Episindan
Episindan Uses, Dosage, Side Effects, Food Interaction and all others data.
Episindan, 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.
Episindan 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. Episindan may also inhibit polymerase activity, affect regulation of gene expression, and produce free radical damage to DNA. Episindan possesses an antitumor effect against a wide spectrum of tumors, either grafted or spontaneous. The anthracyclines are cell cycle-nonspecific.
| Trade Name | Episindan |
| Availability | Prescription only |
| Generic | Epirubicin |
| Epirubicin Other Names | 4'-Epiadriamycin, Epiadriamycin, Epirubicin, Epirubicina, Epirubicine, Epirubicinum, Pidorubicina, Pidorubicine, Pidorubicinum |
| Related Drugs | tamoxifen, letrozole, paclitaxel, Femara, Herceptin, Soltamox |
| Weight | 2mg/ml, 10mg/ml, 50mg/ml |
| Type | Iv Injection, Injection Powder |
| Formula | C27H29NO11 |
| Weight | Average: 543.5193 Monoisotopic: 543.174060775 |
| Protein binding | 77% |
| Groups | Approved |
| Therapeutic Class | Cytotoxic Chemotherapy |
| Manufacturer | Actavis (bots Pvt, Limited), Actavis |
| Available Country | Bangladesh, Indonesia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Episindan Injection is an anthracycline topoisomerase II inhibitor used as a component of adjuvant therapy in patients with evidence of axillary node tumor involvement following resection of primary breast cancer
Episindan is also used to associated treatment for these conditions: Breast Cancer, Breast Cancer Stage II, Breast Cancer Stage III, Colorectal Cancers, Hormone Refractory Prostate Cancer, Non-Small Cell Lung Carcinoma (NSCLC), Ovarian Cancer, Papillary transitional cell carcinoma of bladder, Recurrent Superficial Bladder Cancer, Small Cell Lung Cancer (SCLC), Soft Tissue Sarcoma (STS), Stomach Tumor, Carcinoma in situ of urinary bladder
How Episindan works
Episindan has antimitotic and cytotoxic activity. It inhibits nucleic acid (DNA and RNA) and protein synthesis through a number of proposed mechanisms of action: Episindan 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.
Dosage
Episindan dosage
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.
Side Effects
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.
Toxicity
bone marrow aplasia, grade 4 mucositis, and gastrointestinal bleeding
Precaution
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
Interaction
Paclitaxel and other anthracyclines. Cimetidine, heparin. Antineoplastic drugs, cardiotoxic drugs, radiation, hepatoactive drugs.
Food Interaction
- Drink plenty of fluids. Increased fluid intake increases urine output and the excretion of uric acid.
Episindan Alcohol interaction
[Moderate]
The concomitant or sequential use of epirubicin with agents known to induce hepatotoxicity may potentiate the risk of liver injury.
Episindan undergoes elimination through the hepatobiliary system.
Caution and clinical and laboratory monitoring for signs of liver injury are advisable before, during, or after use of epirubicin with other agents that are potentially hepatotoxic.
Episindan Drug Interaction
Moderate: amoxicillin / clavulanate, amoxicillin / clavulanate, ethanol, ethanol, acetaminophen, acetaminophen, tramadol, tramadol, valproic acid, valproic acidUnknown: paclitaxel protein-bound, paclitaxel protein-bound, aspirin, aspirin, amoxicillin, amoxicillin, aprepitant, aprepitant, esomeprazole, esomeprazole
Episindan Disease Interaction
Major: heart disease/toxicity, liver disease, neutropeniaModerate: myelosuppression/infection, renal impairment
Volume of Distribution
- 21 ± 2 L/kg [60 mg/m2 Dose]
- 27 ± 11 L/kg [75 mg/m2 Dose]
- 23 ± 7 L/kg [120 mg/m2 Dose]
- 21 ± 7 L/kg [150 mg/m2 Dose]
Elimination Route
100%
Half Life
Half-lives for the alpha, beta, and gamma phases of about 3 minutes, 2.5 hours and 33 hours, respectively
Clearance
- 65 +/- 8 L/hour [Patients1 with Solid Tumors Receiving Intravenous Episindan 60 mg/m2]
- 83 +/- 14 L/hour [Patients1 with Solid Tumors Receiving Intravenous Episindan 75 mg/m2]
- 65 +/- 13 L/hour [Patients1 with Solid Tumors Receiving Intravenous Episindan 120 mg/m2]
- 69 +/- 13 L/hour [Patients1 with Solid Tumors Receiving Intravenous Episindan 150 mg/m2]
Elimination Route
Episindan and its major metabolites are eliminated through biliary excretion and, to a lesser extent, by urinary excretion.
