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What is Estradiol?
The active ingredient Estradiol is a hormone and is one of the most important ingredients for contraception and for hormone treatment during and after menopause. Colloquially Estradiol and two other, very similar hormones that occur in the female body, referred to as “estrogen”. Here you can read more about the impact and application of Estradiol, side effects and other interesting facts.
The estrogen preparation – 17-beta-estradiol is identical to endogenous estradiol (formed in the body of women, from the first menstruation up to menopause), produced by the ovaries. In the cells of the organs to which the action of hormones is directed, estrogens form a complex with specific receptors (found in various organs – in the uterus, vagina, urethra, mammary gland, liver, hypothalamus, pituitary), the receptor-ligand complex interacts with estrogen-effector elements genome and specific intracellular proteins inducing the synthesis of i-RNA, proteins and the release of cytokines and growth factors.
Has a feminizing effect on the body. Stimulates the development of the uterus, fallopian tubes, vagina, stroma and ducts of the mammary glands, pigmentation in the nipple and genital area, the formation of secondary sex characteristics by the female type, the growth and closure of the epiphyses of long tubular bones. Promotes timely rejection of the endometrium and regular bleeding, in high concentrations causes endometrial hyperplasia, suppresses lactation, inhibits bone resorption, stimulates the synthesis of a number of transport proteins (thyroxine-binding globulin, transcortin, transferrin, protein binding sex hormones), fibrinogen. It has a procoagulant effect, increases the synthesis in the liver of vitamin K-dependent coagulation factors (II, VII, IX, X), reduces the concentration of antithrombin III.
Increases blood levels of T4, Fe, Cu2 +, etc. It has an anti-atherosclerotic effect, increases the concentration of HDL, reduces – LDL and cholesterol (the concentration of TG increases). Modulates the sensitivity of receptors to progesterone and sympathetic regulation of smooth muscle tone, stimulates the transfer of intravascular fluid into tissues and causes compensatory retention of Na + and water. In large doses, it prevents the degradation of endogenous catecholamines, competing for the active receptors of catechol-O-methyltransferase.
After menopause, only a small amount of estradiol (from estrone in the liver and adipose tissue) is formed in the body. Reduction in the concentration of estradiol produced in ovaries is accompanied in many women by vasomotor and thermoregulatory instability (“hot flushes” of the blood to the skin of the face), sleep disorders, and progressive atrophy of the urogenital system.
Due to estrogen deficiency, osteoporosis develops (mainly the spine). It is known that the oral use of estrogens causes an increase in the synthesis of proteins (including renin), which leads to an increase in blood pressure.
Estradiol in the form of TTS is a plaster that is attached to the skin area. The control membrane provides a gradual and continuous release of estradiol from the reservoir with the active substance through the adhesive layer onto the skin. Due to the lack of the “first pass” effect through the liver, the TTC provides high efficacy when using smaller doses of the drug. TTS delivers estradiol unchanged to the bloodstream and maintains its plasma concentration during therapy at a consistent level adequate for the early or middle phase of the follicle.
(also known as 17-beta-Estradiol) The hormone Estradiol is formed naturally in the human body. In women, the largest amount is produced in the ovaries. In men who have far lower Estradiol levels in the body, it is formed in the adrenal cortex and in the testes.
The term “estrogen” hormones Estradiol, estrone and estriol are summarized. Of all three hormones Estradiol is the most effective, which is why it is also used as a drug (as “Estradiol hemihydrate”, the production conditions still contains some water). Of childbearing age (from the first menstrual period to menopause), it is also the most common estrogen in the body of the woman; during pregnancy estriol accepts this role and after menopause estrone.
The estrogens are not only very important for the formation of female sex characteristics (such as ovaries, uterus, vagina and breasts), but also for their function. The approximately 28-day menstrual cycle is largely dependent on the changing hormone levels in the blood of women:
In the first half of the cycle (follicular phase) distributes the pituitary gland (pituitary) of the hormone FSH, which stimulates the ovaries the maturation of ovarian follicles (follicles). These produce estrogens. This causes on the one hand, that the endometrium grows (in preparation for the possible implantation of a fertilized ovum). On the other hand it is due to rising levels of estrogen in the blood to the release of LH from the pituitary gland. This hormone triggers ovulation from: The most ripened follicle ruptures at the surface of the ovary and releases a mature egg into the fallopian tube, where it remains capable of fertilization for about 24 hours
With the ovulation the second half of the cycle starts named. The blood levels of estrogen, LH and FSH decline now, while increasing the concentration of the corpus luteum hormone. It is produced by the corpus luteum, which has developed after ovulation from the remaining follicles in the ovary. The Progesterone prepares the endometrium further prior to the eventual implantation of the fertilized egg. If fertilization from, the corpus luteum, so no more Progesterone is produced. As a result, it comes to form the thickened endometrium and rear for insertion of menstrual bleeding in which the mucous membrane is excreted along with blood. The menstrual period is already the beginning of a new cycle.
