女性化激素疗法：修订间差异

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==== 非甾体抗雄激素 ====
==== 非甾体抗雄激素 ====
{{See also|比卡鲁胺医疗用途#跨性别激素治疗|尼鲁米特#跨性别激素治疗|氟他胺#跨性别激素治疗}}
{{See also|比卡鲁胺医疗用途#跨性别激素治疗|尼鲁米特#跨性别激素治疗|氟他胺#跨性别激素治疗}}

[[非甾体抗雄激素]]是[[非甾体]]类抗雄激素，因此在[[化学结构]]方面与甾体激素无关<ref name="pmid10637363" /><ref name="LemkeWilliams2008" />。这些药物主要用于治疗前列腺癌<ref name="LemkeWilliams2008" />，但也用于治疗[[痤疮]]、[[多毛症|面部/体毛过度生长]]和女性[[雄激素过多症|高雄激素水平]]等其他目的<ref name="pmid30256230" /><ref name="pmid28379593">{{cite journal | vauthors = Giorgetti R, di Muzio M, Giorgetti A, Girolami D, Borgia L, Tagliabracci A | title = Flutamide-induced hepatotoxicity: ethical and scientific issues | journal = Eur Rev Med Pharmacol Sci | volume = 21 | issue = 1 Suppl | pages = 69–77 | date = 2017-03 | pmid = 28379593 | url = https://www.europeanreview.org/wp/wp-content/uploads/69-77-Flutamide-induced-hepatotoxicity.pdf}}</ref><ref name="pmid24455796">{{cite journal | vauthors = Erem C | title = Update on idiopathic hirsutism: diagnosis and treatment | journal = Acta Clin Belg | volume = 68 | issue = 4 | pages = 268–74 | date = 2013 | pmid = 24455796 | doi = 10.2143/ACB.3267 | s2cid = 39120534 }}</ref><ref name="pmid29211888">{{cite journal | vauthors = Moretti C, Guccione L, Di Giacinto P, Simonelli I, Exacoustos C, Toscano V, Motta C, De Leo V, Petraglia F, Lenzi A | title = Combined Oral Contraception and Bicalutamide in Polycystic Ovary Syndrome and Severe Hirsutism: A Double-Blind Randomized Controlled Trial | journal = J. Clin. Endocrinol. Metab. | volume = 103 | issue = 3 | pages = 824–838 | date = 2018-03 | pmid = 29211888 | doi = 10.1210/jc.2017-01186 | s2cid = 3784055 | doi-access = free }}</ref>。与甾体抗雄激素不同，非甾体抗雄激素对雄激素受体具有[[结合选择性|高度选择性]]，可作为纯雄激素受体拮抗剂<ref name="LemkeWilliams2008" /><ref name="FiggChau2010" />。然而，与螺内酯类似，它们不会降低雄激素水平，而是仅通过阻止雄激素激活雄激素受体来发挥作用<ref name="LemkeWilliams2008" /><ref name="FiggChau2010" />。非甾体抗雄激素是比甾体抗雄激素更[[效能|有效]]的雄激素受体拮抗剂<ref name="pmid10637363" /><ref name="pmid9000189">{{cite journal | vauthors = Caubet JF, Tosteson TD, Dong EW, Naylon EM, Whiting GW, Ernstoff MS, Ross SD | title = Maximum androgen blockade in advanced prostate cancer: a meta-analysis of published randomized controlled trials using nonsteroidal antiandrogens | journal = Urology | volume = 49 | issue = 1 | pages = 71–8 | date = 1997-01 | pmid = 9000189 | doi = 10.1016/S0090-4295(96)00325-1 }}</ref>，因此，与GnRH调节剂一起，在前列腺癌的治疗中已在很大程度上取代了甾体抗雄激素<ref name="LemkeWilliams2008" /><ref name="ChabnerLongo2010">{{cite book|author1=Bruce A. Chabner|author2=Dan L. Longo|title=Cancer Chemotherapy and Biotherapy: Principles and Practice|url=https://books.google.com/books?id=WL4arNFsQa8C&pg=PA680|date=2010-11-8|publisher=Lippincott Williams & Wilkins|isbn=978-1-60547-431-1|pages=680–}}</ref>。

