Flounders
Lastet: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Lastet
ATX code: L01CB01
Active ingredient: etoposide (Etoposide)
Manufacturer: Nippon Kayaku Co. Ltd. (Nippon Kayaku, Co. Ltd.) (Japan)
Description and photo update: 2019-10-07
Lastet is an anticancer drug of plant origin.
Release form and composition
Dosage forms of the drug Lastet:
- concentrate for preparation of solution for infusion: slightly viscous transparent liquid of light yellow color (5 ml each in sealed ampoules of 6 ml neutral glass, equipped with two marking rings and a blue break point, in a cardboard pallet, 10 ampoules each, in a cardboard box 1 pallet 5 ml each in neutral glass vials, sealed with a red plastic lid with the inscription in Japanese "Laste 100 mg / 5 ml", 10 vials in a polystyrene foam pallet, 1 pallet in a cardboard box);
- capsules 25 mg: gelatinous, soft, pale orange, the contents of the capsules are transparent viscous liquid, colorless or light yellow (10 pcs. in PVC / aluminum foil blisters; 4 blisters in a cardboard box);
- capsules 50 mg: gelatinous, soft, light red-orange color, the contents of the capsules are transparent viscous liquid, colorless or light yellow (10 pcs. in PVC / aluminum foil blisters; in a cardboard box 2 blisters);
- capsules 100 mg: gelatinous, soft, dark red-orange color, the contents of the capsules are transparent viscous liquid, colorless or light yellow (10 pcs. in PVC / aluminum foil blisters; in a cardboard box 1 blister).
Each pack also contains instructions for using Lastet.
Composition for 1 ml of concentrate for preparation of solution for infusion:
- active substance: etoposide - 20 mg (in 1 ampoule / vial - 100 mg);
- auxiliary ingredients: polysorbate-80, citric acid, macrogol-400, ethanol.
Composition for 1 capsule:
- active substance: etoposide - 25, 50 or 100 mg;
- auxiliary ingredients: concentrated glycerin (glycerol), macrogol 400, citric acid anhydride, hydroxypropyl cellulose;
- capsule shell: gelatin, D-sorbitol (isotonic sorbitol solution), concentrated glycerin (glycerol), propyl parahydroxybenzoate, ethyl parahydroxybenzoate, titanium dioxide, dye iron oxide red, hydrochloric acid qs, purified water qs
Pharmacological properties
Pharmacodynamics
Lastet is an anticancer drug, the mechanism of action of which is associated with inhibition of topoisomerase II. The active substance of the drug, etoposide, which is a semi-synthetic derivative of podophyllotoxin, is characterized by inhibition of mitosis by blocking cells in the SG 2 -interphase of the cell cycle; against the background of increased doses, etoposide acts in the G 2 -phase of the cell cycle. It also inhibits the penetration of nucleotides across the plasma membrane, interfering with the synthesis and replication of viral DNA (deoxyribonucleic acid).
In relation to healthy cells, the cytotoxic activity of etoposide is observed only when it is used in high doses.
Pharmacokinetics
After oral administration, absorption of etoposide occurs in the gastrointestinal tract. The average bioavailability is 50%, the diet does not affect this indicator. As a result of intravenous administration, C max (maximum concentration) in plasma reaches 30 μg / ml.
The drug is found in pleural fluid, liver tissue, spleen, kidneys, myometrium. Etoposide crosses the placental barrier. Cerebrospinal fluid concentrations of etoposide range from undetectable values to 5% of plasma concentrations. In the lungs in the presence of metastases, the concentration of etoposide is lower than in normal lung parenchyma. In the myometrium, a close concentration of a substance contained in the tissues of primary tumors and in healthy tissues is determined.
The substance binds to plasma proteins at a level of 90%. A direct correlation has been observed between the binding coefficient of etoposide and the level of albumin in the blood plasma of patients with malignant neoplasms and healthy people.
There is information about the release of the drug in human breast milk.
Etoposide is metabolized in the liver.
Excretion of the active substance mainly (44-60%) occurs through the kidneys. Up to 16% of the dose of etoposide is excreted through the intestines, up to 6% with bile.
The mean elimination half-life (T 1/2) of etoposide, which is excreted in a biphasic manner, in patients with normal renal and hepatic function:
- adults: in the initial phase - 0.6–2 hours, in the final phase - 5.3–10.8 hours;
- children: in the initial phase - 0.6–1.4 hours; in the final phase - 3–5.8 hours.
The final T 1/2 is 7 hours on average.
Indications for use
- germ cell tumors (choriocarcinoma, testicular tumor);
- acute non-lymphoblastic leukemia;
- non-small cell and small cell lung cancer;
- lymphogranulomatosis;
- NHL (non-Hodgkin's lymphomas);
- stomach cancer (including in combination therapy);
- breast cancer with metastases to the pleura and / or liver;
- ovarian cancer;
- mesothelioma;
- neuroblastoma;
- Ewing's sarcoma;
- Kaposi's sarcoma.
