Rosuvastatin with Amiodarone Interaction Details

Brand Names Associated with Rosuvastatin

Brand Names Associated with Amiodarone

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Feb 27, 2024

Interaction Effect

Elevations in serum transaminase levels

Interaction Summary

A case report described marked but asymptomatic elevations in serum transaminase levels in a patient receiving rosuvastatin and amiodarone concomitantly. Inhibition of the CYP2C9-mediated rosuvastatin metabolism by amiodarone was proposed as a possible mechanism for this interaction[1]. Use caution when these agents are used concurrently and consider monitoring serum transaminase levels periodically during concurrent therapy. Also, monitor patients for signs/symptoms of liver dysfunction or myopathy.

Severity

Moderate

Onset

Delayed

Evidence

Probable

How To Manage Interaction

Use caution if amiodarone and rosuvastatin are coadministered as this may cause marked elevations in serum transminase levels. If concurrent therapy is required, consider monitoring serum transaminase levels at baseline and periodically during therapy. Also, monitor patients for signs/symptoms of liver dysfunction or myopathy.

Mechanism Of Interaction

Inhibition by amiodarone of CYP2C9-mediated rosuvastatin metabolism

Literature Reports

A) Asymptomatic elevations in serum transaminase levels occurred in a 73-year-old woman after amiodarone 200 mg/day was added to an established treatment regimen that included rosuvastatin 5 mg/day. Prior to this incident, the patient developed mild elevation (3.5 to 6.5 times the normal baseline values) of serum transaminase levels with concurrent use of gemfibrozil 600 mg twice daily and rosuvastatin 5 mg/day. However, the levels had returned to almost normal following discontinuation of gemfibrozil. Subsequently, amiodarone was initiated for aortic valve replacement. Within 14 days, laboratory analysis revealed a 14- to 24-fold increase in aspartate transaminase (AST) level (192 International Units/liter), alanine aminotransferase (ALT) level (336 International Units/liter), and an alkaline phosphatase (ALP) level of (322 International Units/liter) from normal baseline levels of 30, 58, and 99 International Units/liter, respectively. The patient did not report any symptoms of liver dysfunction or myopathy. Approximately 8 days following the discontinuation of rosuvastatin, serum AST, ALT, and ALP concentrations decreased to 68, 126, and 292 International Units/liter, respectively. Amiodarone therapy was continued and transminase levels continued to decline towards normal. At the 2-month follow up, AST, ALT, and ALP levels were 38, 59, and 107 International Units/liter, respectively. The interaction was rated as probable on the Naranjo adverse drug reaction probability scale [1].

References

1 ) Merz T & Fuller SH: Elevated serum transaminase levels resulting from concomitant use of rosuvastatin and amiodarone. Am J Health Syst Pharm 2007; 64(17):1818-1821.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...

Rosuvastatin Overview

• Rosuvastatin is used together with diet, weight-loss, and exercise to reduce the risk of heart attack and stroke and to decrease the chance that heart surgery will be needed in people who have heart disease or who are at risk of developing heart disease. Rosuvastatin is also used to decrease the amount of cholesterol such as low-density lipoprotein (LDL) cholesterol ('bad cholesterol') and triglycerides in the blood and to increase the amount of high-density lipoprotein (HDL) cholesterol ('good cholesterol') in the blood. Rosuvastatin may also be used together with diet to decrease the amount of cholesterol and other fatty substances in the blood in children and teenagers 8 to 17 years of age who have familial heterozygous hypercholesterolemia (an inherited condition in which cholesterol cannot be removed from the body normally). Rosuvastatin is used together with diet, and alone or in combination with other medications, to decrease the amount of cholesterol and other fatty substances in the blood in adults and children and teenagers 7 to 17 years of age who have familial homozygous hypercholesterolemia (an inherited condition in which cholesterol cannot be removed from the body normally). Rosuvastatin is in a class of medications called HMG-CoA reductase inhibitors (statins). It works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body.

• Accumulation of cholesterol and fats along the walls of your arteries (a process known as atherosclerosis) decreases blood flow and, therefore, the oxygen supply to your heart, brain, and other parts of your body. Lowering your blood level of cholesterol and fats with rosuvastatin has been shown to prevent heart disease, angina (chest pain), strokes, and heart attacks.

Amiodarone Overview

• Amiodarone is used to treat and prevent certain types of serious, life-threatening ventricular arrhythmias (a certain type of abnormal heart rhythm when other medications did not help or could not be tolerated. Amiodarone is in a class of medications called antiarrhythmics. It works by relaxing overactive heart muscles.

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Definitions

Severity Categories

Contraindicated

These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.

Major

This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.

Moderate

This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.

Minor

While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.

Onset

Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.

Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.

Evidence

Level of documentation of the interaction.

Established: The interaction is documented and substantiated in peer-reviewed medical literature.

Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.

How To Manage The Interaction

Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.

It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.

Mechanism Of Interaction

The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.

Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.

Where Does Our Information Come From?

Information for our drug interactions is compiled from several drug compendia, including:

• Gold Standard Drug Database
• Micromedex
• Lexicomp
• DrugBank

The prescribing information for each drug, as published on DailyMED, is also used. 

Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.

The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.