已用于跨性别女性的非甾体抗雄激素包括第一代药物[[氟他胺]]（优力霉）、[[尼鲁米特]]（Anandron，Nilandron）和[[比卡鲁胺]]（可苏多）<ref name="pmid30256230" /><ref name="pmid21449788">{{cite journal | vauthors = Gooren LJ | title = Clinical practice. Care of transsexual persons | journal = N. Engl. J. Med. | volume = 364 | issue = 13 | pages = 1251–7 | date = 2011-03 | pmid = 21449788 | doi = 10.1056/NEJMcp1008161 }}</ref><ref name="DahlFeldman2015" /><ref name="Deutsch2016" /><ref name="NeymanFuqua2017">{{cite journal | last1 = Neyman | first1 = A | last2 = Fuqua | first2 = JS | last3 = Eugster | first3 = EA | title = Bicalutamide as an Androgen Blocker with Secondary Effect of Promoting Feminization in Male to Female (MTF) Transgender Adolescents | journal = Hormone Research in Paediatrics | volume = 88 | pages = 1–628 | date = 2017-12 | doi = 10.1159/000481424 | pmid = 28968603 | url = https://www.karger.com/Article/Pdf/481424#page=477| doi-access = free }}</ref>{{Rp|477}}。存在更新且更有效的第二代非甾体抗雄激素药物，如[[恩杂鲁胺]]（安可坦）、[[阿帕鲁胺]]（安列康）和[[达洛鲁胺]]（Nubeqa），但由于没有[[通用名药物|仿制药]]且尚未用于跨性别女性，因此价格非常昂贵<ref name="pmid29730201">{{cite journal | vauthors = Crawford ED, Schellhammer PF, McLeod DG, Moul JW, Higano CS, Shore N, Denis L, Iversen P, Eisenberger MA, Labrie F | title = Androgen Receptor-Targeted Treatments for Prostate Cancer: 35 Years' Progress with Antiandrogens | journal = J. Urol. | volume = 200| issue = 5| pages = 956–966| date = 2018-05 | pmid = 29730201 | doi = 10.1016/j.juro.2018.04.083 | s2cid = 19162538 }}</ref><ref name="pmid29497605">{{cite journal | vauthors = Ito Y, Sadar MD | title = Enzalutamide and blocking androgen receptor in advanced prostate cancer: lessons learnt from the history of drug development of antiandrogens | journal = Res Rep Urol | volume = 10 | pages = 23–32 | date = 2018 | pmid = 29497605 | pmc = 5818862 | doi = 10.2147/RRU.S157116 }}</ref>。氟他胺和尼鲁米特具有相对较高的[[毒性]]，包括相当大的[[肝毒性|肝损伤]]和[[呼吸系统疾病|肺病]]风险<ref name="pmid25270521">{{cite journal | vauthors = Ricci F, Buzzatti G, Rubagotti A, Boccardo F | title = Safety of antiandrogen therapy for treating prostate cancer | journal = Expert Opin Drug Saf | volume = 13 | issue = 11 | pages = 1483–99 | date = 2014-11 | pmid = 25270521 | doi = 10.1517/14740338.2014.966686 | s2cid = 207488100 }}</ref><ref name="pmid28379593" />。由于其风险，现在已经限制且不鼓励在顺性别和跨性别女性中使用氟他胺<ref name="pmid30256230" /><ref name="pmid28379593" /><ref name="DahlFeldman2015" />。临床上氟他胺和尼鲁米特已在很大程度上被比卡鲁胺取代<ref name="Moser2008">{{cite book|author=Lutz Moser|title=Controversies in the Treatment of Prostate Cancer|url=https://books.google.com/books?id=4J4OCRyHWRYC&pg=PA41|date=2008-01-1|publisher=Karger Medical and Scientific Publishers|isbn=978-3-8055-8524-8|pages=41–}}</ref><ref name="Demos2011">{{cite book|title=Prostate Cancer|url=https://books.google.com/books?id=WJkjgbRJe3EC&pg=PA460|date=2011-12-20|publisher=Demos Medical Publishing|isbn=978-1-935281-91-7|pages=460, 504}}</ref>，到2000年代中期，比卡鲁胺占[[美国]]非甾体抗雄激素处方的近90%<ref name="HHS2010">{{citation |title=Bicalutamide BPCA Drug Use Review in the Pediatric Population |first=Stephen |last=Chang | publisher=[[美国卫生及公共服务部|U.S. Department of Health and Human Service]] |date=2010-03-10 |access-date=2016-07-20 |url=https://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/PediatricAdvisoryCommittee/UCM214400.pdf |url-status=live |archive-url=https://web.archive.org/web/20161024181831/https://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/PediatricAdvisoryCommittee/UCM214400.pdf |archive-date=2016-10-24}}</ref><ref name="FiggChau2010">{{cite book|author1=William D. Figg|author2=Cindy H. Chau|author3=Eric J. Small|title=Drug Management of Prostate Cancer|url=https://books.google.com/books?id=4KDrjeWA5-UC&pg=PA72|date=2010-09-14|publisher=Springer Science & Business Media|isbn=978-1-60327-829-4|pages=71–72}}</ref>。相对于氟他胺和尼鲁米特，以及与醋酸环丙孕酮相比，比卡鲁胺具有出色的[[药物耐受性|耐受性]]和[[药物安全性|安全性]]<ref name="pmid8560681">{{cite journal | vauthors = Kolvenbag GJ, Blackledge GR | title = Worldwide activity and safety of bicalutamide: a summary review | journal = Urology | volume = 47 | issue = 1A Suppl | pages = 70–9; discussion 80–4 | date = 1996-01 | pmid = 8560681 | doi = 10.1016/S0090-4295(96)80012-4 }}</ref><ref name="pmid23013078">{{cite journal | vauthors = Vogelzang NJ | title = Enzalutamide--a major advance in the treatment of metastatic prostate cancer | journal = N. Engl. J. Med. | volume = 367 | issue = 13 | pages = 1256–7 | date = 2012-09 | pmid = 23013078 | doi = 10.1056/NEJMe1209041 }}</ref><ref name="RamonDenis2007">{{cite book|author1=J. Ramon|author2=L.J. Denis|title=Prostate Cancer|url=https://books.google.com/books?id=Bg6ZbqhhboUC&pg=PA256|date=2007-06-5|publisher=Springer Science & Business Media|isbn=978-3-540-40901-4|pages=256–}}</ref>。它对女性几乎没有副作用<ref name="pmid24455796" /><ref name="pmid29211888" />。然而，尽管比卡鲁胺的耐受性和安全性大大提高，但仍有很小的肝酶升高风险，并且与非常罕见的肝损伤和肺病病例有关<ref name="pmid30256230" /><ref name="pmid25270521" /><ref name="GretarsdottirBjornsdottir2018">{{cite journal|last1=Gretarsdottir|first1=Helga M.|last2=Bjornsdottir|first2=Elin|last3=Bjornsson|first3=Einar S.|title=Bicalutamide-Associated Acute Liver Injury and Migratory Arthralgia: A Rare but Clinically Important Adverse Effect|journal=Case Reports in Gastroenterology|volume=12|issue=2|year=2018|pages=266–270|issn=1662-0631|doi=10.1159/000485175|s2cid=81661015|doi-access=free}}</ref>。

