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  5. Cyclosporine and Grapefruit juice

INTERACTION STATUS
Major Interaction / Contraindicated
Cyclosporine
Grapefruit juice
Clinical Summary

Grapefruit juice significantly increases blood levels of cyclosporine, an immunosuppressant, potentially leading to toxicity and serious side effects.

Critical Warnings

Completely avoid grapefruit juice and related products (e.g., fresh fruit, marmalade) to prevent interaction.

Even small amounts can cause a significant increase in cyclosporine levels.

Inform healthcare providers of all dietary habits for optimal dose management.

Regular therapeutic drug monitoring is essential for patients on cyclosporine.

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Medical Analysis
Mechanism

Grapefruit juice contains furanocoumarins that irreversibly inhibit the CYP3A4 enzyme in the intestinal mucosa, reducing the first-pass metabolism of cyclosporine and resulting in elevated systemic concentrations.

Clinical Impact & Risks

Heightened risk of cyclosporine toxicity, including nephrotoxicity, hypertension, neurotoxicity (e.g., tremors, headaches), hepatotoxicity, and increased infection risk due to excessive immunosuppression.

Management & Recommendations

Avoid consumption of grapefruit juice or any grapefruit products while taking cyclosporine. If ingested, monitor cyclosporine blood levels closely and adjust dosage as needed under medical supervision. The interaction effect may persist for up to 72 hours after a single serving.

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The content on SafeTo is for informational purposes only and does not constitute medical, veterinary, or professional advice. Always consult with a qualified professional for specific concerns.

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