Estradiol valerate 1mg and 2mg tablets

Where to buy estradiol 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.

What is estradiol?

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

Estradiol Valerate 2mg tabs

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.

In the human body, three types of estrogens are present – estrone (E1), estradiol (E2), and estriol (E3). Among these, estradiol is the most active, followed by estriol, and the least active minor form is estrone. These hormones are synthesized from androgens through a complex enzymatic reaction. This information is crucial for medical professionals conducting research in this area.

How estrogens and progesterone were discovered

In 1889, Charles Broun-Sécar reported the results of his experiment on himself at the Paris Academy. He injected flattened guinea pig testicles under his skin to combat old age, which shocked the public. His successful experiment led to further research into endocrine glands. Different labs searched for a “rejuvenating” substance in sex glands, and in 1932, Adolph Butenandt discovered androstenedione in male urine. However, another scientist isolated testosterone, the true sex hormone, in crystal form.

In 1935, Edgar Doysey discovered pure estradiol using pig ovaries for research. Despite being complicated and expensive, he obtained a hormone identical to one obtained by Erwin Schwenk and Friedrich Hildebrandt in 1933 from estrone found in the urine of pregnant women. They reduced estrone to obtain estradiol, the main hormone of female reproductive glands.

In 1902, gynecologist Ludwig Frenkel suggested the existence of the corpus luteum hormone. Many researchers, including D. W. Corner, W. M. Allen, Boutenandt, Ulrich Westphal, Max Hartmann, and Albert Wettestein, discovered the hormone in the late 1920s, but it’s hard to determine who did it first. Obtaining the hormone was a lengthy and expensive process, requiring a vast amount of source material to produce just a few thousandths of a gram. It took 50,000 pigs to produce one milligram of the hormone, and this is how Butenandt identified its chemical composition. The hormone is now called progesterone.

Estradiol to improve brain function

Estradiol receptors in the brain and serotonin receptors are found on the same neurons. Estradiol increases the expression of tryptophan hydroxylase and serotonin transporter, and it regulates serotonin metabolism through ERα. Estradiol and serotonin working together on the corresponding receptors in the same neurons may be responsible for increased serotonin levels caused by estradiol. This leads to improved learning and memory in women, who also cope better with new situations, recover faster from stress, and have fewer mental health problems when they receive estradiol. These effects may be regulated by the reproductive cycle.

Estradiol helps in acquiring new skills and enhances memory. Post-ovarian removal, taking estradiol significantly improves memory. It also improves learning and memory in both men and women. Low levels of estradiol in healthy men enhance the effect of estrogen on memory.

Estradiol and neuroprotection

Estradiol, a form of estrogen, has been found to increase the survival of neurons in the hypothalamus of rats after a stroke. Female rats showed an increase in the number of surviving neurons, while male rats showed a decrease. This suggests that estradiol may have a protective effect against stroke in females.

Estradiol can induce the synthesis of receptors in the hypothalamus, reduce factors that interfere with neuronal survival, and induce the expression of trophic factors that stimulate the synthesis of new proteins in the cell. These mechanisms may be responsible for the neuroprotective effect of estradiol. Estrogen is known to promote neuron survival and has been found to have neuroprotective effects on the human brain.

Recent studies have shown that these effects are mediated by receptors, specifically estradiol receptors that belong to the class of receptor-tyrosine kinases and estrogen receptor β (ERβ). Estradiol’s interaction with proteins that regulate oxidative stress is thought to be the reason behind its protective effects. Animal experiments have also suggested that estradiol may have protective effects against Alzheimer’s disease.

Role of estradiol in men & women

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.

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.

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.

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