OESTRADIOL — steroid hormone; estra-1,3,5 (10) - triene, 3,17 (a J-diol, or 17r-oestradiol:
AA. is the main and most active natural hormone of group of estrogen (see). Derivatives E. apply in medicine as pharmaceuticals.
In a crystal look E. E. Doyzi in 1935 ostradiol was for the first time received it is synthesized in ovaries (see) and seed bubbles (see), as his direct biosynthetic predecessor serves testosterone (see).
Pier. weight (weight) E. makes 272,4, * °pl 178 °, [a]D + 81 °. Stereoisomer of 17P-oestradiol, a 17a-estra-diol, has t°UJ1 222 °, [a]D + 54 °. It possesses only V350 biol. the activity shown 17P ~ by oestradiol.
The highest concentration E. note in urine of pregnant women, in graafovy bubbles (follicles) and in a placenta. At nonpregnant women of childbearing age about 300 — 700 mkg of oestradiol a day are developed. Contents E. in blood of women with normal ovarian function throughout a menstrual cycle (see) changes as follows: in an early phase of maturing of a follicle concentration E. in blood does not exceed 100, in the period of ovulatory peak increase in concentration E increases up to 200 — 290 pg/ml. in a phase of a yellow body reaches apprx. 150 pg! the ml also gradually decreases, the size of this «plateau» has significant individual differences. Nemeta-bolizirovanny E. it is excreted with urine in the form of conjugates with glucuronic and sulfuric to-tami. Excretion E. at women in the period of ovulatory peak makes 5,07 ± 0,76 mkg a day, in a phase of a yellow body 4,11 ± 0,59 mkg a day; men have from 18 to 60 years excretion E. with urine makes 1,56 ± 0,25 mkg a day.
In medicine as pharmaceuticals apply oestradiol Dipropionas, marked an estrabottom of l and ethinylestradiol (see).
Oestradiol Dipropionas (Oestradioli dipropionas; synonym: oestradiol propionate, Dimenformon dipropionate, Diogyn DP, Diovocyc-lin, Estradiol Dipropionate, Synfor-mon, etc.):
Drug of oestradiol of Dipropionas represents white crystal powder, almost not water soluble, difficult alcohol-soluble and vegetable oils. Drug is slowly soaked up and slowly collapses, exerting long impact on an organism.
Oestradiol Dipropionas is applied at a wedge, manifestations of a hypo-ovaria, primary and secondary amenorrhea, a hypoplasia of generative organs and an underdevelopment of secondary sexual characteristics, at climacteric and postkastratsi-onny frustration, weakness of patrimonial activity, to a rodovozbuzh-deniye at postmature pregnancy.
Administer the drug intramusculary in the form of 0,1% of oil solution on 1 ml of 1 times in 3 — 5 days. The scheme of treatment and its duration are established individually.
As contraindications to use of oestradiol of Dipropionas, as well as other estrogen, serve malignant and benign tumors (including tumors of generative organs), mastopathies, tendency to uterine bleedings, the giperestro-genius in a climacteric.
Form of release: ampoules on 1 ml of 0,1% of solution (1 mg of oestradiol of Dipropionas, 10 000 PIECES) in oil. Storage: in the cool, protected from light place, the joint venture. B.
Estradiola Dipropionas is a part of the combined drug of a klimakteriya, to-ry apply at vegeto-vascular and neurotic frustration and a menopausal syndrome. Drug is produced in ChSSR.
Methyloestradiolum (Methyloe-stradiolum; synonym of Follikosid):
Methyloestradiolum is synthetic oestrogenic drug, the methyl group at the 17th carbon atom in its molecule leads
to strengthening of oestrogenic activity and increases stability of drug in comparison with initial E. Metilestradiol well is soaked up by a mucous membrane of an oral cavity, does not collapse enzymes of saliva and therefore it can sublingual be applied.
Indications and contraindications to use marked an estrabottom of l and the same, as for oestradiol of Dipropionas and other estrogen.
Apply Methyloestradiolum in tablets sublingual (to a full rassasyvaniye) on 0,02 mg (0,00002 g) of 1 — 3 time a day within 10 — 15 days then appoint progestins (see). At most of patients several (3 — 6) courses of treatment are carried out. Sometimes at reception of Methyloestradiolum nausea develops.
Form of release: tablets on 0,02 mg on 20 and 50 tablets in packaging. Storage: in bottles of orange glass in the dry, protected from light place, the joint venture. B.
See also Hormonal therapy.
Bibliography: Rosen V. B. Bases of an endo-krionologiya, M., 1984; Physiology of endocrine system, under the editorship of V. G. Baranov, page 341, L., 1979. V. S. Zelenets of Kai.