Expiration date: 09/2025

Pharmacological action pharmacodynamic anticancer agent from the group of antimetabolites-folic acid antagonists. Acts In the s-phase of mitosis. The mechanism of action is associated with inhibition of the synthesis of purine nucleotides and thymidylate as a result of irreversible binding to dihydrofolate reductase, which prevents the restoration of dihydrofolate into active tetrahydrofolate. More active against fast-growing cells. It has some immunosuppressive effect.Pharmacokinetics slightly penetrates through the BBB (depending on the dose used). With intrathecal administration in a significant amount enters the systemic circulation. Binding to proteins (mainly albumin) plasma about 50%. Biotransformed in the liver. Excreted by the kidneys (unchanged) and bile (less than 10%). T1 / 2 depends on the dose used and has significant individual differences. When re-administration accumulates in the tissues in the form of metabolites.
Indications

•     Acute lymphocytic leukemia,
•     trophoblastic disease,
•     skin cancer,
•     cancer of the cervix and vulva,
•     esophagus cancer,
•     squamous cell head and neck cancer,
•     cancer of the renal pelvis and ureters,
•     osteogenic & soft cell sarcoma,
•     ewing sarcoma,
•     lung cancer,
•     breast cancer,
•     germ cell tumors of the testis and ovaries,
•     liver cancer,
•     kidney cancer,
•     retinoblastoma,
•     medulloblastoma,
•     penile cancer,
•     lymphogranulomatosis,
•     severe forms of psoriasis (in case of failure of adequate therapy),
•     severe form of rheumatoid arthritis (in case of failure of adequate therapy).

Contraindications

•     Severe hepatic and/or renal impairment,
•     leukopenia,
•     thrombocytopenia,
•     pregnancy,
•     methotrexate should not be used in immunodeficiency conditions.