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4'-Epiadriamycin

4'-Epiadriamycin - General Information

An anthracycline which is the 4'

 

Pharmacology of 4'-Epiadriamycin

4'-Epiadriamycin is an antineoplastic in the anthracycline class. General properties of drugs in this class include: interaction with DNA in a variety of different ways including intercalation (squeezing between the base pairs), DNA strand breakage and inhibition with the enzyme topoisomerase II. Most of these compounds have been isolated from natural sources and antibiotics. However, they lack the specificity of the antimicrobial antibiotics and thus produce significant toxicity. The anthracyclines are among the most important antitumor drugs available. Doxorubicin is widely used for the treatment of several solid tumors while daunorubicin and idarubicin are used exclusively for the treatment of leukemia. 4'-Epiadriamycin may also inhibit polymerase activity, affect regulation of gene expression, and produce free radical damage to DNA. 4'-Epiadriamycin possesses an antitumor effect against a wide spectrum of tumors, either grafted or spontaneous. The anthracyclines are cell cycle-nonspecific.

 

4'-Epiadriamycin for patients

Patients should be informed of the expected adverse effects of epirubicin, including gastrointestinal symptoms (nausea, vomiting, diarrhea, and stomatitis) and potential neutropenic complications. Patients should consult their physician if vomiting, dehydration, fever, evidence of infection, symptoms of CHF, or injection-site pain occurs following therapy with ELLENCE. Patients should be informed that they will almost certainly develop alopecia. Patients should be advised that their urine may appear red for 1 to 2 days after administration of ELLENCE and that they should not be alarmed. Patients should understand that there is a risk of irreversible myocardial damage associated with treatment with ELLENCE, as well as a risk of treatment-related leukemia. Because epirubicin may induce chromosomal damage in sperm, men undergoing treatment with ELLENCE should use effective contraceptive methods. Women treated with ELLENCE may develop irreversible amenorrhea, or premature menopause.

4'-Epiadriamycin Interactions

ELLENCE when used in combination with other cytotoxic drugs may show on-treatment additive toxicity, especially hematologic and gastrointestinal effects.

Concomitant use of ELLENCE with other cardioactive compounds that could cause heart failure (e.g., calcium channel blockers), requires close monitoring of cardiac function throughout treatment.

There are few data regarding the coadministration of radiation therapy and epirubicin. In adjuvant trials of epirubicin-containing CEF-120 or FEC-100 chemotherapies, breast irradiation was delayed until after chemotherapy was completed. This practice resulted in no apparent increase in local breast cancer recurrence relative to published accounts in the literature. A small number of patients received epirubicin-based chemotherapy concomitantly with radiation therapy but had chemotherapy interrupted in order to avoid potential overlapping toxicities. It is likely that use of epirubicin with radiotherapy may sensitize tissues to the cytotoxic actions of irradiation. Administration of ELLENCE after previous radiation therapy may induce an inflammatory recall reaction at the site of the irradiation.

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.

Cimetidine increased the AUC of epirubicin by 50%. Cimetidine treatment should be stopped during treatment with ELLENCE.

Drug-Laboratory Test Interactions

There are no known interactions between ELLENCE and laboratory tests.

 

4'-Epiadriamycin Contraindications

Patients should not be treated with ELLENCE Injection if they have any of the following conditions: baseline neutrophil count < 1500 cells/mm3; severe myocardial insufficiency, recent myocardial infarction, severe arrhythmias; previous treatment with anthracyclines up to the maximum cumulative dose; hypersensitivity to epirubicin, other anthracyclines, or anthracenediones; or severe hepatic dysfunction.

 

Additional information about 4'-Epiadriamycin

4'-Epiadriamycin Indication: For use as a component of adjuvant therapy in patients with evidence of axillary node tumor involvement following resection of primary breast cancer
Mechanism Of Action: 4'-Epiadriamycin has antimitotic and cytotoxic activity. It inhibits nucleic acid (DNA and RNA) and protein synthesis through a number of proposed mechanisms of action: 4'-Epiadriamycin forms complexes with DNA by intercalation between base pairs, and it inhibits topoisomerase II activity by stabilizing the DNA-topoisomerase II complex, preventing the religation portion of the ligation-religation reaction that topoisomerase II catalyzes. It also interferes with DNA replication and transcription by inhibiting DNA helicase activity.
Drug Interactions: Cimetidine Cimetidine can increase epirubicin levels
Food Interactions: Liberal fluid intake to increase urine output and help the excretion of uric acid.
Generic Name: Epirubicin
Synonyms: Not Available
Drug Category: Antineoplastic Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Epirubicin: 4'-Epiadriamycin; 4'-Epidoxorubicin; Ellence; Epi-Dx; Epiadriamycin; Epidoxorubicin; Epirubicina [Inn-Spanish]; Epirubicina [Spanish]; Epirubicine [French]; Epirubicine [Inn-French]; Epirubicinum [Inn-Latin]; Epirubicinum [Latin]; IMI 28; Pharmorubicin Pfs; Pidorubicina [Inn-Spanish]; Pidorubicine [Inn-French]; Pidorubicinum [Inn-Latin]; Ridorubicin.
Absorption: 100%
Toxicity (Overdose): bone marrow aplasia, grade 4 mucositis, and gastrointestinal bleeding
Protein Binding: 77%
Biotransformation: Hepatic
Half Life: Half-lives for the alpha, beta, and gamma phases of about 3 minutes, 2.5 hours and 33 hours, respectively
Dosage Forms of 4'-Epiadriamycin: Solution Intravenous
Chemical IUPAC Name: (7S,9S)-7-[(2R,4S,5R,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-8,10-dihydro-7H-tetracene-5,12-dione
Chemical Formula: C27H29NO11
Epirubicin on Wikipedia: http://en.wikipedia.org/wiki/Epirubicin
Organisms Affected: Humans and other mammals