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Estropipate

Estrogen medication From Wikipedia, the free encyclopedia

Estropipate
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Estropipate, also known as piperazine estrone sulfate and sold under the brand names Harmogen, Improvera, Ogen, Ortho-Est, and Sulestrex among others, is an estrogen medication which is used mainly in menopausal hormone therapy in the treatment of menopausal symptoms.[1][2][3][4] It is a salt of estrone sulfate and piperazine, and is transformed into estrone and estradiol in the body.[2][3] It is taken by mouth.[1]

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Medical uses

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Estropipate is used to:[1][additional citation(s) needed]

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Available forms

Estropipate was available in the form of 0.75, 1.5, 3, and 6 mg oral tablets and 1.5 mg/gram vaginal cream. Estropipate is no longer available in the United States.

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Pharmacology

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Pharmacodynamics

Estropipate is a prodrug of estrone and estradiol. Hence, it is an estrogen, or an agonist of the estrogen receptors.

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Pharmacokinetics

Estropipate is hydrolyzed into estrone in the body.[5] Estrone can then be transformed into estradiol by 17β-hydroxysteroid dehydrogenase.

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Chemistry

History

Estropipate was introduced for medical use by Abbott in 1968.[6] It was approved by the FDATooltip Food and Drug Administration in the United States in 1991.[7]

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Generic names

Estropipate is the generic name of the drug and its INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name, and BANTooltip British Approved Name.[2][3][8][5][9]

Brand names

Estropipate was marketed under the brand names Genoral, Harmogen, Improvera, Ogen, Ortho-Est, and Sulestrex among others.[9][2][8][5]

Availability

Estropipate has been discontinued in the United States. In the past, estropipate has also been marketed in Canada, the United Kingdom, Ireland, Switzerland, Australia, South Africa, Mexico, and Indonesia.[9][8][5]

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References

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