Etopozid (etoposide) concentrate for infusions 20 mg/ml. 10 ml. (200 mg.) vial №1

Description

Etopozid 200 mg. Storage
active substance: etoposide;

1 ml of solution contains etoposide 20 mg;

excipients: anhydrous citric acid, benzyl alcohol, macrogol 300, polysorbate 80, ethanol 96%.

Etopozid 200 mg. Dosage form
Concentrate for solution for infusion.

Main physical and chemical properties: clear light yellow solution.

Pharmacotherapeutic group
Antineoplastic and immunomodulatory agents. Alkaloids of plant origin and other drugs of natural origin. Derivatives of podophyllotoxin. ATX code L01C B01.

Pharmacological properties

Pharmacodynamics.

Etoposide is a semisynthetic derivative of podophyllotoxin. It has a pronounced cytotoxic effect, which largely depends on the dose and treatment regimen. Etoposide affects the function of topoisomerase II (an enzyme that cleaves DNA) and inhibits DNA synthesis in the terminal phase. As a result, single-stranded and double-stranded breaks in DNA are formed. The cytotoxic effect depends on the concentration and duration of etoposide exposure. The drug blocks mitosis, causing cell death in the S-phase and early G2-phase of the cell cycle. Unlike other known podophyllotoxins, it does not cause cell accumulation at the metaphase stage. Etoposide phosphate is metabolized in vivo to etoposide by dephosphorylation. The mechanism of action of etoposide phosphate is considered to be the same as that of etoposide.

Etopozid 200 mg. Pharmacokinetics.

Absorption. Following intravenous infusion, Cmax and AUC showed marked intra- and intersubject variability.

Distribution. The average volume of distribution at equilibrium is 18-29 liters. Etoposide slightly penetrates the cerebrospinal fluid. In vitro, etoposide is highly bound to human plasma proteins (97%).

In cancer patients, free etoposide correlates significantly with bilirubin.

Biotransformation. The hydroxy acid metabolite [4′-dimethyl-epipodophilic acid-9- (4,6-O-ethylidene-β-D-glucopyranoside)] is formed by opening the lactone ring and is found in the urine of adults and children. It is also present in human plasma, probably in the form of a trans isomer. Etoposide glucuronide and / or sulphate conjugates are also excreted in human urine. In addition, the corresponding catechol is formed by O-demethylation of the dimethoxyphenol ring with the isoenzyme CYP450 3A4.

Indication

Testicular cancer. Etoposide is indicated for use in combination with other approved chemotherapeutic agents for the treatment of primary, recurrent or refractory testicular cancer in adults.
Small cell lung cancer. Etoposide is indicated for use in combination with other approved chemotherapeutic agents for the treatment of small cell lung cancer in adults.
Hodgkin’s disease (lymphogranulomatosis). Etoposide is indicated for use in combination with other approved chemotherapeutic agents for the treatment of Hodgkin’s lymphoma in adults and children.
Non-Hodgkin’s lymphoma. Etoposide is indicated for use in combination with other approved chemotherapeutic agents for the treatment of non-Hodgkin’s lymphoma in adults and children.
Acute myeloid leukemia. Etoposide is indicated for use in combination with other approved chemotherapeutic agents for the treatment of acute myeloid leukemia in adults and children.
Malignant gestational trophoblastic disease. Etoposide in combination with other approved chemotherapeutic agents is indicated for the treatment of first- and second-line gestational trophoblastic neoplasia in adults.
Ovarian cancer. Etoposide is indicated in combination with other approved chemotherapeutic agents for the treatment of non-epithelial ovarian cancer in adults.
Platinum-resistant epithelial ovarian cancer. Etoposide is indicated for the treatment of platinum-resistant ovarian epithelial cancer in adults.

Contraindication

Hypersensitivity to etoposide or to other components of the drug.
Pregnancy, breastfeeding.
Use of yellow fever vaccine or other live vaccines during treatment with immunosuppressed patients.