Epirubicin Hydrochloride for Injection

Epirubicin is an anthracycline cytotoxic drug. Although anthracyclines are known to interfere with many biochemical and biological functions in eukaryotic cells, the precise mechanisms of epirubicin's cytotoxic and/or antiproliferative effects have not been fully elucidated. The planar ring of epirubicin intercalates between base pairs, thereby binding to DNA to form a complex that inhibits nucleic acid (DNA and RNA) and protein synthesis. This intercalation process also triggers DNA cleavage by topoisomerase II, resulting in cytocidal effects. Epirubicin also inhibits DNA helicase activity, preventing enzyme-induced DNA double-stranded unwinding and interfering with replication and transcription. Epirubicin also participates in oxidation/reduction reactions by generating cytotoxic free radicals. The antiproliferative and cytotoxic effects of epirubicin are due to these and other possible mechanisms of action. Epirubicin has in vitro cytotoxic effects on a variety of established murine and human cell lines and primary cultures of human tumors. It also has in vivo antitumor effects on murine tumors and human cancer xenografts (including breast cancer) in athymic mice.

The main ingredient of this product is epirubicin hydrochloride. Chemical name: (8S, 10S)-10-[(3-amino-2,3,6-trideoxy-α-L-arabinopyranosyl)oxy]-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxy-7,8,9,10-tetrahydrotetracene-5,12-dione hydrochloride

This product is red or orange-red loose lumps or powder and is hygroscopic.

Treatment of malignant lymphoma, breast cancer, lung cancer, soft tissue sarcoma, esophageal cancer, gastric cancer, liver cancer, pancreatic cancer, melanoma, colorectal cancer, ovarian cancer, multiple myeloma, leukemia. Intravesical administration helps treat superficial bladder cancer, carcinoma in situ and prevents recurrence after transurethral resection.

Conventional dose: When epirubicin is used alone, the adult dose is 60-120 mg/m2 per body surface area once. When epirubicin is used as an adjuvant treatment for breast cancer patients with positive axillary lymph nodes in combination with chemotherapy, the recommended starting dose is 100-120 mg/m2 intravenous injection. The total starting dose for each course of treatment can be given once alone or in divided doses for 2-3 consecutive days. It can be repeated at intervals of 21 days depending on the patient's blood picture. Optimized dose: High doses can be used to treat lung cancer and breast cancer. When used alone, the recommended starting dose for adults is up to 135 mg/m2 per body surface area once, given once on the first day of each course of treatment or in divided doses on the first, second, and third days of each course of treatment, once every 3-4 weeks. When combined with chemotherapy, the recommended starting dose is up to 120 mg/m2 per body surface area, given on the first day of each course of treatment, once every 3-4 weeks. Administered by intravenous injection. It can be repeated at intervals of 21 days depending on the patient's blood picture. Intravesical administration: Epirubicin should be instilled through a catheter and should remain in the bladder for about an hour. During instillation, the patient should change position frequently to ensure that the bladder mucosa can be exposed to the drug over the largest area. To avoid inappropriate dilution of the drug by urine, patients should be informed not to drink any liquids 12 hours before instillation. Doctors should instruct patients to empty their urine at the end of treatment. For superficial bladder cancer, epirubicin 50 mg is dissolved in 25 to 50 mL of normal saline and instilled 8 times once a week. For cases with local toxicity (chemical cystitis), the dose can be reduced to 30 mg each time. Patients can also receive 50 mg of the same dose of drug instilled into the bladder once a week for 4 times, and then once a month for a total of 11 times. Doctors can adjust the number of dosing times according to the patient's condition.

