Rosuvastatin

How it works

It competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in hepatic cholesterol synthesis. The resulting upregulation of hepatic LDL receptors increases clearance of circulating LDL-cholesterol.

Prescribing in practice

• Muscle toxicity (myopathy and rarely rhabdomyolysis) can occur — investigate unexplained muscle pain, tenderness or weakness and check creatine kinase; risk rises with higher doses, renal impairment, hypothyroidism and certain interacting drugs.
• Use lower doses and apply a maximum-dose cap in patients of South or East Asian origin, in whom plasma exposure is higher.
• Transaminases may rise and new-onset diabetes can occur; avoid in active liver disease, in pregnancy and breastfeeding, and review interacting drugs (e.g. ciclosporin, certain antivirals, gemfibrozil).

Monitoring

Check a lipid profile and baseline liver function before starting, with liver function rechecked during the early months of treatment; assess the lipid response and reinforce adherence. Measure creatine kinase if muscle symptoms develop, and check renal function and HbA1c/glucose where clinically indicated.

Counselling the patient

• Report promptly any unexplained muscle pain, tenderness, cramps or weakness, particularly if accompanied by feeling unwell or fever.
• Tell us if you become pregnant, are planning pregnancy or are breastfeeding, as this medicine should be stopped.
• Take it regularly as prescribed and continue lifestyle measures; avoid large quantities of grapefruit juice and check before starting new medicines.

Evidence & guidelines

Statins are guideline-recommended for cardiovascular risk reduction (NICE NG238; NICE CG181 lipid modification).