Progestogen (medication)

This article is about progestogens as medications. For the role of progestogens as hormones, see Progestogen.
Progestogen (medication)
Drug class
Progesterone, the natural progestogen in the body and one of the most widely used progestogen medications
Class identifiers
SynonymsProgestagen, gestagen, gestogen; progestin (synthetic progestogen); progesterone receptor agonist
UseHormonal birth control, hormone therapy, gynecological disorders, fertility medicine and pregnancy support, sex-hormone suppression, others
ATC codeG03
Biological targetProgesterone receptors (PR-A, PR-B, PR-C); membrane progesterone receptors (mPRα, mPRβ, mPRγ, mPRδ, mPRε); progesterone receptor membrane components (PGRMC1, PGRMC2)
Chemical classSteroids (pregnanes, norpregnanes, retropregnanes, androstanes, estranes)
Clinical data
Drugs.comDrug Classes
External links
MeSHD011372
Legal status
In Wikidata

A progestogen, also referred to as a progestagen, gestagen, or gestogen, is a type of medication which produces effects similar to those of the natural female sex hormone progesterone in the body.[1] A progestin is a synthetic progestogen.[1] Progestogens are used most commonly in hormonal birth control and menopausal hormone therapy.[1] They can also be used in the treatment of gynecological conditions, to support fertility and pregnancy, to lower sex hormone levels for various purposes, and for other indications.[1] Progestogens are used alone or in combination with estrogens.[1] They are available in a wide variety of formulations and for use by many different routes of administration.[1] Examples of progestogens include natural or bioidentical progesterone as well as progestins such as medroxyprogesterone acetate and norethisterone.[1]

Side effects of progestogens include menstrual irregularities, headaches, nausea, breast tenderness, mood changes, acne, increased hair growth, and changes in liver protein production among others.[1][2] Other side effects of progestogens may include an increased risk of breast cancer, cardiovascular disease, and blood clots.[2] At high doses, progestogens can cause low sex hormone levels and associated side effects like sexual dysfunction and an increased risk of bone fractures.[3]

Progestogens are agonists of the progesterone receptors (PRs) and produce progestogenic, or progestational, effects.[1] They have important effects in the female reproductive system (uterus, cervix, and vagina), the breasts, and the brain.[1] In addition, many progestogens also have other hormonal activities, such as androgenic, antiandrogenic, estrogenic, glucocorticoid, or antimineralocorticoid activity.[1] They also have antigonadotropic effects and at high doses can strongly suppress sex hormone production.[1] Progestogens mediate their contraceptive effects both by inhibiting ovulation and by thickening cervical mucus, thereby preventing fertilization.[4][5] They have functional antiestrogenic effects in certain tissues like the endometrium, and this underlies their use in menopausal hormone therapy.[1]

Progesterone was first introduced for medical use in 1934 and the first progestin, ethisterone, was introduced for medical use in 1939.[6][7][8] More potent progestins, such as norethisterone, were developed and started to be used in birth control in the 1950s.[6] Around 60 progestins have been marketed for clinical use in humans or use in veterinary medicine.[9][10][11][12][13] These progestins can be grouped into different classes and generations.[1][14][15] Progestogens are available widely throughout the world and are used in all forms of hormonal birth control and in most menopausal hormone therapy regimens.[1][9][10][12][11]

  1. ^ a b c d e f g h i j k l m n o Kuhl H (2005). "Pharmacology of estrogens and progestogens: influence of different routes of administration" (PDF). Climacteric. 8 (Suppl 1): 3–63. doi:10.1080/13697130500148875. PMID 16112947. S2CID 24616324.
  2. ^ a b Cite error: The named reference pmid15358281 was invoked but never defined (see the help page).
  3. ^ Thibaut F, De La Barra F, Gordon H, Cosyns P, Bradford JM (2010). "The World Federation of Societies of Biological Psychiatry (WFSBP) guidelines for the biological treatment of paraphilias". World J. Biol. Psychiatry. 11 (4): 604–55. doi:10.3109/15622971003671628. PMID 20459370. S2CID 14949511.
  4. ^ Glasier A (March 20, 2015). "Chapter 134. Contraception". In Jameson JL, De Groot LJ, de Krester D, Giudice LC, Grossman A, Melmed S, Potts Jr JT, Weir GC (eds.). Endocrinology: Adult and Pediatric (7th ed.). Philadelphia: Saunders Elsevier. p. 2306. ISBN 978-0-323-18907-1.
  5. ^ Pattman R, Sankar KN, Elewad B, Handy P, Price DA, eds. (November 19, 2010). "Chapter 33. Contraception including contraception in HIV infection and infection reduction". Oxford Handbook of Genitourinary Medicine, HIV, and Sexual Health (2nd ed.). Oxford: Oxford University Press. p. 360. ISBN 978-0-19-957166-6. Ovulation may be suppressed in 15–40% of cycles by POPs containing levonorgestrel, norethisterone, or etynodiol diacetate, but in 97–99% by those containing desogestrel.
  6. ^ a b Kuhl H (2011). "Pharmacology of Progestogens" (PDF). J Reproduktionsmed Endokrinol. 8 (1): 157–177.
  7. ^ Christian Lauritzen, John W. W. Studd (22 June 2005). Current Management of the Menopause. CRC Press. p. 45. ISBN 978-0-203-48612-2. Ethisterone, the first orally effective progestagen, was synthesized by Inhoffen and Hohlweg in 1938. Norethisterone, a progestogen still used worldwide, was synthesized by Djerassi in 1951. But this progestogen was not used immediately and in 1953 Colton discovered norethynodrel, used by Pincus in the first oral contraceptive. Numerous other progestogens were subsequently synthesized, e.g., lynestrenol and ethynodiol diacetate, which were, in fact, prhormones converted in vivo to norethisterone. All these progestogens were also able to induce androgenic effects when high doses were used. More potent progestogens were synthesized in the 1960s, e.g. norgestrel, norgestrienone. These progestogens were also more androgenic.
  8. ^ Klaus Roth (2014). Chemische Leckerbissen. John Wiley & Sons. p. 69. ISBN 978-3-527-33739-2. Im Prinzip hatten Hohlweg und Inhoffen die Lösung schon 1938 in der Hand, denn ihr Ethinyltestosteron (11) war eine oral wirksame gestagene Verbindung und Schering hatte daraus bereits 1939 ein Medikament (Proluton C®) entwickelt.
  9. ^ a b "IBM Watson Health Products: Please Login".
  10. ^ a b Sweetman, Sean C., ed. (2009). "Sex hormones and their modulators". Martindale: The Complete Drug Reference (36th ed.). London: Pharmaceutical Press. ISBN 978-0-85369-840-1.
  11. ^ a b "List of Progestins".
  12. ^ a b Index Nominum 2000: International Drug Directory. Taylor & Francis. January 2000. ISBN 978-3-88763-075-1.
  13. ^ J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. ISBN 978-1-4757-2085-3.
  14. ^ Cite error: The named reference GordonRydfors2007 was invoked but never defined (see the help page).
  15. ^ Cite error: The named reference Gibbs2008 was invoked but never defined (see the help page).