Pharmacodynamics
Antitumor agent. It is a semi-synthetic derivative of podophyllotoxin. Mechanism of action is associated with inhibition of topoisomerase II. It inhibits mitosis, blocks cells in S-G2-interphase of the cell cycle, in higher doses it acts in G2-phase. Cytotoxic effect against normal healthy cells is observed only when etoposide is used in high doses.
Pharmacokinetics
Atoposide is absorbed from the gastrointestinal tract when taken orally. Bioavailability averages 50%. Distribution in cerebrospinal fluid is low and variable; concentrations in normal lung tissue are higher than in the presence of lung metastases; close concentrations in primary tumor tissues and in normal myometrial tissues are determined.
A direct correlation between etoposide binding coefficient and plasma albumin levels in healthy subjects and patients with cancer was noted. It is metabolized in the liver.
The final T1/2 averages 7 h. Excreted by the kidneys – 44-60%, with feces – up to 16%, with the bile – 6% or less.
Indications
Germ cell tumors (testicular tumors, choriocarcinoma);
ovarian cancer;
small cell and non-small cell lung cancer;
lymphogranulomatosis;
non-Hodgkin’s lymphomas;
stomach cancer (for monotherapy and as part of combination therapy);
Ewing’s sarcoma;
Kaposi’s sarcoma;
neuroblastoma;
breast cancer (with metastases to the liver, pleura);
acute non-lymphoblastic leukemia;
mesothelioma.
Pharmacological effect
Pharmacodynamics
Antitumor agent. It is a semi-synthetic derivative of podophyllotoxin. The mechanism of action is associated with inhibition of topoisomerase II. Inhibits mitosis, blocks cells in the S-G2 interphase of the cell cycle, and in higher doses acts in the G2 phase. Cytotoxic effects on normal healthy cells are observed only when etoposide is used in high doses.
Pharmacokinetics
When taken orally, etoposide is absorbed from the gastrointestinal tract. Bioavailability averages 50%. Distribution in the cerebrospinal fluid is low and variable; the concentration in normal lung tissue is higher than in the presence of metastases in the lungs; a similar concentration level is determined in the tissues of primary tumors and in normal myometrial tissues.
There has been a direct correlation between the binding coefficient of etoposide and the level of albumin in the blood plasma of healthy people and patients with cancer. Metabolized in the liver.
The final T1/2 is on average 7 hours. Excreted by the kidneys – 44-60%, with feces – up to 16%, with bile – 6% or less.
Special instructions
Use with caution in patients with previous radiation or chemotherapy, with chickenpox, herpes zoster, with infectious lesions of the mucous membranes, with cardiac arrhythmias, with an increased risk of myocardial infarction, impaired liver function, diseases of the nervous system (epilepsy), chronic alcoholism, in children over 2 years of age.
If renal function is impaired, the dose is reduced in accordance with the CC values.
Before starting and during therapy, peripheral blood patterns should be monitored.
It is not recommended to vaccinate patients and their families.
Experimental studies have shown that etoposide has a mutagenic effect.
Impact on the ability to drive vehicles and other mechanisms that require increased concentration
During treatment, you should refrain from activities that require increased attention and rapid psychomotor reactions.
Active ingredient
Etoposide
Composition
1 ml (1 bottle) contains:
Active ingredients:
etoposide 20 mg (100 mg).
The bottle contains 5 ml of concentrate.
There is 1 bottle in a cardboard package.
Pregnancy
Etoposide is contraindicated during pregnancy. If necessary, use during lactation should stop breastfeeding.
During treatment and for 3 months after its completion, patients of childbearing age must use effective methods of contraception.
Experimental studies have shown that etoposide has a teratogenic and embryotoxic effect.
Contraindications
Severe myelodepression;
severe dysfunction of the liver and kidneys;
pregnancy;
children under 2 years of age;
hypersensitivity to podophyllin or its derivatives.
Side Effects
From the hematopoietic system: leukopenia, anemia; less often – thrombocytopenia.
From the digestive system: nausea, vomiting; rarely – anorexia, mucositis, diarrhea; when used in high doses – toxic reactions from the liver.
From the central nervous system and peripheral nervous system: drowsiness, increased fatigue; damage to the peripheral nervous system.
Metabolism: hyperuricemia; when using high doses – metabolic acidosis.
From the cardiovascular system: tachycardia, arterial hypotension.
From the reproductive system: azoospermia, amenorrhea.
Allergic reactions: chills, fever, bronchospasm.
Dermatological reactions: alopecia.
gi, metabolic acidosis, hyperuricemia, very rarely – tumor collapse syndrome (sometimes leading to death).
Interaction
When used concomitantly with other drugs that cause myelosuppression, additive suppression of bone marrow function is possible.
When used simultaneously with cisplatin, the clearance of etoposide may decrease and its toxicity may increase.
Cyclosporine in high doses may reduce the clearance of etoposide and prolong its duration of action, which may increase leukopenia.
Storage conditions
At 15–30 °C
Shelf life
3 years
Manufacturer
Lance Farm, Russia
Shelf life | 3 years |
---|---|
Conditions of storage | At 15-30 °C |
Manufacturer | Lance Farm, Russia |
Medication form | solution for infusion |
Brand | Lance Farm |
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