Epirubicin information from DrugsUpdate
P - Cautioned in pregnancy
L - Contraindicated in lactation
FI - Food *
LI - Lab *
Epirubicin is an anthracycline drug used for chemotherapy. It is marketed by Pfizer under the trade name Ellence in the US and Pharmorubicin or Epirubicin Ebewe elsewhere.
Similarly to other anthracyclines, epirubicin acts by intercalating DNA strands. Intercalation results in complex formation which inhibits DNA and RNA synthesis. It also triggers DNA cleavage by topoisomerase II, resulting in mechanisms that lead to cell death. Binding to cell membranes and plasma proteins may be involved in the compound's cytotoxic effects. Epirubicin also generates free radicals that cause cell and DNA damage.
Epirubicin is favoured over doxorubicin, the most popular anthracycline, in some chemotherapy regimens as it appears to cause fewer side-effects. Epirubicin has a different spatial orientation of the hydroxyl group at the 4' carbon of the sugar, which may account for its faster elimination and reduced toxicity. Epirubicin is primarily used against breast and ovarian cancer, gastric cancer, lung cancer, and lymphomas.
Pharmacodynamics
Pharmacokinetics
Epirubicin, 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 by topoisomerase II. It also inhibits DNA helicase and generates cytotoxic free radicals.
Distribution
Rapidly and extensively distributed into body tissues.
Metabolism
Hepatically metabolised
Excretion
Eliminated mainly in bile. Terminal elimination half-life: About 30-40 hours.
Epirubicin Indications / Epirubicin Uses
Information Not Available
Epirubicin Adverse Reactions / Epirubicin Side Effects
Myelosuppression; cardiotoxicity, alopoecia; mucositis; hyperpyrexia; lethargy; amenorrhoea; nausea and vomiting; diarrhoea; fever; rash, skin changes, anorexia; anaphylaxis; photosensitivity; premature menopause; skin and nail hyperpigmentation; harmless reddish appearance of urine for 1-2 days.
Precautions
Information Not Available
Special Precautions
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.
Other Drug Interactions
Paclitaxel and other anthracyclines. Cimetidine, heparin. Antineoplastic drugs, cardiotoxic drugs, radiation, hepatoactive drugs.
Other Interactions
Food Interactions
St. John's wort, alcohol, black cohosh, dong quai.
Dosage
Intravenous
Lymphoma
Adult: As a single agent: 60-90 mg/m2 every 3-4 wk. May divide dose over 2-3 days if desired. May admin as an inj over 3-5 minutes or as an infusion over up to 30 minutes. Max (total cumulative dose limit): 0.9-1 g/m2. For palliative care: 12.5-25 mg/m2 once wkly.
Hepatic impairment: Moderate liver dysfunction (serum bilirubin concentrations: 12-30 mcg/mL): Doses should be halved; severe liver impairment (serum bilirubin >30 mcg/mL): A quarter of the usual dose.
Intravenous
Multiple myeloma
Adult: As a single agent: 60-90 mg/m2 every 3-4 wk. May divide dose over 2-3 days if desired. May admin as an inj over 3-5 minutes or as an infusion over up to 30 minutes. Max (total cumulative dose limit): 0.9-1 g/m2. For palliative care: 12.5-25 mg/m2 once wkly.
Hepatic impairment: Moderate liver dysfunction (serum bilirubin concentrations: 12-30 mcg/mL): Doses should be halved; severe liver impairment (serum bilirubin >30 mcg/mL): A quarter of the usual dose.
Intravenous
Solid tumours
Adult: As a single agent: 60-90 mg/m2 every 3-4 wk. May divide dose over 2-3 days if desired. May admin as an inj over 3-5 minutes or as an infusion over up to 30 minutes. Max (total cumulative dose limit): 0.9-1 g/m2. For palliative care: 12.5-25 mg/m2 once wkly.
Hepatic impairment: Moderate liver dysfunction (serum bilirubin concentrations: 12-30 mcg/mL): Doses should be halved; severe liver impairment (serum bilirubin >30 mcg/mL): A quarter of the usual dose.
