Ezetrol Ezetimibe

For patients who need additional LDL reduction beyond what a statin alone can achieve, or who cannot tolerate a statin, a cholesterol absorption inhibitor offers a distinct and complementary approach to lipid management. Ezetrol tablets contain ezetimibe 10 mg, a selective cholesterol absorption inhibitor that works at the intestinal level rather than in the liver. Ezetimibe can be used alongside a statin for additional LDL reduction, or as monotherapy when a statin is not appropriate. A prescription can only be issued following a clinical consultation.

Ezetrol is a branded oral prescription medicine. The active ingredient is ezetimibe 10 mg. Ezetimibe is a selective cholesterol absorption inhibitor, a class of lipid-lowering medicine that works by blocking the absorption of cholesterol from the small intestine. This mechanism is entirely distinct from statins, which work by reducing cholesterol synthesis in the liver, and from bile acid sequestrants, which work by binding bile acids in the gut.

Ezetrol is licensed in the UK for three indications. The first is primary hypercholesterolaemia in adults and children aged ten and over, used alongside dietary measures either as monotherapy or as an adjunct to a statin. The second is homozygous familial hypercholesterolaemia (HoFH) in adults and children aged ten and over, used alongside a statin (ezetimibe monotherapy has limited effect in HoFH). The third is homozygous sitosterolaemia (also called phytosterolaemia) in adults and children aged six and over, used as adjunctive therapy to diet. Generic ezetimibe tablets are also available from multiple manufacturers. Ezetrol is the originator branded product.

Ezetimibe is available in a single tablet strength of 10 mg. The dose is fixed at 10 mg once daily regardless of indication. A combination product containing ezetimibe 10 mg and simvastatin in various doses (Inegy) is also available as a separate product.

Ezetrol lowers LDL cholesterol through selective inhibition of cholesterol absorption in the small intestine.

Cholesterol Absorption Inhibition. Cholesterol enters the small intestine from two sources: dietary cholesterol from food and biliary cholesterol secreted by the liver into bile. Under normal circumstances, a transport protein called NPC1L1 (Niemann-Pick C1-like 1) on the surface of intestinal cells facilitates the absorption of cholesterol from the gut into the body. Ezetimibe selectively binds to and blocks NPC1L1, preventing cholesterol from crossing the intestinal wall. Unabsorbed cholesterol passes through the gut and is excreted in the faeces.

Compensatory Upregulation of Hepatic LDL Receptors. When less cholesterol is absorbed from the intestine and delivered to the liver, the liver compensates by increasing LDL receptor expression on its surface. These additional LDL receptors capture more LDL cholesterol from the bloodstream, reducing circulating LDL levels. This LDL receptor upregulation is the same mechanism that contributes to the LDL-lowering effect of statins, which is why ezetimibe and statins have complementary and additive effects when used together.

Ezetimibe reduces LDL cholesterol by approximately 15 to 22 per cent as monotherapy. When combined with a statin, it provides an additional LDL reduction on top of what the statin achieves alone, typically an extra 15 to 20 per cent beyond statin monotherapy. The IMPROVE-IT trial demonstrated that adding ezetimibe to simvastatin in patients following acute coronary syndrome produced additional cardiovascular benefit compared to simvastatin alone, supporting the clinical rationale for combination therapy in cardiovascular therapy.

Always take Ezetrol exactly as your prescriber instructs. Read the Patient Information Leaflet supplied with your medicine before starting treatment.

• Take one 10 mg tablet once daily, at any time of day.
• Ezetrol can be taken with or without food.
• Swallow the tablet whole with a glass of water.
• If you are also taking a bile acid sequestrant (such as colestyramine or Colestid granules), take Ezetrol at least two hours before or four or more hours after the sequestrant.

If you miss a dose, take it as soon as you remember. If you only remember the following day, skip the missed dose and continue as normal. Do not take two doses on the same day. Do not stop taking Ezetrol without speaking to your prescriber first.

Your prescriber will arrange blood tests to check your lipid levels before and after starting treatment, typically at four to twelve weeks. If you are also taking a statin, liver function may be monitored as part of the statin monitoring schedule.

