METOTREKSAT (Methotrexatum). 4 - 10-Amino-N metilpteroilglutaminovaya acid or (dezoksi-4- amino-N metilfolievaya acid).

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

     The yellow or orange-yellow powder melkokristallichesky. Almost nerastvorim in water and alcohol.

     Available also as sodium salt (for injection) - leofilizirovannoy dry mass of yellow (to 0,005 g) and the dark yellow to yellow-brown (at 0.05 and 0.1 g) color, soluble in water. Diluted gigroskopichen. In light of the fragile.

     On chemical structure similar to methotrexate folic acid (see), and is antimetabolitom- antagonist.

     In connection with antifolievym effect Mitosis drug suppresses cell growth actively proliferating tissues (including bone marrow), inhibits the growth of malignant neoplasms.

     Methotrexate applied inside as well as a sodium salt intramuscular injection, intravenously and intratekalno. When ingestion maximum concentration in the serum through a 2 - 4 h after intramuscular and intravenous, in the first hour. Quickly out of the body in urine.

     Assign methotrexate and its sodium salt alone or in combination chemotherapy for acute leukemia mieloblastnom limfoblastnom and, in the late stages of chronic mieloleykoza with lymphosarcoma; In combination chemotherapy in patients with breast cancer, lung ovaries. In high doses (under the guise of calcium folinata-see) apply also to diseases sarcoma, Ewing tumors, soft tissue sarcoma, horiokartsinome uterus.

     Inside designate methotrexate in the form of tablets.

     In treatment of leukaemia in adults appoint Mr 0.03 (30 mg), 2 times a week. The maximum daily dose for children 0,02 g (20 mg) for 1 m2 surface of the body. The course of treatment two weeks. With the dramatic rate designate an adult to 0.02 - 0,025 grams (20-25 mg) daily for 5 days. The break between courses 2 - 3 weeks.

     In horiokartsinome uterus appoint 0.05 g (50 mg), 1 in every 5 days. At treated 0,3 - 0,4 city Courses repeated intermittently at least 1 month. Assign well as higher doses : 15 - 30 mg daily for 5 days with breaks 1 - 2 weeks.

     The sodium salt of methotrexate impose intramuscularly, intravenous (struyno drip) or spinal canal. The contents of capsules dissolve in sterile isotonic sodium chloride solution.

     Adults with leukaemia designate sodium salt of parenteral methotrexate usually dose 0,01 - 0,03 g; Daily intake, 0.03 g (30 mg). Enter one or two times a week or one every four days. Children under the age of seven years imposed in a single parenteral and daily dose of 0,003 - 0,005 grams (3 to 5 mg), 7-14-0,005 - 0,015 grams (5-15 mg); In the course treatment introduce children under 7 years - 0,009 0,015 g (9-15 mg), 7-14-0,015 - 0,045 grams (15-45 mg).

     In horiokartsinome uterus using sodium salt metatreksata intramuscularly or intravenously in a single dose of 0.02 g (20 mg) daily for 5 days. Courses repeat 2 - 4 times in the primary treatment intervals from 2 to 4 weeks, with maintenance therapy-1 - 2 times.

     Total dose methotrexate and its sodium salt of 0.2 - 0.4 g (200-400 mg) for the previously sick patients and 0.1 - 0.2 g for patients who have been supportive therapy.

     In neyroleykoze (meningealnoy leukaemia) enter the sodium salt of methotrexate in the spinal canal (0.25% solution in a single dose of 0,005 0,01 g or 10 mg per 1 m 2 body surface at intervals of 3 to 4 days).

     In severe forms of disease and in cases where conventional-dose methotrexate weak (eg, osteosarcoma), methotrexate and its sodium salt sometimes used in high doses. This therapy has been made possible by the discovery of the properties of calcium antidotnyh folinata reducing toxic effects of methotrexate, without significant reduction in antitumor activity.

     When using methotrexate sodium salt in high doses, dissolve the contents of capsules (0.05, or 0.1 g product) in 400 ml isotonic sodium chloride solution. Enter drip for 3 to 4 hours in the adult dose of 200 mg / m 2 to 3 g / m 2 1 day a week. The course of treatment from 1 to 3 introductions. Repeated courses available through 3 to 4 weeks.

     During treatment of methotrexate in high doses required to monitor pH urine; In a day and the next 2 to 3 days reaction urine should be alkaline. This is achieved intravenous drip of a mixture of 40 mL 4, 2% solution of sodium gidrokarbonata and 400-800 ml isotonic sodium chloride solution, day in and day care within the next 2 to 3 days. Maxtrex in higher and higher doses are required, together with the additional hydration of 2 litres per day (ringer solution, 5% glucose solution with the addition panangina or 20 ml of 10% solution of potassium chloride).

     Maxtrex single dose of 2 g and above, to impose control of the drug in blood serum.

     Maxtrex also used to treat psoriasis. Usually appoint 2, 5 - 5, 0 mg inside 2 - 3 times a day, one day a week; Sometimes designate dose of 2, 5 mg 3 - 4 times a day rates 5-7 days with 3-day intervals. Applied also methotrexate in the treatment of psoriasis with pirogenalom.

     The drug is also effective in angioretikuleze Kaposi, mushroom avium and several other Medicine.

     In recent years suggested that methotrexate as a <baseline> in the treatment of rheumatoid arthritis. Applied oral or parenteral doses of 5, 0-7 5-15 0 1 mg once a week (at intervals of 12 to 24 hours between tricks dose). The course of treatment 18 months.

     In all cases of methotrexate should keep in mind that drug may cause side effects : nausea, diarrhea, stomatitis, and with a longer application-destruction ulcerated mucous membranes of the oral cavity with bleeding, hair loss, thrombocytopenia with a bleeding, anemia, perhaps becoming secondary infection ; possible toxic hepatitis, renal failure, etc.

     Applied preparation under the close supervision of a doctor. Diluted protivopokazn pregnancy, liver and kidney diseases, bone marrow.

     During treatment methotrexate to a study of the blood cells and platelets three times a week and at the end of treatment, one day a week during the month.

     While methotrexate should not appoint anticoagulants, musk and drugs that can suppress blood (sulfanilamidy etc.).

     Method of production : tablets, coated to 0.0025 g (2, 5 mg) in a package of 50 pieces; In capsules (for injection) to 0,005; 0.05 and 0.1 g (Methotrexatum 0,005; 0.05 et 0,1 pro injectionibus).

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