METHOTREXATE (Methotrexatum; synonym: Amethopterin, Methopterine, Methylaminopterinum; joint venture. B) — antineoplastic means, 4-amino-N10-methyl-pteroilglutaminovaya to - that.
Yellow or yellow-orange fine-crystalline powder, almost water-insoluble and organic solvents. The m is well soaked up from went. - kish. path.
On the mechanism of action of M. is an antagonist folic acid (see), breaks its turning into tetrahydrofolic to - that. M apply to treatment of an acute leukosis, a horionepitelioma of a uterus, a breast cancer, cancer of a lung, lymphosarcomas, a reticulosarcoma, malignant tumors of a small egg, sarcomas of soft tissues and an osteosarcoma; it can be used for treatment of sarcoma of Kaposha, fungoid mycosis, and also psoriasis. The m possesses an immunodepressive effect and can be applied as an immunosuppressant. The m is a part of medicinal complexes (VAMP, TsAMP, POMP, etc.) for treatment acute leukosis (see), a breast cancer (with Cyclophosphanum and 5-ftoruratsily), horionepitelioma of a uterus (with Actinomycinum of D, hlorambutsily, Olivomycinum, vinblastine), malignant tumors of a small egg (with Olivomycinum, Cyclophosphanum).
M accept inside, enter intramusculary, intravenously, vnutriarterialno, endolyumbalno. At M.'s appointment inside division of a daily dose into several receptions can lead to strengthening of toxic action. The m is appointed on 10 mg daily, on 30 — 40 mg of 1 times in 5 days, on 20 — 25 mg daily within 5 days with the subsequent break to 2 — 4 weeks. The dose on a course of treatment makes 200 — 300 mg. Abroad in some cases at infusion use higher doses of M. (50 — 250 mg/kg) with co-administration of a metabolite folic to - you are a so-called leykovorina.
Symptoms of intoxication of M. are stomatitis, conjunctivitis, diarrhea. At overdose or intolerance there can be vomiting, enteritis, cystitis, a hair loss, an abnormal liver function, a leukopenia, thrombocytopenia.
M. it is contraindicated at diseases of a liver, kidneys, leukopenia and thrombocytopenia.
Forms of release: tablets on 2,5 mg, bottles on 5 mg. Store in the dry, protected from light place.
Bibliography: Perevodchikova N. I. Clinical chemotherapy of tumoral diseases, page 54, M., 1976; Chemotherapy of malignant tumors, under the editorship of H. N. Blochina, M., 1977; Antineoplastic and immunosuppressive agents, ed. by A. Page of Sartorelli a. D. G. Johns, pt. 1—2, B., 1974 — 1975; Holland J. F. a. F of e i E. Cancer medicine, Philadelphia, 1973.
H. I. Perevodchikova, B. A. Gorbunova.