对于希望保持[[性冲动|性欲]]、[[性功能]]和/或[[生育能力]]的跨性别女性来说，相比于抑制睾酮水平并能极大破坏这些功能的抗雄激素，如醋酸环丙孕酮和GnRH调节剂等，比卡鲁胺等非甾体类抗雄激素可能是一个特别有利的选择<ref name="pmid29352423">{{cite journal | vauthors = Gao Y, Maurer T, Mirmirani P | title = Understanding and Addressing Hair Disorders in Transgender Individuals | journal = Am J Clin Dermatol | volume = 19| issue = 4| pages = 517–527| date = 2018-01 | pmid = 29352423 | doi = 10.1007/s40257-018-0343-z | s2cid = 6467968 | quote = 非甾体抗雄激素包括氟他胺、尼鲁米特和比卡鲁胺，它们不会降低雄激素水平，可能对想要保持性欲和生育能力的个体有利[9]。（Non-steroidal antiandrogens include flutamide, nilutamide, and bicalutamide, which do not lower androgen levels and may be favorable for individuals who want to preserve sex drive and fertility [9].）}}</ref><ref name="IversenMelezinek2001">{{cite journal | vauthors = Iversen P, Melezinek I, Schmidt A | title = Nonsteroidal antiandrogens: a therapeutic option for patients with advanced prostate cancer who wish to retain sexual interest and function | journal = BJU International | volume = 87 | issue = 1 | pages = 47–56 | date = 2001-01 | pmid = 11121992 | doi = 10.1046/j.1464-410x.2001.00988.x | s2cid = 28215804 | doi-access = free }}</ref><ref name="MorganteGradini2001">{{cite journal|last1=Morgante|first1=E|last2=Gradini|first2=R|last3=Realacci|first3=M|last4=Sale|first4=P|last5=D'eramo|first5=G|last6=Perrone|first6=G A|last7=Cardillo|first7=M R|last8=Petrangeli|first8=E|last9=Russo|first9=Ma|last10=Di Silverio|first10=F|title=Effects of long-term treatment with the anti-androgen bicalutamide on human testis: an ultrastructural and morphometric study|journal=Histopathology|volume=38|issue=3|year=2001|pages=195–201|issn=0309-0167|doi=10.1046/j.1365-2559.2001.01077.x|pmid=11260298|s2cid=36892099}}</ref>。然而，雌激素会抑制睾酮水平，高剂量会显着破坏性欲、功能和生育能力<ref name="JonesReiter2016">{{cite journal |last1=Jones |first1=C. A. |last2=Reiter |first2=L. |last3=Greenblatt |first3=E. | title=Fertility preservation in transgender patients |journal=International Journal of Transgenderism |volume=17 |issue=2 |year=2016 |pages=76–82 |issn=1553-2739 |doi=10.1080/15532739.2016.1153992 |s2cid=58849546 |quote=传统上，建议患者在开始异性激素治疗之前冷冻保存精子，因为随着时间的推移，高剂量雌激素治疗可能会降低精子活力（Lubbert等，1992）。然而，由于研究有限，雌激素治疗导致的生育力下降仍有争议。（Traditionally, patients have been advised to cryopreserve sperm prior to starting cross-sex hormone therapy as there is a potential for a decline in sperm motility with high-dose estrogen therapy over time (Lubbert et al., 1992). However, this decline in fertility due to estrogen therapy is controversial due to limited studies.）}}</ref><ref name="PayneHardy2007">{{cite book |first1=Anita H. |last1=Payne |first2=Matthew P. |last2=Hardy | title=The Leydig Cell in Health and Disease |url=https://books.google.com/books?id=x4ttqKIAOg0C&pg=PA422 |date=2007-10-28 |publisher=Springer Science & Business Media |isbn=978-1-59745-453-7 |pages=422–431 |quote=雌激素是下丘脑-垂体-睾丸轴的高效抑制剂 (212-214)。除了它们在下丘脑和垂体水平的负反馈作用外，还可能对睾丸产生直接抑制作用（215，216）。[...][用雌激素治疗的]睾丸组织学显示曲细精管紊乱、空泡化和管腔缺失，以及精子发生的区室化。（Estrogens are highly efficient inhibitors of the hypothalamic-hypophyseal-testicular axis (212–214). Aside from their negative feedback action at the level of the hypothalamus and pituitary, direct inhibitory effects on the testis are likely (215,216). [...] The histology of the testes [with estrogen treatment] showed disorganization of the seminiferous tubules, vacuolization and absence of lumen, and compartmentalization of spermatogenesis.）}}</ref><ref name="Salam2003">{{cite book |first=Muhammad A. |last=Salam | title=Principles & Practice of Urology: A Comprehensive Text |url=https://books.google.com/books?id=y50kTcCCfEcC&pg=PA684 |year=2003 |publisher=Universal-Publishers |isbn=978-1-58112-412-5 |pages=684– |quote=雌激素主要通过下丘脑-垂体水平的负反馈来减少LH分泌和睾丸雄激素合成。[...]有趣的是，如果不间断地暴露，3年后停止雌激素治疗，血清睾酮可能会保持在去势水平长达3年。这种长期抑制被认为是雌激素对睾丸间质细胞的直接影响所致。（Estrogens act primarily through negative feedback at the hypothalamic-pituitary level to reduce LH secretion and testicular androgen synthesis. [...] Interestingly, if the treatment with estrogens is discontinued after 3 yr. of uninterrupted exposure, serum testosterone may remain at castration levels for up to another 3 yr. This prolonged suppression is thought to result from a direct effect of estrogens on the Leydig cells.）}}</ref><ref name="pmid7500443">{{cite journal | vauthors = Cox RL, Crawford ED | title = Estrogens in the treatment of prostate cancer | journal = J. Urol. | volume = 154 | issue = 6 | pages = 1991–8 | date = 1995-12 | pmid = 7500443 | doi = 10.1016/S0022-5347(01)66670-9 }}</ref>。此外，长期暴露后，雌激素对性腺功能和生育能力的破坏可能是永久性的<ref name="Salam2003" /><ref name="pmid7500443" />。

==== GnRH调节剂 ====


== 效果 ==
== 效果 ==

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女性化激素疗法（英語：Feminizing hormone therapy）是一种激素替代（HRT）及性別重置療法，旨在将跨性別者的第二性征从男或中性转变为女性气质[1][2][3][4][5][6]。它是一种常见的跨性别激素疗法（另一种是男性化激素疗法），用于治疗跨性別女性和非二元跨女个体。根据个人需要和偏好，一些人，特别是雙性人，但也包括一些双性恋者，也会采取这种形式的治疗。

该疗法的目的是引起患者希望成为的性别的第二性征的发育，例如乳房发育，女性化的毛发、脂肪和肌肉分布等。它无法消除自然青春期产生的许多变化，这可能需要手术和其他治疗来逆转（见下文）。用于女性化激素疗法的药物包括雌激素、抗雄激素、孕激素和促性腺素釋素（GnRH调节剂）。

