SIROLIMUS (Generic for RAPAMUNE)

Sirolimus 1mg, Oral tablet

Grapefruit juice

· Severity: Major

· Notes for Consumers: Do not drink grapefruit juice or eat grapefruit or grapefruit-containing foods while taking sirolimus. Side effects from Sirolimus may get worse. Contact your care team immediately if you experience any new or unusual side effects.

· Notes for Professionals: Advise patients to avoid grapefruit and grapefruit juice during sirolimus treatment due to the risk of increased sirolimus exposure and adverse reactions. Sirolimus is a CYP3A and P-gp substrate and grapefruit juice is a strong CYP3A and P-gp inhibitor.

Sirolimus 1mg, Oral tablet

High Fat Foods

· Severity: Major

· Notes for Consumers: Sirolimus may be taken with or without food, but it is critical that you always take sirolimus consistently with or without food to maintain consistent blood levels of this drug. Avoid grapefruit while taking Sirolimus as grapefruits or grapefruit juice can increase sirolimus concentrations, causing side effects.

· Notes for Professionals: Food may affect the exposure to sirolimus. As compared with the fasted state, administration of sirolimus oral solution with a high-fat meal decreased the peak blood concentration of sirolimus by 34%, increased the Tmax 3.5-fold, and increased the AUC by 35%. As compared with the fasted state, administration of sirolimus tablets with a high-fat meal increased the peak blood concentration of sirolimus by 65%, increased the Tmax by 32%, and increased the AUC by 23%. To minimize variability, sirolimus should be taken consistently with or without food.

<b>DISCLAIMER:</b><em> This drug information content is provided for informational purposes only and is not intended to be a substitute for professional medical advice, diagnosis, or treatment. Patients should always consult their physician with any questions regarding a medical condition and to obtain medical advice and treatment. Drug information is sourced from GSDD (Gold Standard Drug Database ) provided by Elsevier.</em>