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Estrogens, gestagena; Their homologues and antagonists
The groupMan follikuliarnami league are formed ovaries estradiol, estron and estriol. These hormones called estrogenami because they cause castrate female animals tecku (estrus).
However, hormone yellow body follikuliarnae hormones involved in the regulation of menstrual cycle and reproduction functions. During pregnancy a hormone follikuliarnah considerably strengthened large number are in the urine.
The state-of-the-art in the relevant bodies (organa-misheni) are specialized receptors for estrogen, through interaction which are their effects.
With the organism estrogenic drugs (natural and synthetic origin) of a specific mode Effects : proliferatiou endometrium, promoting a uterus and women's secondary sexual characteristics, especially when nedorazvitia mitigate and eliminate common disorders (osteoporosis, arteriosclerosis, atrophic skin and mucous urogenital system) arising in the body of women on the grounds of insufficient sex glands menopausal or after gynecological operations (ovarioektomii). Estrogens involved in the formation and maintenance of the strength of the bone, reduce its resorption, normalize balance between osteoblastami and osteoclastami (both cells contain estrogen receptors). The violation of estrogen in the body (in menopause, and ovarioektomii, etc.) has been accompanied by an increase in rezorbtion bone development of osteoporosis and increased bone fractures.
Estrogenic drugs used in the pathological conditions associated with a lack of ovarian function : in primary and secondary amenoree, secondary sexual failure hypoplastic sexual apparatus and secondary sexual characteristics, as climacteric or postcastraih disorders, for the prevention and treatment of osteoporosis in menopausal women with barrenness, the weakness of labor activity, perenosenna pregnancy, etc. Sometimes they appoint as in hypertensive disease for women in menopause and with the peripheral spazmah receptacles.
Estrogens are гипохолестеринемичес кое act, but their use for the treatment and prevention of atherosclerosis in men is complicated by the fact that the long-term use is feminization. Because of estrogena proliferativee changes in endometrii to protect against hyperplasia in hormone replacement therapy for women intaktna the uterus must be within 10 to 12 days each cycle of treatment in postmenopause add gestagen (Klimonorm, Divina, etc.) and postmenopause with continuous admission appoint daily combination of estrogen with gestagenom (Klimodien).
Admission oestrogen preparations should be carried out under the close medical supervision. Estrogenic drugs protivopokazana women with malignant and benign tumors of the reproductive organs, mammary glands and other organs (under age 60), with mastopatii, endometrite, propensity for bleeding of the uterus, and the phase giperestrogenna menopause.
Effects estrogen antiestrogenami weakened. Products of this group specifically associated with estrogenozawisimami receptors (estrogen receptor) in the Hypothalamus and aicnikah. In small doses, they increased secretion gipofizarnah gonadotropinov (prolactin, фолликулостимулирующ его luteinizirutego and hormones), and stimulate ovulation, that is, have a moderate oestrogenic effect which clinically manifests itself only with insufficient endogenous estrogen. However, with a high level of estrogen these drugs cause the opposite effect. Decreasing levels of circulating estrogen, oppressive highly incretia gonadotropinov, they increase the secreta. In high doses antiestrogena down gonadotropinov secretion. Gestagenna and androgenna activity they do not have.
Gestagena (hormones, the ovaries producyruemye) on the feedback block the secretion of factors gipotalamicakih release and luteinizirutego фолликулостимулирующ его hormones, hurt education gipofizom gonadotroponah hormones and prevent ovulation.
Testimony to the application gestagenov are functions of the ovaries caused by insufficient yellow body, dysfunctional uterine bleeding, menstrual irregularities (amenorea, oligomenorea, algomenorea) and others.
Based on gestagenov and estrogen (and androgennah and antiandrogennah preparations with the addition, in some cases, for other pharmaceutical groups) created a large number of combined drugs, including ""антиклимактерически х"" and preparations for the treatment of oncological diseases. It should be borne in mind that, along with the act they may have side effects inherent within their composition components.
Hormonal preparations containing gestagena, estrogena or combinations used as oral contraceptives.
Gestagenov use as a contraceptive based on their ability to block the release of rilizing-factorov (and luteinizirutego фолликулостимулирующ его) hypothalamus, oppress secretion gipofizom gonadotroponah hormones and inhibit ovulation. The combined application with gestagenov estrogenami reliability of contraception increased. Along with the impact on the gonadotroponuu a role in the contraceptive effects are other factors (for example, changes in the chemistry vaginal environment and increasing viscosity sheecna mucus impeding the mobility of sperm, or endometrium, making egg implantation, etc.). Modern oral contraceptives divided into groups :
a) monofaznae gestagen-estrogenne drugs (Logest, Jeanine, Ovidon, Rigevidon, Miniziston, etc.);
b) two-and three gestagen-estrogenne drugs (Anteovin, Triziston, Triqvilar, Tri-regol, etc.);
c) monegromonale gestagenne preparations mini-pili (Mikrolut).
Gestagennami components gestagen-estrogennykh contraceptives are levonorgestrel, gestoden, dienoguest and other synthetic gestagena, superior activity progesterone and operating at the level of receptors without metabolic transformations, and oestrogenic component is ethinylestradiol-quality oral mode tool.
Monofaznae products shall also endometriose, dysfunctional uterine artistic methods, amenoree, predmenstrualnom, menopausal syndrome and other gynecological diseases.
The ability gestagena such as acetate ciproteron antiandrogennah properties led to the development of combined hormonal drug Diana, 35, it is shown to women who themselves against unwanted pregnancies and suffering androgenzawisimami diseases (acne, girsutizm, palliative, androgenetica alopecia).
Two, three drugs produced in the form of tablets with different quantities gestagena and estrogen and are "kalendarno" " the emotional flow menstrual cycle. Three drugs are usually appointed if monofaznah use of hormonal contraceptives is bleeding repeal or a breakthrough bleeding.
Mini-pili contain minimum number gestagena needed for contraception; Assigned mainly with contraindications to the use of combined gestagen-estrogennykh drugs. Even a lower number of hormone into the body, to use intrauterine гормоновысвобождающу ю system, which directly to the uterus is a daily 20 µ g levonorgestrel.
If the effect of oral contraceptives dispensed with the constant applied for a certain period of time and reliability of contraception depends to a great extent on the carefully with a reception, the uterus system gestagenom (Mirena) guarantees contraceptive effect comparable to sterilization.