Everolimus

Generic Name: everolimus

Kinase Inhibitor [EPC]Over-the-Counter (OTC)

Brand Names:

Everolimus

Everolimus is a macrolide immunosuppressant available as tablets in 0.25 mg, 0.5 mg, 0.75 mg, and 1 mg strengths for organ rejection prophylaxis.

Overview

Everolimus is a macrolide immunosuppressant available as tablets in 0.25 mg, 0.5 mg, 0.75 mg, and 1 mg strengths for organ rejection prophylaxis.

Uses

Indicated for organ rejection prophylaxis in adult transplant recipients. Use in kidney transplant at low-moderate immunologic risk and in liver transplant 30 or more days post-transplant.

Dosage

Kidney transplant: Initial dose 0.75 mg orally twice daily. Liver transplant: Initial dose 1 mg orally twice daily, starting 30 or more days post-transplant. Adjust dose based on trough concentrations (target 3-8 ng/mL). Reduce initial dose for hepatic impairment.

Side Effects

Common reactions in kidney transplant (20% or greater): peripheral edema, constipation, hypertension, nausea, anemia, urinary tract infection, hyperlipidemia. In liver transplant (greater than 10%): diarrhea, headache, peripheral edema, hypertension, nausea, pyrexia.

Interactions

Strong CYP3A4 inhibitors (ketoconazole, cyclosporine, erythromycin) and inducers (rifampin) affect levels. Grapefruit juice should be avoided. Cannabidiol may increase everolimus levels.

Warnings

WARNING: MALIGNANCIES and SERIOUS INFECTIONS; KIDNEY GRAFT THROMBOSIS; NEPHROTOXICITY; and MORTALITY IN HEART TRANSPLANTATION. Only experienced physicians should prescribe. Increased risk of infections, malignancies, kidney graft thrombosis, nephrotoxicity with cyclosporine. Contraindicated with hypersensitivity to everolimus or sirolimus.

Pregnancy

Based on animal studies and mechanism of action, everolimus can cause fetal harm. Advise females of reproductive potential to use effective contraception during and 8 weeks after treatment. Not recommended during breastfeeding.

Frequently Asked Questions

What is Everolimus used for?

Indicated for organ rejection prophylaxis in adult transplant recipients. Use in kidney transplant at low-moderate immunologic risk and in liver transplant 30 or more days post-transplant.

What are the side effects of Everolimus?

Common reactions in kidney transplant (20% or greater): peripheral edema, constipation, hypertension, nausea, anemia, urinary tract infection, hyperlipidemia. In liver transplant (greater than 10%): diarrhea, headache, peripheral edema, hypertension, nausea, pyrexia.

Can I take Everolimus during pregnancy?

Based on animal studies and mechanism of action, everolimus can cause fetal harm. Advise females of reproductive potential to use effective contraception during and 8 weeks after treatment. Not recommended during breastfeeding.

What are the important warnings for Everolimus?

WARNING: MALIGNANCIES and SERIOUS INFECTIONS; KIDNEY GRAFT THROMBOSIS; NEPHROTOXICITY; and MORTALITY IN HEART TRANSPLANTATION. Only experienced physicians should prescribe. Increased risk of infections, malignancies, kidney graft thrombosis, nephrotoxicity with cyclosporine. Contraindicated with hypersensitivity to everolimus or sirolimus.

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Medical Disclaimer

This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.