Ezetrol

Ezetimibe is a cholesterol absorption inhibitor used to reduce elevated LDL cholesterol (low-density lipoprotein, often called 'bad cholesterol').

It is marketed under the brand name Ezetrol and works by a mechanism distinct from statins, making it a valuable addition to cholesterol-lowering therapy.

Ezetimibe selectively inhibits the Niemann-Pick C1-Like 1 (NPC1L1) protein in the brush border of the small intestine, blocking the absorption of dietary and biliary cholesterol.

This reduces cholesterol delivery to the liver, which in turn upregulates LDL receptor expression and increases LDL clearance from the blood.

As monotherapy, ezetimibe reduces LDL cholesterol by approximately 15-20%.

Ezetimibe is most commonly used in combination with a statin for patients who have not achieved their LDL target with a statin alone.

The IMPROVE-IT trial demonstrated that adding ezetimibe to simvastatin reduced cardiovascular events compared to simvastatin alone, providing robust evidence for this combination strategy.

Take one 10 mg tablet once daily at any time of day, with or without food. Ezetimibe can be taken at the same time as a statin for convenience.

No dose adjustment is needed based on timing relative to meals. Continue alongside dietary measures and lifestyle modifications.

Regular cholesterol blood tests will be arranged to monitor your response.

10 mg once daily. The dose is the same whether used as monotherapy or in combination with a statin. No dose titration is required.

No dose adjustment is needed in mild to moderate hepatic impairment or renal impairment. Avoid in severe hepatic impairment when combined with a statin.

Common (1 in 10 to 1 in 100): headache, abdominal pain, and diarrhoea.

Uncommon (1 in 100 to 1 in 1,000): fatigue, elevated liver enzymes (particularly when combined with a statin), myalgia, and flatulence.

Rare (less than 1 in 1,000): myopathy, rhabdomyolysis (very rare, mainly in combination with statin), hepatitis, pancreatitis, thrombocytopenia, and hypersensitivity reactions.

The side effect profile is generally favourable, and ezetimibe is well tolerated as monotherapy.

When used with a statin, liver function should be monitored as per statin guidelines. Report any unexplained muscle pain, tenderness, or weakness, as this may indicate myopathy.

Ezetimibe is not recommended during pregnancy or breastfeeding. Cyclosporine levels should be monitored if co-administered.

Bile acid sequestrants should be taken at least 2 hours before or 4 hours after ezetimibe.

Known allergy to ezetimibe or any excipient. Active liver disease or unexplained persistent elevations in liver transaminases. When combined with a statin, contraindications of the statin also apply.

Pregnancy and breastfeeding.