Estradiol for contraception
By taking Estradiol is the release of (FSH – follicle stimulating hormone) are suppressed – it will be no longer ovulation, fertilization and pregnancy which are not possible in the sequence. In adaptation to the natural hormonal fluctuations “the pill” is taken only 21 days. Then added terminate seven days or occupies only a drug-free tablet.
Estradiol for hormone replacement therapy in menopause
After menopause, ie after cessation of monthly menstrual period in middle age, the Estradiol levels decrease in the body. Since the hormone acts not only on the female organs, but also affects the psyche and acts on the overall performance and the bone density, the hormone decrease, during or after menopause lead to various ailments:. And bone loss
These symptoms can alleviate with Estradiol therapy often, if not eliminate it altogether. Earlier women were administered to very large doses of hormone, which has led in part to Estradiol side effects such as breast and. Meanwhile, lower dose and thereby secure hormone preparations in use.
Up, reduction and elimination of Estradiol
After taking a tablet Estradiol is absorbed through the intestine into the blood. There, it reaches its highest level after about four to six hours. In the liver, it is converted into estrone, which acts about ten-fold weaker. This is then mainly via the kidneys (ie in the urine) excreted.
Do not confuse with 17-alpha-Estradiol
The same structure, but in three dimensions differently shaped active substance 17-alpha-Estradiol (also called Alfatradiol), unlike the well-known 17-beta-Estradiol no effect as a female hormone. However, it is applied to, the excessively high levels of DHT (dihydrotestosterone, a related substance with testosterone) comes about. It inhibits the production of DHT and therefore its negative effect on hair growth.
When to use Estradiol?
Estradiol is mainly applied to hormone replacement therapy (“hormone replacement therapy”, HRT). When used for birth of drug related ethinylEstradiol is far more often used, as this affects even more targeted and can be taken with it in smaller amounts of active compound. Very often combi tablets for contraception (eg norethindrone or drospirenone) used of an estrogen (ethinyl Estradiol or Estradiol) and a progestogen, as this makes the contraceptive protection more secure.
Estradiol Way of Using
Inside, not liquid, squeezed a small amount of liquid, 2 mg Estradiol / day, for 21 days, followed by a break for 7 days, after which they continue treatment. The duration of treatment is up to 6 months, after which a survey is conducted to decide whether to continue the substitution of estrogen therapy. In women with a deleted uterus or in women in menopause, treatment can begin any day. With the saved menstrual cycle, the first tablet is taken from the 5th day of the cycle (1 day of the cycle = 1 day of menstruation).
V / m, a 0.1% solution of estradiol dipropionate in the oil: the primary amenorrhea with hypoplasia of the genital organs and the secondary sexual characteristics – Estradiol 1-2 mg daily or every other day for 1-2 months or more, to increase uterine palpable; after this – progesterone in / m, 5 mg daily for 6-8 days. If necessary, repeat courses of hormone therapy. In secondary amenorrhea – 1 mg daily for 15-16 days, followed by the appointment of progesterone or pregnin for 6-8 days. If the persistent clinical effect is absent, the course of treatment is repeated. When hypo- and oligomenorrhea, dysmenorrhea, infertility due to hypofunction of ovarian and uterine hypoplasia – 0.5-1 mg over 15-16 days after menstruation, and then, if indicated, – or progesterone pregnin for 6-8 days. The course of treatment can be repeated several times at the same time, after the end of menstruation. When pathological phenomena associated with the onset of the climacteric period and with surgical removal of the ovaries, – 0.5-1 mg daily or after 1-2 days, courses of 10-15 injections. When the symptoms resume, the course of treatment is repeated. Doses should be selected strictly individually depending on the phase of the climacteric period, the severity of the disease. With the weakness of labor and a pregnant pregnancy – in / m, 4-5 mg for 2-3 hours before the introduction of rhodostimulating drugs. As hemostimulating PM when reducing the number of leukocytes of less than 2 thousand / ml blood (typically 10-20 days after irradiation under severe lesions and 15-18 days – under milder lesions) -. 1 mg every 1-2 days. The course of treatment with estradiol is 10 injections (if necessary, up to 15 injections).
