Will Crestor (Rosuvastatin) cause elevated liver enzymes, specifically hepatocellular injury or cholestasis, leading to hypertransaminasemia?

From the Guidelines

Yes, Crestor (rosuvastatin) can elevate liver enzymes in some patients, as evidenced by the 2019 study published in the Journal of the American College of Cardiology 1. This is a known side effect of all statin medications, including Crestor. During treatment, liver enzyme levels (specifically ALT and AST) may increase, typically within the first few months of therapy. Most elevations are mild and temporary, not requiring discontinuation of the medication. However, your doctor will likely monitor your liver function with blood tests before starting Crestor and periodically during treatment. If enzyme levels rise to more than three times the upper limit of normal and persist, your doctor may reduce the dose or switch you to a different medication. This effect occurs because statins are metabolized in the liver, and the processing of the medication can stress liver cells in some individuals. Some key points to consider:

• The incidence of elevated liver enzymes is generally dose-dependent, as noted in the 2002 study published in Circulation 1.
• Severe statin-associated hepatotoxicity is rare, and the incidence is not impacted by routine monitoring of transaminases, as stated in the 2019 study 1.
• Statins can be used in patients with chronic, stable liver disease, such as nonalcoholic fatty liver disease, and may even have potential benefits, as suggested by the 2021 study published in Clinical and Molecular Hepatology 1. If you're taking Crestor and experience symptoms like unusual fatigue, pain in the upper right abdomen, dark urine, or yellowing of the skin or eyes, contact your healthcare provider promptly as these could indicate liver problems requiring medical attention. It's also important to note that the benefits of statin therapy, including Crestor, generally outweigh the risks of new-onset diabetes mellitus, as discussed in the 2019 study 1. Overall, while Crestor can elevate liver enzymes in some patients, the risk is generally manageable with proper monitoring and dose adjustment.

From the FDA Drug Label

Increases in serum transaminases have been reported with use of rosuvastatin [see Adverse Reactions (6. 1)] . In most cases, these changes appeared soon after initiation, were transient, were not accompanied by symptoms, and resolved or improved on continued therapy or after a brief interruption in therapy. In a pooled analysis of placebo-controlled trials, increases in serum transaminases to more than three times the ULN occurred in 1.1% of patients taking rosuvastatin versus 0. 5% of patients treated with placebo. Yes, rosuvastatin may elevate liver enzymes, as indicated by increases in serum transaminases in some patients. Patients who consume substantial quantities of alcohol and/or have a history of liver disease may be at increased risk for hepatic injury 2.

From the Research

Crestor and Liver Enzymes

• Crestor, a type of statin, may cause elevations in liver enzymes, as noted in studies 3, 4, 5.
• These elevations are typically mild, with alanine aminotransferase (ALT) or aspartate aminotransferase (AST) levels less than 3 times the upper limit of normal (ULN) 3, 5.
• The risk of hepatic injury caused by statins, including Crestor, is estimated to be about 1 percent, similar to that of patients taking a placebo 5.
• Elevations in liver enzymes may persist over time, but are often clinically and statistically insignificant, and should not deter physicians from prescribing or continuing statins 4.

Monitoring Liver Enzymes

• Liver function tests (LFTs) should be ordered before starting statin therapy, 12 weeks after initiation, with any dose increase, and periodically for long-term maintenance therapy 3.
• LFTs are an inexpensive, noninvasive, and quick first-line investigation to monitor liver status 4.
• Patients with transaminase levels no more than three times the upper limit of normal can continue taking statins, and often the elevations will resolve spontaneously 5.

Evaluation of Abnormal Liver Chemistries

• The evaluation of hepatocellular injury includes testing for viral hepatitis A, B, and C, assessment for nonalcoholic fatty liver disease and alcoholic liver disease, screening for hereditary hemochromatosis, autoimmune hepatitis, Wilson's disease, and alpha-1 antitrypsin deficiency 6.
• A history of prescribed and over-the-counter medicines should be sought, as some medications may cause liver injury 6.
• A liver biopsy may be considered when serologic testing and imaging fails to elucidate a diagnosis, to stage a condition, or when multiple diagnoses are possible 6.