Estradiol valerate 1mg and 2mg tablets

What is estradiol?

Active ingredient: estradiol valerate.
Popular brand names: Progynova, Estrace, and many others.

Estradiol Valerate 2mg tabs
Estradiol valerate 2mg tablets

Estradiol is the major female sex hormone, the most active estrogen, which is produced mainly by the follicular apparatus of the ovaries in women. In smaller amounts it is formed in the testicles and peripheral tissues in men and in the reticular cortex of the adrenal glands in both sexes. In addition, during gestation, estradiol is produced by the placenta.


Estradiol was first isolated from sheep in 1934 by the Austrian chemist Adolf Butenandt. It was given its name from its chemical structure which is similar to the estriol that can be found in human urine. It is the main estrogen found in males. Estradiol, unlike estrone and estriol, is not an endogenous hormone. It is, therefore, synthesized from androgenic precursors, i.e. the steroid testosterone or dihydrotestosterone.
In the 1950s, estrone and estradiol were discovered. Estradiol in its natural form was determined to be the most potent estrogen in 1958, as later determined by binding to the uterus. Later, a number of steroidal estrogens including estradiol were also discovered in plants, and this was followed by synthesis of a variety of steroidal estrogens, of which estradiol remains one of the most widely prescribed estrogens.
The hormone is mainly found in women, but in men it is also synthesized in small quantities. In addition to this, estrogens (estradiol and estrone) are also secreted by men. Estradiol is responsible for many of the physical changes that occur during puberty and after puberty, in both men and women.
Before puberty, its blood levels in boys and girls are about the same. When a girl enters puberty, active production of estradiol begins. While in boys its level in the body does not change.
In women, the hormone is synthesized by the sex glands (ovaries), adrenal glands, as well as other tissues of the body.
During pregnancy, the placenta is responsible for the synthesis of estradiol. In women, the hormone promotes the development of secondary sexual characteristics, regulates the cycle of menstruation, promotes successful conception and carrying a child.
Estrogens also have a positive effect on the heart, bone, and other organ systems. Estradiol plays an important role in the development of the female skeleton. It is responsible for the formation of peak bone mass. Bone resorption is decreased in premenopausal women as well as in postmenopausal women. Estrogen therapy is commonly prescribed for the prevention of osteoporosis in postmenopausal women.

Pharmacological action: estrogenic.

Replaces the insufficient production of endogenous estrogen. Regulates the metabolism of fats, proteins and carbohydrates, water-electrolyte balance, lowers the level of LDL cholesterol in the blood. causes proliferative changes in the endometrium, prevents a decrease in bone mass and osteoporosis. Cures somatic, mental and other menopausal symptoms during pre- and postmenopause or after ovariectomy.

Contraindications

Hypersensitivity, endometrial hyperplasia, endometriosis, myoma, breast cancer or suspicion of it, other hormone-dependent neoplasms or suspicion of them, benign or malignant liver tumors (including in the anamnesis), severe liver dysfunction, thromboembolic processes (including in the anamnesis). including in the anamnesis), diabetes mellitus, congenital disorders of fat metabolism, hypertriglyceridemia, Dubin-Johnson and Rotor syndromes, vaginal bleeding of unclear genesis, otosclerosis with exacerbation during previous pregnancy, pregnancy, breastfeeding.

Uses

Estradiol valerate is used for:
-Menopausal symptoms
-Endometriosis
-Luteal phase defect
-Pregnancy and labor induction
-Postmenopausal syndrome
-Estradiol and estrogen-deficient states
-Mild estrogen deficiency
-Premature ovarian failure
-Estrogen replacement therapy in surgical menopause
-Hypogonadism, especially secondary hypogonadism, in men
-Hormone replacement therapy in men
-Estrogen-induced bone loss prevention

What is Estradiol 2mg for?

  • A single dose of Estradiol in a dosage of 2 mg is prescribed for short-term use.
  • Estradiol in a dosage of 2mg is recommended for long-term use in combination with anti-estrogens and/or progestogens.
  • A single dose of Estradiol in a dosage of 2 mg is used for the prevention of osteoporosis in post-menopausal women.
  • Estradiol in a dosage of 2mg is used for the treatment of endometriosis.
  • Estradiol 2mg is used for the treatment of fibroids.
  • Estradiol 2mg is used for the treatment of menopausal vasomotor symptoms.
  • Estradiol 2mg is used for the treatment of menopausal atony.
  • Estradiol in a dosage of 2mg is used for the prevention of prostatic carcinoma.
  • Estradiol 2mg is used for the treatment of pulmonary arterial hypertension.
  • Estradiol 2mg is used for the treatment of premenstrual syndrome.
  • Estradiol 2mg is used for the treatment of primary ovarian insufficiency.
  • Estradiol 2mg is used for the treatment of dysmenorrhea.
  • Estradiol 2mg is used for the treatment of uterine fibroids.
  • Estradiol 2mg is used for the treatment of uterine atony.
  • Estradiol 2mg is used for the treatment of premenstrual syndrome.
  • Estradiol 2mg is used for the prevention of breast cancer.