Contraindications
Absolute:
- severe violations of liver and kidney function;
- acute infections;
- severe myelosuppression with neutrophil counts less than 1500 / μl and / or platelets less than 75,000 / μl;
- period of pregnancy;
- breast-feeding;
- children's age: solution - up to 2 years, capsules - up to 3 years;
- hypersensitivity to podophylline, as well as to its derivatives;
- individual intolerance to the components of the drug.
Care must be taken when using Lastet in patients with mild to moderate renal impairment, infectious lesions of the mucous membranes, cardiac arrhythmias, increased risk of myocardial infarction, in children over 2 years of age (for solution) and over 3 years of age (for capsules), with impaired liver function, epilepsy and other serious diseases of the nervous system, chronic alcoholism, chickenpox, herpes zoster, after previous radiation or chemotherapy.
Laste, instructions for use: method and dosage
The doctor prescribes the dosage form and dosage regimen individually, taking into account the indications, the severity of the disease, the antitumor therapy regimen used and the state of the hematopoietic system.
The use of Lastet is required to be carried out in the presence of qualified medical personnel with experience in the treatment of oncological diseases in order to control the effectiveness.
Capsules
Lastet capsules are intended for oral use and should be taken on an empty stomach.
Recommended dosage regimen:
- monotherapy: the initial dose is 100-200 mg / m 2 for 5 consecutive days or 200 mg / m 2 on the 1st, 3rd and 5th days of the therapy cycle with an interval of 3-4 weeks. If the daily dose exceeds 200 mg, it should be divided into two doses in equal amounts;
- combination therapy: the initial dose is 100-200 mg / m 2 for 5 consecutive days or 200 mg / m 2 on the 1st, 3rd and 5th days of the therapy cycle with an interval of 3-4 weeks, simultaneously with other prescribed drugs.
An alternative dosage regimen: 50 mg / m 2 daily for 14-21 days, with a repetition of the course every 28 days or with a resumption of admission after myelosuppression.
When choosing a dose of etoposide, one should take into account the myelosuppressive activity of other drugs taken simultaneously, as well as the effect of previous radiation and chemotherapy. A neutrophil count of less than 500 / μL for more than 5 days requires an initial dose adjustment.
Also, dose adjustment is necessary for patients with fever, infectious diseases, in the case of a decrease in the number of platelets less than 25,000 / μl, with the development of toxicity of grade 3 or 4 and a decrease in CC (creatinine clearance) below 50 ml / min (for patients with CC 15-50 ml / min the dose is recommended to be reduced by 25%).
A new course of etoposide is not started if, during the previous therapy, the neutrophil count fell below 1500 / μl (neutropenia) and / or the platelet count fell below 100,000 / μl (thrombocytopenia). Re-treatment is carried out after the normalization of the results of peripheral blood tests.
Concentrate for solution for infusion
The solution prepared from the concentrate is intended for intravenous infusion.
The recommended dosage regimen: 50-100 mg / m 2 for 5 consecutive days or 100-125 mg / m 2 on the 1st, 3rd and 5th days of the therapy cycle, with an interval of 3-4 weeks. The time of administration of one dose is 30-60 minutes.
When choosing a dose, one should take into account the myelosuppressive effect of other drugs, if Lastet is used as part of a complex treatment, as well as the effect of previous radiation and chemotherapy.
Before starting intravenous administration, the concentrate must be diluted in 250 ml of 0.9% sodium chloride solution or 5% dextrose solution. The final concentration of the prepared solution is 0.2–0.4 mg / ml. The resulting solution is used immediately after preparation. Avoid contact of the drug with buffered aqueous solutions, the pH of which is greater than 8. Before administration, the solution should be visually assessed for the presence of solid particles or discoloration.
Since the concentrate for the preparation of a solution for intravenous administration Lastet contains ethyl alcohol as an auxiliary component, this can become an additional risk factor for liver diseases, epilepsy, alcoholism, and also in children.
For patients with impaired renal function with a CC of 15-50 ml / min, it is recommended to reduce the dose by 25%. There are no data on the safety and efficacy of Lastet in patients with CC below 15 ml / min.