女性化激素疗法已被证明可以缓解与性別不一致相关的部分或全部不适[7]。

要求

主条目：跨性别激素疗法 § 要求和跨性别激素疗法 § 可及性

许多医生按照世界跨性别人士健康专业协会（WPATH）的护理标准（SoC）模式运作，要求跨性别者接受心理治療并提供心理治疗师的推荐信，以便获得激素治疗[8]。其他医生按照知情同意模式运作，除了同意之外，对跨性别激素疗法没有任何要求[8]。某些不受监管的互联网網路藥房也出售用于跨性别激素治疗的药物，无需处方，一些跨性别女性购买这些药物并使用自己动手（DIY）或自我用药的方法自行治疗[9][10]。许多跨性别者在/r/TransDIY和/r/MtFHRT等Reddit社区讨论和分享有关DIY激素治疗的信息[9][10][11][12]。许多跨性别者转向DIY激素疗法的一个原因是，由于在世界某些地区（例如英国），看医生的费用通常很高，而且限制性标准使一些人没有资格接受治疗[9][10]。

跨性别激素治疗的可及性在全世界各个国家有所不同[8]。

药物

跨性别女性药品和剂量[13][3][5][6][14][a]
药品 商品名 类型 途径 剂量[b]
雌二醇 多种 雌激素 口服 2–10毫克/日
多种 雌激素 舌下 1–8毫克/日
康美华（Climara）[c] 雌激素 透皮贴片 25–400微克/日
迪维舒凝胶（Divigel）[c] 雌激素 透皮凝胶 0.5–5毫克/日
多种 雌激素 皮下植入 50–200毫克每6–24个月
戊酸雌二醇 补佳乐（Progynova） 雌激素 口服 2–10毫克/日
补佳乐（Progynova） 雌激素 舌下 1–8毫克/日
Del雌激素（Delestrogen）[c] 雌激素 肌肉注射，皮下注射 2–10毫克/周或
5–20毫克每2周
环戊丙酸雌二醇（英语：Estradiol cypionate） 狄波－雌二醇（Depo-Estradiol） 雌激素 肌肉注射，皮下注射 2–10毫克/周或
5–20毫克每2周
苯甲酸雌二醇（英语：Estradiol benzoate） 保女荣－B（Progynon-B） 雌激素 肌肉注射，皮下注射 0.5–1.5毫克每2–3日
雌三醇 欧维婷（Ovestin）[c] 雌激素 口服 4–6毫克/日
螺内酯 安体舒通（Aldactone） 抗雄激素 口服 100–400毫克/日
醋酸环丙孕酮 色普龙（Androcur） 抗雄激素；
孕激素		 口服 5–100毫克/日
色普龙长效（Androcur Depot） 肌肉注射 300毫克/月
比卡鲁胺（英语：Bicalutamide） 康士得（Casodex） 抗雄激素 口服 25–50毫克/日
恩扎卢胺（英语：Enzalutamide） 安可坦（Xtandi） 抗雄激素 口服 160毫克/日
促性腺激素释放激素类似物（英语：GnRH analogue） 多种 促性腺激素释放激素调节剂 多种 多变
噁拉戈利（英语：Elagolix） Orilissa 促性腺激素释放激素拮抗剂 口服 150毫克/日或
200毫克每日两次
非那斯特莱 保法止（Propecia） 5α-还原酶抑制剂（英语：5α-Reductase inhibitor） 口服 1–5毫克/日
度他雄胺（英语：Dutasteride） 安福达（Avodart） 5α-还原酶抑制剂 口服 0.25–0.5毫克/日
孕酮 Prometrium[c] 孕激素 口服 100–400毫克/日
醋酸甲羟孕酮 普维拉（Provera） 孕激素 口服 2.5–40毫克/日
狄波－普维拉（Depo-Provera） 孕激素 肌肉注射 150毫克每3个月
狄波－皮下普维拉104（Depo-SubQ Provera 104） 孕激素 皮下注射 104毫克每3个月
己酸羟孕酮（英语：Hydroxyprogesterone caproate） 普罗路通（Proluton） 孕激素 肌肉注射 250毫克/周
地屈孕酮 达芙通（Duphaston） 孕激素 口服 20毫克/日
屈螺酮（英语：Drospirenone） Slynd 孕激素 口服 3毫克/日
多潘立酮[d] 吗丁啉（Motilium） 催乳素释放剂 口服 30–80毫克/日[e]
  1. ^ 其他来源：[15][16][17][18][19][20][21][22][23][24][25][26][27][28][29][30][31][32][33][34][35][36][37][38][39][40][41][42][43][44][45]
  2. ^ 如果与一种促性腺激素释放激素激动剂或拮抗剂组合使用，青少年的起始剂量可以更少。
  3. ^ 3.0 3.1 3.2 3.3 3.4 也有其他商品名。
  4. ^ 专门为了诱导泌乳（英语：induction of lactation）从而实现母乳哺育。
  5. ^ 分次给药。

各种不同的性激素药物用于跨性别女性的女性化激素疗法[13][8][3][4]。其中包括雌激素，用于诱导女性化并抑制睾酮水平；抗雄激素，如雄激素受体拮抗剂、抗促性腺激素、GnRH调节剂和5α-还原酶抑制剂，以进一步对抗睾酮等雄激素的作用；以及孕激素，以获得各种可能但不确定的益处[13][8][3][4]。雌激素与抗雄激素联合使用是跨性别女性女性化激素疗法的主流[46][47]。

雌激素

参见：雌激素 (药物) § 跨性别女性和雌二醇 (药物) § 跨性别女性
在患有前列腺癌的男性中，单次肌肉注射320 mg聚磷酸雌二醇（一种雌二醇酯聚合物和前体药物）后12周内的雌二醇和睾酮水平[48]。展示肠外雌二醇抑制睾酮的水平。
在跨性别女性中，单用口服雌二醇或联合抗雄激素治疗期间，睾酮水平与雌二醇水平（和相应雌二醇剂量）的关系[49]。紫色虚线是女性/去势患者范围的上限（~50 ng/dL），灰色虚线是术后跨性别女性对照组的睾酮水平（21.7 ng/dL）[49]。

