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Progestogen (medication)
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{{short description|Medication producing effects similar to progesterone}} {{cs1 config|name-list-style=vanc}} {{About|progestogens as medications|the role of progestogens as hormones|Progestogen}} {{Infobox drug class | Image = Progesterone.svg | ImageClass = skin-invert-image | Caption = [[Progesterone (medication)|Progesterone]], the natural progestogen in the body and one of the most widely used progestogen medications | Width = 225px | Synonyms = Progestagen, gestagen, gestogen; progestin (synthetic progestogen); progesterone receptor agonist <!-- Class identifiers --> | Use = [[Hormonal contraceptive|Hormonal birth control]], [[hormone replacement therapy|hormone therapy]], [[gynecological disorder]]s, [[fertility medicine]] and [[pregnancy]] support, [[antigonadotropin|sex-hormone suppression]], others | ATC_prefix = G03 | Biological_target = [[Progesterone receptor]]s ([[Progesterone receptor A|PR-A]], [[Progesterone receptor B|PR-B]], [[Progesterone receptor C|PR-C]]); [[membrane progesterone receptor]]s ([[mPRα]], [[mPRβ]], [[mPRγ]], [[mPRδ]], [[mPRε]]); [[progesterone receptor membrane component]]s ([[PGRMC1]], [[PGRMC2]]) | Chemical_class = [[Steroid]]s ([[pregnane]]s, [[norpregnane]]s, [[retropregnane]]s, [[androstane]]s, [[estrane]]s) <!-- Clinical data --> | Drugs.com = {{Drugs.com|drug-class|progestins}} | Consumer_Reports = <!-- External links --> | MeshID = D011372 }} <!-- Definition and medical uses --> 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 product|natural]] female [[sex hormone]] [[progesterone]] in the body.<ref name="pmid16112947t">{{cite journal | vauthors = Kuhl H | title = Pharmacology of estrogens and progestogens: influence of different routes of administration | journal = Climacteric | volume = 8 | pages = 3–63 | year = 2005 | issue = Suppl 1 | pmid = 16112947 | doi = 10.1080/13697130500148875 | s2cid = 24616324 | url = http://hormonebalance.org/images/documents/Kuhl%2005%20%20Pharm%20Estro%20Progest%20Climacteric_1313155660.pdf}}</ref> A '''progestin''' is a ''[[synthetic compound|synthetic]]'' progestogen.<ref name="pmid16112947t" /> Progestogens are used most commonly in [[hormonal contraception|hormonal birth control]] and [[menopausal hormone therapy]].<ref name="pmid16112947t" /> They can also be used in the treatment of [[gynecological condition]]s, to support [[fertility]] and [[pregnancy]], to lower [[sex hormone]] levels for various purposes, and for other indications.<ref name="pmid16112947t" /> Progestogens are used alone or in combination with [[estrogen (medication)|estrogen]]s.<ref name="pmid16112947t" /> They are available in a wide variety of [[drug formulation|formulation]]s and for use by many different [[route of administration|routes of administration]].<ref name="pmid16112947t" /> Examples of progestogens include natural or [[bioidentical]] [[progesterone (medication)|progesterone]] as well as progestins such as [[medroxyprogesterone acetate]] and [[norethisterone]].<ref name="pmid16112947t" /> <!--Side effects--> [[Side effect]]s of progestogens include [[irregular menstruation|menstrual irregularities]], [[headache]]s, [[nausea]], [[breast tenderness]], [[mood (psychology)|mood]] changes, [[acne]], [[hirsutism|increased hair growth]], and changes in [[liver protein production]] among others.<ref name="pmid16112947t" /><ref name="pmid15358281" /> Other side effects of progestogens may include an increased risk of [[breast cancer]], [[cardiovascular disease]], and [[blood clot]]s.<ref name="pmid15358281" /> At high doses, progestogens can cause [[hypogonadism|low sex hormone levels]] and associated side effects like [[sexual dysfunction]] and an [[osteoporosis|increased risk of bone fractures]].<ref name="pmid20459370">{{cite journal | vauthors = Thibaut F, De La Barra F, Gordon H, Cosyns P, Bradford JM | title = The World Federation of Societies of Biological Psychiatry (WFSBP) guidelines for the biological treatment of paraphilias | journal = World J. Biol. Psychiatry | volume = 11 | issue = 4 | pages = 604–55 | year = 2010 | pmid = 20459370 | doi = 10.3109/15622971003671628 | s2cid = 14949511 }}</ref> <!-- Mechanism of action --> Progestogens are [[agonist]]s of the [[progesterone receptor]]s (PRs) and produce '''progestogenic''', or '''progestational''', effects.<ref name="pmid16112947t" /> They have important effects in the [[female reproductive system]] ([[uterus]], [[cervix]], and [[vagina]]), the [[breast]]s, and the [[brain]].