TTS is attached to a clean, dry and intact skin area of the body (lumbar region, stomach) 2 times a week. Treatment begins with a TTC of 50 mcg, followed by an individual dose selection (the appearance of a feeling of tension in the mammary gland or intermittent bleeding is a sign of increased dosage, which must be reduced). If signs and symptoms of estrogen deficiency do not stop after 2-3 weeks, the dose should be increased. TTS is applied cyclically: after 3 weeks of treatment (6 applications) – an interval of 7 days, during which metrorrhagia is possible. Continuous, non-cyclic therapy is prescribed to women after hysterectomy or in cases where symptoms of estrogen deficiency again strongly manifest during a 7-day interval. Follow-up therapy with gestagens should be carried out according to the following scheme: with the continuous use of TTS, it is recommended to additionally prescribe progestin (10 mg of medroxyprogesterone acetate, 5 mg of norethisterone, 5 mg of norethisterone acetate or 20 mg of dydrogesterone in the first 10-12 days of each month). When cycling TTS is recommended, in the last 10-12 days of estradiol therapy, it is recommended to take progestin so that the fourth week of each cycle remains free of therapy with any hormone. In both cases, after the end of 10-12-day gestagen therapy, bleeding occurs.
Estradiol gel used 1 time per day in the morning or evening, 1.5 mg (2.5 g dose of gel or 1-2) – applied thinly on clean skin of the abdomen, the lumbar region, shoulder and forearm. The area of application should be equal to 1-2 palms. The gel should be absorbed in less than 2-3 min. If it persists on the surface of the skin for more than 5 minutes, then the drug was applied to too small a surface of the skin. The gel is administered continuously or in cycles. The doses and duration of therapy are set individually.
As a contraceptive (contraceptive) is ingested Estradiol in the form of tablets once a day, always at about the same time each day. After 21 days, a tablet-free interval of seven days in the future (at 28 tablets per month pack containing the last seven tablets no active ingredient).
When hormone replacement therapy, the doctor will decide whether Estradiol should be applied continuously or in cycles. In the latter case also takes place after three weeks of treatment, a therapy-free week. The formulations of Estradiol are here diverse, there are both tablets and an Estradiol gel and Estradiol patch available. The patches give the hormone usually over a few days evenly through the skin into the body from. It must therefore only be changed every three to four days.
They are used in both applications (contraception, hormone replacement therapy) as long as the effect is desired.
What are the side effects of Estradiol?
Estradiol side effects are at a ten to one hundred patients treated headaches, depression, abdominal pain, nausea, leg cramps, weight gain, sensitive breast or chest pain. In the latter, the doctor should be informed and possibly chosen a lower dose.
What are special instructions for taking estradiol?
The common use of substances in the body via the same enzymes (cytochrome P450 in the liver) are broken down as Estradiol, can accelerate its degradation and thus weaken its effect. These include, for example, remedy for convulsions and epilepsy (phenobarbital, Phenytoin, Carbamazepine), the tuberculosis agent rifampicin, certain agents against HIV (nevirapine, efavirenz) and herbal antidepressant St John’s wort.
A long duration of therapy or high dose of Estradiol may increase the risk of breast and uterine cancer under certain circumstances. Through a very low dosage and possibly through the addition of progestogens can minimize this risk.
Also, by the Estradiol application the risk of the formation of blood clots, which then may clog a vessel (as in the case of pulmonary embolism) may be increased. This is especially true if a woman smokes or has other risk factors (high cholesterol, obesity, etc.).
The active ingredient Estradiol should be applied only to girls and women from the onset of menstruation, but not for pregnant or lactating. Should it occur during treatment of pregnancy, treatment must be discontinued immediately and a doctor can be contacted.
How to get Estradiol?
The active ingredient Estradiol is prescription in each dose and can be purchased only with a medical prescription at the pharmacy. But you may buy Estradiol online in UK over the counter.
Since when Estradiol is known?
steroid hormones, including estrogens such as Estradiol, testosterone and cortisone but also include, were recognized very early on as an important support function in the body. Already in 1929 the first estrogens were isolated from the chemist Adolf Butenandt and elucidated its structure. For this he received in 1939 together with the steroid researcher Leopold Ruzicka the Nobel Prize for Chemistry. In 1930, the first time an oral estrogen was introduced to therapy. It was at that time still extracted from the urine of pregnant women. Worthwhile chemical manufacturing process for the active ingredient Estradiol have been developed only in the second half of the 20th century.