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===Antigonadotropins=== [[File:Estradiol and testosterone levels with a single intramuscular injection of 320 mg polyestradiol phosphate in men.png|thumb|right|300px|class=skin-invert-image|Estradiol and testosterone levels following a single intramuscular injection of 320 mg [[polyestradiol phosphate]], a [[polymer]]ic estradiol ester and prodrug, in men with prostate cancer.<ref name="pmid8610057">{{cite journal | vauthors = Stege R, Gunnarsson PO, Johansson CJ, Olsson P, Pousette A, Carlström K | title = Pharmacokinetics and testosterone suppression of a single dose of polyestradiol phosphate (Estradurin) in prostatic cancer patients | journal = Prostate | volume = 28 | issue = 5 | pages = 307–10 | year = 1996 | pmid = 8610057 | doi = 10.1002/(SICI)1097-0045(199605)28:5<307::AID-PROS6>3.0.CO;2-8 | s2cid = 33548251 }}</ref>]] [[File:Testosterone and luteinizing hormone levels with 100 mg per day oral cyproterone acetate in men.png|thumb|right|300px|class=skin-invert-image|Testosterone and luteinizing hormone levels with 100 mg/day oral [[cyproterone acetate]] in men.<ref name="FourcadeMcLeod2015">{{cite journal| vauthors = Fourcade RO, McLeod D |title=Tolerability of Antiandrogens in the Treatment of Prostate Cancer|journal=UroOncology|volume=4|issue=1|year=2015|pages=5–13|issn=1561-0950|doi=10.1080/1561095042000191655}}</ref>]] [[Antigonadotropin]]s are drugs that suppress the GnRH-mediated [[secretion]] of [[gonadotropin]]s from the [[pituitary gland]].<ref name="FarmerWalker2012" /> Gonadotropins include [[luteinizing hormone]] (LH) and [[follicle-stimulating hormone]] (FSH) and are [[peptide hormone]]s that signal the [[gonad]]s to produce [[sex hormone]]s. By suppressing gonadotropin secretion, antigonadotropins suppress gonadal sex hormone production and by extension circulating androgen levels.<ref name="FarmerWalker2012" /> [[GnRH modulator]]s, including both [[GnRH agonist]]s and [[GnRH antagonist]]s, are powerful antigonadotropins that are able to suppress androgen levels by 95% in men.<ref name="Urotext2001">{{cite book|author=Urotext|title=Urotext-Luts: Urology|url=https://books.google.com/books?id=6zjtA37qDsMC&pg=PA71|date=1 January 2001|publisher=Urotext|isbn=978-1-903737-03-3|pages=71–|access-date=2016-12-27|archive-date=2023-01-11|archive-url=https://web.archive.org/web/20230111061908/https://books.google.com/books?id=6zjtA37qDsMC&pg=PA71|url-status=live}}</ref> In addition, estrogens and progestogens are antigonadotropins via exertion of [[negative feedback]] on the [[hypothalamic–pituitary–gonadal axis]] (HPG axis).<ref name="Brueggemeier2006" /><ref name="pmid10997774">{{cite journal |vauthors=de Lignières B, Silberstein S | title = Pharmacodynamics of oestrogens and progestogens | journal = Cephalalgia: An International Journal of Headache | volume = 20 | issue = 3 | pages = 200–7 |date=April 2000 | pmid = 10997774 | doi = 10.1046/j.1468-2982.2000.00042.x| s2cid = 40392817 | doi-access = free }}</ref><ref name="pmid368741">{{cite journal | vauthors = Neumann F | title = The physiological action of progesterone and the pharmacological effects of progestogens--a short review | journal = Postgraduate Medical Journal | volume = 54 | issue = Suppl 2 | pages = 11–24 | year = 1978 | pmid = 368741 }}</ref> High-dose estrogens are able to suppress androgen levels to castrate levels in men similarly to GnRH modulators,<ref name="pmid7000222">{{cite journal | vauthors = Jacobi GH, Altwein JE, Kurth KH, Basting R, Hohenfellner R | title = Treatment of advanced prostatic cancer with parenteral cyproterone acetate: a phase III randomised trial | journal = Br J Urol | volume = 52 | issue = 3 | pages = 208–15 | year = 1980 | pmid = 7000222 | doi = 10.1111/j.1464-410x.1980.tb02961.x}}</ref> while high-dose progestogens are able to suppress androgen levels by up to approximately 70 to 80% in men.