Estrone acetate

Estrone_acetate.svg

Estrone acetate is a synthetic estrogen, a derivative of estrone, which is a naturally occurring estrogen hormone. It is used in hormone replacement therapy (HRT) for menopausal symptoms and in the treatment of certain hormonal disorders.

Chemical Structure and Properties

Estrone acetate is an acetate ester of estrone. Its chemical structure is characterized by the addition of an acetate group to the 3-hydroxyl group of estrone. This modification increases the lipophilicity of the molecule, enhancing its absorption and bioavailability when administered orally.

Pharmacology

Estrone acetate functions as an estrogen receptor agonist. Upon administration, it is hydrolyzed to estrone, which then exerts its effects by binding to estrogen receptors in various tissues. This binding leads to the modulation of gene expression and the regulation of various physiological processes, including the maintenance of the female reproductive system and secondary sexual characteristics.

Medical Uses

Estrone acetate is primarily used in hormone replacement therapy for the management of menopausal symptoms such as hot flashes, vaginal atrophy, and osteoporosis. It is also used in the treatment of hypoestrogenism due to hypogonadism, ovarian failure, or oophorectomy.

Side Effects

Common side effects of estrone acetate include nausea, headache, breast tenderness, and fluid retention. Long-term use of estrogens has been associated with an increased risk of endometrial cancer, breast cancer, and cardiovascular disease. Therefore, it is often prescribed in combination with a progestogen in women with an intact uterus to mitigate the risk of endometrial hyperplasia and cancer.

Contraindications

Estrone acetate is contraindicated in individuals with a history of breast cancer, endometrial cancer, thromboembolic disorders, liver disease, and undiagnosed vaginal bleeding. It should be used with caution in patients with risk factors for cardiovascular disease and stroke.

See Also

• Estrone
• Estrogen
• Hormone replacement therapy
• Menopause
• Hypoestrogenism

External Links

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