What are the side effects and dosing recommendations for Rosuvastatin (generic name for Crestor), a statin medication?

From the Guidelines

Rosuvastatin should be prescribed at starting doses of 5-10 mg once daily for most patients, with a maximum dose of 40 mg daily, while monitoring for side effects such as muscle pain, liver problems, and increased blood sugar levels, as recommended by the 2018 AHA/ACC/AACVPR/AAPA/ABC/ACPM/ADA/AGS/APhA/ASPC/NLA/PCNA guideline on the management of blood cholesterol 1.

Side Effects and Dosing

• Common side effects include muscle pain or weakness, headache, nausea, and constipation.
• More serious but rare side effects include rhabdomyolysis (severe muscle breakdown), liver problems, and increased blood sugar levels.
• Patients should take rosuvastatin at the same time each day, with or without food, and avoid grapefruit products which can increase the risk of side effects.
• Regular blood tests are necessary to monitor liver function and cholesterol levels.
• Rosuvastatin works by inhibiting HMG-CoA reductase, an enzyme involved in cholesterol production in the liver, thereby reducing LDL ("bad") cholesterol and increasing HDL ("good") cholesterol.

Monitoring and Follow-up

• Patients should report any unexplained muscle pain, tenderness, or weakness to their healthcare provider immediately, especially if accompanied by fever or malaise, as these could indicate serious muscle problems.
• The 2018 AHA/ACC/AACVPR/AAPA/ABC/ACPM/ADA/AGS/APhA/ASPC/NLA/PCNA guideline recommends monitoring LDL-C levels and adjusting the dose of rosuvastatin accordingly 1.
• A study published in 2024 found that high-intensity statin therapy, including rosuvastatin, was associated with a increased risk of new-onset diabetes, highlighting the need for regular monitoring of blood sugar levels 1.

Special Considerations

• The choice of statin and dosage regimen should be individualized based on the patient's specific needs and medical history, as recommended by the expert panel on integrated guidelines for cardiovascular health and risk reduction in children and adolescents 1.
• Patients should be advised about potential drug-drug interactions and the need for regular monitoring of liver function and cholesterol levels.

From the FDA Drug Label

Rosuvastatin may cause myopathy [muscle pain, tenderness, or weakness associated with elevated creatine kinase (CK)] and rhabdomyolysis. The concomitant use of rosuvastatin with cyclosporine or gemfibrozil is not recommended Rosuvastatin dosage modifications are recommended for patients taking certain antiviral medications, darolutamide, and regorafenib Initiate at 5 mg once daily. Do not exceed 10 mg once daily. DarolutamideDo not exceed 5 mg once daily. RegorafenibDo not exceed 10 mg once daily

The side effects of rosuvastatin include:

• Myopathy
• Rhabdomyolysis
• Immune-mediated necrotizing myopathy
• Hepatic dysfunction
• Proteinuria and hematuria

The dosing for rosuvastatin is as follows:

• Initiate at 5 mg once daily
• Do not exceed 10 mg once daily for most patients
• Do not exceed 5 mg once daily for patients taking darolutamide
• Do not exceed 10 mg once daily for patients taking regorafenib 2

From the Research

Side Effects of Rosuvastatin

• The studies 3, 4, 5, 6, 7 show that rosuvastatin is generally well-tolerated with rare adverse effects.
• Adverse events were equally observed in the rosuvastatin and atorvastatin groups in the study 4.
• The study 5 found no significant difference between rosuvastatin and atorvastatin at any dose ratio for adverse events.
• The most common adverse events associated with rosuvastatin were not specified in the provided studies.

Dosing of Rosuvastatin

• The study 3 investigated the efficacy and safety of a fixed-dose combination of rosuvastatin 2.5 mg and ezetimibe 10 mg.
• The study 4 compared the efficacy of rosuvastatin 10 mg with atorvastatin 10 mg in achieving an LDL-C goal of < 1.00 g/l.
• The study 5 compared the efficacy and safety of rosuvastatin with atorvastatin at different dose ratios (1:1:2, and 1:4).
• The study 6 reviewed the efficacy and safety of a fixed-dose combination of rosuvastatin and ezetimibe in patients with hypercholesterolemia.
• The study 7 examined the effects of rosuvastatin 10,20, and 40 mg on non-HDL-C, apolipoproteins, and lipid ratios in patients with hypercholesterolemia.

Comparison with Other Statins

• The study 4 found that rosuvastatin 10 mg was more effective than atorvastatin 10 mg in achieving an LDL-C goal of < 1.00 g/l.
• The study 5 found that rosuvastatin was more efficacious than atorvastatin at 1:1 and 1:2 dose ratios, but not at a 1:4 dose ratio.
• The study 7 found that rosuvastatin 10 to 40 mg was more efficacious in improving the lipid profile of patients with hypercholesterolemia than milligram-equivalent doses of atorvastatin and milligram-equivalent or higher doses of simvastatin and pravastatin.