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Zexat
Medical expert of the article
Last reviewed: 03.07.2025
Zexat is an antitumor cytostatic agent belonging to the pharmacological group of antimetabolites. International nonproprietary name - Methotrexat; other trade names: Methotrexate Ebeve, Ebetrex, Ebetrexat, Otrexup, Sactiva, Antifolan. ATC code - L01BA01.
Zexat is produced by the pharmaceutical company Fresenius Kabi Oncology Limited (India).
ATC classification
Active ingredients
Pharmacological group
Pharmachologic effect
Indications Zexat
Zexat is used for acute leukemia and neuroleukemia; lymphomas (except lymphogranulomatosis) and lymphosarcomas; malignant neoplasms of the uterus (including choriocarcinoma), ovaries and mammary glands; cancer of the esophagus, lungs, kidneys, bladder; skin cancer (including granuloma fungoides), retina, squamous cell carcinoma of the head and neck; sarcomas of bones and soft tissues. The drug can also be used in the treatment of refractory forms of psoriasis, rheumatoid arthritis, systemic lupus erythematosus.
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Release form
Injection solution in vials (15 mg/3 ml, 50 mg/2 ml) in a cardboard box.
Pharmacodynamics
The active substance of Zexat is a structural analogue of folic acid methotrexate, which competitively inhibits the activity of the folate-using enzyme dihydrofolate reductase (DHFR), which is involved in the production of DNA nucleic acids. Thus, Zexat suppresses the synthesis of DNA in atypical cells, which leads to the cessation of the process of tumor cell division at the stage of DNA replication.
Zexate also suppresses the body's immune responses, and its immunosuppressive properties are used in the treatment of a number of autoimmune diseases.
Pharmacokinetics
After the introduction of Zexat into the muscle, the maximum concentration of the drug in the blood is observed on average after 45 minutes; at this time, almost half of the administered drug binds to plasma proteins.
Biotransformation of Zexat occurs primarily in the liver, forming an active metabolite that continues to inhibit the synthesis of cellular enzymes and the nucleotide deoxythymidine, which functions as a synchronizer of mitosis in atypical cells.
The total half-life of the drug ranges from 5 to 14 hours, complete elimination is observed after 22-24 hours, although repeated administration of the drug leads to accumulation of metabolites.
Excretion occurs through the kidneys (90%) and through the intestines (10%).
Dosing and administration
The method of administration of Zexat is by infusions and injections (intramuscular, intravenous, into an artery or into the cerebrospinal fluid system).
The introduction of the drug into the treatment regimen is carried out by an oncologist in compliance with recommendations regarding dosage and route of administration for a specific diagnosis.
For tumors of various localizations, Zexat is administered intravenously (jet) at a dosage of 30-40 mg/m² - once a week. For leukemia and lymphomas, intravenous infusion is performed once every 14 or 28 days - 200-500 mg/m².
When calculating the dose for children (from 6 mg/m² to 12 mg/m²), not only the diagnosis and general condition are taken into account, but also age.
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Use Zexat during pregnancy
Use during pregnancy and breastfeeding is contraindicated.
Contraindications
Zexat is contraindicated for use in cases of decreased kidney and liver function, any infectious diseases, and pathologically altered ratio of leukocytes and platelets in the blood.
Zexat should be used with caution in cases of fluid accumulation in the abdominal cavity (ascites) or pleural effusion; in the presence of a history of gastric ulcer and duodenal ulcer, complicated inflammation of the colon mucosa (colitis), kidney stones, gout, as well as after chemotherapy and radiation therapy.
Side effects Zexat
The most common side effects of Zexat include: inflammation of the oral mucosa (stomatitis) and pharynx, skin reactions, upset stomach and liver, loss of appetite, nausea and vomiting, headache, abdominal pain and pain when urinating, increased levels of liver enzymes, as well as changes in the composition of blood cells, gastrointestinal bleeding, dizziness, confusion, depression, seizures, increased sensitivity to light, darkening of the skin, alopecia, etc.
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Overdose
An overdose of the drug increases its toxic effect on the body and enhances side effects. To neutralize the overdose, there is a specific antidote to folic acid antagonist drugs - Calcium folinate (Leivorin, Hemifolin), injections of which restore folate metabolism and help protect bone marrow cells.
Interactions with other drugs
When high doses of Zexat are used simultaneously with aspirin, salicylates and NSAIDs, the toxicity of the drug increases to a lethal level.
The same risk arises with the parallel use of sulfonamide drugs, penicillin and tetracycline antibiotics, indirect anticoagulants and cholesterol-lowering drugs.
Zexate increases the negative effects of retinoids and live vaccines, as well as nitrous oxide used in anesthesia.
Storage conditions
Store in a dark place at a temperature not exceeding +25° C. Do not freeze the drug.
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Shelf life
24 months.
Manufacturer
Attention!
To simplify the perception of information, this instruction for use of the drug "Zexat" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.