Epirubicin is used in the treatment of various cancers, including:

• Breast cancer: Adjuvant therapy for early-stage breast cancer and metastatic breast cancer.
• Ovarian cancer: In combination with other chemotherapy agents for metastatic ovarian cancer.
• Lung cancer: Small cell lung cancer in combination with other agents.
• Bladder cancer: For transitional cell carcinoma of the bladder.
• Gastric cancer: Used in combination therapy for advanced gastric cancer.

 

1. Dosage Forms

• Injection: Available as a sterile, clear red solution in vials.
  • Strengths: 2 mg/mL and 10 mg/5 mL.

 

2. Pharmacokinetics

• Absorption: Epirubicin is not absorbed orally; therefore, it is given intravenously.
• Distribution: It is widely distributed in tissues, especially in the liver, heart, and lungs. It crosses the blood-brain barrier to some extent and is minimally bound to plasma proteins.
• Metabolism: Epirubicin is extensively metabolized in the liver. The metabolites include aglycone forms that contribute to its anticancer activity.
• Elimination: Epirubicin is eliminated primarily through the liver (bile), with only small amounts excreted in the urine. The drug has a half-life of approximately 30–40 hours.

 

3. Mechanism of Action

Epirubicin is a chemotherapy drug that interferes with DNA replication and RNA transcription. It works by inhibiting the topoisomerase II enzyme, which is essential for DNA unwinding during cell division. This leads to DNA damage, cell cycle arrest, and cell death, particularly in rapidly dividing cancer cells.

 

 

4. Dosage and Administration

• Dosage for Breast Cancer (Adjuvant):
  • 60–90 mg/m² IV, administered every 21 days for 4–6 cycles.
• Dosage for Breast Cancer (Metastatic):
  • 60–120 mg/m² IV, administered every 21–28 days, depending on the patient’s response and tolerance.
• Dosage for Ovarian Cancer (Metastatic):
  • 60 mg/m² IV in combination with other chemotherapy agents.
• Dosage for Bladder Cancer (Metastatic):
  • 50–100 mg/m² IV every 3–4 weeks.

Note: The exact dosage and schedule may vary based on the cancer type, patient condition, and the use of combination therapies. Always refer to a specific oncologist’s recommendation for individual patient treatment.

 

 

5. Administration

• Route: Intravenous (IV) administration. Epirubicin should be infused slowly over 30 minutes to 1 hour.
• Preparation: Epirubicin must be diluted before administration. The solution should be inspected for any particulate matter or discoloration before use.
• Handling: Epirubicin is a cytotoxic agent, so proper handling precautions should be followed, including the use of gloves and protective clothing. Dispose of waste materials properly.

 

6. Contraindications

• Hypersensitivity: Known hypersensitivity to epirubicin or other anthracyclines.
• Severe Myelosuppression: Epirubicin is contraindicated in patients with severe bone marrow suppression (e.g., neutrophil count < 1000 cells/mm³).
• Severe Hepatic Impairment: In patients with severe liver dysfunction (bilirubin > 3 mg/dL).
• Cardiac Dysfunction: Patients with a history of severe heart disease, including those with a decreased left ventricular ejection fraction (LVEF), are generally not candidates for epirubicin therapy.

 

7. Warnings and Precautions

• Cardiotoxicity: Epirubicin can cause dose-dependent cardiotoxicity, leading to congestive heart failure (CHF). Patients should undergo regular cardiac monitoring.
• Bone Marrow Suppression: Myelosuppression, including neutropenia, thrombocytopenia, and anemia, is common. Complete blood count (CBC) monitoring is required.
• Secondary Malignancies: The use of epirubicin is associated with an increased risk of secondary cancers, including leukemia, due to its mutagenic properties.
• Extravasation Risk: Extravasation (leakage of the drug from the vein into surrounding tissues) may cause severe tissue necrosis. Immediate intervention is required if extravasation occurs.

 

8. Adverse Effects

• Common Side Effects:
  • Hematologic: Neutropenia, thrombocytopenia, anemia.
  • Gastrointestinal: Nausea, vomiting, stomatitis, diarrhea.
  • Cardiovascular: Heart failure, arrhythmias, and cardiotoxicity.
  • Hair Loss: Alopecia (hair loss) is a common and reversible side effect.
  • Skin: Redness or irritation at the injection site, skin discoloration.
  • Other: Fatigue, fever, and mucositis.
• Serious Adverse Effects:
  • Cardiotoxicity (including congestive heart failure)
  • Severe myelosuppression (requiring dose adjustments)
  • Severe allergic reactions (e.g., anaphylaxis)

 

9. Drug Interactions

• Other Chemotherapy Agents: Combining epirubicin with other drugs that cause myelosuppression or cardiotoxicity (e.g., cyclophosphamide) may increase the risk of side effects.
• CYP3A4 Inhibitors/Inducers: Epirubicin is metabolized by the CYP3A4 enzyme. Strong inhibitors (e.g., ketoconazole) may increase epirubicin levels, while inducers (e.g., rifampin) may decrease its effectiveness.
• Live Vaccines: Patients undergoing epirubicin treatment should avoid live vaccines due to immunosuppression.

 

10. Monitoring

• Cardiac Function: Regular monitoring of left ventricular ejection fraction (LVEF) and cardiac function is required, particularly in patients receiving cumulative doses > 300 mg/m².
• Hematologic Status: Regular blood counts to monitor for neutropenia, thrombocytopenia, and anemia.
• Liver Function: Liver enzyme tests should be monitored in patients with liver impairment.

 

11. Pregnancy and Lactation

• Pregnancy: Epirubicin is classified as a Category D drug (positive evidence of risk). It can cause fetal harm, and its use should be avoided during pregnancy unless the benefits outweigh the risks.
• Lactation: Epirubicin is excreted in breast milk. It is recommended that breastfeeding be discontinued during treatment with epirubicin.

 

12. Overdose

Symptoms of overdose may include severe myelosuppression, nausea, vomiting, and cardiotoxicity. Immediate medical attention is required. Treatment of overdose typically involves supportive care and management of complications.

 

 

13. Storage

• Storage Conditions: Store at 2°C to 8°C (36°F to 46°F). Do not freeze.