<ref name="WeinKavoussi2011">{{cite book|vauthors=Wein AJ, Kavoussi LR, Novick AC, Partin AW, Peters CA|title=Campbell-Walsh Urology: Expert Consult Premium Edition: Enhanced Online Features and Print, 4-Volume Set|url=https://books.google.com/books?id=fu3BBwAAQBAJ&pg=PA2938|date=25 August 2011|publisher=Elsevier Health Sciences|isbn=978-1-4160-6911-9|pages=2938–|access-date=27 December 2016|archive-date=11 January 2023|archive-url=https://web.archive.org/web/20230111061407/https://books.google.com/books?id=fu3BBwAAQBAJ&pg=PA2938|url-status=live}}</ref><ref name="pmid519881">{{cite journal | vauthors = Kjeld JM, Puah CM, Kaufman B, Loizou S, Vlotides J, Gwee HM, Kahn F, Sood R, Joplin GF | title = Effects of norgestrel and ethinyloestradiol ingestion on serum levels of sex hormones and gonadotrophins in men | journal = Clinical Endocrinology | volume = 11 | issue = 5 | pages = 497–504 | year = 1979 | pmid = 519881 | doi = 10.1111/j.1365-2265.1979.tb03102.x| s2cid = 5836155 }}</ref> Examples of GnRH agonists include [[leuprorelin]] (leuprolide) and [[goserelin]], while an example of a GnRH antagonist is [[cetrorelix]].<ref name="LemkeWilliams2012" /> Estrogens that are or that have been used as antigonadotropins include estradiol, [[estradiol ester]]s like [[estradiol valerate]], [[estradiol undecylate]], and [[polyestradiol phosphate]], conjugated estrogens, ethinylestradiol, diethylstilbestrol (no longer widely used), and [[bifluranol]].<ref name="pmid18268497">{{cite journal | vauthors = Norman G, Dean ME, Langley RE, Hodges ZC, Ritchie G, Parmar MK, Sydes MR, Abel P, Eastwood AJ | title = Parenteral oestrogen in the treatment of prostate cancer: a systematic review | journal = Br. J. Cancer | volume = 98 | issue = 4 | pages = 697–707 | year = 2008 | pmid = 18268497 | pmc = 2259178 | doi = 10.1038/sj.bjc.6604230 }}</ref><ref name="pmid6258683">{{cite journal | vauthors = Dekanski JB | title = Anti-prostatic activity of bifluranol, a fluorinated bibenzyl | journal = Br. J. Pharmacol. | volume = 71 | issue = 1 | pages = 11–6 | year = 1980 | pmid = 6258683 | pmc = 2044395 | doi = 10.1111/j.1476-5381.1980.tb10903.x}}</ref> Progestogens that are used as antigonadotropins include [[chlormadinone acetate]], cyproterone acetate, gestonorone caproate,<ref name="pmid694436">{{cite journal | vauthors = Sander S, Nissen-Meyer R, Aakvaag A | title = On gestagen treatment of advanced prostatic carcinoma | journal = Scand. J. Urol. Nephrol. | volume = 12 | issue = 2 | pages = 119–21 | year = 1978 | pmid = 694436 | doi = 10.3109/00365597809179977}}</ref> [[hydroxyprogesterone caproate]], medroxyprogesterone acetate, [[megestrol acetate]], and oxendolone.<ref name="Brueggemeier2006" /><ref name="PrentkyBurgess2000">{{cite book| vauthors = Prentky RA, Burgess AW |title= Forensic Management of Sexual Offenders|url=https://books.google.com/books?id=-50Of8_n_TAC&pg=PA219 |date=31 July 2000|publisher=Springer Science & Business Media|isbn=978-0-306-46278-8|pages=219–}}</ref><ref name="pmid294107">{{cite journal | vauthors = Sudo K, Yamazaki I, Masuoka M, Nakayama R | title = Anti-androgen TSAA-291. IV. Effects of the anti-androgen TSAA-291 (16 beta-ethyl-17 beta-hydroxy-4-oestren-3-one) on the secretion of gonadotrophins | journal = Acta Endocrinol Suppl (Copenh) | volume = 229 | pages = 53–66 | year = 1979 | pmid = 294107 | doi = 10.1530/acta.0.092s053}}</ref>
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