Etoposide-LENS, 20 mg/ml 5 ml

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

Active ingredient

Composition

1 ml (1 vial) contains:

Active ingredients:

Tetoposide 20 mg (100 mg).

In a bottle of 5 ml of concentrate.

There is 1 vial in the carton pack.

How to take, the dosage

V/v, for 30-60 minutes (pre-diluted with 0.9% sodium chloride solution or 5% glucose solution to the final concentration of 0.2-0.4 mg/ml) – 50-100 mg/m2 /day for 4-5 days, every 3-4 weeks, or 100-125 mg/m2 on days 1, 3, 5. The drug is mainly used in combination with other chemotherapeutic agents. Repeated courses are carried out only after normalization of peripheral blood parameters.

Interaction

In concomitant use with other drugs causing myelodepression, additive suppression of bone marrow function is possible.

Concomitant use with cisplatin may decrease etoposide clearance and increase its toxicity.

Cyclosporine in high doses may decrease etoposide clearance and increase its duration of action, and leukopenia may increase.

Special Instructions

With caution, use in patients with previous radiation or chemotherapy, with chicken pox, herpes zoster, infectious mucous membrane lesions, cardiac rhythm disorders, increased risk of myocardial infarction, liver function disorders, nervous system diseases (epilepsy), chronic alcoholism, children over 2 years old.

In case of impaired renal function, the dose is reduced in accordance with the CK values.

Peripheral blood count should be monitored before and during therapy.

Patients and family members should not be vaccinated.

Itoposide has been found in experimental studies to have mutagenic effects.

Impact on the ability to drive vehicles and other mechanisms requiring increased concentration

At the time of treatment, one should refrain from activities requiring increased attention and rapid psychomotor reactions.

Contraindications

Side effects

Blood system disorders: leukopenia, anemia; rarely – thrombocytopenia.

In the digestive system: nausea, vomiting; rarely – anorexia, mucositis, diarrhea; when used in high doses – toxic liver reactions.

CNS and peripheral nervous system disorders: drowsiness, increased fatigue; peripheral nervous system disorders.

Metabolic disorders: hyperuricemia; metabolic acidosis in high doses.

Cardiovascular system: tachycardia, arterial hypotension.

Reproductive system: azoospermia, amenorrhea.

Allergic reactions: chills, fever, bronchospasm.

Dermatological reactions: alopecia.

Gy, metabolic acidosis, hyperuricemia, very rare – tumor decay syndrome (sometimes leading to death).

Pregnancy use

Etoposide is contraindicated in pregnancy. Breast-feeding should be stopped if use is necessary during lactation.

During treatment and for 3 months after its completion, patients of childbearing age should use effective contraceptive methods.

Itoposide has teratogenic and embryotoxic effects in experimental studies.