Uses of Episindan

Episindan is an anti-cancer drug belonging to the Anthracycline group, with the main active ingredient being Epirubicin. Episindan is given by intravenous infusion or by injection into the bladder. The following article provides you with information on how to use and note when using Episindan.

Episindan contains the active ingredient Epirubicin hydrochloride. The drug is prepared in the form of lyophilized powder for injection with the content of Episindan 10mg and Episindan 50mg.
Epirubicin is the 4'-epime of doxorubicin, a semi-synthetic derivative of daunorubicin. Epirubicin is an anthracycline antineoplastic agent with cytotoxic effects similar to Daunorubicin and Doxorubicin.
The mechanism of action of Epirubicin is to form complexes with DNA by interleaving between base pairs, which leads to inhibition of DNA-dependent DNA and RNA synthesis. Besides, protein synthesis is also inhibited. The intercalation of Epirubicin between base pairs activates topoisomerase, resulting in DNA cleavage and cell death. DNA helicase is also inhibited so that replication and transcription are prevented. The drug also generates free radicals that are toxic to cells.
Animal studies and in vitro tests show that the mechanism of action and anti-tumor effects of Doxorubicin and Epirubicin are similar, however, Epirubicin has a better therapeutic index, less cardiac and hematological toxicity when using the equivalent molar dose. To induce a comparable degree of myelosuppression, the dose of epirubicin may be approximately 20% higher than that of doxorubicin. Because Epirubicin and Doxorubicin have the same mechanism of action, both drugs have a similar spectrum of action against many solid tumors and blood cancers. In vitro showed complete cross-resistance between these two anthracyclines. Epirubicin is commonly used to treat breast and bladder surface cancers. Epirubicin is used in combination with other antineoplastic agents to treat acute leukemia, multiple myeloma, lymphoma, gastric cancer, and Wilm's cancer.
Episindan is indicated for treatment in the following cases:
Breast carcinoma. Advanced ovarian cancer. Stomach cancer . Small cell lung cancer. In addition, Episindan is also used to treat: Transitional cell carcinoma in bladder cancer, carcinoma in situ in bladder cancer, or to prevent recurrence of bladder carcinoma after surgery. urethral resection.
Episindan is contraindicated in patients with hypersensitivity to Epirubicin hydrochloride or any of its ingredients and in nursing women.
When injected/intravenously, contraindicated in: Patients with chronic bone marrow failure or bone marrow failure due to chemotherapy or radiation therapy, severe liver failure, who have been treated with the maximum cumulative dose of Epirubicin and/or other antineoplastic agents, patients with existing or history of heart failure, severe myocardial failure, myocardial infarction, unstable angina, and acute infection.
When used for injection in the bladder, Episindan is contraindicated for: People with urinary tract infections, cystitis, invasive tumors that are penetrating the bladder.

Episindan is administered by injection/intravenous or intravesical. Epirubicin lyophilized powder should be mixed with 0.9% NaCl solution or water for injection before use. The solution should be used within 1 hour after reconstitution. Patients should not drink any fluids for 12 hours before the infusion. During the infusion, the patient should not turn around and avoid urinating after the infusion is complete. 2.1 Intravenous Injection/Infusion Epirubicin should be given through a free-flowing saline solution, after verifying that the needle is in place. Extravasation should be avoided.
Usual dose: When using Epirubicin alone, the recommended dose in adults is 60-90 mg/m2, the interval between two consecutive doses is 21 days, depending on the patient's blood and spinal cord condition. If signs of toxicity such as fever with neutropenia and thrombocytopenia are observed (which may persist until day 21), the dose should be adjusted or the next dose discontinued.
Lung cancer: Epirubicin is used alone in high doses in the treatment of lung cancer.
Small cell lung cancer (previously failed treatment): 120mg/m2 on the first day, repeat after 3 weeks. When taking high doses, Epirubicin should be given as a rapid intravenous infusion over 3-5 minutes or a slow infusion over 30 minutes.
Breast cancer: When adjuvant treatment of early breast cancer, the usual dose is 100mg/m2 (single dose on day 1) - 120mg/m2 (divided dose on days 1 and 8), repeated every 3 -4 weeks, should be combined with infusion of cyclophosphamide and 5-fluorouracil and oral tamoxifen. Lower doses (common dose: 60-75 mg/m2, high dose 105-120 mg/m2) are indicated in patients with impaired marrow function due to chemotherapy or radiation therapy, age, or cancer. bone marrow letter. The dosage in each cycle should be divided into 2-3 days.
Usual Epirubicin Dosage Table (mg/m2)*:

The dose is administered on day 1 or day 1, 2, 3 then repeated after 21 days.
When used in combination:
When using Episindan in combination with other agents, the drug should be reduced in dose, the usual dose is as shown in the table above.
Patients with liver failure: The dose of Episindan should be adjusted according to the bilirubin concentration as follows:

Patients with renal impairment: No dose adjustment of Episindan is required in this patient.
2.2 Intravestical Injection Episindan should not be injected into the bladder to treat invasive tumors when the tumor has penetrated the bladder wall. Dosage of Episindan for the treatment of bladder carcinoma is as follows: 50mg/50ml drip every 8 weeks (diluted with sterile saline or water for injection). If toxicity occurs, reduce dose to 30mg/50ml. Carcinoma in situ : Over 80mg/ 50ml . Prophylaxis: 50ng/50ml every 4 weeks, then drip at the same dose every 11 months. Instructions for dilution of intravesical solution:

