Epirubicin Injection is an anthracycline topoisomerase II inhibitor indicated as a component of adjuvant therapy in patients with evidence of axillary node tumor involvement following resection of primary breast cancer.
Epirubicin Hydrochloride, an anthracycline with cytotoxic properties. It inhibits DNA and RNA synthesis by steric obstruction after intercalating between DNA base pairs that triggers DNA cleavage by topoisomerase II. It also inhibits DNA helicase and generates cytotoxic free radicals.
Distribution: Following IV administration, Epirubicin is rapidly and widely distributed into the tissues. Binding of Epirubicin to plasma proteins, predominantly albumin, is about 77% and is not affected by drug concentration.
Metabolism: Epirubicin is extensively and rapidly metabolized by the liver and is also metabolized by other organs and cells, including red blood cells.
Excretion: Epirubicin and its major metabolites are eliminated through biliary excretion and, to a lesser extent, by urinary excretion. Terminal elimination half-life is 30-40 hrs.
Acute leukaemias; Lymphoma; Multiple myeloma; Solid tumours: As a single agent: 60-90 mg/m2 3-4 wkly. Max (total cumulative dose): 0.9-1 g/m2. Palliative care: 12.5-25 mg/m2 once wkly. Adjuvant treatment in axillary-node positive breast cancer: Recommended starting doses: 100-120 mg/m2 as a single dose on day 1 or as 2 divided doses on days 1 and 8 of each 28-day cycle. Repeat for 6 cycles. Intravesical Local treatment of bladder carcinoma: As 0.1% soln: 50 mg/wk for 8 wk; reduce dose if chemical cystitis develops. For carcinoma in-situ: 80 mg in 50 mL wkly. For prevention of recurrence in patients who have undergone transurethral resection: 50 mg/wk for 4 wk, followed by 50 mg/mth for 11 mth; retain soln in the bladder for 1 hr during each administration.
Cardioactive Compounds: Concomitant use of Epirubicin with other cardioactive compounds that could cause heart failure (e.g., calcium channel blockers), requires close monitoring of cardiac function throughout treatment.
Cimetidine: Cimetidine increases the exposure to Epirubicin. Cimetidine should be stopped during treatment with Epirubicin.
Other Cytotoxic Drugs: Epirubicin used in combination with other cytotoxic drugs may show on treatment additive toxicity, especially hematologic and gastrointestinal effects.
Paclitaxel: The administration of Epirubicin immediately prior to or after Paclitaxel increased the systemic exposure of Epirubicin, Epirubicinol and 7-deoxydoxorubicin aglycone.
Docetaxel: The administration of Epirubicin immediately prior to or after Docetaxel did not have an effect on the systemic exposure of Epirubicin, but increased the systemic exposure of Epirubicinol and 7-deoxydoxorubicin aglycone.
Radiation Therapy: Administration of Epirubicin after previous radiation therapy may induce an inflammatory recall reaction at the site of the irradiation.
Hepatic Function: Epirubicin is extensively metabolized by the liver. Changes in hepatic function induced by concomitant therapies may affect Epirubicin metabolism, pharmacokinetics, therapeutic efficacy, and/or toxicity.
Cardiac impairment, severe or recent Ml; previous full cumulative doses of anthracyclines. Hypersensitivity; severe hepatic dysfunction. Not for intravesical use where invasive tumours have penetrated the bladder wall; urinary infections, bladder inflammation or catheterisation problems. Pregnancy, lactation. Previous extensive radiotherapy, bone infiltration by tumour, severe renal and hepatic dysfunction. May cause tumor lysis syndrome or radiation recall. Elderly women >70 yr. CV disease, hypertensive cardiomyopathy; monitor hematological and cardiac function regularly. Extravasation during IV admin may result in severe local tissue necrosis. Do not give via IM/SC routes as extravasation can lead to severe local necrosis.
In early breast cancer, acute adverse events occurring in ?10% of patients are leucopenia, neutropenia, anemia, thrombocytopenia, amenhorrhea, lethargy, nausea/vomiting, mucositis, diarrhea, infection, conjunctivitis/keratitis, alopecia, local toxicity and rash/itch. Long term adverse events occurring at a frequency of 1-2% are asymptomatic drops in LVEF and CHF and secondary leukemia.
Discontinue nursing prior to taking Epirubicin. Not known if excreted in breast milk.
If an overdose occurs, supportive treatment should be provided (including antibiotic therapy, blood and platelet transfusions, colony-stimulating factors, and intensive care as needed) until the recovery of toxicities. Delayed CHF has been observed months after anthracycline administration. Patients should be observed carefully over time for signs of CHF and provided with appropriate supportive therapy.
Store in refrigerator or at 2-8°C. Do not freeze. Protect from light and keep out of the reach of children.
.png&w=384&q=75)