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 adults with high cholesterol, with a maximum dose of 40 mg daily, while monitoring for potential side effects such as muscle pain, liver damage, and increased blood sugar levels, as supported by the most recent and highest quality study 1.

Key Considerations

• The dosing of rosuvastatin is crucial, with high-intensity statin therapy (such as rosuvastatin 20 mg) being more effective in reducing LDL-C levels but also associated with a higher risk of new-onset diabetes, as shown in a recent individual participant data meta-analysis 1.
• Common side effects of rosuvastatin include muscle pain or weakness, headache, nausea, and constipation, while more serious but rare side effects include rhabdomyolysis, liver damage, 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 side effect risks.
• Regular blood tests are necessary to monitor liver function and cholesterol levels, and patients should immediately report unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or malaise.

Mechanism of Action

• Rosuvastatin works by inhibiting HMG-CoA reductase, an enzyme crucial for cholesterol production in the liver, thereby reducing LDL ("bad") cholesterol and increasing HDL ("good") cholesterol, which helps prevent cardiovascular disease.

Clinical Guidelines

• The 2018 AHA/ACC/AACVPR/AAPA/ABC/ACPM/ADA/AGS/APhA/ASPC/NLA/PCNA guideline on the management of blood cholesterol recommends rosuvastatin as a high-intensity statin option for patients with high cholesterol, with a goal of reducing LDL-C levels by 50% or more 1.
• The guideline also emphasizes the importance of monitoring patients for potential side effects and adjusting the dose or switching to a different statin if necessary.

From the FDA Drug Label

Rosuvastatin tablets may cause serious side effects, including: Muscle pain, tenderness and weakness (myopathy). The most common side effects may include headache, nausea, muscle aches and pains, weakness, and constipation. Your healthcare provider may do blood tests to check your liver before you start taking rosuvastatin tablets and if you have symptoms of liver problems while you take rosuvastatin tablets Rosuvastatin tablets can be taken at any time of day, with or without food. Do not change your dose or stop rosuvastatin tablets without talking to your healthcare provider, even if you are feeling well.

Side Effects and Dosing for Rosuvastatin:

• The dosing for rosuvastatin is as follows:
  • Initiate at 5 mg once daily for certain medications
  • Do not exceed 10 mg once daily for certain medications
  • Do not exceed 5 mg once daily for darolutamide
  • Do not exceed 10 mg once daily for regorafenib
• Common Side Effects: headache, nausea, muscle aches and pains, weakness, and constipation
• Serious Side Effects: muscle pain, tenderness and weakness (myopathy), liver problems, protein and blood in the urine
• Patients should be instructed to promptly report any unexplained muscle pain, tenderness or weakness, particularly if accompanied by malaise or fever 2
• Rosuvastatin dosage modifications are recommended for patients taking certain antiviral medications, darolutamide, and regorafenib 2

From the Research

Side Effects of Rosuvastatin

• The most common side effects of rosuvastatin include myalgia, increased alanine aminotransferase, and creatine kinase 3.
• Rosuvastatin has been shown to have a similar risk of adverse events compared to atorvastatin at 1:1 and 1:2 dose ratios 3.
• The percentages of change in glomerular filtration rate (GFR) improved significantly with both rosuvastatin and atorvastatin treatments 3.

Dosing of Rosuvastatin

• Rosuvastatin is available in doses of 10,20,40, and 80 mg 4.
• The efficacy of rosuvastatin in improving lipid profiles has been shown to be dose-dependent, with higher doses resulting in greater reductions in non-HDL-C and apo B 4.
• Rosuvastatin 10 to 40 mg has been shown to be more efficacious in improving lipid profiles compared to milligram-equivalent doses of atorvastatin and milligram-equivalent or higher doses of simvastatin and pravastatin 4.

Mechanism of Action and Additional Benefits

• Rosuvastatin acts by competitively inhibiting the 3-hydroxy-3-methylglutaryl coenzyme A reductase, a liver enzyme responsible for the rate-limiting step in cholesterol synthesis 5.
• In addition to its cholesterol-lowering effects, rosuvastatin has anti-inflammatory, antioxidant, and antithrombotic properties, making it a valuable tool for cardiovascular primary and secondary prevention 5.
• Recent data have highlighted the beneficial effects of rosuvastatin in several other fields, beyond its cholesterol-lowering effects 5.