What are the risks associated with Crestor (rosuvastatin) due to its black box warning?

From the Guidelines

Crestor (rosuvastatin) does not have a black box warning, and its potential side effects, including muscle pain, liver enzyme elevations, and a small increased risk of diabetes, are listed as regular warnings rather than black box warnings. While Crestor is associated with a rare but serious potential side effect, rhabdomyolysis (severe muscle breakdown), this occurs in less than 0.1% of patients 1. Patients taking Crestor should be aware of symptoms like unexplained muscle pain or weakness, especially with fever, and report these to their doctor immediately. Regular monitoring of liver enzymes and kidney function is recommended, particularly when starting therapy or adjusting dosage, as supported by studies on statin safety in patients with chronic kidney disease 1. Certain medications and conditions can increase the risk of side effects when taken with Crestor, so patients should always inform their healthcare providers about all medications they are taking. The FDA has approved Crestor as an adjunct to diet to lower LDL cholesterol in adolescent boys and postmenarcheal girls aged 10–18 years with heterozygous familial hypercholesterolemia (HeFH) and LDL cholesterol ≥190 mg/dL, or ≥160 mg/dL with a family history of premature cardiovascular disease and ≥2 cardiovascular risk factors in the pediatric patient 1.

Key Considerations

• Regular monitoring of liver enzymes and kidney function is crucial when taking Crestor, especially in patients with pre-existing kidney disease 1.
• Patients should be aware of the rare but serious risk of rhabdomyolysis and report any symptoms of muscle pain or weakness to their doctor immediately.
• Crestor is approved for use in adolescents with HeFH and high LDL cholesterol levels, with specific guidelines for dosage and monitoring 1.
• The potential benefits of Crestor in reducing cardiovascular risk must be weighed against the potential risks and side effects, particularly in patients with underlying medical conditions.

Recommendations for Patients Taking Crestor

• Inform healthcare providers about all medications being taken to minimize the risk of drug interactions.
• Report any symptoms of muscle pain, weakness, or fever to the doctor immediately.
• Undergo regular monitoring of liver enzymes and kidney function, especially when starting or adjusting Crestor therapy.
• Follow the recommended dosage and treatment guidelines for Crestor, as approved by the FDA for specific patient populations 1.

From the FDA Drug Label

Myopathy and Rhabdomyolysis Advise patients that rosuvastatin may cause myopathy and rhabdomyolysis Inform patients that the risk is also increased when taking certain types of medication and they should discuss all medication, both prescription and over-the-counter, with their healthcare provider.

Hepatic Dysfunction Inform patients that rosuvastatin may cause liver enzyme elevations and possibly liver failure.

The black box warning for Crestor (rosuvastatin) is associated with the following risks:

• Myopathy and Rhabdomyolysis: Rosuvastatin may cause myopathy and rhabdomyolysis, and the risk is increased when taking certain types of medication.
• Hepatic Dysfunction: Rosuvastatin may cause liver enzyme elevations and possibly liver failure. 2

From the Research

Risks Associated with Crestor (Rosuvastatin)

The black box warning for Crestor (rosuvastatin) highlights the risk of myopathy and rhabdomyolysis, which are serious adverse effects associated with statin use. Some of the key risks include:

• Myopathy: a rare but serious condition characterized by muscle weakness and pain 3, 4, 5
• Rhabdomyolysis: a life-threatening condition that occurs when muscle tissue breaks down and releases myoglobin into the bloodstream, leading to kidney damage 3, 4, 5
• Increased risk of myopathy and rhabdomyolysis with high doses of rosuvastatin (above 40 mg) 5
• Renal failure: higher doses of rosuvastatin have been associated with cases of renal failure 6
• Proteinuria: rosuvastatin-induced inhibition of low-molecular-weight protein reabsorption by the renal tubules may lead to proteinuria 6
• Drug-drug interactions: co-administration of rosuvastatin with certain drugs, such as vitamin K antagonists, cyclosporine, gemfibrozil, and antiretroviral agents, may increase the risk of toxicity 6

Patient Factors that Increase the Risk of Adverse Effects

Certain patient factors may increase the risk of adverse effects associated with rosuvastatin, including:

• Advanced age: older patients may be more susceptible to the adverse effects of rosuvastatin 6
• Renal impairment: patients with chronic kidney disease may be at increased risk of myopathy and rhabdomyolysis 3
• Concomitant use of certain medications: patients taking medications that interact with rosuvastatin may be at increased risk of adverse effects 6
• Genetic factors: certain genetic variants, such as the CYP2C9*1/*3 genotype, may increase the risk of myopathy and rhabdomyolysis 3

Importance of Proper Dosing and Monitoring

Proper dosing and monitoring are crucial to minimizing the risk of adverse effects associated with rosuvastatin. This includes:

• Starting with a low dose and gradually increasing as needed and tolerated 7
• Monitoring liver enzymes and creatine kinase levels regularly 7
• Adjusting the dose or discontinuing treatment if adverse effects occur 3, 4, 5
• Educating patients about the risks and benefits of rosuvastatin and the importance of reporting any adverse effects 3, 4, 5