Intravenous
Acute leukaemias
Adult: As a single agent: 60-90 mg/m2 every 3-4 wk. May divide dose over 2-3 days if desired. May admin as an inj over 3-5 minutes or as an infusion over up to 30 minutes. Max (total cumulative dose limit): 0.9-1 g/m2. For palliative care: 12.5-25 mg/m2 once wkly.
Hepatic impairment: Moderate liver dysfunction (serum bilirubin concentrations: 12-30 mcg/mL): Doses should be halved; severe liver impairment (serum bilirubin >30 mcg/mL): A quarter of the usual dose.
Intravenous
Adjuvant treatment of axillary-node positive breast cancer.
Adult: Recommended starting dose: 100-120 mg/m2. Dose may be given as a single dose on day 1 or in 2 equally-divided doses on days 1 and 8 of each 28-day cycle. Repeat for 6 cycles. Lower starting doses may be considered in patients with pre-existing bone marrow depression or in the presence of neoplastic bone marrow infiltration.
Renal impairment: Dosage adjustment may be needed in severe impairment.
Hepatic impairment: Moderate liver dysfunction (serum bilirubin concentrations: 12-30 mcg/mL): Doses should be halved; severe liver impairment (serum bilirubin >30 mcg/mL): A quarter of the usual dose.
Intravesical
Local treatment of bladder carcinoma
Adult: As 0.1% solution (in normal saline or sterile water): 50 mg wkly for 8 wk; may reduce to 30 mg in 50 ml if chemical cystitis develops. For carcinoma in-situ: May increase dose to 80 mg in 50 ml wkly. For prevention of recurrence in patients who have undergone transurethral resection: 50 mg wkly for 4 wk, followed by 50 mg once a mth for 11 mth; retain solution in the bladder for 1 hr during each admin.
Hepatic impairment: Moderate liver dysfunction (serum bilirubin concentrations: 12-30 mcg/mL): Doses should be halved; severe liver impairment (serum bilirubin >30 mcg/mL): A quarter of the usual dose.
Special Populations
Patients with heavy pre-treatment, preexisting bone marrow depression, or the presence of neoplastic bone marrow infiltration: Starting dose of 75-90 mg/m2. Dosage modifications after the 1st treatment cycle: Nadir platelet counts < 50,000/mm2, ANC < 250/mm2, neutropenic fever, or grades 3 or 4 nonhaematogenic toxicity: Reduce day 1 dose in subsequent cycles to 75% of the day 1 dose in the current cycle. Day 1 chemotherapy in subsequent courses of treatment should be delayed until platelet counts are exceeding 100,000/mm3, ANC exceeding 1500/mm3, and nonhaematogenic toxicities have recovered to almost grade 1. In addition, for patients receiving divided dose (day 1 and day 8) regimen: Day 8 platelet counts 75,000-100,000/mm3 and ANC 1000-1499/mm3: dose should be 75% of the day 1 dose. Day 8 platelet counts <75,000/mm3, ANC <1000/mm3 or grade 3 or 4 nonhaematologic toxicity: Omit day 8 dose.
Food(before/after)
Information Not Available
List of Contraindications
Epirubicin and Pregnancy
Contraindicated in pregnancy.
Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Epirubicin and Lactation
Contraindicated in lactation
Epirubicin and Children
The safety and effectiveness of Epirubicin in pediatric patients have not been established in adequate and well-controlled clinical trials. Pediatric patients may be at greater risk for anthracycline-induced acute manifestations of cardiotoxicity and for chronic CHF.
Epirubicin and Geriatic
Although a lower starting dose of Epirubicin hydrochloride injection was not used in trials in elderly female patients, particular care should be taken in monitoring toxicity when Epirubicin hydrochloride injection is administered to female patients ≥ 70 years of age.
Epirubicin and Other Contraindications
Cardiac impairment, severe or recent MI; 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.
Storage
Intravenous
Refrigerate at 2-8°C.
Intravesical
Refrigerate at 2-8°C.
Lab interference
Intravenous
Refrigerate at 2-8°C.
Intravesical
Refrigerate at 2-8°C.
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