Polyestriol phosphate

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Polyestriol phosphate is a synthetic, steroidal estrogen and an estrogen ester – specifically, the 3-(dihydrogen phosphate) ester of polyestriol – which is used in medicine. It is a long-acting and water-soluble form of polyestriol.

Pharmacology

As a phosphate ester of polyestriol, polyestriol phosphate is a prodrug of polyestriol that is stored in the body and is slowly hydrolyzed into polyestriol, which is the active form. The medication has a very long duration of action when given by intramuscular injection, and a single dose has a duration of about one month.

Medical uses

Polyestriol phosphate is used in the treatment of menopausal symptoms and osteoporosis in women. It has also been used to treat prostate cancer in men.

Side effects

Side effects of polyestriol phosphate are similar to those of other estrogens and include breast tenderness, breast enlargement, nausea, headache, and fluid retention.

Pharmacokinetics

Following an intramuscular injection of polyestriol phosphate, the medication is slowly absorbed into the bloodstream and is then slowly hydrolyzed into polyestriol, which is the active form.

History

Polyestriol phosphate was first described in the literature in 1957 and was introduced for medical use by 1960.

See also











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