Ethinylestradiol 3-benzoate

Ethinylestradiol 3-benzoate is a synthetic, steroidal estrogen that is used in hormone replacement therapy and as a component of hormonal contraception. It is a derivative of ethinylestradiol, a potent synthetic estrogen, with a benzoate ester added at the 3-position. This modification enhances the drug's lipid solubility, allowing it to be administered via intramuscular injection.

Pharmacology

Ethinylestradiol 3-benzoate acts as an agonist of the estrogen receptor, a nuclear receptor that is activated by the hormone estrogen. Upon binding to the receptor, ethinylestradiol 3-benzoate induces a conformational change that allows the receptor to bind to specific DNA sequences known as estrogen response elements. This binding regulates the transcription of various genes, leading to the physiological effects of estrogen.

Clinical Use

Ethinylestradiol 3-benzoate is used in hormone replacement therapy to treat symptoms of menopause, such as hot flashes and vaginal dryness. It is also used in hormonal contraception to prevent ovulation and pregnancy. In addition, it may be used to treat certain conditions that are caused by low estrogen levels, such as osteoporosis and hypoestrogenism.

Side Effects

Like other estrogens, ethinylestradiol 3-benzoate can cause a number of side effects, including nausea, bloating, breast tenderness, and an increased risk of blood clots. Long-term use can also increase the risk of certain types of cancer, including breast cancer and endometrial cancer.

See Also

• Estradiol benzoate
• Estradiol valerate
• Estradiol cypionate