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Zexate
Last reviewed: 23.04.2024
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Zexat is an antitumor cytostatic agent related to the pharmacological group of antimetabolites. International non-proprietary name - Methotrexat; other trade names: Methotrexate Ebwe, Ebetrex, Ebetrexat, Otrexup, Sactiva, Antifolan. The PBX code is L01BA01.
Produces Zexate pharmaceutical company Fresenius Kabi Oncology Limited (India).
Indications Zexate
Zexate is used for acute leukemia and neuroleukemia; lymphomas (except for lymphogranulomatosis) and lymphosarcoma; malignant neoplasms of the uterus (including choriocarcinoma), ovaries and breast; cancer of the esophagus, lungs, kidneys, bladder; cancer of the skin (including mushroom granuloma), retina of the eyes, 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
Solution for injection in vials (15 mg / 3 ml, 50 mg / 2 ml) in a carton.
Pharmacodynamics
The active substance of Zexate is a structural analogue of folic acid methotrexate, which competitively inhibits the activity of the folate-using enzyme dihydrofolate reductase (DHFR) involved in the production of DNA nucleic acids. Thus, Zexat suppresses the synthesis of the DNA of atypical cells, which leads to a halt in the process of dividing the tumor cells 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 administration of Zexate to the muscle, the maximum concentration of the drug in the blood is noted on average 45 minutes; while almost half of the injected drug binds to plasma proteins.
Biotransformation Zexate occurs predominantly in the liver, and an active metabolite is formed, which continues to inhibit the synthesis of cellular enzymes and the nucleotide deoxythymidine, which acts as a synchronizer for the mitosis of atypical cells.
The total duration of the 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 a cumulation of metabolites.
Excretion is carried out by the kidneys (90%) and through the intestine (10%).
Dosing and administration
Method of application Zexate - by infusion and injection (intramuscular, intravenous, artery or liquor system).
The management of the drug in the treatment regimen is carried out by an oncologist with the observance of recommendations regarding the dosage and the mode of administration for a specific diagnosis.
With tumors of different locations, Zexate is administered intravenously (jet) at a dosage of 30-40 mg / m² - once a week. With leukemias and lymphomas, intravenous infusion is performed 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, but also age is taken into account.
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Use Zexate during pregnancy
Use during pregnancy and breastfeeding is contraindicated.
Contraindications
Zexate is contraindicated to use with a decrease in kidney and liver function, with any infectious diseases, as well as with a pathologically altered ratio of leukocytes and platelets in the blood.
With caution, Zexate is used for fluid accumulation in the abdominal cavity (ascites) or pleural effusion; in the presence of a history of: peptic ulcer of the stomach and duodenum, complicated inflammation of the colonic mucosa (colitis), kidney stone disease, gout, and also after chemotherapy and radiation therapy.
Side effects Zexate
The most common side effects of Zexate 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 urination, increased liver enzymes, and changes in the composition of blood cells, gastrointestinal bleeding, dizziness, confusion, depression, convulsions, increased photosensitivity, darkening of the skin, alopecia, etc.
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Overdose
Overdosing of the drug increases its toxic effect on the body and intensifies side effects. To neutralize the overdose, there is a specific antidote for folic acid antagonists - Calcium folinate (Leyvorin, Chemifolin), whose injections restore the metabolism of folates and promote the protection of bone marrow cells.
Interactions with other drugs
In the case of high doses of Zexate concurrent with aspirin, salicylates and NSAIDs, the toxicity of the drug is increased to a lethal level.
The same risk arises with concurrent use of sulfonamide drugs, penicillin-type antibiotics and tetracycline group, indirect anticoagulants and drugs for lowering cholesterol.
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 of no higher than + 25 ° C, it is inadmissible to freeze the drug.
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Shelf life
24 months.
Attention!
To simplify the perception of information, this instruction for use of the drug "Zexate" 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.