雌激素是女性体内主要的性激素，负责发育和维持女性的第二性征，如乳房、宽臀部及女性的脂肪分布模式[4]。雌激素通过结合并激活雌激素受体（ER）发挥作用，ER是它们在体内的靶点[50]。有多种不同形式的雌激素可供医学使用[50]。跨性别女性最常用的雌激素包括雌二醇，它是女性体内最主要的天然雌激素，以及雌二醇酯，如戊酸雌二醇和环戊丙酸雌二醇，它们是雌二醇的前体药物[13][4][50]。用于绝经期激素治疗（MHT）的結合型雌激素（普力马），以及用于避孕药的炔雌醇，过去曾用于跨性别女性，但由于其血栓和心血管问题的风险较高，现在不再推荐，也很少使用[4][13][8][5]。雌激素可通过口服、舌下含服、透皮/外用（通过贴片或凝胶）、直肠、肌肉或皮下注射或植入的方式给药[50][51][52][53][54]。首选肠外（非口服）途径，因为这样血凝块和心血管问题的风险可最小或可忽略不计[5][55][56][57][58]。

除了产生女性化外，雌激素还具有抗促性腺激素作用，抑制性腺产生性激素[51][49][59]。雌激素主要负责抑制跨性别女性的睾酮水平[51][59]。雌二醇水平在200 pg/mL及以上，可抑制睾酮水平约90%，而雌二醇水平在500 pg/mL及以上，可抑制睾酮水平约95%，或达到与睾丸切除术和GnRH调节剂相当的程度[60][61]。较低的雌二醇水平也可以显著抑制睾酮的产生，但不完全[49]。当单独的雌二醇不足以抑制睾酮水平时，可以使用抗雄激素来抑制或阻断残留睾酮的作用[51]。口服雌二醇往往难以充分抑制睾酮水平，因为所产生的雌二醇水平相对较低[49][62][63]。

在睾丸切除术（手术切除性腺）或性别重置手术前，用于跨性别女性的雌激素剂量通常高于用于顺性别女性的替代剂量[64][65][66]。这有助于抑制睾酮水平[65]。内分泌学会（2017）建议将雌二醇水平大致维持在绝经前妇女的正常平均范围内，约100至200 pg/mL[13]。然而他们指出，这种生理水平的雌二醇通常无法将睾酮水平抑制到女性范围内[13]。2018年考科藍的一项综述计划对将跨性别女性雌二醇水平保持在较低水平提出质疑，这会导致睾酮水平的不完全抑制，并且需要加入抗雄激素[67]。综述计划指出，高剂量的非经肠雌二醇已知是安全的[67]。内分泌学会本身建议注射会导致雌二醇水平明显超出正常女性范围的雌二醇酯剂量，例如每周10 mg戊酸雌二醇肌肉注射[13]。单次注射，雌二醇峰值水平约为1,250 pg/mL，7天后200 pg/mL左右[68][69]。当在睾丸切除术或性别重置手术后，不再需要抑制性腺睾酮时，可以减少雌激素的剂量[5]。

抗雄激素

参见：抗雄激素 § 跨性别激素治疗

抗雄激素是防止体内雄激素作用的药物[70][71]。雄激素，如睾酮和双氢睾酮（DHT），是有睾丸个体的主要性激素，负责发育和维持男性的第二性徵，如低沉的声音、宽阔的肩膀和男性化的毛发、肌肉和脂肪分布[72][73]。此外，雄激素刺激性欲和自发勃起的频率，并导致痤疮、体臭和雄激素依赖性脱发[72][73]。它们还在乳房中有功能性抗雌激素作用，并阻止雌激素介导的乳房发育，即使在低水平时也如此[74][75][76][77]。雄激素通过结合并激活雄激素受体发挥作用，雄激素受体是它们在体内的靶点[78]。抗雄激素阻止雄激素与雄激素受体结合，和/或阻断或抑制雄激素的合成，达到抗雄激素目的[70]。

直接阻断雄激素受体的抗雄激素称为雄激素受体拮抗剂或阻滞剂，而抑制雄激素酶促生物合成反应的抗雄激素称为雄激素合成抑制剂，抑制性腺中雄激素产生过程的抗雄激素称为抗促性腺激素[71]。雌激素和孕激素是抗促性腺激素，因此是功能性抗雄激素[51][79][80][81]。在跨性别女性中使用抗雄激素的目的是阻断或抑制单雌激素无法抑制的残留睾酮[51][70][59]。如果睾酮水平在正常女性范围内或接受了睾丸切除术，则不一定需要额外的抗雄激素治疗[51][70][59]。然而，睾酮水平在正常女性范围内，但仍持续存在雄激素依赖性皮肤和/或头发症状（如痤疮、皮脂溢、油性皮肤或头皮脱发）的个体仍可能受益于服用抗雄激素，因为抗雄激素可以减轻或消除这些症状[82][83][84]。

甾体抗雄激素

参见：螺内酯 § 跨性别激素治疗和醋酸环丙孕酮 § 跨性别激素治疗

甾体抗雄激素是在化学结构上类似于甾体激素如睾酮、孕酮的抗雄激素[85]。它们是跨性别女性中最常用的抗雄激素药物[8]。螺内酯（安体舒通）相对安全且价格低廉，是在美国最常用的抗雄激素药物[86][87]。醋酸环丙孕酮（安得卡）未在美国上市，但在欧洲、加拿大和世界其他地区广泛使用[8][70][86][88]。醋酸甲羟孕酮（普维拉，狄波－普维拉）是一种类似的药物，在美国有时用于代替醋酸环丙孕酮[89][90]。

在跨性别人群中，单用雌二醇（E2）、或与抗雄激素（AA）如螺内酯（SPL）或醋酸环丙孕酮（CPA）联用时的睾酮水平[91]。在几乎所有情况下，雌二醇都以口服戊酸雌二醇（EV）的形式使用[91]。水平虚线是女性/去势患者范围的上限（~50 ng/dL)。

