Last Updated on March 16, 2024
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What is estradiol?
Estradiol is a hormone and is one of the most important components for contraception and for hormone therapy during and after menopause. In common parlance, estradiol and two other, very similar hormones that are produced in the female body are called “estrogen”. Here you can read more about the effects and uses of Estradiol, side effects and other interesting facts.
Pharmacological action
Estrogenic drug – 17-beta-estradiol is identical to endogenous estradiol (it is formed in a woman from the first menstruation until menopause), is produced by the ovaries. In the cells of the organs targeted by the hormones, estrogens form a complex with specific receptors (found in various organs – uterus, vagina, urethra, breast, liver, hypothalamus, pituitary), the receptor-ligand complex interacts with the estrogen-effector gene and specific intracellular proteins, inducing synthesis of i-RNA, proteins and the release of cytokines and growth factors. It has a feminizing effect on the body. Stimulates the development of the uterus, fallopian tubes, vagina, mammary gland stroma and ducts, nipple and genital pigmentation, formation of female secondary sexual characteristics, growth and closure of epiphyses of long tubular bones. Promotes timely endometrial rejection and regular bleeding, in high concentrations causes endometrial hyperplasia, suppresses lactation, inhibits bone resorption, stimulates synthesis of several transport proteins (thyroxine-binding globulin, transcortin, transferrin, sex hormone-binding protein), fibrinogen. Has a procoagulant effect, increases the synthesis in the liver of vitamin K-dependent clotting factors (II, VII, IX, X), reduces the concentration of antithrombin III. Increases the levels of T4, Fe, Cu2+ and so on.д. in the blood. It has anti-atherosclerotic effect, increases HDL concentration, lowers LDL and cholesterol (increases TG concentration). Modulates sensitivity of receptors to progesterone and sympathetic regulation of smooth muscle tone, stimulates the transport of intravascular fluid in tissues and causes compensatory retention of Na+ and water. At high doses, it prevents the degradation of endogenous catecholamines by competing for active catechol-O-methyltransferase receptors. After menopause, only small amounts of estradiol are formed in the body (from estrone in the liver and fatty tissue). A decrease in the concentration of estradiol produced in the ovaries is accompanied in many women by vasomotor and thermoregulatory instability ("hot flashes" blood to the skin of the face), sleep disturbances, progressive atrophy of the urogenital system. Osteoporosis (mostly of the spine) develops because of estrogen deficiency.
Oral estrogen use is known to cause increased protein synthesis (including renin), which leads to increased blood pressure. Estradiol in the form of TTCs is a patch that is applied to an area of skin. A control membrane ensures a gradual and continuous release of estradiol from the reservoir of the active substance through a sticky layer onto the skin. Due to its lack of effect "of the first passage" Through the liver, TTC provides high efficacy at lower doses of the drug. TTC delivers estradiol in its unchanged form into the bloodstream and maintains its plasma concentration at a constant level during therapy, sufficient for the early to mid-phase follicle. (also known as 17-beta-estradiol) The hormone estradiol is produced naturally in the human body. In women, the highest amount is produced in the ovaries. In men, who have much lower levels of estradiol in the body, it is formed in the adrenal cortex and in the testicles. By the term "estrogen" The hormones estradiol, estrone and estriol are generalized. Of the three hormones, estradiol is the most effective, so it is also used as a drug (as "Estradiol hemihydrate", Under production conditions, it still contains some water). During childbearing age (from first menstruation to menopause), it is also the most abundant estrogen in the female body; during pregnancy, estriol takes this role, and after menopause, estrone. Estrogens are not only very important for the formation of female sexual characteristics (such as the ovaries, uterus, vagina, and breasts), but also for their function. The approximately 28-day menstrual cycle is highly dependent on changes in hormone levels in women: In the first half of the cycle (follicular phase), the pituitary gland secretes the hormone FSH, which stimulates the ovaries to mature ovarian follicles (follicles). They produce estrogens. This leads, on the one hand, to the growth of the endometrium (to prepare for possible implantation of a fertilized egg). On the other hand, it is associated with an increase in the level of estrogen in the blood before LH is released from the pituitary gland. This hormone triggers ovulation: the most mature 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 ovulation begins the second half of the cycle called. Estrogen, LH, and FSH levels in the blood now decrease, the concentration of luteal corpus luteum hormone increases. It is produced by the corpus luteum, which develops after ovulation from the remaining follicles in the ovary. Progesterone prepares the endometrium for implantation of the fertilized egg. If fertilization occurs, the luteal lining of the uterus stops producing progesterone. The result is a thickened endometrium and the posterior part to introduce menstrual bleeding, in which the mucous membrane is excreted along with the blood. Menstruation is already the beginning of a new cycle.
