Equilenin sulfate

Equilenin sulfate

Equilenin sulfate is a steroidal estrogen that is derived from equilin. It is a component of conjugated estrogens (Premarin), along with several other related estrogens. Equilenin sulfate is formed from equilenin by sulfation, which is catalyzed by sulfotransferase enzymes.

Chemistry

Equilenin sulfate, also known as 6,8-didehydroestrone 3-sulfate or as estra-1,3,5(10),6,8-pentaen-3-ol-17-one 3-sulfate, is a synthetic, steroidal estrogen and a derivative of estrone. It is more specifically a derivative of equilin, and is a member of the class of compounds known as equine estrogens. Equilenin sulfate is the C3 sulfate ester of equilenin, and acts as a prodrug of equilenin in the body.

Pharmacology

Equilenin sulfate is a prodrug of equilenin in the body. Upon ingestion, it is hydrolyzed into equilenin by esterase enzymes in the intestine and liver. Equilenin is then sulfated and/or glucuronidated and is excreted in urine. Equilenin sulfate has been found to possess approximately 1.5 times the potency of conjugated estrogens like estrone sulfate in terms of systemic estrogenic effect.

Medical uses

Equilenin sulfate is used in hormone replacement therapy for menopausal symptoms and to prevent osteoporosis in postmenopausal women. It is also used in the treatment of breast cancer and prostate cancer.

Side effects

Side effects of equilenin sulfate are similar to those of other estrogens and may include nausea, vomiting, bloating, abdominal pain, breast tenderness, headache, and weight changes. More serious side effects may include blood clots, stroke, heart attack, breast cancer, endometrial cancer, and gallbladder disease.

See also

• List of estrogens
• List of estrogen esters
• List of steroidal estrogens