螺内酯是一种抗鹽皮質激素（盐皮质激素受体的拮抗剂）和保钾利尿剂，主要用于治疗其他利尿劑引起的高血壓、水肿、高醛固酮和低钾等，以及其他用途[92]。螺内酯作为一种抗雄激素，最初是一种无意发现的次要作用[92]。它主要通过作为雄激素受体拮抗剂，发挥抗雄激素作用[93]。该药物也是一种弱甾体生成抑制剂，可抑制雄激素的酶促合成[94][93][95]。然而，这种作用的效力很低，螺内酯对激素水平的影响参差不齐[94][93][95][96][97]。在任何情况下，通常螺内酯不会改变睾酮水平[94][93][95][96][97]。对跨性别女性的研究发现，螺内酯不会改变[49]或降低睾酮水平[91]。螺内酯一般认为是一种相对较弱的抗雄激素[98][99][100]。它广泛用于治疗女性的痤疮、毛发过度生长和雄激素过多症，因女性的睾酮水平远低于男性[96][97]。由于其抗盐皮质激素活性，螺内酯具有抗盐皮质激素的副作用[101]，可导致高鉀血症[102][103]。螺内酯导致的高钾可能导致住院和/或死亡[102][103][104]，但在服用螺内酯的人群中，若本身没有风险因素，高钾风险似乎很小[97][105][106]。因此，在大多数情况下可能不需要监测血钾水平[97][105][106]。已发现螺内酯可降低高剂量口服雌二醇的生物利用度[49]。尽管广泛使用，由于螺内酯用于该目的各种缺点，近来有人质疑，在跨性别女性中是否应将此药用作为抗雄激素药物[49]。

醋酸环丙孕酮是一种抗雄激素和孕激素，可用于治疗多种雄激素依赖性疾病，也可用作避孕药中的孕激素[107][108]。它主要作为抗促性腺激素起作用，其次是其强效孕激素活性，并强烈抑制性腺生产雄激素[107][59]。已发现5至10 mg/天剂量的醋酸环丙孕酮可将男性的睾酮水平降低约50至70%[109][110][111][112]，而100 mg/天的剂量可降低约75%[113][114]。25 mg/天的醋酸环丙孕酮和适量雌二醇的组合可将跨性别女性的睾酮水平抑制约95%[115]。与雌激素联合使用10、25和50 mg/天醋酸环丙孕酮均显示出相同程度的睾酮抑制[116]。除了抗促性腺激素的作用外，醋酸环丙孕酮还是一种雄激素受体拮抗剂[107][70]。然而，这种作用在低剂量时相对微不足道，在用于治疗前列腺癌的高剂量醋酸环丙孕酮中（100-300 mg/天）时更为重要[117][118]。醋酸环丙孕酮可导致肝酶升高和肝损伤，包括肝功能衰竭[70][119]。然而，这主要发生在服用非常高剂量醋酸环丙孕酮的前列腺癌患者身上；跨性别女性尚未报告肝毒性[70]。醋酸环丙孕酮还有其他多种副作用，如疲勞和体重增加，以及如血栓和良性脑瘤等风险[59][70][120]。在醋酸环丙孕酮治疗期间，建议定期监测肝酶和催乳素水平。

醋酸甲羟孕酮是一种与醋酸环丙孕酮有关的孕激素，有时作为后者的替代[89][90]。在美国专门用作醋酸环丙孕酮的替代品，因为醋酸环丙孕酮尚未批准用于医疗用途且无法获得[89][90]。醋酸甲羟孕酮抑制跨性别女性的睾酮水平，效果与醋酸环丙孕酮类似[90][49]。已发现口服醋酸甲羟孕酮可在20至100 mg/天的剂量范围内，将男性的睾酮水平抑制约30至75%[121][122][123][124][125]。然而，与醋酸环丙孕酮相比，醋酸甲羟孕酮不同时是雄激素受体拮抗剂[50][126]。醋酸甲羟孕酮的副作用和风险与醋酸环丙孕酮相似，但与肝脏问题无关[127][101]。

许多其他孕激素和抗促性腺激素也用于抑制男性的睾酮水平，并且可能对跨性别女性也有用[128][129][130][131][132][133][134]。单独使用孕激素通常能够将男性的睾酮水平抑制最多约70%至80%，在以足够高的剂量使用时能达到略高于女性/去势去势水平[135][136][137]。足量孕激素与极小剂量雌激素（例如，每天口服0.5-1.5 mg雌二醇）的组合在抗促性腺激素作用方面具有协同作用，并且能够完全抑制性腺睾酮的产生，从而降低睾酮水平到女性/去势范围[138][139]。

非甾体抗雄激素

参见：比卡鲁胺医疗用途 § 跨性别激素治疗、尼鲁米特 § 跨性别激素治疗和氟他胺 § 跨性别激素治疗

非甾体抗雄激素是非甾体类抗雄激素，因此在化学结构方面与甾体激素无关[85][140]。这些药物主要用于治疗前列腺癌[140]，但也用于治疗痤疮、面部/体毛过度生长和女性高雄激素水平等其他目的[17][141][142][143]。与甾体抗雄激素不同，非甾体抗雄激素对雄激素受体具有高度选择性，可作为纯雄激素受体拮抗剂[140][144]。然而，与螺内酯类似，它们不会降低雄激素水平，而是仅通过阻止雄激素激活雄激素受体来发挥作用[140][144]。非甾体抗雄激素是比甾体抗雄激素更有效的雄激素受体拮抗剂[85][145]，因此，与GnRH调节剂一起，在前列腺癌的治疗中已在很大程度上取代了甾体抗雄激素[140][146]。

