How should an adult take rosuvastatin, including dose, timing, food considerations, and adjustments for renal impairment or liver disease?

How to Take Rosuvastatin

Rosuvastatin should be taken once daily at any time of day, with or without food, starting at 5-10 mg for most adults, with dose adjustments based on cardiovascular risk and renal function. 1, 2

Standard Dosing and Administration

Timing and Food Considerations

• Take rosuvastatin once daily at any time of day, consistently at the same time. 2, 3
• Food does not affect rosuvastatin absorption—it can be taken with or without meals. 2, 4
• Maximum plasma concentration is reached at approximately 5 hours after administration under fasting conditions. 3

Starting Dose for Most Adults

• For moderate-intensity therapy, start with rosuvastatin 5-10 mg once daily. 1
• For high-intensity therapy (requiring >50% LDL-C reduction), use rosuvastatin 20-40 mg once daily. 1
• The typical starting dose is 10 mg daily for primary or secondary prevention in patients without renal impairment. 5, 2

Dose Adjustments for Renal Impairment

Severe Renal Impairment (CrCl <30 mL/min/1.73 m²)

• Start with rosuvastatin 5 mg once daily and do not exceed 10 mg once daily. 5, 6
• Rosuvastatin has significant renal excretion and requires dose limitation in severe renal impairment. 5, 6
• For patients with stage 4 CKD (eGFR 15-29 mL/min/1.73 m²), atorvastatin is preferred over rosuvastatin because it requires no renal dose adjustment. 6

Dialysis Patients

• Do not initiate rosuvastatin in patients already on dialysis, as major trials showed no cardiovascular benefit. 5, 6
• If already taking rosuvastatin when dialysis begins, continuation is reasonable but not initiation. 6

Mild to Moderate Renal Impairment (eGFR ≥30 mL/min/1.73 m²)

• No dose adjustment is required. 6

Dose Adjustments for Liver Disease

• Rosuvastatin is contraindicated in active liver disease or unexplained persistent elevations in serum transaminases. 2, 4
• Monitor ALT/AST at baseline and 12 weeks after initiation or dose changes. 7

Special Population Considerations

Asian Patients

• Start with rosuvastatin 5 mg daily regardless of renal function due to 2-fold higher plasma concentrations in Asian populations. 5

Elderly Patients (>75 years)

• For those already on statin therapy, continue rosuvastatin. 1
• For new initiations, consider starting with moderate-intensity therapy (5-10 mg daily) after discussing benefits and risks. 1

Patients with Diabetes

• For patients aged 40-75 years with diabetes at higher cardiovascular risk, use high-intensity statin therapy (rosuvastatin 20-40 mg) to achieve ≥50% LDL-C reduction and target LDL-C <70 mg/dL. 1

Critical Drug Interactions

Medications Requiring Dose Limitation

• If taking cyclosporine, tacrolimus, everolimus, or sirolimus, limit rosuvastatin to 5 mg daily maximum. 5
• Significant interactions occur with gemfibrozil—avoid this combination. 2
• Warfarin co-administration requires monitoring as both are metabolized by CYP2C9. 8

Medications with Statistically Significant Interactions

• Erythromycin, fluconazole, itraconazole, and antacids show statistically significant interactions with rosuvastatin. 3
• Darunavir/ritonavir interaction is considered both statistically and clinically relevant. 3

Monitoring Strategy

Lipid Panel Assessment

• Reassess lipid panel 4-12 weeks after starting or changing dose to ensure adequate LDL-C reduction. 5
• For CKD patients ≥50 years with eGFR <60 mL/min/1.73 m², do not use LDL-C levels to guide treatment decisions—treatment is based on cardiovascular risk, not lipid targets. 6

Safety Monitoring

• Monitor for muscle symptoms (myalgia, weakness) at each visit. 7
• Check CPK only if muscle symptoms develop—routine CPK monitoring is not recommended. 7
• Evaluate ALT/AST at 12 weeks after each dose change, then annually. 7

Dose Titration Algorithm

If LDL-C Goal Not Achieved

• Increase rosuvastatin dose sequentially: 5 mg → 10 mg → 20 mg → 40 mg. 9
• Each dose increase provides approximately 5-6 percentage points additional LDL-C reduction. 9
• If maximum tolerated rosuvastatin dose does not achieve goal, add ezetimibe 10 mg daily. 1, 7

Maximum Approved Dose

• The maximum approved daily dose is 40 mg. 3
• Doses of 80 mg have been studied but are not approved. 2

Common Pitfalls to Avoid

• Do not use rosuvastatin as first-line therapy in severe renal impairment (CrCl <30 mL/min)—atorvastatin is preferred. 5, 6
• Do not initiate rosuvastatin in dialysis-dependent patients. 6
• Do not combine rosuvastatin with gemfibrozil due to increased myopathy risk. 2
• Do not exceed 5 mg daily when co-administered with cyclosporine or other immunosuppressants. 5
• The risk of proteinuria is significantly higher with 40 mg compared to 20 mg daily. 9