PODOPHYLLINUM (Podophyllinum; joint venture. A) — the antineoplastic means relating to group of alkaloids. Represents mix of the connections which are contained in roots of a may-apple thyroid (Podophyllum peltatum L.). The most active connections in this mix are podophyllotoxin, alpha and beta peltatiny.
The item is alcohol-soluble, water-insoluble also oil.
The item has cytopathic activity, blocking mitoses in a stage of metaphase and suppressing proliferative processes in fabrics, has also laxative and cholagogue effect.
Earlier P. applied locally (at papillomas of a bladder, a papillomatosis of a throat, sharp-pointed condylomas, etc.). New semi-synthetic derivative P. are of interest: Vm-26 (synonym: Epipodophyllotoxin Vm-26, tenipozid) and Vp-16 (synonym: Epipodophyllotoxin Vp-16-213, etopozid). Both drugs have low molecular weight, badly rastvorima in water, are characterized by limited stability in solutions. Epiiodo-fillotoksina block a cellular cycle in the phase G2, reducing a mitotic index.
Drugs are removed by kidneys in 3 days, Vm-26 of hl. obr. in a meta-bolizirovannom look, a Vp-16 — generally in not changed look.
Despite a similar chemical structure and the mechanism of action, the drugs Vm-26 and Vp-16 have various range of antineoplastic activity.
Vm-26 apply to treatment of tumors of a brain, a lymphogranulomatosis and lymphosarcomas, ovarian cancer and a bladder; Vp-16 is effective at small-celled cancer of a lung, lymphosarcomas, an acute myeloleukemia, malignant tumors of a small egg.
Vm-26 enter intravenously 30 mg/m 2 (0,8 mg/kg) daily within 3 — 5 days in 2 — 4 weeks or on 100 mg/m 2 (2,7 mg/kg) intravenously once a week during 2 — 4 weeks of Vp-16 enter intravenously or orally. There are three schemes of intravenous administration: on 50 mg/m of % (1,4 mg/kg) daily within 5 days in 2 — 4 weeks; on 125 — 140 mg/m 2 (3,4 — 3,8 mg/kg) every other day 3 times; on 200 — 300 mg/m 2 (5,4 — 8,1 mg/kg) once a week during 2 — 4 weeks. It is orally possible to apply 60 mg/m 2 (1,6 mg/kg) daily within 5 days in 2 — 4 weeks and on 160 mg/m 2 (4,3 mg/kg) 3 times a week during 2 — 4 weeks.
At treatment of Vm-26 and Vp-16 oppression of a hemopoiesis, nausea, vomiting, diarrhea, anorexia, stomatitis, an alopecia, decrease in the ABP, arrhythmia, phlebitis, fervescence, paresthesias, numbness of finger-tips, decrease in reflexes, seldom trophic disturbances can be observed.
Form of release: bottles on 25 — 100 mg, capsules on 25 — 50 mg. Keep in the dry, cool, protected from light place.
See also Antineoplastic means .
Bibliography: Bulkina 3. P. Antineoplastic drugs, page 91, Kiev, 1978; Larionov L. F. Chemotherapy of malignant tumors, page 223, M., 1962; Radice P. A., Bunn P. And. and. I h d e D. Page of Therapeutic trials with VP-16-213 and VM-26, active agents in small lung cancer, non-Hodgkin’s lymphomas and other malignancies, Cancer Treatm. Rep., v. 63, p. 1231, 1979.
H. I. Perevodchikova.