Side effects
- from the hematopoietic system: anemia, leukopenia; rarely, thrombocytopenia;
- on the part of the central and peripheral nervous system: increased fatigue, drowsiness, damage to the peripheral nervous system;
- from the digestive system: nausea, vomiting; rarely - diarrhea, mucositis, anorexia; against the background of the use of high doses of Lastet - toxic reactions from the liver;
- on the part of the cardiovascular system: arterial hypotension, tachycardia;
- from the immune system: allergic reactions in the form of fever, chills, bronchospasm, tachycardia, shortness of breath and low blood pressure;
- from the side of metabolism: hyperuricemia; against the background of the use of high doses of Lastet - metabolic acidosis;
- from the reproductive system: amenorrhea, azoospermia;
- dermatological reactions: reversible alopecia;
- local reactions (for concentrate): phlebitis, if the drug gets on the skin - a pronounced local irritating effect, necrosis of the surrounding tissues is possible;
- others: occasionally - metallic taste in the mouth, interstitial pneumonitis / pulmonary fibrosis, urticaria, skin rash, malignant exudative erythema (Stevens-Johnson syndrome), muscle cramps, transient cortical blindness, hot flashes, optic neuritis, Lyell's syndrome (toxic epidermal); if the drug gets under the skin (for concentrate) - a pronounced local irritant effect.
Overdose
Cases of overdose of etoposide in humans have not yet been recorded. Probably, the main manifestations of an overdose could be toxic effects from the gastrointestinal tract, hepatobiliary system and hematopoietic system.
In this case, symptomatic therapy is recommended. The specific antidote for etoposide is unknown.
special instructions
Before using Lastet, a clinical analysis of the peripheral blood picture should be performed. After starting treatment, regular monitoring of blood counts is required.
If anaphylactic reactions are suspected, the use of etoposide is discontinued and corticosteroids and / or antihistamines are prescribed during infusion therapy.
Extravasation requires immediate interruption of the injection. The infusion should be discontinued if a burning sensation occurs. Hydrocortisone is injected subcutaneously around the affected area and 1% hydrocortisone ointment is applied under a dry dressing for 24 hours until erythema subsides. The remaining portion of the solution should be injected into another vein.
The immunosuppressive effect of Lastet can contribute to the development of a severe infection, therefore, during the period of anticancer therapy, immunization of patients and their families with live vaccines is contraindicated.
The results of experimental studies indicate the mutagenic, teratogenic and embryotoxic effects of etoposide.
Possible development of irreversible loss of fertility in men as a result of treatment with etoposide. In this regard, the attending physician should recommend that they preserve sperm before using Lastet.
Influence on the ability to drive vehicles and complex mechanisms
During therapy with Lastet, it is recommended to refrain from all types of activities, the implementation of which requires increased attention and high speed of psychomotor reactions, including driving.
Application during pregnancy and lactation
The use of Lastet is contraindicated during the period of gestation and breastfeeding.
If necessary, the appointment of the drug during lactation, breastfeeding should be discontinued.
Both women of childbearing age and their partners should use reliable methods of contraception both during anticancer therapy and within 6 months after its end.
Pediatric use
The efficacy and safety of etoposide in pediatric patients have not been studied. The drug Lastet in children and adolescents 3-18 years old should be used only when the expected benefit from therapy outweighs the potential risk.
The appointment of Lastet is contraindicated for the treatment of children under 2 years old (for solution) and under 3 years old (for capsules).
In children over 2 years of age (for solution) and over 3 years of age (for capsules), Lastet should be used with caution.
With impaired renal function
The appointment of Lastet for cancer patients with severe renal dysfunction is contraindicated.
The drug should be prescribed with caution in case of mild to moderate renal failure.
For violations of liver function
It is contraindicated to use Lastet in severe liver dysfunction.
Caution is advised when treating patients with hepatic impairment.
Drug interactions
Against the background of the use of Lastet simultaneously with other drugs that cause myelodepression, the likelihood of additive suppression of bone marrow function increases.
Combination therapy with cisplatin may decrease the clearance of etoposide and increase its toxicity.
High doses of cyclosporine can cause a decrease in the clearance of etoposide, increasing the duration of its action and increasing the risk of increased leukopenia.
Analogs
Lastet's analogs are Vepesid, Etoposide, Etoposide-Teva, Etoposide-Ebeve, Etoposide-Mili, Etoposide-LENS, Fitoside, Etozid, Etopos, Cytoposide, Filotid, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperature: capsules - 2–8 ° C, solution - 2–25 ° C.
Shelf life: concentrate for preparation of solution for infusion, Lastet 50 and 100 mg capsules - 3 years; capsules 25 mg - 2.5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Lastet
Reviews of Lastet are rare. In one of the limited tests, more than 80% of respondents gave a positive answer to the question: does the drug help or not.
Much more often in social networks there are requests from patients or their relatives to share information about how and where to buy Lastet, since in many regions it is not available in pharmacies.
Price for Lastet in pharmacies
The price of Lastet for a package containing 10 ampoules with a solution can range from 2,990 rubles.
Average cost of the drug in capsules: Laste 50 mg, for 20 pcs. in the package - 4 125 rubles; Paddles 100 mg, for 10 pcs. in the package - 4 610 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
