EZETROL 10MG TABLETS 28`S

EZETROL contains ezetimibe, a lipid-lowering agent that selectively inhibits the absorption of dietary and biliary cholesterol at the brush border of the small intestine by blocking a transporter protein.

Unlike statins (which inhibit hepatic cholesterol synthesis), ezetimibe reduces the amount of cholesterol entering the body from the gut.

EZETROL 10 mg is indicated as an adjunct to dietary measures for:

·       hypercholesterolemia — as add-on therapy to a statin when statin alone is insufficient to reach LDL-C targets;

·       Monotherapy in patients who cannot tolerate statins

·       Homozygous familial hypercholesterolaemia (HoFH) — in combination with a statin and other lipid-lowering treatments;

·       Homozygous sitosterolaemia (phytosterolaemia).

The standard dose of ezetimibe is 10 mg once daily.

•       May be taken at any time of day, with or without food.

•       Swallow whole with water.

•       Can be taken at the same time as a statin or at any different time of day.

Renal and Hepatic Impairment

•       Renal impairment: no dose adjustment required.

•       Mild hepatic impairment: no dose adjustment required.

•       Moderate to severe hepatic impairment (Child-Pugh B or C): not recommended — ezetimibe is extensively glucuronidated in the liver and gut wall; exposure is significantly altered.

Ezetimibe is typically given with a statin for maximum LDL reduction. Fixed-dose combination products (e.g., ezetimibe/simvastatin — Inegy/Vytorin) provide the convenience of a single tablet.

Common Side Effects (in monotherapy)

•       Gastrointestinal: diarrhoea, abdominal pain, flatulence.

•       Fatigue.

•       Arthralgia, myalgia.

Common Side Effects (in combination with a statin)

•       Headache, fatigue.

•       Myalgia — the statin component is primarily responsible, but ezetimibe may contribute.

•       Elevated liver enzymes (ALT, AST) — more common in combination therapy.

Serious Side Effects

•       Myopathy or rhabdomyolysis — rare but can occur, particularly in combination with statins at higher doses. Report severe or unexplained muscle pain.

•       Hepatitis — rare; monitor LFTs if symptoms occur.

•       Pancreatitis — very rare.

•       Allergic reactions: rash, urticaria, angioedema — rare.

Combination with Statins — Liver Monitoring

When ezetimibe is combined with a statin, the statin's liver monitoring requirements apply. Check LFTs before starting combination therapy and at 12 weeks. If ALT or AST rises above 3 times the upper limit of normal, investigate and consider dose reduction or discontinuation of the statin. Ezetimibe itself rarely causes significant liver enzyme elevation when used alone.

Statin Intolerance — Monotherapy Use

Ezetimibe monotherapy reduces LDL-C by approximately 18–25%, less than an effective statin dose. However, for statin-intolerant patients, ezetimibe provides a meaningful alternative, particularly when combined with evolocumab or alirocumab (PCSK9 inhibitors). Ezetimibe is also a useful stepping stone while evaluating whether mild statin myalgia is truly drug-related.

Fibrates Interaction

Co-administration of ezetimibe with a fibrate is not recommended as both agents increase cholesterol excretion into bile, potentially increasing the risk of cholelithiasis (gallstones). If gallstones are suspected, suspend treatment pending investigation.

•       Bile acid sequestrants (cholestyramine, colestipol) — significantly reduce ezetimibe absorption; take ezetimibe at least 2 hours before or 4 hours after the bile acid sequestrant.

•       Ciclosporin — substantially increases ezetimibe plasma levels; use with caution in transplant patients; monitor closely.

•       Fibrates (fenofibrate, gemfibrozil) — increase ezetimibe plasma levels; risk of cholelithiasis; co-administration not recommended.

•       Warfarin — ezetimibe may increase free warfarin concentrations; monitor INR when initiating or adjusting ezetimibe.

•       Statins — intentionally combined; statins' liver and muscle monitoring requirements apply to the combination.

•       Store below 25 degrees Celsius.

•       Store in original packaging, away from light and moisture.

•       Keep out of reach of children.

•       Do not use after the expiry date.

EZETROL is a prescription-only medicine (POM) in Kenya, regulated by the Pharmacy and Poisons Board (PPB). It is prescribed by cardiologists, general physicians, and general practitioners managing patients with hypercholesterolaemia.

Initiation alongside a statin should be guided by LDL-C targets set according to cardiovascular risk assessment (SCORE/Framingham), dietary optimisation, and statin dosing adequacy.

LDL-C Reduction Expectations

Ezetimibe monotherapy: approximately 18–25% LDL-C reduction. Ezetimibe added to a statin: approximately an additional 18–25% LDL-C reduction on top of the statin effect. Example: high-intensity statin (rosuvastatin 20 mg) reduces LDL by approximately 50%; adding ezetimibe achieves approximately 60–65% reduction — often sufficient to reach guideline targets in very high cardiovascular risk patients (LDL target less than 1.4 mmol/L).

Role in Cardiovascular Risk Reduction

The IMPROVE-IT trial established that ezetimibe added to simvastatin further reduced cardiovascular events beyond what simvastatin alone achieved (7-year NNT approximately 56 for MACE prevention). This provides level 1A evidence supporting ezetimibe's use beyond cholesterol-lowering as a standalone surrogate marker.

Statin-Intolerant Patients

In patients with genuine statin intolerance (myalgia confirmed to be statin-related on rechallenge), ezetimibe 10 mg provides moderate LDL lowering without myopathy risk. If additional LDL lowering is needed, ezetimibe can be combined with a low-dose statin, rosuvastatin every-other-day, or PCSK9 inhibitors (evolocumab, alirocumab) for patients at very high cardiovascular risk.

Fixed-Dose Combination Available

Ezetimibe 10 mg + simvastatin 40 mg (Inegy) and ezetimibe 10 mg + atorvastatin (various brands) are available as fixed-dose combinations that improve adherence. Where EZETROL is co-prescribed with a statin, confirm whether the patient would benefit from switching to a single combination tablet.

How is EZETROL different from a statin like atorvastatin?

Statins like atorvastatin work by reducing cholesterol production in the liver. EZETROL (ezetimibe) works differently — it blocks the absorption of cholesterol from your gut (both the cholesterol from food and the cholesterol recycled from bile). When used together, they target two different pathways of cholesterol management, giving a greater combined reduction in LDL cholesterol than either medicine alone.

Can I take EZETROL if I cannot tolerate statins due to muscle pain?

Yes — EZETROL does not cause the same muscle-related side effects as statins because it works in the gut rather than in muscle cells. It is commonly prescribed for patients who experience significant muscle pain (myalgia) on statins but still need to lower their cholesterol. While ezetimibe alone provides less LDL reduction than a full statin dose, it is a meaningful option for statin-intolerant patients.

How long will I need to take EZETROL?

Hypercholesterolaemia is a chronic condition, and cholesterol levels typically return to previous levels if the medicine is stopped. Most patients need to take EZETROL long-term as part of an ongoing lipid management strategy. Your doctor will monitor your cholesterol levels and cardiovascular risk at regular intervals to assess ongoing benefit from treatment.