Summary

Amiodarone significantly increases rosuvastatin blood levels by inhibiting drug transporters, potentially leading to statin-related toxicity including muscle damage. This interaction requires careful monitoring and possible dose adjustments when both medications are used together.

Introduction

Rosuvastatin is a potent HMG-CoA reductase inhibitor (statin) commonly prescribed to lower cholesterol and reduce cardiovascular risk. Amiodarone is a class III antiarrhythmic medication used to treat serious heart rhythm disorders, including atrial fibrillation and ventricular arrhythmias. Both medications are frequently prescribed in cardiovascular patients, making their potential interaction clinically significant.

Mechanism of Interaction

Amiodarone inhibits several drug transporters, particularly OATP1B1 (organic anion transporting polypeptide 1B1) and BCRP (breast cancer resistance protein), which are responsible for rosuvastatin uptake and elimination. This inhibition reduces rosuvastatin clearance from the body, leading to increased plasma concentrations. Unlike other statins that are primarily metabolized by cytochrome P450 enzymes, rosuvastatin relies heavily on transporter-mediated processes, making it particularly susceptible to this interaction.

Risks and Symptoms

The primary risk of this interaction is statin-induced toxicity, particularly myopathy (muscle pain and weakness) and potentially life-threatening rhabdomyolysis (severe muscle breakdown). Increased rosuvastatin levels may also elevate the risk of hepatotoxicity and new-onset diabetes. Studies have shown that amiodarone can increase rosuvastatin exposure by 2-3 fold, significantly raising the likelihood of adverse effects. Patients with additional risk factors such as advanced age, kidney disease, or hypothyroidism face even higher risks.

Management and Precautions

When co-prescribing these medications, consider reducing the rosuvastatin dose by 50% or switching to a lower-risk statin such as pravastatin or fluvastatin. Monitor patients closely for signs of myopathy including unexplained muscle pain, tenderness, or weakness. Obtain baseline and periodic creatine kinase (CK) levels, especially if symptoms develop. Liver function tests should also be monitored. Educate patients about recognizing symptoms of muscle toxicity and advise them to report any unusual muscle symptoms immediately. Consider the lowest effective rosuvastatin dose and evaluate the continued need for both medications regularly.

Rosuvastatin interactions with food and lifestyle

Grapefruit and grapefruit juice should be avoided or consumed with caution while taking rosuvastatin, as they can increase blood levels of the medication and potentially increase the risk of side effects. Excessive alcohol consumption should be limited as it may increase the risk of liver problems when combined with rosuvastatin. Patients should maintain consistent dietary habits and inform their healthcare provider about any significant changes in diet or lifestyle.

Amiodarone interactions with food and lifestyle

Grapefruit and grapefruit juice should be avoided as they can significantly increase amiodarone blood levels and risk of toxicity. Alcohol consumption should be limited or avoided as it may increase the risk of liver toxicity when combined with amiodarone. Patients should maintain consistent dietary habits and avoid excessive sun exposure, as amiodarone can cause photosensitivity reactions and skin discoloration with prolonged sun exposure.