Description drugs: Methotrexate (Methotrexatum)

Methotrexate (Methotrexatum). 4-Amino-N 10 -metilpteroilglutaminovaya acid or (deoxy-4-amino-N metilfolievaya acid).

Synonyms: Abifrexate, A-methopterin, Antifolan , Folex, Methotrexate, Methylaminopterinum, Mexate and others.

Yellow or orange yellow crystalline powder. Practically insoluble in water and alcohol.

Also available as the sodium salt (for injection) - leofilizirovannoy yellow dry porous mass (0,005 g), and yellow from dark brown to yellow (0.05 g and 0.1) color, water-soluble. Hygroscopic drug. Unstable to light.

The chemical structure of methotrexate similar to folic acid (cm.) And is an antimetabolite antagonist.

Antifolievym Due to the effect of the drug inhibits cell mitosis, increase in actively proliferating tissues (including bone marrow), inhibits the growth of malignant neoplasms.

Methotrexate used inside as well as in the form of sodium salt intramuscularly, intrathecally and intravenously. When administered in the maximum serum concentration observed after 2 - 4 hours after intramuscular and intravenous - during the first hour. Quickly excreted from the body in urine.

Assign methotrexate and its sodium salt alone or in combination chemotherapy for acute lymphoblastic leukemia and myeloid, in the later stages of chronic myeloid leukemia, with lymphosarcoma; with combination chemotherapy in patients with breast cancer, lung, ovaries. In high doses (under the guise of calcium folinate - cm.) Is also used in osteogenic sarcoma, Ewing tumors, soft tissue sarcoma, uterine choriocarcinoma.

Inside designate methotrexate in pill form.

When the complex treatment of leukemia designate an adult to 0.03 g- (30 mg) 2 times a week. The maximum daily dose for children 0.02g (20 mg) per 1 m2 of body surface. The course of treatment 2 weeks. When administered adult intensive course of 0.02 - 0.025 g (20 - 25 mg) daily for 5 days. Breaks between courses 2 - 3 weeks.

When uterine choriocarcinoma appoint 0.05 g (50 mg) 1 every 5 days. In the course of treatment of 0.3 - 0.4 g Courses repeated at intervals of not less than 1 month. Assign also at higher doses: 15 - 30 mg daily for 5 days with intervals 1 - 2 weeks.

The sodium salt of methotrexate is administered intramuscularly, intravenously (bolus or infusion) or in the spinal canal. The contents of ampoules were dissolved in sterile isotonic sodium chloride solution.

Adults with leukemia designate sodium salt of methotrexate parenterally typically at a dose of 0.01 - 0.03 g; daily dose - 0.03 g (30 mg). Administered 1 or 2 times per week or one every 4 days. Children under the age of 7 injected parenterally and in a single daily dose of 0.003 - 0.005 g (3 - 5 mg), 7 - 14 - 0.005 - 0.015 g (5 - 15 mg); per course of treatment is administered to children under 7 years of 0.009 - 0.015 g (9 - 15 mg), 7 - 14 years - 0.015 - 0.045 g (15 - 45 mg).

When uterine choriocarcinoma sodium salt of methotrexate is used intramuscularly or intravenously in a single dose of 0.02 g (20 mg) daily for 5 days. Courses are repeated 2 - 4 times in the primary treatment at intervals of 2 - 4 weeks, with maintenance therapy - 1 - 2 times.