Proginova

Estrogen drugs – 17-beta-Estradiol identical эndogennomu эstradiolu (formed in the body women, from the first menses until menopause), produced by the ovaries. The cells of, for which directed the action of hormones, Estrogens are complexed with specific receptors (found in various organs – in utero, vagina, urethra, mammary gland, liver, gipotalamuse, gipofize), receptor-ligand complex is reacted with the effector elements of estrogen-genome specific intracellular proteins, and induces the synthesis of RNA, proteins and the release of cytokines and growth factors. It has a feminizing effect on the body. It stimulates the development of the uterus, the fallopian tubes, vagina, stromal and ductal mammary, pigmentation in the nipples and genitals, formation of secondary sexual characteristics of female type, growth and epiphyseal closure of the long bones. It contributes to the timely and regular rejection of the endometrium bleeding, in large concentrations causes endometrial hyperplasia, suppresses lactation, inhibits bone resorption, It stimulates the synthesis of a number of transport proteins (tiroksinsvяzыvaющiй globulin, transcortin, transferrin, protein, sex hormone binding), fibrinogen.

It has procoagulant effect, increases synthesis in liver vitamin K-dependent coagulation factors (II, VII, IX, X), reduces the concentration of antithrombin III. It increases blood concentrations of T4, Fe, 2 и др. It has anti-atherosclerotic effect, increases the concentration of HDL, decreases – LDL and cholesterol (concentration increases TG). Modulates sensitivity to progesterone receptors and the regulation of sympathetic tone of smooth muscles, It stimulates transition intravascular fluid into the tissue and causes a compensatory delay Na and water. In large doses, it prevents the degradation of endogenous catecholamines, competing for receptor activity of catechol-O-methyltransferase.

After menopause, the body is formed only a small amount of estradiol (of estrone, located in the liver and adipose tissue). Reducing the concentration of estradiol produced by the ovaries is accompanied by many women and thermoregulatory vasomotor instability (“tides” of blood to the skin of the face), sleep disorders, and progressive atrophy of the urogenital system. As a result of estrogen deficiency develop osteoporosis (mainly spine). Known, that oral administration of estrogen causes an increase in protein synthesis (incl. Renin), which leads to increased blood pressure. Estradiol as a transdermal patch, attachable to the skin portion. The control membrane provides a gradual and continuous release of estradiol from the reservoir with the active substance through the adhesive layer to the skin. Due to the lack of effect “first pass” through the liver TTS provides high efficiency in the use of smaller doses of the drug. TTS delivering estradiol unaltered to the bloodstream and maintains its concentration in plasma during therapy constant, adequate level in the early or middle phase of the follicle.

Estrogen deficiency in menopause and surgical menopause on the non-malignant neoplasms, after radiation castration; primary and secondary amenorrhea, gipomenoreя, spanomenorrhea, dysmenorrhoea, secondary estrogen deficiency. Hirsutism in polycystic ovary syndrome, vaginitis (in girls and in old age), gipogenitalizm, infertility, uterine inertia, prolonged pregnancy, to suppress lactation, virilnoe hypertrichosis in women. Postmenopausal osteoporosis. Breast and breast cancer, prostate cancer, urogenital disorders (dyspareunia, Atrophic vulvovaginitis, uretrit, tryhonyt), alopecia in giperandrogenemii. As PM, stimulating hematopoiesis in men with acute radiation injury.

Hypersensitivity, pregnancy, estrogen-dependent malignant tumors or suspicion on them, unusual or undiagnosed genital or uterine bleeding, thrombophlebitis or thromboembolic disease in active phase (except for the treatment of breast and prostate).C care. Thrombophlebitis, thrombosis or thromboembolism (while taking estrogens in history); family hyperlipoproteinemia, pancreatitis, endometriosis, gallbladder disease in history (especially cholelithiasis), severe liver failure, jaundice (incl. a history of previous pregnancy during), hepatic porphyria, leyomyoma, hypercalcemia, associated with bone metastases of breast cancer. Only for the treatment of breast and prostate: diseases of the coronary or cerebral vessels, active thrombophlebitis or thromboembolic disease (High doses of estrogen, used to treat, increase the risk of myocardial infarction, pulmonary vessels, tromboflebita).

Women: soreness, sensitivity and increase the size of the breast, amenorrhea, bleeding “Breakthrough”, menorragija, intermenstrual “mazhuschie” vaginal discharge, mastoncus, increased libido. In men, pain and sensitivity of the breast, gynecomastia, decreased libido. Peripheral edema, obstruction of the gallbladder, hepatitis, pancreatitis. Kišečnaâ or how želčnaâ, flatulence, anorexia, nausea, diarrhea, dizziness, headache (incl. migraine), intolerance to contact lenses, vomiting (mainly central origin, mainly in large doses). In the treatment of breast and prostate (additionally): thromboembolism, thrombosis. When using TTS: irritation and redness kozhi.Peredozirovka. Symptoms: nausea, vomiting, in some cases – metrorragija. Treatment: removal of the drug, simptomaticheskaya therapy, aimed at maintaining vital functions.

Inside, without chewing, drinking a small amount of liquid, by 2 mg / day, during 21 day, followed by a break in the 7 days, then continue treatment.

The duration of treatment up 6 Months, and then carried out a survey to decide on whether to continue replacement estrogen therapy.

