ESTROGEN SINTETYCHES of KIA NESTEROIDNYE — the chemical compounds having oestrogenic activity, but unlike natural estrogen not being steroids or their derivatives; in medicine are applied as pharmaceuticals.
Use E. the page of N in medical practice is caused by need a wedge, uses of the drugs having various oestrogenic activity and duration of action, different portability, and also a possibility of their use in oncology. K E. pages of N, being pharmaceuticals, belong hexestrol (see), Dimoestrolum (see), benzestrol, Sygethinum, and also diethylstulbestrole which is more and more forced out by Fosfestrolum (see) which does not have negative side effect of diethylstulbestrole. All these drugs in the chemical relation represent derivatives of stilbene:
AA. pages of N are crystal substances, not soluble or low solubility in water and well alcohol-soluble, ether, vegetable oils.
AA. the village of N, derivatives of stilbene, have fiziol. activity of estrogen (see), on to-ruyu the route of administration of drug also influences. So at intake activity of derivatives of stilbene is located in
the following sequence: diethylstulbestrole> dienestrol (one of synthetic nonsteroid estrogen)> hexestrol (Hexoestrolum) whereas at parenteral administration the order of their activities changes: diethylstulbestrole> hexestrol> dienestrol. Degree fiziol. activities E. the page of N, as well as natural estrogen, determine by their ability to cause a spout (estrus) in the castrated mice or rats. Activity E. pages of N express in so-called mouse or rat units (PIECE).
The pharmaceuticals which are E. pages of N, apply generally according to the same indications, as estrone (see), oestradiol (see) and other oestrogenic drugs. AA. pages of N appoint at a hypo-ovaria, an underdevelopment of generative organs, primary and secondary amenorrhea, climacteric and postkastratsionny frustration, dysfunctional uterine bleedings, weakness of patrimonial activity, etc.
Treatment E. villages of N, as well as other estrogen, carry out under control of tests of functional diagnosis. After achievement of a sufficient estrogenization (see. A menstrual cycle) progestins appoint (see): 0,5 — 1 ml of 1% of solution of progesterone intramusculary within 6 — 8 days or 2 ml of 12,5% of solution of pregnenoldione of a kapronat intramusculary once. AA. villages of N use also at treatment of adenoma and prostate cancer at men, and also at women 60 years are more senior than a breast cancer.
Usually these drugs are transferred well, however nausea, vomiting, dizziness are in some cases noted. At appointment E. pages of N in high doses can appear signs of toxic damage of a liver, excessive proliferation of an endometria and uterine bleedings at women, feminization at men. Gastrointestinal frustration and an allergy are in rare instances possible.
AA. pages of N are contraindicated at pregnancy, diseases of a liver and kidneys, tumors of mammary glands (at women 60 years are younger) and a uterus, at acute inflammatory diseases of generative organs.
Oktestro of l (Octoestrolum; synonym: Benzestrol, Benzestrolum, Os-tofolin) — 2,4-di-(? oxyphenyl) - 3-ethyl-hexane:
Drug of benzestrol represents white crystal powder, difficult soluble in ho
to fine water, easily soluble in hot water and not alcohol-soluble.
On activity benzestrol is similar to hexestrol (biol. activity of 1 mg of benzestrol corresponds to 10 OOO ED). At intake drug is quickly soaked up and does not collapse in went. - kish. path. At an underdevelopment on -» lovy bodies, an amenorrhea, an oligomenorrhea daily appoint 0,001 — 0,003 g of benzestrol. At the expressed oestrogenic insufficiency and an underdevelopment of generative organs the course of treatment can be prolonged up to 3 — 6 months, and in the beginning administration of drug can be continuous, without connection of gestagenny hormones.
Form of release: tablets on 1 mg (0,001 g). Storage: in the place protected from light, the joint venture.
B. S and e t and N (Sygethinum) — di-kal iyevy salt zhezo-3,4-di-(p-sul-fofenil) - hexane:
Drug of Sygethinum represents white crystal powder, easily soluble in hot water. Sygethinum has no specific oestrogenic effect, but in connection with influence on gonadotropic function of a hypophysis and on the hypothalamic centers (see Gipota-lamo-gipofizarnaya system) is effective at easy climacteric frustration. Sygethinum strengthens reduction of a uterus and improves placental blood circulation, possesses hypolipidemic action.
Sygethinum is generally appointed for treatment of pre-natal asphyxia of a fruit. At the same time to the woman in labor enter intravenously 2 — 4 ml of 1% of solution of Sygethinum into 20 — 40 ml of 20% of solution of glucose. For prevention of the menacing pre-natal asphyxia of a fruit of the pregnant woman intramusculary or intravenously enter 1 — 2 ml of 1% of solution of Sygethinum daily within 10 days. At climacteric frustration Sygethinum is appointed inside on 0,1 g once a day or on 0,1 g of 1 times in 2 days.
At the time of delivery at massive blood loss at the woman in labor and premature placental detachment use of Sygethinum is contraindicated.
Form of release: tablets on 0,1 g and ampoules on 1 and 2 ml of 1% of solution. Storage: in the dry, protected from light place, the joint venture. B.
Bibliogrkosheleva N. G. Use of Sygethinum for prevention of perinatal mortality and incidence after the complicated current of the first half of pregnancy, Akush. and ginek., JSft 3, page 40, 1971; The Medicines
used in endocrinology under the editorship of H. T. Starkova and M. I. Balabolkin, page 97, etc., M., 1983; Marinbakhe. B. Prostate cancer, page 135, M., 1980. A. A. Pishchulin.