From the Guidelines
Rosuvastatin (Crestor) for hyperlipidemia is typically started at 5-10 mg once daily, with a usual dosage range of 5-40 mg once daily, as recommended by the most recent guidelines 1. The recommended starting dose is 10 mg once daily for most patients, though 5 mg may be appropriate for patients requiring less aggressive LDL reduction or those with predisposing factors for myopathy.
Key Considerations
- Elderly patients and those with renal impairment should start at 5 mg daily, as indicated in the guidelines for patients with chronic kidney disease 1.
- Dosage adjustments can be made at 2-4 week intervals based on lipid levels and tolerability.
- The maximum dose is 40 mg daily, reserved for patients with severe hypercholesterolemia requiring aggressive reduction.
- Asian patients should start at 5 mg due to higher systemic exposure.
Administration and Mechanism
- Rosuvastatin should be taken at the same time each day, with or without food, and patients should follow a lipid-lowering diet during treatment.
- The medication works by inhibiting HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis, thereby reducing LDL cholesterol production and increasing LDL receptor activity in the liver, which enhances clearance of LDL from the bloodstream.
Guideline Recommendations
- High-intensity statin therapy, which includes rosuvastatin 20-40 mg, is recommended for patients who require a significant reduction in LDL cholesterol levels 1.
- Moderate-intensity statin therapy, which includes rosuvastatin 5-10 mg, is recommended for patients who require a moderate reduction in LDL cholesterol levels 1.
From the FDA Drug Label
Rosuvastatin reduces Total-C, LDL-C, ApoB, non-HDL-C, and TG, and increases HDL-C, in adult patients with hyperlipidemia and mixed dyslipidemia In a multicenter, double-blind, placebo-controlled study in patients with hyperlipidemia, rosuvastatin given as a single daily dose (5 to 40 mg) for 6 weeks significantly reduced Total-C, LDL-C, non-HDL-C, and ApoB, across the dose range Table 10: Lipid-modifying Effect of Rosuvastatin in Adult Patients with Hyperlipidemia (Adjusted Mean % Change from Baseline at Week 6) DoseNTotal-CLDL-CNon-HDL-CApoBTGHDL-C Placebo13-5-7-7-3-33 Rosuvastatin 5 mg17-33-45-44-38-3513 Rosuvastatin 10 mg17-36-52-48-42-1014 Rosuvastatin 20 mg17-40-55-51-46-238 Rosuvastatin 40 mg18-46-63-60-54-2810
The dosing for Crestor (rosuvastatin) in hyperlipidemia treatment is as follows:
- Initial dose: 5-10 mg once daily
- Dose range: 5-40 mg once daily
- Titration: The dose may be increased at 6-week intervals to achieve the desired lipid levels
- Maximum dose: 40 mg once daily 2
From the Research
Dosing for Crestor (Rosuvastatin) in Hyperlipidemia Treatment
- The approved doses for rosuvastatin (Crestor) are 10-40 mg once daily to reduce low-density lipoprotein (LDL) cholesterol, increase high-density lipoprotein (HDL) cholesterol, and improve other lipid measures in dyslipidemic patients 3.
- Rosuvastatin 10 mg reduces LDL cholesterol significantly more than atorvastatin 10 mg, simvastatin 10-40 mg, and pravastatin 10-40 mg, and enables significantly more patients to achieve National Cholesterol Education Program and Joint European Societies LDL cholesterol goals compared with each of these statins 3.
- In a dose-ranging study in mild/moderate hypercholesterolemia, rosuvastatin reduced LDL cholesterol by 52-63% at 10-40 mg 3.
- The efficacy and safety of rosuvastatin have been compared with other statins, such as atorvastatin, in high-risk patients with hypercholesterolemia, with rosuvastatin 10 mg being more efficacious than atorvastatin 20 mg at reducing LDL-C and enabling LDL-C goal achievement 4.
Alternative Dosing Regimens
- Every-other-day dosing of rosuvastatin 10 mg has been compared with once-daily dosing, with results showing that every-other-day dosing may be an alternative regimen for cost savings, without a major decrease in therapeutic benefit or increase in adverse events, in patients with hypercholesterolemia 5.
- The percentage of patients who achieved LDL-C goals according to National Cholesterol Education Program-Adult Treatment Panel III guidelines was not significantly different between the once-daily (85%) and every-other-day (70%) groups 5.
Combination Therapy
- The combination of rosuvastatin and ezetimibe has been shown to be safe and effective in patients with hypercholesterolemia or dyslipidemia, enabling higher proportions of patients to achieve recommended LDL-C goals than rosuvastatin monotherapy or the simvastatin/ezetimibe combination, without additional adverse events 6.