Usually: Timely supportive measures are needed, especially when taking high doses of Episindan. Patients should be informed of drug toxicity prior to use. When taking high doses of Episindan will increase the risk of stomatitis, mucositis. Cardiovascular toxicity: Acute toxicity: Tachycardia or ECG abnormalities such as nonspecific ST-T wave changes, ventricular tachycardia, bradycardia, atrioventricular block. Late onset toxicity, usually progressive at the end of the course of treatment or within 2 -3 months after the end of treatment: decreased LVEF or symptoms of congestive heart failure. Congestive heart failure may develop several weeks after stopping treatment with Epirubicin and may not respond to any specific treatment. Caution should be exercised when epirubicin is combined with other cardiotoxic drugs. An electrocardiogram should be performed before and after the end of treatment. Discontinue use of Episindan at the first signs of impaired heart function. Patients with hepatic impairment: Episindan should not be used in patients with severe hepatic impairment, reduce the dose in patients with mild and moderate hepatic impairment. Pregnant women: Epirubicin can cause mutations and cancer. Episindan should not be used by pregnant women. Explain to women of childbearing age about the risks to the fetus when taking Epirubicin. Patients during treatment with Episindan should avoid becoming pregnant. Lactation: It is not known whether Epirubicin is excreted in human milk. However, other anthracyclines pass into breast milk and because Epirubicin carries the risk of very serious side effects in the infant, the mother must stop breastfeeding while being treated with Episindan.

Episindan is a drug with high toxicity, low therapeutic index. Response to treatment with Epirubicin is often accompanied by signs of toxicity. The main toxic effects of Epirubicin are on rapidly proliferating normal tissues, especially bone marrow, oral mucosa, gastrointestinal tract, and hair follicles. Systemic: Fever, infection, anorexia and anaphylaxis (rare). Infusion/potency site: Venous irritation, necrosis at the site of epirubicin extravasation when injected. Skin and mucous membranes: Hair loss, darkening of skin and nails, mucositis, photosensitivity, keratitis, conjunctivitis, rash, rash and itching. Blood: leukopenia, reversible agranulocytosis. WBCs usually decrease on days 10-14 after dosing and return to pre-dose levels by day 21. Bone marrow can be strongly suppressed. This effect of the drug is dose dependent. Gastrointestinal: Nausea, vomiting and diarrhea. Cardiovascular: Early manifestations are sinus tachycardia, abnormal electrocardiogram (nonspecific ST-T wave changes), ventricular tachycardia, atrioventricular block. Late manifestations: myocardial damage, reduced left ventricular ejection fraction, congestive heart failure and possibly death. The risk of cardiotoxicity is increased if the patient has pre-existing cardiovascular disease, has been previously treated with anthracyclines or anthracedions, and irradiates the mediastinum, precordial region; Concomitant use of Epirubicin with cardiotoxic drugs. The cardiotoxic effects of Epirubicin are dose dependent and exhibit limited cumulative dose toxicity. The probability of patients with congestive heart failure responding to the cumulative dose of epirubicin 550, 700 and 900 mg/m2 was 0.9%; 1.6% and 3.3%. The risk of congestive heart failure in patients increases rapidly when the cumulative dose exceeds 900 mg/m2. Assess left ventricular ejection fraction frequently and discontinue Episindan as soon as symptoms of heart failure develop. Patients at high risk for epirubicin toxicity should closely monitor cardiac function, weighing the benefits of epirubicin against the risk of heart failure. Thrombophlebitis, pulmonary embolism, and arterial thrombosis may occur. Nervous: Hot flashes. Urology, genitourinary: Irreversible amenorrhea in women, chromosomal disorders in sperm. If you experience these symptoms, the patient should notify the doctor for appropriate treatment.

Episindan interacts with other anticancer drugs and increases the pharmacological and toxicological effects of the two drugs when administered concurrently. In case it is necessary to combine with other anti-cancer drugs, the dose of Episindan must be reduced. Administration of Episindan immediately after administration of paclitaxel may increase the toxicity of Epirubicin. Because Paclitaxel slows the conversion of Epirubicin to Epirubicinol, which is a less toxic bone marrow metabolite than Epirubicin. Epirubicin and Cardiotoxic Drugs: Concomitant administration of drugs with cardiac effects has the potential to cause congestive heart failure (calcium channel blockers such as verapamil). Epirubicin and drugs that affect the liver: Epirubicin is extensively metabolised in the liver, so liver function may be altered when used concomitantly with drugs that affect the liver, affecting the pharmacokinetics, metabolism, and effects effects and toxicity of these drugs acting on the liver. Phenytoin: Epirubicin reduces the absorption of the drug when used concomitantly. Fluorouracil: Epirubicin may inhibit the metabolism of the drug. Above is all information about Episindan, patients need to carefully read the instructions for use, consult a doctor / pharmacist before using. Episindan is a prescription drug, patients absolutely should not self-treat at home because there may be unwanted side effects.