FTORURATsYL (Phthoruracilum; synonym: NSC — 19893, 5-ftoruratsit; cn. A) — antineoplastic means from group of antimetabolites, 2,4-dioxy-5-ftorpirimidin. On chemical structure it is close to a natural metabolite to uracil (see the Pirimidinovy bases).
White crystal powder with slightly yellowish shade. It is slightly soluble in water and alcohol. It is easily dissolved in hot water and solutions of alkalis.
Antineoplastic activity F. it is caused by the inhibition of enzyme thymidylate-sintetazy leading to disturbance of synthesis of DNA (see. Deoxyribonucleic acid), to synthesis of defective proteins (see the Mutation) and, eventually, to so-called bestiminovy death of tumor cells.
T. apply to cancer therapy of a stomach, colonic and direct guts, a pancreas, ovaries. Drug has a weak immunodepressive effect. Studying of cumulative properties F. showed that its full removal on -
«goes in 48 hours in this connection to lay down. it is necessary to appoint a dose of a ftoruratsil every other day. The drug is administered intravenously in a single dose of 10 — 15 mg/kg every other day, by no more than 5 times; total dose of 3 — 7 g. The course of treatment is repeated every 4 — 6 weeks. T. apply in a combination with derivatives of a nitrozomochevina (see. Antineoplastic means).a also radiation therapy (see).
T. causes by-effects in the form of nausea, vomiting, a loss of appetite, diarrhea, stomatitis and oppression of a hemopoiesis. Nausea and vomiting as a rule, are not the indication to drug withdrawal. At emergence of the first symptoms of stomatitis and diarrhea treatment shall be stopped. Toxic action F. on blood it is shown by a leukopenia and thrombocytopenia. At quantity of leukocytes 2500 — 3000, and thrombocytes 100 000 in 1 mkl blood treatment should be stopped.
Contraindications — - a cachexia, a serious cardiovascular illness, jaundice, the viral hepatitis postponed in the recent past, parasitic diseases of a liver.
Form of release: 5% solution in ampoules on 5 ml containing 250 mg of a ftoruratsil. Storage: in the dark, cool place at f not lower than 5 °.
See also Antineoplastic means.
Bibliography: Blochina N. G. and With about -
r about to and N and G. A. Conservative treatment of primary and recurrent malignant tumors of a stomach, Vestn. USSR Academy of Medical Sciences, No. I, page 86, 1981; Fleas
on N. G., etc. Antineoplastic drug Phthorafurum, M., 1981; Malignant new growths, under the editorship of A. N. Novikov and B. E. Peterson, century 1 (3), page 158, M., 1965; Duschinsky R.,
Ple ven E. H e i d e 1 b e r g e r C. The synthesis of 5-fluoropyrimidines, J. Amer.
• ehem. Soc., v. 78, p. 4559, 1957.
H. G. Blochina.