Ezetrol 10 mg is the only available strength. The dose is always 10 mg once daily, regardless of whether Ezetrol is used as monotherapy or in combination with a statin. No dose titration is required or available. This fixed dosing schedule is simpler than many other lipid lowering medicines.

For the homozygous familial hypercholesterolaemia (HoFH) indication, Ezetrol 10 mg once daily is used alongside a statin. In HoFH, the LDL receptor pathway is severely impaired and ezetimibe alone is generally not sufficient; the statin combination is required to achieve meaningful LDL reduction. For sitosterolaemia, Ezetrol 10 mg once daily reduces absorption of plant sterols from the gut, a rare inherited condition requiring specialist management. All treatment decisions are made by your prescriber.

Ezetrol is generally well tolerated.

Common Side Effects (may affect up to 1 in 10 people):

• Gastrointestinal effects including abdominal pain, diarrhoea, and flatulence.
• Headache.
• Fatigue.

Uncommon Side Effects (may affect up to 1 in 100 people):

• Raised liver enzymes, more likely when combined with a statin and monitored accordingly.
• Muscle aches or weakness, with a slightly increased risk when combined with a statin.
• Nausea.
• Skin rash or itching.

Rare but Serious Side Effects — Seek Urgent Medical Attention: Go to your nearest accident and emergency department or call 999 immediately if you experience signs of a serious allergic reaction such as sudden swelling of the face, lips, tongue, or throat, difficulty breathing, or severe skin rash; severe muscle pain, weakness, or cramps with dark, tea coloured urine (myopathy/rhabdomyolysis, particularly when combined with a statin); or signs of significant liver problems such as yellowing of the skin or eyes, or severe abdominal pain.

Ezetrol tablets may be suitable if you:

• Are an adult or a young person aged ten and over (six and over for sitosterolaemia) with primary hypercholesterolaemia or mixed dyslipidaemia where further LDL reduction is needed.
• Are already taking a statin and have not achieved target LDL levels, and your prescriber has determined that adding ezetimibe is appropriate.
• Cannot tolerate a statin and require an alternative approach to cholesterol lowering as monotherapy.
• Have homozygous familial hypercholesterolaemia or homozygous sitosterolaemia under specialist care.
• Are already prescribed Ezetrol and require a repeat prescription through an online prescribing service.

Ezetrol tablets are not suitable if you:

• Are pregnant or planning to become pregnant. Ezetimibe is contraindicated in pregnancy when used in combination with a statin, and monotherapy is also not recommended as a precaution.
• Are breastfeeding.
• Have moderate or severe liver impairment.
• Are under ten years of age for the primary hypercholesterolaemia indication (under six for sitosterolaemia).
• Have a known allergy or hypersensitivity to ezetimibe or any excipient listed in the SmPC.

Important Drug Interactions: Bile acid sequestrants (colestyramine, Colestid granules, Cholestagel) can reduce ezetimibe absorption significantly — take Ezetrol at least two hours before or four or more hours after. Ciclosporin levels may increase, requiring monitoring. Fibrates increase the risk of gallstones and raise ezetimibe blood levels — this combination is generally not recommended. Warfarin requires INR monitoring when ezetimibe is added. Statins require liver function monitoring as clinically indicated.

Ezetrol is a Prescription Only Medicine. The clinical consultation is the essential first step. A prescription will only be issued if a registered prescriber concludes, based on their individual assessment of your circumstances, that Ezetrol is clinically appropriate for you.

During your online consultation with Pharmacy Planet, a registered prescriber will review your cholesterol levels, current lipid lowering medicines, relevant medical history, and the reason for seeking Ezetrol. The prescriber will determine whether Ezetrol is appropriate as monotherapy or as combination therapy alongside a statin, and whether online prescribing is suitable for your individual situation.

Not all consultations will result in a prescription. The prescriber may recommend a statin, a different approach to lipid management, or advise that a full cardiovascular risk assessment by your GP is needed before proceeding.