Pregnancy & Breastfeeding use
Discontinue nursing prior to taking Episindan. Not known if excreted in breast milk
Contraindication
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.
Innovators Monograph
You find simplified version here Episindan
Episindan contains Epirubicin see full prescribing information from innovator Episindan Monograph, Episindan MSDS, Episindan FDA label
FAQ
What is Episindan used for?
Episindan is an anthracycline drug used for chemotherapy. Episindan is used in combination with other medications to treat breast cancer in patients who have had surgery to remove the tumor.
How safe is Episindan?
Episindan may increase your risk for developing leukemia (cancer of the white blood cells), especially when it is given in high doses or together with certain other chemotherapy medications. Episindan can cause a severe decrease in the number of blood cells in your bone marrow.
How does Episindan work?
Episindan works by slowing or stopping the growth of cancer cells in your body.
What are the common side effects of Episindan?
Common side effects of Episindan are include;
- Black, tarry stools
- bleeding, redness, or ulcers in the mouth or throat
- chest pain
- cough or hoarseness
- fever or chills
- lower back or side pain
- pain or burning in the mouth or throat
- painful or difficult urination
- sore throat
- sores, ulcers, or white spots in the mouth or on the lips
- swollen glands
- trouble breathing
- unusual bleeding or bruising
- unusual tiredness or weakness
Is Episindan safe during pregnancy?
Use is contraindicated. US FDA pregnancy category: Not assigned. Risk Summary: Based on findings from animal studies and its mechanism of action, this drug can cause fetal harm when administered to a pregnant woman.
Is Episindan safe during breastfeeding?
Use is contraindicated. Because of the potential for serious adverse reactions in the breastfed child, advise lactating women not to breastfeed during therapy and for at least 7 days after.
Can I drink alcohol with Episindan?
Frequent or heavy alcohol consumption during chemotherapy is generally a bad idea. One reason for this is that alcohol can worsen some chemotherapy side effects, such as dehydration, diarrhea, and mouth sores. Additionally, alcohol and chemotherapy drugs are both processed by the liver.
Can I drive after taking Episindan?
If you have any of these symptoms, do not drive, operate machinery, or do anything else that could be dangerous. Be careful when drinking alcohol while you are taking this medicine. If you drink alcohol, dizziness or light- headedness may be worse.
How do I take Episindan?
Episindan comes as a solution (liquid) to be injected intravenously (into a vein) by a doctor or nurse in a medical facility along with other chemotherapy medications.
How long does Episindan take to work?
It can take up to 30 minutes if you have it on its own but it might take longer if you have it with other drugs. For bladder cancer, you might have Episindan every week, for up to 8 weeks.
How long does Episindan stay in my system?
This medicine may turn your urine red for 1 or 2 days after your treatment.
How long can I take Episindan?
Chemotherapy is often given for a specific time, such as 6 months or a year.
Who should not take Episindan?
You should not use Episindan if you have an untreated or uncontrolled infection, severe liver disease, severe heart problems, or if you have recently had a heart attack. You may not be able to use Episindan if you have already been treated with a certain amount of other cancer medications. You should not use this medication if you are allergic to Episindan or similar medications.
What happens if I miss a dose?
Call your doctor for instructions if you miss an appointment for your Episindan injection.
What happen if I overdose on Episindan?
If you've taken more than the recommended amount of a drug or enough to have a harmful effect on your body's functions, you have overdosed. An overdose can lead to serious medical complications, including death.
Can Episindan affect my heart?
Episindan can cause dangerous effects on your heart that may not be reversible and could occur months to years after you receive Episindan.
Can Episindan cause fertility problems?
Episindan can stop your ovaries from working. This causes infertility, which can be temporary or permanent. It can also bring on the menopause.
Is Episindan an irritant?
Episindan should be administered only into a vein. However, it may leak into surrounding tissue causing severe irritation or damage.
