Home Drug Guide Everolimus

Drug Guide

Generic Name

Everolimus

Brand Names Zortress, Afinitor, Afinitor Disperz

Classification

Therapeutic: Antineoplastic agent, Immunosuppressant

Pharmacological: mTOR inhibitor

FDA Approved Indications

  • Renal cell carcinoma, advanced
  • Neuroendocrine tumors of gastrointestinal or lung origin, progressive, metastatic
  • Breast cancer, hormone receptor-positive, HER2-negative, advanced ( Afinitor)
  • Renal transplantation as prophylaxis against rejection (Zortress)
  • Subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis complex (Afinitor Disperz)

Mechanism of Action

Everolimus inhibits mTOR (mammalian target of rapamycin), a key regulatory kinase involved in cell proliferation, growth, and angiogenesis. It binds to FKBP-12, and the complex inhibits mTORC1, leading to cell cycle arrest and decreased angiogenesis.

Dosage and Administration

Adult: Dosing varies based on indication; typically, 5-10 mg orally once daily for cancer. In transplant patients, 0.75 mg twice daily, adjusted as needed.

Pediatric: Dosing depends on the condition; for SEGA, 0.75 mg/m² twice daily, with adjustments based on blood levels.

Geriatric: Start at lower doses due to increased sensitivity and comorbidities, monitor closely.

Renal Impairment: Adjust dose based on response; no specific guidelines, but careful monitoring recommended.

Hepatic Impairment: Use with caution; no specific dose adjustments established.

Pharmacokinetics

Absorption: Well-absorbed orally, with a bioavailability of approximately 30%.

Distribution: Widely distributed; high protein binding (~74%).

Metabolism: Primarily metabolized by CYP3A4 and CYP2C8 enzymes.

Excretion: Excreted mainly via feces (80%), with some urinary excretion.

Half Life: Approximately 30 hours.

Contraindications

  • Hypersensitivity to everolimus, sirolimus, or any component of the formulation.

Precautions

  • Use caution in patients with impaired liver function, infections, or bleeding disorders. Monitor blood counts and liver function regularly. Pregnancy category D; effective contraception required during treatment and for some time after discontinuation. Risk of serious infections and non-infectious pneumonitis.

Adverse Reactions - Common

  • Stomatitis (Very common)
  • Infections (viral, bacterial, fungal) (Common)
  • Fatigue (Common)
  • Peripheral edema (Common)

Adverse Reactions - Serious

  • Non-infectious pneumonitis (Less common but serious)
  • Hepatotoxicity (Less common)
  • Thrombocytopenia, leukopenia (Less common)
  • Gastrointestinal perforation (Rare)

Drug-Drug Interactions

  • CYP3A4 inhibitors (ketoconazole, clarithromycin), CYP3A4 inducers (rifampin, carbamazepine), live vaccines.

Drug-Food Interactions

  • Grapefruit juice may increase blood levels.

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor for signs of infection, blood counts, liver function, lung symptoms, and wound healing.

Diagnoses:

  • Risk for infection
  • Impaired tissue integrity
  • Risk for bleeding

Implementation: Administer as scheduled; monitor therapeutic levels if applicable; counsel on signs of infection and other adverse effects.

Evaluation: Assess efficacy (tumor response, graft function), monitor for adverse reactions, adjust dose accordingly.

Patient/Family Teaching

  • Report signs of infection, bleeding, or lung problems.
  • Avoid grapefruit and grapefruit juice.
  • Keep regular follow-up appointments for blood tests and monitoring.
  • Do not stop medication abruptly.

Special Considerations

Black Box Warnings:

  • Increased risk of infections leading to serious or fatal infections.
  • Liver failure, renal failure, or non-infectious pneumonitis.

Genetic Factors: Pharmacogenetic variations in CYP3A4 may affect drug levels.

Lab Test Interference: May affect blood glucose, lipid levels, and liver function tests.

Overdose Management

Signs/Symptoms: Severe mucositis, infections, hepatotoxicity, hematologic abnormalities.

Treatment: Supportive care, monitor vital signs, and laboratory parameters; specific antidote not available.

Storage and Handling

Storage: Store at 20°C to 25°C (68°F to 77°F). Keep in original container.

Stability: Stable for the duration of the labeled shelf life when stored properly.

🛡️ 5 Critical Medication Safety Tips for Nurses

1

Triple-Check High-Risk Medications

Always have another nurse verify insulin, heparin, warfarin, and chemotherapy drugs. These "high-alert" medications cause the most serious errors. Check concentration, dose calculation, and pump settings twice.

2

Know Look-Alike, Sound-Alike Drugs

Common mix-ups: hydromorphone/morphine, Celebrex/Celexa, Zyprexa/Zyrtec. Always use BOTH generic and brand names, read labels twice, and use barcode scanning when available. One wrong letter can be fatal.

3

Assess Before AND After Giving Meds

Check vitals before cardiac meds, pain levels before analgesics, and blood glucose before insulin. Always reassess within 30 minutes to evaluate effectiveness and watch for adverse reactions.

4

Watch for Drug Interactions

Common dangerous combinations: warfarin + aspirin (bleeding), ACE inhibitors + potassium (hyperkalemia), digoxin + diuretics (toxicity). Always check drug interactions before administering new medications.

5

Educate Your Patients

Teach patients medication names, purposes, major side effects, and what to report. Informed patients catch errors and improve compliance. Always encourage questions - an educated patient is a safer patient.

⚡ Remember: When in doubt, don't give it out! It's always safer to double-check than regret later.

⚠️ Medical Disclaimer

This drug guide is for educational purposes only and is NOT intended for clinical use. Always consult current prescribing information, healthcare providers, and institutional protocols before administering any medication. Do not use this information for patient care decisions.