Epirubicin Medak (epirubicin) solution for injections 2 mg/ml. vial 10 ml.

Description

Epirubicin Medak Storage
active substance: epirubicin hydrochloride;

1 ml of solution for injection contains 2 mg of epirubicin hydrochloride;

Excipients: sodium chloride, concentrated hydrochloric acid, water for injections.

Epirubicin Medak Dosage form
Solution for injection.

Main physical and chemical properties: transparent red solution, free from visible mechanical inclusions.

Pharmacotherapeutic group
Antineoplastic agents. ATX code L01D B03.

Pharmacological properties

Pharmacodynamics.

Epirubicin is an antibiotic of the anthracycline group with cytotoxic activity. The mechanism of action of epirubicin is related to its ability to bind to DNA. Cell culture studies have shown rapid cell penetration, localization in the nucleus, inhibition of nucleic acid synthesis and mitosis. Epirubicin has been shown to be active against a wide range of experimental tumors, including leukemia L1210 and P388, sarcomas SAI 80 (solid and ascites), melanoma B16, breast cancer, Lewis lung cancer, and colon cancer 38. Epirubicin activity has also been demonstrated. humans transplanted into non-thymus nude mice (melanoma, breast, lung, prostate, and ovarian cancer).

Pharmacokinetics.

In patients with normal hepatic and renal function, plasma levels after intravenous injection of 60-150 mg / m2 of the drug demonstrated a three-exponential reduction model with a very rapid first phase, a slow terminal phase and a mean half-life of approximately 40 hours. These doses are within the pharmacokinetic linearity both in terms of plasma clearance values ​​and metabolic pathway. In the range between 60 and 120 mg / m2 is a wide range of pharmacokinetic linearity, the dose of 150 mg / m2 is located on the border of dose linearity. The main identified metabolites are epirubicinol (13 ‑ OH epirubicin), as well as glucuronides of epirubicin and epirubicinol.

In pharmacokinetic studies in patients with in situ bladder carcinoma, low plasma levels of epirubicin are usually detected after intravesical instillation (<10 ng / ml). Thus, it is impossible to assume the presence of significant systemic resorption. Patients with damage to the bladder mucosa (eg, tumor, cystitis, surgery) can expect a higher rate of resorption.

4` ‑ O ‑ glucuronidation distinguishes epirubicin from doxorubicin and may explain the faster elimination of epirubicin and its reduced toxicity. The levels of the main metabolite in blood plasma, 13 ‑ OH derivative (epirubicinol), respectively, are lower and actually parallel to the levels of unchanged active substance.

Epirubicin is excreted mainly by the liver; high plasma clearance (0.9 l / min) indicates that such a slow elimination occurs due to the large tissue distribution. Urinary excretion after 48 hours is approximately 9-10% of the administered dose.

Excretion through the biliary tract is the main route of elimination, approximately 40% of the administered dose is detected in the bile after 72 hours. The active substance does not cross the blood-brain barrier.

Epirubicin Medak Indication
Epirubicin is used to treat a number of neoplastic conditions, including:

breast cancer;
ovarian cancer;
stomach cancer;
lung cancer;
malignant lymphoma;
soft tissue sarcomas;
liver cancer;
pancreatic cancer;
rectal cancer;
cervical ‑ facial cancer;
leukemia.
It has been shown that epirubicin when administered intravesically is effective for the treatment of:

papillary transitional cell carcinoma of the bladder;
in situ carcinomas of the bladder;
intravesical prevention of recurrence of superficial carcinoma of the bladder after transurethral resection.

Contraindication
Hypersensitivity to epirubicin or to any of the excipients, to other anthracyclines and anthracenediones;
breastfeeding period.
Intravenous administration of epirubicin is contraindicated in the following diseases:

persistent myelosuppression due to previous chemotherapy or radiation therapy;
active depression of bone marrow function due to previous courses of treatment with other anticancer drugs or radiotherapy;
severe liver dysfunction;
cardiac diseases, including in the anamnesis (in particular myocardial insufficiency of the IV degree, acute myocardial infarction or myocardial infarction in the anamnesis which caused myocardial insufficiency of the III or IV degree, acute inflammatory heart diseases, arrhythmias with serious hemodynamic disturbances);
cardiomyopathy;
unstable angina;
obtaining previously the maximum cumulative dose of other anthracyclines (eg, doxorubicin or daunorubicin);
acute systemic (generalized) infections.

Contraindications for intravesical use:

urinary tract infections;
invasive tumors that penetrate the bladder wall;
catheterization problems (urethral obstruction caused by significant intravesical neoplasms);
inflammation of the bladder;
hematuria.