已用于跨性别女性的非甾体抗雄激素包括第一代药物氟他胺（优力霉）、尼鲁米特（Anandron，Nilandron）和比卡鲁胺（可苏多）[17][22][5][3][147]:477。存在更新且更有效的第二代非甾体抗雄激素药物，如恩杂鲁胺（安可坦）、阿帕鲁胺（安列康）和达洛鲁胺（Nubeqa），但由于没有仿制药且尚未用于跨性别女性，因此价格非常昂贵[148][149]。氟他胺和尼鲁米特具有相对较高的毒性，包括相当大的肝损伤和肺病风险[150][141]。由于其风险，现在已经限制且不鼓励在顺性别和跨性别女性中使用氟他胺[17][141][5]。临床上氟他胺和尼鲁米特已在很大程度上被比卡鲁胺取代[151][152]，到2000年代中期，比卡鲁胺占美国非甾体抗雄激素处方的近90%[153][144]。相对于氟他胺和尼鲁米特，以及与醋酸环丙孕酮相比，比卡鲁胺具有出色的耐受性和安全性[154][155][156]。它对女性几乎没有副作用[142][143]。然而，尽管比卡鲁胺的耐受性和安全性大大提高，但仍有很小的肝酶升高风险，并且与非常罕见的肝损伤和肺病病例有关[17][150][157]。

对于希望保持性欲、性功能和/或生育能力的跨性别女性来说，相比于抑制睾酮水平并能极大破坏这些功能的抗雄激素，如醋酸环丙孕酮和GnRH调节剂等，比卡鲁胺等非甾体类抗雄激素可能是一个特别有利的选择[158][159][160]。然而，雌激素会抑制睾酮水平，高剂量会显着破坏性欲、功能和生育能力[161][162][163][164]。此外，长期暴露后，雌激素对性腺功能和生育能力的破坏可能是永久性的[163][164]。

GnRH调节剂

效果

跨性别女性进行女性化激素疗法的效果
效果 效果发生的预期时间[a] 效果最大化的预期时间[a][b] 激素治疗停止后的持久性
乳腺发育和乳头/乳晕增大 2–6个月 1–3年 永久
胡须/体毛变稀疏/生长（英语：hair growth）减缓 4–12个月 >3年[c] 可逆
男性模式脱发的停止/逆转 1–3个月 1–2年[d] 可逆
皮肤变软/油质（英语：oily skin）和痤疮减少 3–6个月 未知 可逆
脂肪组织以一种女性模式重新分布（英语：Gynoid fat distribution） 3–6个月 2–5年 可逆
肌肉质量/力量下降（英语：Muscle atrophy） 3–6个月 1–2年[e] 可逆
骨盆变宽和变圆（英语：Widening of the hips）[f] 不明确 不明确 永久
心境、情绪性（英语：emotionality）和行为变化 不明确 不明确 可逆
性冲动减少 1–3个月 3–6个月 可逆
自发性/夜间阴茎勃起减少 1–3个月 3–6个月 可逆
勃起功能障碍和少精液症 1–3个月 多变 可逆
精子产量/生育能力（英语：male fertility）下降 未知 >3年 可逆或永久[g]
睾丸变小 3–6个月 2–3年 未知
阴茎变小 无[h] 不存在 不存在
前列腺变小 不明确 不明确 不明确
声音变化 无[i] 不存在 不存在
脚注和来源
脚注：
  1. ^ 1.0 1.1 估计值代表了发表和未发表的临床观察结果。
  2. ^ 这时候最大维持剂量不太可能造成更进一步的变化。最大效果很大程度上取决于遗传学、身体状态（英语：body habitus）、年龄和生殖腺去除的状态。通常而言，拥有完整生殖腺的年老个体可能总体上女性化程度较低。
  3. ^ 完全去除男性胡须和体毛需要电解、激光脱毛（英语：laser hair removal），或两者都进行。暂时脱毛可以通过剃毛、脱毛器（英语：epilator）、 蜡脱毛（英语：waxing）和其他方法完成。
  4. ^ 如果停止服用雌激素，家族性脱发可能发生。
  5. ^ 显著地取决于体能锻炼量。
  6. ^ 只在还没有完成骨骺闭合（英语：epiphyseal closure）的处于青春期年龄的个体中发生。
  7. ^ 需要进一步的研究来确定持久性，但雌激素治疗对精子质量（英语：sperm quality）的某种永久性影响是可能的，应该建议和考虑在开始治疗前选择精子保存。
  8. ^ 报告存在争议，没有在跨性别女性中观察到的报告，但在通过雄激素剥夺疗法（英语：androgen deprivation therapy）治疗前列腺癌的男性中报告了虽然轻微但显著的阴茎变小。[165][166][167][168]
  9. ^ 为声音训练（英语：Voice therapy (transgender)）进行的言语治疗是有效的。
来源： 指导方针：[13][8][6] 报告/图书章节： [15] [169][170] [171][27][33][37][172] 研究：[173][174]

