Ethinylestradiol sulfate

Ethinylestradiol sulfate is a sulfate conjugate of ethinylestradiol, a synthetic derivative of the natural estrogen estradiol. It is one of the most commonly used medications in hormonal contraception and is found in almost all modern formulations of combined oral contraceptive pills.

Pharmacology

Ethinylestradiol sulfate is a prodrug of ethinylestradiol. Upon ingestion, it is converted by the gastrointestinal tract and liver into ethinylestradiol. This conversion is necessary as ethinylestradiol itself is not orally bioavailable due to extensive first-pass metabolism in the liver. The sulfate conjugation of ethinylestradiol increases its water solubility, allowing it to be absorbed more efficiently in the gastrointestinal tract.

Clinical Use

Ethinylestradiol sulfate is used primarily in hormonal contraception. It is combined with a progestin in oral contraceptive pills to prevent ovulation and thus prevent pregnancy. It can also be used in hormone replacement therapy for menopausal women, and in the treatment of hormone-sensitive cancers such as breast cancer and prostate cancer.

Side Effects

As with all medications, ethinylestradiol sulfate can cause side effects. The most common side effects are related to its estrogenic activity and can include nausea, breast tenderness, weight gain, and mood changes. More serious side effects can include an increased risk of blood clots, stroke, and certain types of cancer.

See Also

• Estradiol
• Oral contraceptive pill
• Hormone replacement therapy
• Progestin

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  Ethinylestradiol sulfate