What is Estradiol 1mg for?

  • Estradiol in a dosage of 1mg is used for the treatment of peri-menopausal symptoms.
  • Estradiol in a dosage of 1mg is used for the treatment of menopausal vasomotor symptoms.
  • Estradiol 1mg is used for the treatment of menopausal symptoms.
  • Estradiol 1mg is used for the treatment of endometriosis.
  • Estradiol 1mg is used for the treatment of fibroids.
  • Estradiol 1mg is used for the treatment of menopausal atony.
  • Estradiol 1mg is used for the treatment of primary ovarian insufficiency.
  • Estradiol 1mg is used for the treatment of dysmenorrhea.
  • Estradiol 1mg is used for the treatment of uterine fibroids.
  • Estradiol 1mg is used for the treatment of uterine atony.
  • Estradiol 1mg is used for the treatment of premenstrual syndrome.
  • Estradiol 1mg is used for the prevention of breast cancer.

Pharmacokinetics

After oral administration estradiol valerate is quickly and completely absorbed from the gastrointestinal tract. Binding to plasma proteins is 50%.
It is rapidly metabolized in the liver to form estriol and estrone. When taken orally in a dose of 1-2 mg, the maximum plasma concentration is reached after 3-6 hours. T1/2 is about 1 hour.
It is subject to the effect of “first passage” through the liver and, to some extent, enterohepatic recirculation.
It is excreted in the urine as sulfate and glucuronide esters together with a small amount of unchanged substance. Other metabolites have also been identified.

Pharmacodynamics

Estrogen, a substitution therapy agent. Estradiol valerate has a specific estrogenic action: it causes proliferation of endometrium, stimulates development of uterus and secondary female sexual characteristics in case of their underdevelopment, softens and eliminates general disorders arising in a woman on the basis of insufficient function of gonads in menopausal period or after gynecological operations.
Estradiol valerate maintains the balance between osteoblasts and osteoclasts, reduces bone resorption and promotes bone formation.

Estradiol to improve brain function

The receptors for estradiol in the brain and for serotonin are located on approximately the same neurons. Estradiol increases the expression of tryptophan hydroxylase and serotonin transporter. Furthermore, estradiol regulates serotonin metabolism through its effects on the estradiol receptor α (ERα).

The combined actions of estradiol and serotonin on their corresponding receptors in the same neurons could be a factor that causes estradiol to increase serotonin levels. This increase in serotonin in the neurons could, in turn, cause improved learning and memory in the estradiol-treated women. Women who are given estradiol are better able to cope with new situations, they recover more quickly from stress, and they suffer from mental disorders less often. The effects of estradiol and serotonin on memory also provide support for the hypothesis that the action of estradiol in the brain is regulated by the reproductive cycle.

Estradiol may also play a role in the ability to acquire new skills. The memory of people whose gonads had been removed after their ovaries were removed and estrogen was administered improved dramatically. Estradiol may improve the learning and memory of healthy women and men. It has been suggested that this estrogen effect increases when estradiol levels are low in healthy men.

Estrogen and neuroprotection

The effects of estrogen on the neuronal survival of the hypothalamus of rats increased after stroke. In addition, the number of neurons that had survived after the stroke increased in female rats, while the number of neurons that had survived in male rats decreased. The results of these studies suggest that estradiol may have a protective effect against stroke in females.

There are various ways in which estradiol can have a neuroprotective effect. First, estradiol may induce the synthesis of estradiol receptors, especially in the hypothalamus, thus increasing the effects of estradiol. Estradiol may also reduce the expression of factors that interfere with neuronal survival. Furthermore, estradiol may induce the expression of trophic factors in neuronal cells. These proteins stimulate the synthesis of new proteins in the cell, and the increase in these proteins may be responsible for the neuroprotective effect. Estrogen also promotes the survival of neurons. Furthermore, it has been suggested that estradiol may promote the survival of neurons in the human brain.

Some neuroprotective effects of estradiol appear to be mediated via estradiol receptors. The results of recent studies suggest that estradiol receptors that belong to the class of receptor-tyrosine kinases could have neuroprotective effects. These receptors mediate the effects of estradiol on neuronal survival. Estradiol receptors that belong to the class of estrogen receptor β (ERβ) have also been shown to have neuroprotective effects.

Studies in laboratory animals have suggested that the protective effects of estradiol could be attributed to its interaction with proteins that regulate oxidative stress. The results of experiments on animals have also suggested that estradiol may have protective effects against Alzheimer’s disease.

Where to buy online?

If you are interested in buying estradiol online, you should know that this drug is not available without a prescription. You can buy estradiol online only from a licensed pharmacy. If you are looking for a way to buy estradiol online, you should know that there are many online pharmacies that offer this medication. You can buy estradiol online by selecting the product you want to buy and adding it to the shopping cart. That is why an online shop will always be good if you want to buy estradiol tablets online in UK.

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