Etoposide is a semisynthetic drug that belongs to topoisomerase II inhibitors. The agent has a cytotoxic effect due to its ability to damage the DNA of cancer cells.
Composition, form and packaging
The active ingredient is etoposide.
1 ml of the drug contains 20 mg of etoposide.
Issued by the Indian company Okasa Pharma and the Chinese concern Jiangsu Hengrui Medicine Co.
Indications for use
Usage indicated if:
- Small-cell lung cancer;
- Diseases of Hodgkin;
- Germicidal testicular carcinoma;
- Non-Hodgkin's lymphoma( as an induction therapy);
- Acute myelomonocytic and myelocytic leukemia( as a component of combined treatment);
- Placental chorion carcinoma;
- Non-small cell lung cancer( as a palliative treatment);Acute leukemia
Etoposide is not recommended for the following conditions:
- Slowing of hematopoiesis in the bone marrow( severe forms: leukopenia less than 2 thousand / μL, neutropenia - 1,5 thousand / μL, thrombocytopenia less than 75 thousand / μL);
- Presence in the anamnesis of a failure of kidneys and a liver;
- Acute infectious processes( pathogens may become fungi, viruses and bacteria);
- Various types of heart rhythm disturbances;
- Pregnancy and lactation.
Caution is necessary to use a cytotoxic drug with the following concomitant pathologies:
- Chemotherapy or radiotherapy in anamnesis;
- Against chicken pox;
- Dysfunction of kidney function;
- Pathologies of the nervous system;
- Chronic alcoholism;
- Early childhood.
Etoposide is a cytotoxic drug from the podophyllotoxin derivative group. It promotes damage to the DNA molecule due to inhibition of the structure of the topoisomerase II enzyme. The agent is specific for the G2 phase and the late S-phase of the mitotic cycle. The drug is not able to disrupt the assembly of microtubules.
Pharmacodynamics and pharmacokinetics
Etoposide has antitumor activity. It is capable of leading to a phase-specific cytotoxic effect. Experts note the dose-dependence of the drug.
High-dose( more than 10 μg / ml) intake promotes the lysis of cells that have entered mitosis. The use of a lower concentration( 0.3-10 μg / ml) will prevent the entry of cells into the prophase of mitotic division.
The main macromolecular effect of the drug is the ability to change DNA.
It leads to a change in the structure of topoisomerase II, due to which the inhibition of its activity occurs. As a result, DNA replication is broken, proliferation, the cell cycle slows down. The ability of the drug to disrupt the transport of nucleotides interferes with the recovery and synthesis of DNA.
During oral administration, etoposide has a variable absorption that decreases with increasing dosage. The average bioavailability is 50%.
With intravenous administration, the elimination half-life can be up to 11 hours. Etoposide is not cumulated by plasma if used for 5 days at 100 mg / m2.
The preparation practically does not pass through GEB.Concentration in the cerebrospinal fluid and tumor tissues is lower than the content in the plasma. The unbound fraction of the drug in cancer patients is determined by the level of bilirubin in the blood.
Metabolism of etoposide occurs in the liver. It is excreted in the urine mainly in the unchanged form( up to 60%), with calories( 16%) and bile( less than 6%).Special laboratory tests on animals to determine the carcinogenicity of the drug was not conducted. Etoposide is considered to be potentially carcinogenic to humans compounds.
Instructions for use Etoposide: dosage
According to the annotation, intravenous drip introduction of the preparation is preferred. Dosage is determined in individual mode.
Antitumor preparation can be mixed with dextrose( concentration of the solution is 0.2-0.4 mg / l).Any contact of Etoposide with buffer solutions exceeding pH 8 is prohibited.
- At 100 mg /m once daily for up to 5 days. The cycle is repeated a month later;
- For 125 mg / sq. M.m in the first, third and fifth days of treatment. The course is repeated after 3 weeks;
- At 50 mg / sq.m orally every day for 3 weeks. The course is repeated after 1 month;
Important! The course of therapy can be repeated after restoring the parameters of peripheral blood.
