TAMOXIFENUM (Tamoxifen; synonym: Nolvadex, Zitazonium; joint venture. B) — the antineoplastic means relating to group of anti-oestrogenic drugs; citrate 1-[4-(2-dimethyl-amino-этокси) phenyl] - trance-1,2-diphenyl-1-butene:
Colourless crystal powder, without taste, soluble in hot water, in methanol.
T. specific oestrogenic antagonist. It forms a complex with oestrogenic receptors and interferes with linkng of estrogen (oestradiol) with them in target tissues (a mammary gland, a uterus, etc.). As a result of it it is oppressed biol. effect of estrogen.
T. apply at cancer therapy of a mammary gland. An opportunity a wedge, uses of T is studied. at an oligospermatism, anovulatory infertility, the termination of a lactation after the delivery, and also at a hysterocarcinoma, a kidney and a prostate. According to indications it is appointed in combination with other antineoplastic means and radiation therapy. At the disseminated forms of a breast cancer efficiency of T. at the women who are in a menopause fluctuates, according to various data, from 27 to 52%. Women in the preklimakterichesky period have an efficiency of T. below, and objective improvement is observed at 25 — 38% of patients. T. can be effective at emergence of resistance to other hormonal drugs, and also at metastasises in a bone. The greatest efficiency of T. it is noted at metastatic defeat of soft tissues and rather smaller — at metastasises of a tumor in bones and internals. In the presence in tumoral tissue of oestrogenic receptors efficiency of treatment considerably increases. On the contrary, at patients with the tumors deprived of oestrogenic receptors, positive action decreases. Tamoxifenum does not concede by efficiency to estrogen and androgens, but considerably surpasses them in portability.
T. appoint inside in tablets on 10 — 20 mg twice a day for a long time. Breaks in treatment are undesirable. The general duration of a course of treatment depends on a form of a tumor, portability of drug and its efficiency. The minimum duration of a course — apprx. 3 months. At effective treatment the health of patients usually improves, pains are stopped, functions of the struck bodies are normalized, primary tumor and metastasises are exposed to full or partial regression.
T. it is well transferred by patients. By-effects are observed infrequently and are expressed much more weakly, than during the use of estrogen and androgens. Anorexia, nausea can be observed, it is rare — vomiting. Anti-oestrogenic action at nek-ry patients is expressed in emergence of inflows, an itch in a crotch, bloody allocations from a genital tract, an enanthesis of the person, a breast and a back. At a part of patients in the first 1,5 — 2 weeks of treatment temporary strengthening of pains in zones where tumoral nodes are located is noted. Extremely seldom there are hypostases, thrombophlebitises, a cataract develop, the level of sugar in blood increases. By-effects usually disappear at decrease in a daily dose of drug or a short-term break in treatment.
T. it is contraindicated at pregnancy.
Form of release — tablets on 10 mg. Store in the dry place protected from light at a temperature not over 25 °.
See also Antineoplastic means .
Bibliography: Dementieva N. P., Assn.Ya. and Vozny E. K. Experience of use of Tamoxifenum for patients with the disseminated breast cancer, Klin, medical, t. 57, No. 5, page 50, 1979; D I eat e with N of t e in and N. P., etc. Tamoxifenum in treatment of patients with the disseminated breast cancer, Vopr. onkol., t. 27, No. 8, page 30, 1981; Fabian C. and. lake of Clinical pharmacology of tamoxifen in patients with breast cancer correlation with clinical data, Cancer, v. 48, p. 876, 1981; Ferrazzi E.a. o. Tamoxifen in disseminated breast cancer, Tumori, v. 63, p. 463, 1977; Pritchard K. I. a. o. Tamoxifen therapy in premenopausal patients with metastatic breast cancer, Cancer Treat. Rep., v. 64, p. 787, 1980.
V. D. Sokolova.