From the Guidelines
Crestor (rosuvastatin) is contraindicated in patients with active liver disease, unexplained persistent elevations of serum transaminases, hypersensitivity to rosuvastatin, pregnant women, nursing mothers, and those with concomitant use of cyclosporine or gemfibrozil. The primary concern with Crestor is its potential to cause hepatotoxicity, especially in patients with pre-existing liver conditions 1. Additionally, the risk of myopathy is increased when Crestor is used with certain medications, such as cyclosporine or gemfibrozil, due to significantly increased rosuvastatin plasma concentrations 1.
Some key points to consider when prescribing Crestor include:
- Patients with severe renal impairment (creatinine clearance <30 mL/min) should not use standard doses as drug clearance is reduced
- Asian patients may require lower starting doses due to higher systemic exposure
- Caution is needed in patients consuming excessive alcohol or those with a history of liver disease, as these factors increase the risk of hepatotoxicity
- Rosuvastatin works by inhibiting HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis, which explains why it affects developing fetuses and why liver function monitoring is important during treatment
It is essential to carefully evaluate patients for these contraindications and precautions before initiating Crestor therapy to minimize the risk of adverse effects and ensure the best possible outcomes in terms of morbidity, mortality, and quality of life. According to the 2013 ACC/AHA guideline on the treatment of blood cholesterol, it is reasonable to evaluate and treat muscle symptoms, including pain, tenderness, stiffness, cramping, weakness, or fatigue, in statin-treated patients according to a specific management algorithm 1.
From the FDA Drug Label
Rosuvastatin tablets are contraindicated in the following conditions: Acute liver failure or decompensated cirrhosis [see Warnings and Precautions (5.3)] . Hypersensitivity to rosuvastatin or any excipients in rosuvastatin tablets. Hypersensitivity reactions including rash, pruritus, urticaria, and angioedema have been reported with rosuvastatin tablets [see Adverse Reactions (6.1)] .
The contraindications for Crestor (rosuvastatin) are:
- Acute liver failure or decompensated cirrhosis
- Hypersensitivity to rosuvastatin or any excipients in rosuvastatin tablets, which may manifest as hypersensitivity reactions including rash, pruritus, urticaria, and angioedema 2.
From the Research
Contraindications for Crestor (Rosuvastatin)
There are no specific contraindications mentioned in the provided studies. However, the following points can be considered:
- The studies do not provide a comprehensive list of contraindications for Crestor (rosuvastatin) 3, 4, 5, 6, 7.
- Rosuvastatin is generally well tolerated, with most adverse events being mild to moderate in severity 3, 5.
- The most commonly reported treatment-related adverse events were myalgia, constipation, asthenia, abdominal pain, and nausea 3.
- Rosuvastatin has been shown to be safe and effective in patients with dyslipidemias, with no significant increases in liver enzymes or declines in renal function 4.
Special Considerations
- Patients with elevated hsCRP levels and normal LDL-C levels may benefit from rosuvastatin treatment, but the mechanism of benefit is not fully understood 5.
- Rosuvastatin has been shown to be effective in reducing LDL-C levels and improving lipid profiles in patients with hypercholesterolemia 3, 6, 7.
- The drug has a favorable pharmacologic profile, with a high affinity for the active site of HMG-CoA reductase and minimal metabolism by cytochrome P450 enzymes 6, 7.