Side effects of
The data of numerous studies allow to distinguish such side effects:
- Violation of blood indices. During the course of development, leukopenia, anemia, thrombocytopenia develops. Restoration of bone marrow functionality is observed after 3 weeks;
- Development of acute leukemia;
- Gastrointestinal toxicity suggests the development of: nausea and vomiting( in 35% of patients), abdominal pain( 2%), anorexia in 12% of cases, diarrhea( 13%), stomatitis( 6%), liver diseases( 3%).Nausea and vomiting require the withdrawal of the drug in 1% of cancer patients, to improve the general condition prescribed antiemetics;
- Hypotension( up to 2%). Transient decrease in blood pressure develops as a consequence of the rapid administration of etoposide, it is not associated with cardiotoxicity of the drug or changes in the ECG.To reduce the severity of the side effect, it is sufficient to increase the duration of the infusion;
- Allergy( up to 2%). It is possible to develop the following anaphylactic reactions during the administration: chills, fever, bronchospasm, increased heart rate, decreased blood pressure. Within a few hours, the general state is normalized. Perhaps the appearance of puffiness of the face, laryngospasm, cough, cyanosis, increased sweating, loss of consciousness. In rare cases, anaphylaxis causes the patient to die;
- Dermatological reactions manifest as: reversible alopecia, which causes complete hair loss, rash, itching;
- Toxic effects on the central nervous system: fatigue, difficulty walking, numbness of limbs, weakness, convulsions;
- Etoposide in 2% of the patient causes damage to the peripheral nervous system.
Occasionally, patients notice an unpleasant aftertaste in the mouth, skin pigmentation, blindness of cortical origin, dysphagia, development of phlebitis at the site of administration.
Increasing the therapeutic dose leads to the development of severe mucositis, disruption of the bone marrow, the development of metabolic acidosis, liver pathologies, death of the patient.
There is no special antidote to etoposide. Therefore, when an overdose is used, symptomatic treatment.
Prescribe Etoposide should only an oncologist who has experience with this cytotoxic drug.
Special conditions are also necessary that will effectively stop the complications of therapy( sterile boxes, a wide range of antibiotics, drugs for replacement treatment with blood components).
Reactions that indicate a patient's hypersensitivity to Etoposide develop after the first administration. When they appear, it is necessary to stop the introduction of cytotoxic drugs, to start therapy with antiallergic drugs.
With the development of thrombocytopenia during treatment, it is necessary to perform with care invasive manipulations, dental therapy. Such patients need regular examination of places of administration of drugs, skin and mucous membrane in order to determine the development of bleeding in time. It is necessary to exclude the intake of alcohol, aspirin, which increases the risk of gastric bleeding.
In patients with cancer patients with leukopenia, the risk of developing an infection is increased. In such cases it is necessary to use antibiotics. It is necessary to vaccinate the patient and his family members, refuse to use oral polio vaccine.
Avoid zykstvazalnogo introduction due to damage to the vein. The drug has a pronounced irritant effect on the tissue, so the injection site must be chopped with hydrocortisone, after applying a bandage with hormonal ointment for a day.
During therapy for patients of reproductive age, regardless of gender, reliable contraceptives should be used.
Joint reception with drugs that cause oppression of bone marrow functionality, causes additive myelodepression.
Use with cisplatin leads to a decrease in the concentration in the blood of etoposide, increasing the toxicity of the drug.
High doses of Cyclosporine reduce the clearance of cytotoxic agents, increase the duration of its action, cause the development of leukopenia.
Marina, 47 years, Moscow:
Used a drug to treat lymphoma. During the first 2-3 days I felt very bad. Etoposide reduced the main blood counts, which had to be restored with expensive injections for a long time.
Oleg, 50, Moscow:
The doctor appointed Etoposide to cope with lymphogranulomatosis. After the beginning of therapy, there was a rash, nausea and vomiting, photophobia. On the fifth day, convulsions began.
Prices in Moscow
The cost of etoposide in the pharmacies of the capital depends on the dose and amount of the drug:
- 20mg / ml 5ml - 350 rubles per bottle;
- 100mg / ml 5ml - 415 rubles;
- 20mg / ml 10ml - 580 rudders;
- 200mg / ml 10ml - 670 rubles.
Analogues of Etoposide
The following are the analogues:
Synonyms of etoposide are:
- This is a pop;
Conditions for dispensing from pharmacies
The product belongs to the drugs of list A, therefore it can be bought at pharmacies strictly according to the prescription.
Storage conditions and expiration dates
The cytotoxic agent should be stored in a dark place where sunlight can not penetrate. The temperature regime is 15-25 ° C. Etoposide can be used for 3 years from the date of manufacture.