Estropipate Explained

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. It is taken by mouth.

Medical uses

Estropipate is used to:

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.

Pharmacology

Pharmacodynamics

See also: Pharmacodynamics of estradiol.

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

Pharmacokinetics

See also: Pharmacokinetics of estradiol.

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

Chemistry

See also: Estrogen ester and List of estrogen esters.

History

Estropipate was introduced for medical use by Abbott in 1968.[5] It was approved by the in the United States in 1991.[6]

Society and culture

Generic names

Estropipate is the generic name of the drug and its,, and .[7] [8] [9]

Brand names

Estropipate was marketed under the brand names Genoral, Harmogen, Improvera, Ogen, Ortho-Est, and Sulestrex among others.

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.

Notes and References

  1. Web site: Ogen, estropipate tablets, USP . Pharmacia & Upjohn Co . U.S. Food and Drug Administration . December 2004 .
  2. Book: Elks J . The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. 14 November 2014. Springer. 978-1-4757-2085-3. 900–.
  3. Book: Morton IK, Hall JM . Concise Dictionary of Pharmacological Agents: Properties and Synonyms. 6 December 2012. Springer Science & Business Media. 978-94-011-4439-1. 114–.
  4. Book: William Andrew Publishing. Pharmaceutical Manufacturing Encyclopedia . 3rd . 22 October 2013. Elsevier. 978-0-8155-1856-3. 1484–.
  5. Book: Budoff, Penny Wise . vanc . No more hot flashes, and other good news. registration. 1 August 1983. Putnam. 978-0-399-12793-9. 28.
  6. Book: P & T.. July 1993. CORE Medical Journals.
  7. Book: Index Nominum 2000: International Drug Directory. 2000. Taylor & Francis. 978-3-88763-075-1. 408–.
  8. Book: Sweetman SC . Sex hormones and their modulators . Martindale: The Complete Drug Reference . 36th . 2009 . 2101 . Pharmaceutical Press . London. 978-0-85369-840-1.
  9. Web site: Estropipate . Drugs.com .