Women with hysterectomy or in menopausal women, treatment can begin at any day. When you save the menstrual cycles of the first pills start with 5 day cycle (1 day of the cycle = 1 day of menstruation). / M, as 0.1% estradiol dipropionate solution in oil: with primary amenorrhea with hypoplasia of the genital organs and secondary sexual characteristics – by 1-2 mg daily or every other day for 1-2 months or more, to the palpable increase in uterine; thereafter – Progesterone / m, by 5 mg daily for 6-8 days.

If necessary to repeat courses of hormone therapy. In secondary amenorrhea – by 1 mg daily for 15-16 days, followed by administration of progesterone or pregnina for 6-8 days. If persistent clinical effect is absent, repeat the treatment. When hypo- and oligomenoree, dysmenorrhoea, infertility due to ovarian hypofunction and hypoplasia of the uterus – by 0.5-1 mg for 15-16 day after menses and then, when indicated, – progesterone or pregnin for 6-8 days. The course of treatment can be repeated several times in the same period, after menstruation.

When pathological phenomena, associated with the onset of menopause and surgical ovariectomy, – by 0.5-1 mg daily or every 1-2 day, courses on 10-15 injection. With the resumption of symptoms, repeat the treatment. Doses should be selected strictly individually depending on the phase of menopause, disease severity. With the weakness of labor and prolonged pregnancy – / m, by 4-5 mg for 2-3 h before the administration rodostimuliruyuschih PM.

As hemostimulating drugs while reducing the number of leukocytes below 2 th. / ml of blood (usually 10-20 days after irradiation with heavy defeats and 15-18 day – while lighter injuries) – by 1 mg after 1-2 day. Course of treatment 10 injection (if necessary – to 15 injection). TTS is attached to the net, dry and intact area of ​​skin body (poyasnychnaya region, life) 2 times a week. Treatment starts with TTC 50 g, followed by individual selection of doses (appearance sense voltage in the mammary gland or intermediate bleeding is a sign of increased dosages, which must be reduced). If after 2-3 weeks of the signs and symptoms of estrogen deficiency are not cropped, the dose should be increased. TTS is applied cyclically: after 3 weeks of treatment (6 applications) – interval 7 days, during which possible metrorrhagia. Nonstop, non-cyclic therapy is prescribed for women after hysterectomy or in cases, when the symptoms of estrogen deficiency occur again strongly during the 7-day interval. Subsequent therapy progestins should be as follows: with continuous use of the TTC is recommended to appoint an additional progestogen (10 mg of medroxyprogesterone acetate, 5 mg norethisterone, 5 mg norethisterone acetate or 20 mg dydrogesterone first 10-12 days of each month). For repeated application is recommended in addition TTS, in the last 10-12 days of therapy with estradiol, so take progestogen, to the fourth week of each cycle remained free of any hormone therapy. In both cases, after the 10-12 day progestin therapy begins bleeding.

The gel is applied 1 once a day, in the morning or evening, by 1.5 mg (2.5 or g gel 1-2 dose) – put a thin layer to clean skin of the abdomen, lumbar region, shoulders and forearms. The area of ​​application should be equal in magnitude 1-2 Palm. The gel should be absorbed in less than 2-3 m. If it remains on the skin surface over 5 m, means the drug was applied to the skin surface is too small. The gel is administered continuously or cycles. Dose and duration of therapy is determined individually.

Treatment should be preceded by a thorough gynecological examination, that long-term therapy should be repeated at least 1 once a year. During treatment requires systematic monitoring of liver function and blood pressure, and patients with diabetes – the concentration of glucose in the blood. Therapy estradiol necessarily be combined with the use of progestogens. Long-term treatment with estradiol increases the risk of breast cancer and endometrial (It depends on the duration of treatment and the dose of estrogen). Giperplaziya (or atypical glandular) often precedes endometrial cancer. The combination of estrogen with progestin has a protective effect on the endometrium. Treatment should be discontinued 4-6 weeks before the planned surgery. It is not a contraceptive and does not protect against pregnancy. When irregular menses during treatment (in women with an intact uterus) necessary to carry out diagnostic curettage to exclude malignancy of the uterus. The use of estradiol should be stopped immediately in case of deep vein thrombosis, thromboembolism, etc.. Localization, jaundice, the gain or the appearance of previously-existing migraine pain, sudden blurred vision, a significant increase in blood pressure. TTS can not be attached to the skin of the breast and 2 times in a row in the same area of ​​skin. Attach TTS should not get the sun's rays. Avoid getting gel on the breast and the mucous membranes of the vulva and vagina.

It improves the effectiveness of lipid-lowering drugs. Reduces the effects of male sex hormones, hypoglycemic, diuretic, antihypertensive drugs, and anticoagulants. It reduces glucose tolerance (may require correction dosing regimen hypoglycemic drugs). Barbiturates, anxiolytic drugs (trankvilizatorы), narcotic analgesics, Drugs for general anesthesia, Some antiepileptic drugs (Carbamazepine, phenytoin), Inductors of microsomal liver enzymes accelerates metabolism of estradiol. The plasma concentration is reduced while using certain antibiotics and phenylbutazone (ampicillin, rifampicin), due to changes in the gut microflora. Folic acid and thyroid medications increase the effect of oestradiol.