Ezetimibe / Rosuvastatin

What it is and how it works

Ezetimibe inhibits intestinal absorption of dietary and biliary cholesterol by blocking the NPC1L1 sterol transporter. Rosuvastatin competitively inhibits HMG-CoA reductase, reducing hepatic cholesterol synthesis and up-regulating LDL receptors. The complementary mechanisms produce greater LDL-cholesterol reduction than either drug alone.

Indications

Adjunct to diet in primary hypercholesterolaemia or mixed dyslipidaemia in adults adequately controlled with the individual components at the same doses, or not adequately controlled with a statin alone; prevention of cardiovascular events in patients with coronary heart disease as substitution therapy.

Dosage and administration (summary)

Oral, one tablet once daily at any time of day, with or without food; the strength (ezetimibe 10 mg with rosuvastatin 5–40 mg) is chosen according to prior therapy and lipid targets.

Contraindications

Active liver disease or unexplained persistent rise in serum transaminases, myopathy, concomitant ciclosporin, severe renal impairment (for higher rosuvastatin strengths), pregnancy, breastfeeding and women of child-bearing potential not using contraception.

Warnings and precautions

Statins can cause myalgia, myopathy and rarely rhabdomyolysis; risk factors include hypothyroidism, renal impairment, high doses, Asian ancestry and interacting drugs (e.g. gemfibrozil, some antiretrovirals); creatine kinase should be measured if muscle symptoms occur. Liver function should be checked before treatment, and statins may slightly increase the risk of diabetes in predisposed patients.

Pregnancy

Contraindicated in pregnancy.

Storage and supply

Store below 30 °C in the original package to protect from moisture.

Source: reference summary prepared from the EU SmPC/EPAR, BNF and WHO Model Formulary. The approved product information in Iran governs.