Ezetimibe (Ezetrol, Merck Sharp & Dohme) is a cholesterol‑absorption inhibitor that blocks the intestinal absorption of dietary and biliary cholesterol and related plant sterols, without affecting the uptake of triglycerides or fat‑soluble vitamins. Because of this mechanism of action, ezetimibe can be combined with a statin to provide either a complementary or an alternative mode of cholesterol reduction.
Ezetimibe, with a statin or as monotherapy, has a marketing authorisation in the UK. It is licensed in combination with an HMG‑CoA reductase inhibitor (statin) as an adjunctive therapy to diet for primary heterozygous‑familial or non‑familial hypercholesterolaemia that is not appropriately controlled with a statin alone. Ezetimibe monotherapy has a marketing authorisation as an adjunctive therapy to diet for primary heterozygous‑familial or non‑familial hypercholesterolaemia when a statin is considered inappropriate or is not tolerated.
Adverse reactions with ezetimibe as monotherapy or with a statin are usually mild and transient. When given as monotherapy, they most commonly include abdominal pain, diarrhoea, flatulence and fatigue. When taken with a statin, the most common additional adverse reactions include increased alanine transaminase, aspartate transaminase or both, headache and myalgia. For full details of adverse effects and contraindications, see the summaries of product characteristics.
Ezetimibe is taken orally at a dose of 10 mg once daily. Ezetimibe is available as 10‑mg tablets (28‑tablet pack) at a net price per pack of £26.31 (excluding VAT; 'British national formulary' [BNF]; accessed September 2015). A fixed‑dose combination tablet (Inegy, Merck Sharp & Dohme) containing ezetimibe 10 mg and simvastatin 20 mg (28‑tablet pack) is available at a net price per pack of £33.42, ezetimibe 10 mg and simvastatin 40 mg (28‑tablet pack) at a net price per pack of £38.98, and ezetimibe 10 mg and simvastatin 80 mg (28‑tablet pack) at a net price per pack of £41.21 (excluding VAT; BNF; accessed September 2015). Costs may vary in different settings because of negotiated procurement discounts.