Estradiol

Chemical name

(17бета)-Эс� ffa �ра-1,3,5(10)-три ен-3,17-диол

Gross

C18-H24-O2

Characteristics

The white crystalline powder. Virtually nerastvorim water, it is difficult soluble in alcohol and vegetable oils.

Of drugs

Drugs, the mode. Penetrates into the nucleus of cells Organs, has been associated with selective receptor estrogennami and constitute retseptor-ligand. The latter interacts with the эстроген-эффекторным�� of the genome and the specific intrazellliarnami protein initiates I-rnk synthesis, protein and the release of Cytokines and factors Rosta.okazavaet feminizirutee impact on the organism that stimulates the vagina, uterus, fallopian tubes, and stroma ERCP mammary glands, pigmentatia of nipples and genitals, development of the secondary sex characteristics of the women's model (redistribution of adipose tissue, etc.), the growth and closure epifizov long tubular bones. Has enough time endometrium and regular bleeding, in high concentrations is giperplaziu endometrium, suppresses bone resorption tissue induces synthesis of a number of transport proteins (transkortin, tiroksinswyazawati OKT3, protein binding sex hormones, transferin) fibrinoguena. Increases concentration in the blood tiroksina, iron, copper, etc.; Provides prokoagulyantnoe effect on the blood, increases the synthesis in the liver vitamin K-zawisimah factors out (II, VII, IX, X), reduces antitrombina III. And антиатеросклеротичес кой activity increases the LPVP reduces certainty - and cholesterol (LDL level increases); modulating receptors to progesteronu and sympathetic regulation of the smooth muscle layer is the shift vnutrisosudistoi fluid in the tissue and compensatornuu delay sodium and water; in high doses prevents degradation of endogenous catecholamines (competes for active receptors �атехол-О-метилтрансф��разы).После reception inside quickly and completely absorbed (bioavailability about 100%). The "first pass" through the liver metabolized to less intensive products : estrona and estriola. The blood is almost entirely associated with belcom-perenoschikom. Are jelchew clearance in the small bowel and re-absorbed. The final loss of activity occurs as a result of oxidation in the liver. Products biodegradation are mainly news in the form of sulphate and glukuronidov; In the urine detected a small number of seconds, and estrona estriola.

Indications

Estrogennaya lack menopausal and after gynaecological operations delayed puberty in girls with alopecia giperandrogenemii, girsutizm with rheumatoid polikistozhnykh ovaries, weak clan of primary biliary cirrhosis in women, uterine bleeding, postkoichalnaya contraception, migraine and prevention of osteoporosis among women predmenopauzne period breast cancer for men and women with cancer (palliative therapy), carcinoma of prostate cancer (palliative therapy).

Contraindications

Hypersensitivity, cancer of the uterus, ovaries, breast estrogenzawisimae neoplasticskie processes endometriosis, disruption of tumors and liver, diabetes mellitus (insulinzawisimy to defeat receptacles), sickle cell anemia, herpes, otoscleros the deteriorating hearing, jaundice or permanent feat ff9 ure in the period before pregnancy, nediagnostirovannoe breeding bleeding, and throm embolic state (including the history), pregnancy, breast-feeding.

Side-Effects

Headache, dizziness, depression, migraine, trochaic, a violation of (the change of curvature of cornea), the AD embolism, nausea, vomiting, pain in epigastralna area, flatulence, holetsaticeski hepatitis, jelchnokamennaya disease, uterine bleeding, giperplazia endometrium, the increase in the size of the uterus, changes fibrosnye Oxytocics vaginal candidiasis, compaction and increased breast, changes Yeah, oedema, increased body mass index, lower tolerance to carbohydrates, attacks porfirii, hloazma, melanodermia, contact dermatitis, itching and hyperemia skin (on the ground software patch), allergic reactions.

Patient interaction

Effect reduce narcotic analgesics, tranquilizers, anaesthetic and anti preparations induktora mikrosomaionah enzymes Pecheni.umenishaet gipotenziveh activity, and antikoagulih gipoglikemicakih funds.

Overdosing

Symptoms : nausea, vomiting, and in some cases uterine Krovotechenia.lechenie : maintaining vital functions (in the face of the drug).

Precautions

With long-term therapy at least once a year a preventive examination.

Dosing and Administration

Inside. Primary and secondary estrogennaya inadequacy 1-2 mg once a day for 3 weeks, then break (1 week); Supporting dose selected SAC to the minimum effective. Cancer prostate-1-2 mg three times a day; Breast cancer for men and women, with a distant metastasis-10 mg three times a day for at least 3 months. To prevent osteoporosis - 0.5 mg once a day for 23 days, then five Pererav.gel cause once a day for the skin on the bottom of the front wall of the abdomen or between the left and right buttocks. Initial dose 1 g gel (1 mg seconds). The average dose-ranging gel grams a day. Area of the same size 1-2 Ladonyam.plastury be on the skin once a week. Treatment out continuously or three weekly courses with a break of one hour. At the same time, progesterone designate each month during the 10-12 Dnei.v / m, 0.1% solution in the oil and 1 ml once every 3-5 days.

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