What are the side effects of ezetimibe (cholesterol absorption inhibitor)?

From the Guidelines

Ezetimibe is generally well-tolerated, with common side effects including upper respiratory tract infection, diarrhea, arthralgia, sinusitis, and pain in extremities, which occur in less than 5% of patients.

Side Effects of Ezetimibe

The side effects of ezetimibe can be categorized into common and serious side effects.

• Common side effects include:
  • Upper respiratory tract infection
  • Diarrhea
  • Arthralgia
  • Sinusitis
  • Pain in extremities
• Serious side effects are rare but can include:
  • Allergic reactions (rash, itching, swelling)
  • Liver problems (yellowing of skin/eyes, dark urine, persistent nausea)
  • Severe muscle pain or weakness (especially when combined with statins) Ezetimibe works by blocking cholesterol absorption in the small intestine rather than affecting liver function like statins, which explains its generally favorable side effect profile 1.

Dosage and Administration

The standard dose of ezetimibe is 10 mg once daily, taken with or without food, and it can be used alone or combined with statins 1. If you experience persistent or severe side effects, contact your healthcare provider immediately, but do not stop taking the medication without medical advice. In a prespecified safety analysis, IMPROVE-IT participants who achieved an LDL-C level of <30 mg/dL were compared with those achieving higher LDL-C and were found to have no significant increase in risk for 9 prespecified safety outcomes, including muscle, hepatobiliary, and neurocognitive events 1. Overall, ezetimibe is a safe and effective medication for lowering LDL-C levels and reducing the risk of ASCVD events, with a favorable side effect profile compared to other cholesterol-lowering medications 1.

From the FDA Drug Label

Ezetimibe tablets may cause serious side effects including: increased liver enzymes. muscle pain, tenderness, and weakness (myopathy). The most common side effects of ezetimibe tablets taken alone include: upper respiratory tract infection joint pain pain in arms or legs flu-like symptoms diarrhea inflammation of the sinuses feeling tired The most common side effects of ezetimibe tablets taken with a statin include: runny nose, sore throat joint pain flu-like symptoms muscle aches and pains diarrhea pain in arms or legs upper respiratory tract infection back pain feeling tired

The possible side effects of ezetimibe include:

• Serious side effects: increased liver enzymes, muscle pain, tenderness, and weakness (myopathy)
• Common side effects when taken alone: upper respiratory tract infection, joint pain, pain in arms or legs, flu-like symptoms, diarrhea, inflammation of the sinuses, feeling tired
• Common side effects when taken with a statin: runny nose, sore throat, joint pain, flu-like symptoms, muscle aches and pains, diarrhea, pain in arms or legs, upper respiratory tract infection, back pain, feeling tired 2

From the Research

Side Effects of Ezetimibe

The side effects of ezetimibe, a cholesterol absorption inhibitor, have been studied in various clinical trials and case reports. Some of the reported side effects include:

• Mild elevations of liver transaminases, mainly in combination with a statin 3
• Myopathy, although rare, with some case reports attributing myopathy to ezetimibe use 3, 4
• Rhabdomyolysis, with uncertain risk due to low event rates and wide confidence intervals 4
• Hepatopathy, with little or no difference in risk when adding ezetimibe to statins 4
• Cancer, gallbladder-related disease, and discontinuation due to adverse events, with little or no difference in risk between treatment groups 4
• Nausea, myalgias, and transient elevation in liver enzymes, as reported in individual case studies 5, 6
• Severe jaundice and isolated hyperbilirubinemia, as reported in a case study of a patient with occult cirrhosis 6

Rare but Serious Side Effects

Some rare but serious side effects of ezetimibe include:

• Serious hepatocellular drug-induced liver disease, as reported in a case study 7
• Toxic hepatitis, which may require prompt withdrawal of the drug 7
• Severe liver injury, which may be more likely in patients with pre-existing liver disease 6

Monitoring and Safety Precautions

To minimize the risk of side effects, patients taking ezetimibe should be monitored regularly for:

• Liver function tests, especially if they have pre-existing liver disease 3, 6
• Muscle pain or weakness, which may indicate myopathy or rhabdomyolysis 3, 4
• Signs of hepatotoxicity, such as jaundice or elevated liver enzymes 7, 6