Estradiol for contraception
Taking estradiol suppresses the release of (FSH – follicle stimulating hormone) – no more ovulation, fertilization and pregnancy, which are impossible in sequence. In adaptation to natural hormonal fluctuations "pill" Is only taken for 21 days. Then the added interrupts seven days or takes only the pill without the medication.
Estradiol for menopausal hormone replacement therapy
After menopause, that is, after the cessation of monthly menstruation in middle age, estradiol levels in the body decrease. Because the hormone acts not only on women’s organs, but also affects the psyche, affects overall performance and bone density, a decrease in the hormone during or after menopause leads to various diseases:. And bone loss These symptoms may be relieved by estradiol therapy often, if not eliminated completely. Previously, women were prescribed very high doses of the hormone, which in part led to Estradiol side effects such as breast enlargement and. Meanwhile, the dose reduction and thus the safety of hormonal drugs in the use of the.
Estradiol withdrawal
After taking the pill, estradiol is absorbed through the intestine into the bloodstream. There it reaches its highest level in about four to six hours. In the liver, it is converted to estrone, which acts about ten times weaker. It is then excreted mainly through the kidneys (t.е. with urine).
Not to be confused with 17-alpha-estradiol
The same in structure but different in three dimensions, the active substance 17-alpha-estradiol (also called alfatradiol), unlike the well-known 17-beta-estradiol, has no action as a female hormone. However, its use causes excessively high levels of DHT (dihydrotestosterone, a related substance to testosterone). It suppresses the production of DHT and therefore its negative effect on hair growth.
When should you use Estradiol?
Estradiol is mainly used for hormone replacement therapy ("Hormone replacement therapy", HRT). When used for drug-related delivery, ethinyl estradiol is much more commonly used because it is even more targeted and can be taken along with it in smaller amounts of the active compound. Combination pills (e.g., norethindrone or drospirenone) of estrogen (ethinyl estradiol or estradiol) and progestagen are very often used for contraception, as this makes contraception more reliable.
The way to use estradiol
By mouth, not in liquid form, squeeze a small amount of liquid, 2 mg estradiol/day, for 21 days, then take a break for 7 days, after which treatment continues. The treatment duration is up to 6 months, after which the patient is examined to decide whether to continue the oestrogen replacement therapy. In women with a removed uterus or in menopausal women, treatment can be started any day. If the menstrual cycle is intact, the first tablet is taken on the 5th day of the cycle (1 day of the cycle = 1 day of menstruation). I/m, a 0.1% estradiol dipropionate solution in oil: primary amenorrhea with genital hypoplasia and secondary sexual signs – estradiol 1-2 mg daily or every other day for 1-2 months or more, until the palpable uterus increases; after that – progesterone v/m, 5 mg daily for 6-8 days.If necessary, repeated courses of hormone therapy.
In secondary amenorrhea – 1 mg daily for 15-16 days, after which progesterone or pregnin is prescribed for 6-8 days. In the absence of a persistent clinical effect the therapy is repeated.
In hypo- and oligomenorrhea, dysmenorrhea, infertility due to ovarian hypofunction and uterine hypoplasia – 0.5-1 mg for 15-16 days after menstruation and then, if indicated, or progesterone pregnin for 6-8 days. The course of treatment may be repeated several times at the same time, after the end of menstruation.
In pathological phenomena associated with the onset of menopause and with surgical removal of the ovaries – 0.5-1 mg daily or every 1-2 days, in courses of 10-15 injections. If symptoms return, the course of treatment is repeated. Doses should be chosen strictly individually, depending on the phase of the menopausal period, the severity of the disease.
In cases of obstructed labour and low birth weight – intravenous, 4-5 mg, 2-3 hours before the administration of labor inducing drugs. As a hemostimulatory drug when the white blood cell count is below 2,000/ml (usually 10-20 days after exposure for severe lesions and 15-18 days for milder lesions) -. 1 mg every 1-2 days. The course of treatment with estradiol is 10 injections (if necessary, up to 15 injections).
