ETHINYLESTRADIOL (Aethinyloe-stradiolum; synonym: Microfollinum (V), Diolyn, Dyloform, Ethynilestradiol, Ethynilestradiolum, Kolpolyn, Ora-diol, Ostral, etc.) — synthetic steroid hormone, in medicine is used as medicine. AA. treats group of estrogen (see) and represents 19-holes-17 and-pregna l-1,3,5 (10) -
triene-20-in-3,17 r-dio l:
On fiziol. activities at hypodermic introduction E. it is adequate to oestradiol (see), however at intake its activity considerably exceeds activity of this estrogen and its derivatives.
Pier. weight (weight) E. makes 296,41; g°pl 146 ° [a]D + 1 ° (in dioxane). AA. synthesize by addition of acetylene to estrone (see) in the presence of sodium amide. Small amounts E. synthesize by addition of acetylide of lithium to estrone in a dimethyl sulfoxide.
AA., as well as other oestrogenic drugs, apply at a hypo-ovaria, decrease in gonadotropic function of a hypophysis, an amenorrhea, a hypogenitalism, an underdevelopment of secondary sexual characteristics, climacteric and postkastratsionny frustration, infertility, dysfunctional uterine bleedings. Ethinylestradiol is a part of the majority combined oral estrogen-gestagennykh of contraceptives (see).
Drug represents powder of cream color, almost not water soluble, but alcohol-soluble and vegetable oils. Apply E. inside, doses select individually. At a hypogenitalism (primary amenorrhea) appoint usually 0,05 — 0,1 mg (0,00005 — 0,0001 g) of 1 — 2 time a day during 3 — 4 weeks then appoint gestagenny drugs (see Progestins). The course of treatment is repeated by 5 — 6 times. At a hypo-ovaria and a secondary amenorrhea drug is usually accepted in the same dosage during
2 — 3 weeks, then appoint gestagenny drugs throughout
6 — 8 days. At climacteric frustration to women up to 45 years E. appoint 0,01 — 0,02 — 0,05 mg daily within 12 — 15 days in a row with the subsequent reception of Pregninum within 6 — 8 days or other gestagenny drugs. The course of treatment is repeated by 2 — 3 times.
AA. it is, as a rule, transferred well, at reception of high doses nausea, dizziness are possible. Contraindications to use E. malignant and benign tumors of generative organs, however serve E. it can be applied (usually in combination with radiation therapy) at cancer therapy of a mammary gland at women 60 years are more senior, and also at a prostate cancer. In these cases drug is appointed in rather high doses (to 3 mg a day). Prolonged treatment. Besides, E. it is contraindicated at a mastopathy, an endometritis, tendency to uterine bleedings.
Form of release: tablets on 0,01 and 0,05 mg (0,00001 and 0,00005 g according to). Storage: in the place protected from light, the joint venture. B.
Bibliography: Gynecologic endocrinology, under the editorship of K. N. Zhmakin, M., 1980; The Medicines used in endocrinology under the editorship of H. T. Starkova and M. I. Balabolkin, page 110, M., 1983; Manuylova I. A. Modern contraceptive means, M.,
1983. „A. A. Pishchulin.