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  138. ^ Schröder, Fritz H.; Radlmaier, Albert. Steroidal Antiandrogens. V. Craig Jordan; Barrington J. A. Furr (编). Hormone Therapy in Breast and Prostate Cancer有限度免费查阅，超限则需付费订阅. Humana Press. 2009: 325–346. ISBN 978-1-60761-471-5. doi:10.1007/978-1-59259-152-7_15. 如前所述，CPA会导致血浆睾酮水平的不完全抑制，降低约70%并保持在去势值的三倍左右。[Rennie等人]发现CPA与极低剂量（0.1 mg/d）的DES联合使用可以非常有效地去除血浆睾酮和组织中的双氢睾酮雄激素。[...]该方案结合了两种化合物的睾酮降低作用，因此只需少量雌激素即可将血浆睾酮降低至接近去势水平。（CPA, as mentioned earlier, leads to an incomplete suppression of plasma testosterone levels, which decrease by about 70% and remain at about three times castration values. [Rennie et al.] found that the combination of CPA with an extremely low dose (0.1 mg/d) of DES led to a very effective withdrawal of androgens in terms of plasma testosterone and tissue dihydrotestosterone. [...] this regimen combines the testosterone-reducing effects of two compounds, therefore, only small amounts of estrogen are required to bring down plasma testosterone to approximately castrate levels.） 
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  158. ^ Gao Y, Maurer T, Mirmirani P. Understanding and Addressing Hair Disorders in Transgender Individuals. Am J Clin Dermatol. 2018-01, 19 (4): 517–527. PMID 29352423. S2CID 6467968. doi:10.1007/s40257-018-0343-z. 非甾体抗雄激素包括氟他胺、尼鲁米特和比卡鲁胺，它们不会降低雄激素水平，可能对想要保持性欲和生育能力的个体有利[9]。（Non-steroidal antiandrogens include flutamide, nilutamide, and bicalutamide, which do not lower androgen levels and may be favorable for individuals who want to preserve sex drive and fertility [9].） 
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  161. ^ Jones, C. A.; Reiter, L.; Greenblatt, E. Fertility preservation in transgender patients. International Journal of Transgenderism. 2016, 17 (2): 76–82. ISSN 1553-2739. S2CID 58849546. doi:10.1080/15532739.2016.1153992. 传统上，建议患者在开始异性激素治疗之前冷冻保存精子，因为随着时间的推移，高剂量雌激素治疗可能会降低精子活力（Lubbert等，1992）。然而，由于研究有限，雌激素治疗导致的生育力下降仍有争议。（Traditionally, patients have been advised to cryopreserve sperm prior to starting cross-sex hormone therapy as there is a potential for a decline in sperm motility with high-dose estrogen therapy over time (Lubbert et al., 1992). However, this decline in fertility due to estrogen therapy is controversial due to limited studies.） 
  162. ^ Payne, Anita H.; Hardy, Matthew P. The Leydig Cell in Health and Disease. Springer Science & Business Media. 2007-10-28: 422–431. ISBN 978-1-59745-453-7. 雌激素是下丘脑-垂体-睾丸轴的高效抑制剂 (212-214)。除了它们在下丘脑和垂体水平的负反馈作用外，还可能对睾丸产生直接抑制作用（215，216）。[...][用雌激素治疗的]睾丸组织学显示曲细精管紊乱、空泡化和管腔缺失，以及精子发生的区室化。（Estrogens are highly efficient inhibitors of the hypothalamic-hypophyseal-testicular axis (212–214). Aside from their negative feedback action at the level of the hypothalamus and pituitary, direct inhibitory effects on the testis are likely (215,216). [...] The histology of the testes [with estrogen treatment] showed disorganization of the seminiferous tubules, vacuolization and absence of lumen, and compartmentalization of spermatogenesis.） 
  163. ^ 163.0 163.1 Salam, Muhammad A. Principles & Practice of Urology: A Comprehensive Text. Universal-Publishers. 2003: 684–. ISBN 978-1-58112-412-5. 雌激素主要通过下丘脑-垂体水平的负反馈来减少LH分泌和睾丸雄激素合成。[...]有趣的是，如果不间断地暴露，3年后停止雌激素治疗，血清睾酮可能会保持在去势水平长达3年。这种长期抑制被认为是雌激素对睾丸间质细胞的直接影响所致。（Estrogens act primarily through negative feedback at the hypothalamic-pituitary level to reduce LH secretion and testicular androgen synthesis. [...] Interestingly, if the treatment with estrogens is discontinued after 3 yr. of uninterrupted exposure, serum testosterone may remain at castration levels for up to another 3 yr. This prolonged suppression is thought to result from a direct effect of estrogens on the Leydig cells.） 
  164. ^ 164.0 164.1 Cox RL, Crawford ED. Estrogens in the treatment of prostate cancer. J. Urol. 1995-12, 154 (6): 1991–8. PMID 7500443. doi:10.1016/S0022-5347(01)66670-9. 
  165. ^ Elliott S, Latini DM, Walker LM, Wassersug R, Robinson JW. Androgen deprivation therapy for prostate cancer: recommendations to improve patient and partner quality of life. J Sex Med. September 2010, 7 (9): 2996–3010. PMID 20626600. doi:10.1111/j.1743-6109.2010.01902.x. 
  166. ^ Higano CS. Side effects of androgen deprivation therapy: monitoring and minimizing toxicity. Urology. February 2003, 61 (2 Suppl 1): 32–8. PMID 12667885. doi:10.1016/S0090-4295(02)02397-X. 
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  171. ^ Radix, Asa E. Medical Transition for Transgender Individuals. Lesbian, Gay, Bisexual, and Transgender Healthcare. 2016: 351–361. ISBN 978-3-319-19751-7. doi:10.1007/978-3-319-19752-4_19. 
  172. ^ Levy A, Crown A, Reid R. Endocrine intervention for transsexuals. Clin. Endocrinol. (Oxf). October 2003, 59 (4): 409–18. PMID 14510900. S2CID 24493388. doi:10.1046/j.1365-2265.2003.01821.x. 
  173. ^ de, Blok Christel; Klaver, Maartje; Nota, Nienke; Dekker, Marieke; den, Heijer Martin. Breast development in male-to-female transgender patients after one year cross-sex hormonal treatment. Endocrine Abstracts. 2016. ISSN 1479-6848. doi:10.1530/endoabs.41.GP146. 
  174. ^ de Blok CJ, Klaver M, Wiepjes CM, Nota NM, Heijboer AC, Fisher AD, Schreiner T, T'Sjoen G, den Heijer M. Breast Development in Transwomen After 1 Year of Cross-Sex Hormone Therapy: Results of a Prospective Multicenter Study. J. Clin. Endocrinol. Metab. February 2018, 103 (2): 532–538. PMID 29165635. S2CID 3716975. doi:10.1210/jc.2017-01927 可免费查阅. 

扩展阅读

外部链接

主題
雌激素酯（英语：Estrogen ester）
相關激素

Template:雌激素类和孕激素类

激动药
抗雄激素
AR受体拮抗剂
类固醇生成抑制剂（英语：Steroidogenesis inhibitor）
5α-还原酶（英语：5α-Reductase inhibitor）
其它
抗促性腺激素（英语：Antigonadotropin）
其它
黃體素
（及黄体制剂）
孕酮衍生物
逆孕酮衍生物
17α-羟孕酮衍生物
(and closely related)
19-去甲孕酮衍生物
(incl. 17α-substituted)
17α-乙炔基睾酮（英语：17α-Ethynyltestosterone）衍生物
19-去甲睾酮衍生物
17α-Spirolactosteroid（英语：17α-Spirolactosteroid）
其他
SPRM（英语：Selective progesterone receptor modulator）s
Antiprogestogen（英语：Antiprogestogen）s
取自“https://zh.wikipedia.org/w/index.php?title=女性化激素疗法&oldid=69658018”