1 Common symptoms include alopecia (approximately 70-80% of patients), bone marrow suppression (approximately 50-60%, white blood cells can drop to the lowest point 10-14 days after medication, and gradually recover in about 3 weeks, anemia and obvious thrombocytopenia are rare), loss of appetite, nausea, and vomiting, but compared with doxorubicin at equivalent doses, the degree is milder than that of doxorubicin. 2 Myocardial toxicity is also milder than doxorubicin, and its incidence and severity are proportional to the cumulative amount of this product. Although abnormal heart rhythm and tachycardia are common after medication, they are mostly transient and recover quickly; delayed severe ejection heart failure mostly occurs half a year after medication or when the total dose exceeds 700-800mg. It should be noted that this severe myocardial damage can sometimes occur suddenly without any warning, and even routine electrocardiograms do not show abnormal findings. Monitoring left ventricular ejection index (LVEF) and PEP/LVEF is the most sensitive. 3. If the injection site overflows, it may cause redness, swelling, local pain, and even cellulitis or necrosis. 4. Damage to liver and kidney function is rare, but it may cause elevated serum alanine aminotransferase or even jaundice when there is chronic liver disease or liver metastasis. Bone marrow suppression, leukopenia, hair loss, and gastrointestinal reactions. Arrhythmia, heart failure in some cases, myocardial damage, and drug fever. It may cause liver damage. About half of the patients may experience varying degrees of hair loss, but it is milder than doxorubicin. Bone marrow suppression occurs in about 50% to 70% of patients, and generally can be reduced to the lowest point within 10 to 14 days after medication, and most of them gradually recover in 3 to 4 weeks. Anemia and thrombocytopenia are rare. Anorexia, nausea, and vomiting are also milder than doxorubicin. Myocardial toxicity is closely related to the total cumulative dose, but it is milder than doxorubicin. In addition to transient reversible abnormal heart rhythm and tachycardia after medication, severe myocardial damage is mainly delayed ejection heart failure, which often occurs when the total amount reaches more than 700 mg, often half a year or even longer after the start of medication. There may be no precursors or obvious symptoms before heart failure occurs, but if the left ventricular ejection index (LVEF) and PEP/LVEF (PEP is the pre-ejection interval) can be monitored, most of them can be seen abnormal. Overflow of the drug solution can cause local redness, swelling, pain, necrosis or even cellulitis. Liver and kidney function damage is rare, and reversible transaminase elevation may occur occasionally.

1. Similar to doxorubicin, but to a lower degree, especially cardiac toxicity and bone marrow suppression toxicity; 2. Other adverse reactions include: hair loss, which may occur in 60-90% of cases and is generally reversible, and males may have suppressed beard growth; mucositis, which occurs on the 5th to 10th day of medication, usually occurring on the lateral and sublingual mucosa of the tongue; gastrointestinal dysfunction, such as nausea, vomiting, and diarrhea; there have been reports of occasional fever, chills, urticaria, pigmentation, and joint pain.

Precautions for children: There are no special requirements for children. Precautions for pregnancy and lactation: There is no conclusive data to show whether epirubicin has adverse effects on human fertility, teratogenicity or other harmful effects on the fetus. However, there are experimental data suggesting that epirubicin, like most anti-tumor drugs and immunosuppressants, exhibits mutagenicity and carcinogenicity in animals under specific experimental conditions. It can reduce the survival rate of the fetus. Therefore, this product is not recommended for use during pregnancy and is contraindicated for breastfeeding women. Precautions for the elderly: Elderly patients with reduced heart function should use it with caution or reduce the dosage.

1. Epirubicin can be used in combination with other anti-tumor drugs, but the dosage of epirubicin should be reduced. When used in combination, they must not be used in the same syringe. 2. Epirubicin cannot be mixed with heparin for injection, because the two are chemically incompatible and precipitation reactions will occur at certain concentrations. 3. Epirubicin is mainly metabolized in the liver. Any drug that can cause changes in liver function during concomitant treatment will affect the metabolism, pharmacokinetics, efficacy and/or toxicity of epirubicin. 4. The use of paclitaxel drugs before the administration of epirubicin will cause an increase in the blood concentration of the original epirubicin drug and metabolites, of which the metabolites are neither active nor toxic. When paclitaxel or docetaxel drugs are used in combination with epirubicin, giving epirubicin first will have no effect on its pharmacokinetics.

Keep away from light and store in sealed container.

10mg

24 months

Shandong Newtime Pharmaceutical Co., Ltd.

• Founded in:

  2001-03-30

• Address:

  No. 1 North Outer Ring Road, Fei County, Shandong

• Tax NO.:

  9137130072755352X1

• Registered Funds:

  358.238 million yuan

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