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About EZETROL® (ezetimibe)

Updated on 06/09/2018

CARDIOVASCULAR

EZETROL is a once daily cholesterol absorption inhibitor used for the treatment of hypercholesterolaemia and has been available in the UK since 2003.1 Hypercholesterolaemia is characterised by very high level of LDL cholesterol (LDL-C) in the blood that leads to the blocking of blood vessels.2 The blocking of blood vessels causes cardiovascular (CV) events, such as heart attacks and strokes.2

Statins have been the mainstay of cholesterol lowering treatment as they have proven to reduce CV events over 20 years of research.3 EZETROL in combination with a statin was granted a license for the reduction in CV events4 in March 2016. EZETROL has proven lipid lowering efficacy when added to both atorvastatin 40 mg5 and atorvastatin 20 mg.6

EZETROL works by inhibiting the action of the Niemann-Pick C1-Like 1 (NPC1L1) protein preventing the uptake of cholesterol from the small intestine therefore reducing the amount of LDL-C in the blood stream.1

This is a different mode of action to statins which inhibit LDL-C production rather than absorption. As the mode of actions are complementary EZETROL reduces LDL-C without significantly increasing side effects.1

Many professional bodies in the UK and globally have written guidelines on the appropriate cholesterol lowering agents to use in different patient groups.

Therapeutic indications for EZETROL1

Primary hypercholesterolaemia

EZETROL, co-administered with a statin (HMG-CoA reductase inhibitor) is indicated as adjunctive therapy to diet in patients with primary (heterozygous familial and non-familial) hypercholesterolaemia who are not appropriately controlled with a statin alone.

EZETROL monotherapy is indicated as adjunctive therapy to diet in patients with primary (heterozygous familial and non-familial) hypercholesterolaemia in whom a statin is considered inappropriate or is not tolerated.

Prevention of cardiovascular events

EZETROL is indicated to reduce the risk of cardiovascular events in patients with coronary heart disease (CHD) and a history of acute coronary syndrome (ACS) when added to ongoing statin therapy or initiated concomitantly with a statin.

Homozygous familial hypercholesterolaemia (HoFH)

EZETROL, co-administered with a statin, is indicated as adjunctive therapy to diet in patients with HoFH. Patients may also receive adjunctive treatments.

Homozygous sitosterolaemia (phytosterolaemia)

EZETROL is indicated as adjunctive therapy to diet in patients with homozygous familial sitosterolaemia.

EZETROL mode of action1

EZETROL is a cholesterol absorption inhibitor which means that it stops cholesterol absorption from the small intestine. Cholesterol is prevented from leaving the small intestine by the selective inhibition of the sterol transporter Niemann-Pick C1-Like 1 (NPC1L1). EZETROL is taken orally and localises at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in cholesterol in the bloodstream.

This is a differing mode of action from statins, the main treatment for high cholesterol, which reduce cholesterol synthesis in the liver.7 Therefore, statins and EZETROL can work synergistically to lower blood cholesterol levels. Please play the video for a full explanation.

References

  1. EZETROL Summary of Product Characteristics.
  2. Task Force for the management of dyslipidaemias of the European Society of Cardiology (ESC) and the European Atherosclerosis Society (EAS). ESC/EAS Guidelines for the management of dyslipidaemias. Eur Heart J 2011; 32(14): 1769-1818.
  3. Randomised trial of cholesterol lowering in 4444 patients with coronary heart disease: the Scandinavian Simvastatin Survival Study (4S). Lancet 1994; 344: 1383-89.
  4. Cannon CP et al. Ezetimibe added to Statin Therapy after Acute Coronary Syndromes. N Engl J Med 2015; 372: 2387-2397.
  5. Leiter LA et al. Am J Cardiol 2008; 102: 1495-1501.
  6. Bays et al. Efficacy and safety of Ezetimibe added to atorvastatin versus atorvastatin uptitration or switching to rosuvastatin in patients with primary hypercholesterolemia. Am J Cardiol 2013; 112: 1885-1895.
  7. Shepherd J. The role of the exogenous pathway in hypercholesterolaemia. Eur Heart J Suppl 2001; 3(suppl E): E2-E5.

Related content

 

Supporting documentation

Prescribing Information | Summary of Product Characteristics | Patient Information Leaflet

CARD-1247020-0002 | Date of Preparation: September 2018