Information last reviewed: May 2026 — for educational purposes only.
Rosuvastatin, sold as Crestor, is a synthetic, highly potent HMG-CoA reductase inhibitor (statin) used to lower LDL cholesterol, total cholesterol, and triglycerides, and to raise HDL cholesterol. It is one of the most effective statins milligram-for-milligram, with rosuvastatin 10 mg approximately equivalent in LDL-lowering efficacy to atorvastatin 20 mg. It is prescription-only and is available in generic form since 2016. Rosuvastatin is taken once daily and can be taken at any time of day with or without food.
Indications for Rosuvastatin
- Primary hyperlipidaemia and mixed dyslipidaemia — reduce elevated LDL, total cholesterol, non-HDL cholesterol, and triglycerides; raise HDL
- Primary prevention of cardiovascular events — in patients with no prior cardiovascular disease but elevated CRP (JUPITER trial) and multiple risk factors
- Secondary prevention — after a heart attack, stroke, or established coronary artery disease
- Familial hypercholesterolaemia — including heterozygous and homozygous forms; rosuvastatin 40 mg can reduce LDL by 50–60%
- Hypertriglyceridaemia as part of broader dyslipidaemia management
Why Rosuvastatin Is Not Affected by CYP3A4 Interactions
Unlike most other statins (atorvastatin, simvastatin, lovastatin), rosuvastatin is minimally metabolised by CYP3A4. It is primarily taken up by hepatic OATP1B1 transporters and is primarily excreted unchanged in faeces. This means the many drug interactions that affect CYP3A4-metabolised statins (e.g., grapefruit juice, diltiazem, verapamil, clarithromycin, HIV protease inhibitors, antifungals) are much less relevant for rosuvastatin. However, some drugs do increase rosuvastatin exposure: cyclosporine, certain HIV medications (lopinavir/ritonavir, atazanavir/ritonavir), and antacids containing aluminium/magnesium (separate by 2 hours).
Tablet Strengths
- 5 mg — starting dose for elderly, Asian patients (higher blood levels in Asian populations), or patients at increased myopathy risk
- 10 mg — usual starting dose; reduces LDL by approximately 46%
- 20 mg — moderate-intensity to high-intensity; reduces LDL by approximately 52%
- 40 mg — maximum dose; high-intensity statin; reduces LDL by approximately 55–60%; reserved for patients requiring significant additional LDL reduction (e.g., familial hypercholesterolaemia)
All strengths are taken once daily at any time of day, with or without food. Unlike simvastatin (which should be taken in the evening due to nocturnal cholesterol synthesis), rosuvastatin’s long half-life means timing is not clinically significant.
Price of Generic Rosuvastatin
Generic rosuvastatin has been available since 2016 and is affordable. A 30-day supply of rosuvastatin 10 mg costs approximately $10–$30 with a pharmacy discount card in the US. Brand-name Crestor is significantly more expensive; generics are therapeutically equivalent.
Frequently Asked Questions
Is rosuvastatin the strongest statin available?
Rosuvastatin 40 mg and atorvastatin 80 mg are both considered the highest-intensity statin dosing available for clinical use. Rosuvastatin achieves the highest percentage LDL reduction per milligram, making it particularly valuable when aggressive LDL lowering is needed (e.g., post-ACS, familial hypercholesterolaemia). Both are considered high-intensity statins per ACC/AHA cholesterol guidelines.
Can I take rosuvastatin with grapefruit juice?
Unlike simvastatin and atorvastatin (both CYP3A4-metabolised), rosuvastatin is not significantly affected by grapefruit juice. There is no clinically relevant interaction between grapefruit and rosuvastatin — patients on rosuvastatin can consume grapefruit or grapefruit juice without concern for increased drug levels.
What monitoring is required while on rosuvastatin?
Before starting rosuvastatin, a baseline fasting lipid panel and liver function tests (LFTs) are typically obtained. Routine periodic LFT monitoring during treatment is no longer universally recommended unless symptoms of hepatic dysfunction arise. Patients should report unexplained muscle pain, tenderness, weakness, or dark urine (potential signs of rhabdomyolysis) immediately. Lipid levels are rechecked 4–12 weeks after initiating therapy.
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