Rosuvastatin grapefruit
Pro Research Analysisby 
Searched over 200M research papers for "rosuvastatin grapefruit"
Consensus Meter
Rosuvastatin and Grapefruit Juice Interaction: A Comprehensive Overview
Introduction to Rosuvastatin and Grapefruit Juice Interaction
Rosuvastatin is a widely used statin for lowering cholesterol levels and preventing cardiovascular diseases. Grapefruit juice (GFJ) is known to interact with various medications, potentially altering their pharmacokinetics and leading to adverse effects. This article explores the interaction between rosuvastatin and grapefruit juice, drawing on recent research findings.
Mechanisms of Interaction: OATP2B1 and CYP3A4 Inhibition
Grapefruit juice can affect drug pharmacokinetics through multiple mechanisms, including the inhibition of cytochrome P450 3A4 (CYP3A4) and organic anion transporting polypeptides (OATP2B1). CYP3A4 inhibition by GFJ reduces presystemic metabolism, thereby increasing the bioavailability of drugs metabolized by this enzyme. Additionally, GFJ inhibits OATP2B1, which plays a crucial role in the intestinal absorption of various drugs, including rosuvastatin .
Clinical Implications of Rosuvastatin and Grapefruit Juice Interaction
A study investigating the effects of GFJ on the pharmacokinetics of rosuvastatin found that GFJ significantly reduced the exposure of rosuvastatin compared to the control phase, indicating that rosuvastatin is a substrate for OATP2B1. This reduction in drug exposure could potentially diminish the therapeutic efficacy of rosuvastatin.
Genetic Factors Influencing Drug Interaction
The pharmacokinetics of rosuvastatin can also be influenced by genetic polymorphisms. Individuals with the ABCG2 421C/A genotype exhibited significantly higher exposure to rosuvastatin compared to those with the ABCG2 421C/C genotype, regardless of GFJ consumption. This suggests that genetic factors can modulate the extent of drug interaction and should be considered in clinical settings.
Potential Risks: Rhabdomyolysis and Other Adverse Effects
While rosuvastatin is not primarily metabolized by CYP3A4, the inhibition of this enzyme by GFJ can still pose risks. A case report highlighted a patient who developed rhabdomyolysis after consuming pomegranate juice, which, like GFJ, inhibits CYP3A4. This suggests that similar risks could arise with GFJ consumption during rosuvastatin therapy, despite the drug's minimal reliance on CYP3A4 for metabolism.
Conclusion
The interaction between rosuvastatin and grapefruit juice is primarily mediated through the inhibition of OATP2B1, leading to reduced drug absorption and potentially diminished therapeutic effects. Genetic factors, such as the ABCG2 421C/A polymorphism, can further influence this interaction. Although rosuvastatin is not extensively metabolized by CYP3A4, caution is advised due to the potential risk of adverse effects like rhabdomyolysis. Patients on rosuvastatin therapy should be counseled to avoid grapefruit juice to ensure optimal drug efficacy and safety.
Sources and full results
Most relevant research papers on this topic