Medication Description: Cyclophosphan (Cyclophosphanum)
N-bis- (b-Chloroethyl) -N -O-trimethylene ether of phosphoric diamide.
Synonyms: Cyclophosphamide, Cyclophosphamide, Endoxan, Cyclophosphamide, Cyclophosphamidum, Cytofosfan, Cytophosphan, Cytoxan, Endoxan, Enduxan, Genoxal, Mitoxan, Procytox, Sendoxan, etc.
White crystalline powder. Soluble in water (1:50), easily soluble in alcohol, it is difficult in an isotonic solution of sodium chloride.
It is an alkylating cytostatic drug with a characteristic chemical structure: its molecule has two phosphamide bonds and one phosphoric ester bond; the synthesis was carried out in such a way that the drug had selective antitumor activity, i.e., that it was inactive while in the blood, but when it entered the tumor cells, it quickly decomposed under the influence of the relatively large amount of phosphatases (phosphamidases) contained in them with the release bis- (b-chloroethyl) -amine.
Thus, the drug can be considered as a prodrug with a <transport> function, delivering the active cytostatic substance to the tumor cells. Recently it has been established that phosphorus-containing active metabolites of cyclophosphane, which play an important role in the antitumor effect, are formed in the body. The drug has a relatively broad antitumor spectrum of action and has a milder effect than thrombocytopoiesis than other similar drugs.
Cyclophosphamide is used in small cell lung cancer, ovarian cancer, breast cancer, reticulosarcoma, lymphosarcoma, chronic lymphocytic leukemia, acute lymphoblastic leukemia, multiple myeloma, Williams tumor, bone reticulosarcoma, Ewing tumor, angiosarcoma.
Enter intravenously, intramuscularly inside, as well as in the cavity.
Different treatment regimens are used: a) 200 mg (3 mg / kg) daily or 400 mg (6 mg / kg) every other day (orally, intravenously or intramuscularly); b) 1 g (15 mg / kg) 1 time in 5 days intravenously; c) 2–3 g (30–45 mg / kg) 1 time in 2–3 weeks intravenously. The course dose for all treatment regimens is 6–14 g. Other treatment regimens are also used.
When fluid accumulates as a result of a cancerous process in the abdominal and pleural cavities, in addition to intravenous infections, 0.4–1.0 g of cyclophosphane is injected into the cavities (at each puncture). The amount of the drug injected into the vein, while reducing accordingly. After the end of the main course of treatment with cyclophosphamide, supportive therapy can be applied: 2 times a week they are administered intravenously (or intramuscularly) in 0.1 0.2 g of the drug or administered orally in the form of tablets in 0.05-0.1 g 2 times in day. Taking the drug inside is convenient for long-term therapy.
Cyclophosphamide is also used as an immunosuppressive agent. It suppresses (like other cytostatics) the proliferation of lymphocyte clones involved in the immune response. At the same time, it acts primarily on the lymphocytes. There is evidence of the use of cyclophosphamide in glomerulonephritis, lupus erythematosus, rheumatoid arthritis, nonspecific aortoarterititis.