ESTR O N — steroid hormone; 3 - a gidroksiestra - 1,3,5(10) - triene - 17 - it;
AA. is one of natural estrogen (see), it biol. activity is lower, than at oestradiol (see). In medical practice estrone is used as medicine. Fiziol. effect of the estrone entered into a human body or an animal, substantially is defined by his turning into oestradiol, from to-rogo it differs in presence at a molecule of ketogroup at the 17th situation.
Pier. the weight (weight) of estrone makes 270,38; * 0PL2590, [a] D + 160 ° (in chloroform). AA. contains in urine of pregnant women and animals, ovaries and a placenta; it is found also in stones of garnet (17 mg/kg) and in palm oil.
In 1929 E. Doyzi and A. Butenandt independently from each other received E. in a crystal look, having allocated it from urine of pregnant women. In 1948 G. Anner and Misher (To. Miescher) carried out chemical analysis E. Now small amounts E. receive from urine of pregnant animals (most often horses), and large numbers — pyrolysis androsta-1,4-di-en-3,17-diona, formed of cholesterol or sitosterol by microbic oxidation, or the method offered by the Marker (R. E. Marker) and consisting in transformation of the diosgenin (see Saponins) received from plants of the sort Dios-sogea into progesterone (see). This method since 1950 is one of the main a lab. methods of receiving all steroid hormones (see). Estrone serves as mother substance for chemical synthesis of others pharmacological of important estrogen — oestradiol and ethinylestradiol (see).
Estrone is an end product of a steroidogenesis in ovaries and seed bubbles (see). Most part E., circulating in blood, it is formed of oestradiol since balance of a reversible test an estra-diol-17 of P+ of N of A D+ ^ estrone + OVER • N is displaced towards formation of estrone. This reaction oestradiol — 17 r-degidro-genaza catalyzes enzyme (KF 1.1. 1. 62). Synthesis E. occurs as in cells of a granular layer of the ripening follicle (see. Menstrual cycle), and in peripheral fabrics. At pregnancy synthesis E. sharply and steadily
niya of this hormone increase in a placenta from the degidroepiandrosteron arriving from adrenal glands of a fruit for the account obrazova-.
In blood E. circulates in the form of a conjugate with a chamois to - that (estrone-sulfate), to-ry E. Dinamika of changes of concentration E is metabolized more slowly, than actually. in blood at women throughout a menstrual cycle reminds dynamics of concentration of an estradnol, however it is less expressed. In the period of ovulatory peak concentration E. reaches 100 — 350 pg/ml; men have a concentration E. in blood it is normal equal 30 — 60 pg! ml.
Daily excretion E. with urine at women in the period of ovulatory peak makes 9,2±1,3 mkg (definition by a colorimetric method), in a phase of a yellow body of a menstrual cycle it is lower — 6,8±1 mkg; at men aged from 18 up to 60 years removal E. with urine 2,3±0,2 mkg a day are equal.
Estrone as drug. Estrone (Oestronum; synonym: Folliculin, Gristallovar, Estronum, Estrone, Estrugenone, Glandubolin, Men-formon, Oestrobin, etc.) represents white crystal matter, not water soluble and alcohol-soluble, ether, oils.
At introduction to an organism E. has the specific effect inherent to all oestrogenic drugs: causes proliferation of an endometria, stimulates development of a uterus and female secondary sexual characteristics at their underdevelopment, levels the general frustration resulting from a hypo-ovaria, castration and also in a climacteric.
Activity E., defined, as well as activity of other estrogen, on ability to cause in the castrated females of mice or rats a spout (estrus), is expressed in so-called mouse or rat units (PIECE); 1 mg of drug contains 10 000 PIECES.
Estrone is applied, as well as other oestrogenic drugs, at a hypo-ovaria and patol. states, related: at primary and secondary amenorrhea, secondary sexual insufficiency, a hypoplasia of generative organs and an underdevelopment of secondary sexual characteristics, climacteric and pooggkast-ratsionny disorders, infertility, weakness of patrimonial activity, for a rodovozbuzhdeniye at postmature pregnancy. Sometimes E. appoint at increase in the ABP in a climacteric and at spasms of peripheral vessels. AA. enter intramusculary in the form of oil solutions. At primary amenorrhea with an underdevelopment of generative organs and secondary sexual characteristics enter 10 000 — 20 000 PIECES of drug daily or every other day within
1 — 2 month and more before emergence of a symptom of «pupil» (see. Menstrual cycle), after that appoint progesterone within 6 — 8 days on 5 — 10 mg daily or other progestins (see) in equivalent doses. If necessary the course of treatment is repeated. At a secondary amenorrhea enter on 10 000 PIECES of estrone within 15 — 16 days, in the subsequent progesterone or Pregninum. At an oligomenorrhea, the infertility connected with a hypo-ovaria and an underdevelopment of a uterus, AA. appoint from
the 5th day of a menstrual cycle daily on 5000 — 10 000 PIECES of drug within 15 days, then within 6 — 8 days carry out therapy by progesterone or Pregninum. The course of treatment can be repeated several times.
At climacteric or post-kastratsionnom syndromes with the expressed vegeto-vascular or psychological frustration (a depression, etc.) estrone is entered on 5000 — 10 000 PIECES daily or in 1 — 2 day courses on 10 — 15 injections with the subsequent purpose of progestins. During the resuming of symptoms of a disease treatment by estrone is continued, however it is necessary to select strictly individually minimal effective doses of drug. At weakness of patrimonial activity and for a rodovozbuzhdeniye at postmature pregnancy appoint E. (or other oestrogenic drugs) for the purpose of sensitization of a uterus to oksito-tichesky substances, especially at a so-called unripe neck of uterus (see Childbirth). Intramusculary or 2 — 3 times enter every 2 — 3 hour 20 000 — 30 000 PIECES of estrogen into a back lip of a neck of uterus.
Contraindications to appointment E., as well as other oestrogenic drugs, malignant and high-quality new growths, a breast cancer (at women 60 years are younger), a mastopathy, tendency to uterine bleedings serve.
Form of release: the domestic
drug Solutio Folli-culini oleosa pro injectionibus in ampoules on 1 ml of 0,05% (5000 PIECES) and 0,1% (10 0000 PIECES) of solution (an oily liquid of light yellow color). Storage: in the cool, protected from light place.
Bibliography: Gynecologic endocrinology, under the editorship of K. N. Zhmakin, M., 1980; Rosen V. B. Fundamentals of endocrinology, M., 1984; Fizer JI. and Fizer M. Steroids, the lane with English, M., 1964.
V. S. Zelenetskaya.