<ref name="pmid16112947t" /> In addition, many progestogens also have other hormonal activities, such as [[androgen]]ic, [[antiandrogen]]ic, [[estrogen (medication)|estrogen]]ic, [[glucocorticoid]], or [[antimineralocorticoid]] activity.<ref name="pmid16112947t" /> They also have [[antigonadotropic]] effects and at high doses can strongly suppress [[sex hormone]] production.<ref name="pmid16112947t" /> Progestogens mediate their contraceptive effects both by inhibiting [[ovulation]] and by thickening [[Cervix#Cervical mucus|cervical mucus]], thereby preventing [[fertilization]].<ref name="JamesonDeGroot2015">{{cite book | vauthors = Glasier A |author-link=Anna Glasier |date=March 20, 2015|chapter=Chapter 134. Contraception| veditors = Jameson JL, De Groot LJ, de Krester D, Giudice LC, Grossman A, Melmed S, Potts Jr JT, Weir GC |title=Endocrinology: Adult and Pediatric|edition=7th|location=Philadelphia|publisher=Saunders Elsevier|page=2306|isbn=978-0-323-18907-1}}</ref><ref name="PattmanNathan2010">{{cite book|title=Oxford Handbook of Genitourinary Medicine, HIV, and Sexual Health|date=November 19, 2010|publisher=Oxford University Press|isbn=978-0-19-957166-6| veditors = Pattman R, Sankar KN, Elewad B, Handy P, Price DA |edition=2nd|location=Oxford|page=360|chapter=Chapter 33. Contraception including contraception in HIV infection and infection reduction|quote=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. |chapter-url=https://books.google.com/books?id=sTWXAwAAQBAJ&pg=PA353}}</ref> They have functional [[antiestrogen]]ic effects in certain tissues like the [[endometrium]], and this underlies their use in menopausal hormone therapy.<ref name="pmid16112947t" /> <!-- History, society, and culture --> Progesterone was first introduced for medical use in 1934 and the first progestin, [[ethisterone]], was introduced for medical use in 1939.<ref name="Kuhl2011t">{{cite journal | author = Kuhl H | title = Pharmacology of Progestogens | journal = J Reproduktionsmed Endokrinol | year = 2011 | volume = 8 | issue = 1 | pages = 157–177 | url = http://www.kup.at/kup/pdf/10168.pdf}}</ref><ref name="LauritzenStudd2005">{{cite book|author1=Christian Lauritzen|author2=John W. W. Studd|title=Current Management of the Menopause|url=https://books.google.com/books?id=WD7S7677xUUC&pg=PA45|date=22 June 2005|publisher=CRC Press|isbn=978-0-203-48612-2|page=45|quote=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.}}</ref><ref name="Roth2014">{{cite book|author=Klaus Roth|title=Chemische Leckerbissen|url=https://books.google.com/books?id=FsKpBAAAQBAJ&pg=PA69|year=2014|publisher=John Wiley & Sons|isbn=978-3-527-33739-2|page=69|quote=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.}}</ref> More [[potency (pharmacology)|potent]] progestins, such as [[norethisterone]], were developed and started to be used in birth control in the 1950s.<ref name="Kuhl2011t" /> Around 60 progestins have been marketed for clinical use in humans or use in [[veterinary medicine]].<ref name="Micromedex">{{cite web | url=http://www.micromedexsolutions.com | title=IBM Watson Health Products: Please Login}}</ref><ref name="Martindale">{{cite book |editor=Sweetman, Sean C. |chapter=Sex hormones and their modulators |title=Martindale: The Complete Drug Reference |edition=36th |year=2009 |publisher=Pharmaceutical Press |location=London|isbn=978-0-85369-840-1|chapter-url=https://www.medicinescomplete.com/mc/martindale/}}</ref><ref name="Drugs.com">{{cite web | url=https://www.drugs.com/drug-class/progestins.html | title=List of Progestins}}</ref><ref name="IndexNominum2000">{{cite book|title=Index Nominum 2000: International Drug Directory|url=https://books.google.com/books?id=5GpcTQD_L2oC|date=January 2000|publisher=Taylor & Francis|isbn=978-3-88763-075-1}}</ref><ref name="Elks2014">{{cite book|author=J. Elks|title=The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies|url=https://books.google.com/books?id=0vXTBwAAQBAJ|date=14 November 2014|publisher=Springer|isbn=978-1-4757-2085-3}}</ref> These progestins can be grouped into different classes and generations.<ref name="pmid16112947t" /><ref name="GordonRydfors2007" /><ref name="Gibbs2008" /> Progestogens are available widely throughout the world and are used in all forms of hormonal birth control and in most menopausal hormone therapy regimens.<ref name="pmid16112947t" /><ref name="Micromedex" /><ref name="Martindale" /><ref name="IndexNominum2000" /><ref name="Drugs.com" /> {{TOC limit|3}}
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