TTC is applied to a clean, dry and intact area of the body skin (lumbar region, abdomen) twice a week. Treatment begins with a TTC of 50 mcg, then the dose is adjusted individually (the appearance of a feeling of tension in the breast or recurrent bleeding is an indication that the dose should be increased, which should be reduced). If signs and symptoms of estrogen deficiency do not cease after 2-3 weeks, the dose should be increased. TDS is used cyclically: after 3 weeks of treatment (6 applications) – interval of 7 days, during which metrorrhagia may occur. Continuous, non-cyclic therapy administered to women after hysterectomy or when symptoms of estrogen deficiency are again pronounced within a 7-day interval. Subsequent therapy with gestagens should follow the following pattern: if TTCs are continuously used, an additional progestins (10 mg medroxyprogesterone acetate, 5 mg norethisterone acetate, or 20 mg didrogesterone in the first 10-12 days of each month) are recommended. When cyclic TTC is recommended, in the last 10-12 days of estradiol therapy it is advisable to take progestin, so that the fourth week of each cycle remains free of any hormone therapy. In both cases, bleeding occurs after the end of 10 to 12 days of gestagen therapy. Estradiol gel is applied once a day in the morning or evening, 1.5 mg (2.Dose 5 g gel or 1-2) – applied in a thin layer to clean skin on the abdomen, lumbar region, upper arm and forearm. The area of application should be equal to 1-2 palms. The gel has to be absorbed in less than 2-3 minutes. If it persists on the skin surface for more than 5 minutes, it means the drug was applied to too small a skin surface. The gel is administered continuously or in cycles. The doses and duration of therapy are set individually.
As a contraceptive (birth control), Estradiol is taken in pill form once a day, always at about the same time each day. After 21 days, the interval without pills is seven days in the future (at 28 pills per month, the package containing the last seven pills contains no active ingredient). In hormone replacement therapy, the doctor decides whether Estradiol should be used continuously or in cycles. In the latter case, after three weeks of treatment, there is also a week of no therapy.
Estradiol preparations are varied, there are tablets as well as estradiol gel and estradiol patch. The patches administer the hormone usually for several days evenly through the skin into the body from. Therefore it only needs to be changed every three to four days. Used in both cases (contraception, hormone replacement therapy) as long as the effect is desired.
What are the side effects of estradiol?
Estradiol side effects occur in ten in one hundred treated patients headaches, depression, abdominal pain, nausea, leg cramps, weight gain, sensitive breasts or breast pain. In the latter case, you should inform your doctor and possibly choose a lower dose.
What are the special instructions for taking estradiol?
The combined use of substances, which in the body through the same enzymes (cytochrome P450 in the liver) are degraded as Estradiol, can accelerate its degradation and thus weaken its action. These include, for example, seizure and epilepsy medications (phenobarbital, phenytoin, carbamazepine), the anti-tuberculosis drug rifampicin, some HIV medications (nevirapine, efavirenz) and the herbal antidepressant St. John’s wort. Prolonged therapy or a high dose of estradiol may increase the risk of breast and uterine cancer in certain circumstances. By using a very low dosage and possibly by adding progestagens, this risk can be minimized. Also, estradiol use may increase the risk of blood clots, which can then clog a vessel (as in the case of a pulmonary embolism). This is especially true if the woman smokes or has other risk factors (high cholesterol, obesity, etc.д.).). The active ingredient estradiol should only be used for girls and women from the beginning of menstruation, but not for pregnant or lactating women. If pregnancy occurs during treatment, it is necessary to stop treatment immediately and consult a doctor.
How to get estradiol?
The active ingredient estradiol is prescribed in each dose and can only be purchased with a prescription from a pharmacy. But you can buy Estradiol online in the UK without a prescription.
Since when is estradiol known??
Steroid hormones, including estrogens such as estradiol, testosterone and cortisone, but also including, were recognized very early on as an important supporting function in the body. As early as 1929, the first estrogens were isolated by chemist Adolf Butenandt and its structure was figured out. For this he received the Nobel Prize in Chemistry in 1939 along with the steroid researcher Leopold Ruzicka. In 1930, oral estrogen was first introduced into therapy. At that time it was still being extracted from the urine of pregnant women. A decent chemical process for producing the active ingredient Estradiol were not developed until the second half of the 20th century.
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