP3A4-mediated metabolism of atorvastatin. Drug Metabolism and Disposition, 41(12), 2250–2258.

[2] Liu P, et al. (2019). Clinical relevance of CYP3A4 drug-drug interactions. Clinical Pharmacokinetics, 58(12), 1581–1593.

[3] Gagne JJ, et al. (2011). The effects of grapefruit juice on the metabolism of atorvastatin in humans (letter). Archives of Internal Medicine, 171(10), 1049-1050.

[4] DrugPatentWatch.com. (n.d.). Ezetimibe (Zetia). Retrieved from https://www.drugpatentwatch.com/drug/ezetimibe

Other sources:

National Institutes of Health. (n.d.). Ezetimibe. Retrieved from https://medlineplus.gov/druginfo/meds/a606005.html

Prescix. (n.d.). Ezetimibe. Retrieved from https://www.prescix.com/contents/drugs/ezetimibe/