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Aly (代词:她)来自美国加利福尼亚州,是一名跨性别女性。她对女性化激素疗法抱有浓厚兴趣。Aly 于 2010 年代初开始了性别转变过程,此后热衷于探究跨性别医学文献的工作。她以优异成绩毕业于[加州大学][wiki-uc],取得学士学位。Aly 还完成了若干医学预科课程,并在加州大学的研究室担任一年的助教。
Aly (代词:她)来自美国加利福尼亚州,是一名跨性别女性。她对女性化激素疗法抱有浓厚兴趣。Aly 于 2010 年代初开始了性别转变过程,此后热衷于探究跨性别医学文献的工作。她以最优异成绩毕业于[加州大学][wiki-uc],取得学士学位。Aly 还完成了若干医学预科课程,并在加州大学的研究室担任一年的助教。
Aly 已作为志愿者在英文维基百科社区活跃多年。她曾在数年间连续位列维基百科医学栏目最佳编辑者前十名之内。\
Aly 在性激素药理学方面耕耘多年,贡献颇多;从她的[编辑历史][aly-stat]<sup>([备用链接][aly-stat-alt])</sup>、[最佳条目][aly-top]、[新建文章][aly-create]与[已上传图片][aly-image]<sup>([备用链接][aly-image-alt])</sup>等记录中可见一斑。Aly 有时也在维基百科上简短引用本站内容,其中绝大部分来自她本人的文章。
Aly 已作为志愿者在维基百科社区活跃多年。她曾在数年间连续位列维基百科医学栏目最佳编辑者前十名之内。\
Aly 在性激素药理学方面耕耘多年,贡献颇多。Aly 有时也在维基百科上简短引用本站内容,其中绝大部分来自她本人的文章。
除较低孕激素效力以外,口服孕酮还会被过多地代谢成为[别孕烷醇酮][wiki161]、[孕烷醇酮][wiki162]等[神经甾体][wiki153];这些代谢物作为强效的 [γ-氨基丁酸 A 型(GABA-A)受体异构激动剂][wiki163],会产生类似于[酒精][wiki164]的不良副作用——包括镇静,认知、记忆与运动障碍,以及情绪变化等<sup>([维基][wiki160-ne]; [维基][wiki160-fpean])</sup>。
**AR 拮抗剂**可作用于阻断睾酮、双氢睾酮(DHT)等雄激素的[生物靶点][wiki332],直接阻断其作用。它们与 AR 结合而不激活,从而阻止雄激素与受体结合。由于其作为雄激素的竞争性阻断剂的机制,其抗雄效力与剂量及睾酮水平高度相关。其并不通过降低睾酮水平来发挥作用——尽管其中某些会有额外的抗雄激素活性、从而使睾酮水平降低。因此,与可降低睾酮水平的抗雄制剂不同,当使用它们时,血检的参考价值可能不大。\
AR 拮抗剂种类包括[甾体类抗雄制剂][wiki169] (SAA),如[螺内酯][wiki170] (Aldactone)和[醋酸环丙孕酮][wiki171][CPA; 品牌 Androcur (俗称“色谱龙”——译者注)];以及[非甾体类抗雄制剂][wiki172] (NSAA),如[比卡鲁胺][wiki173][品牌 Casodex(“康士得”)]。
对于许多女性倾向跨性别者,雌二醇合并螺内酯的处方并不足以抑制其睾酮,因为螺内酯对睾酮水平的影响有限且高度不稳定,其 AR 拮抗效力亦较弱。这样会导致她们的去男性化、女性化、乳房发育等效果不理想。这些效果如使用其它抗雄手段——诸如比卡鲁胺、CPA、GnRH 调节剂与高剂量雌二醇单药疗法等——则应该会更佳;这些手段要么可更高效地阻断雄激素,要么可将睾酮水平降低并稳定于女性范围。\
比卡鲁胺对 AR 的选择性很强,其在女性当中未发生任何[脱靶激素活性][wiki152],也几乎不产生任何副作用<sup>([维基][wiki173-se]; [Erem, 2013][E13]; [Moretti et al., 2018][M18])</sup>;在一项严谨的有关比卡鲁胺用于顺性别妇女治疗多毛症的临床试验中,其仅引起一项明显副作用,即[总胆固醇][wiki345]、[LDL(“不良”)胆固醇][wiki344]水平显著升高<sup>([Moretti et al., 2018][M18])</sup>。因此,比卡鲁胺的耐受性应该是非常好的。其副作用相对较少,与螺内酯、CPA 等抗雄制剂形成鲜明对比——此二者会产生抗盐皮质激素活性、强孕激素活性等脱靶效应,以及一系列副作用与风险。
比卡鲁胺对雄激素受体的选择性很强,其在女性当中未发生任何[脱靶激素活性][wiki152],也几乎不产生任何副作用<sup>([维基][wiki173-se]; [Erem, 2013][E13]; [Moretti et al., 2018][M18])</sup>;在一项严谨的有关比卡鲁胺用于顺性别妇女治疗多毛症的临床试验中,其仅引起一项明显副作用,即[总胆固醇][wiki345]、[LDL(“不良”)胆固醇][wiki344]水平显著升高<sup>([Moretti et al., 2018][M18])</sup>。因此,比卡鲁胺的耐受性应该是非常好的。其副作用相对较少,与螺内酯、CPA 等抗雄制剂形成鲜明对比——此二者会产生抗盐皮质激素活性、强孕激素活性等脱靶效应,以及一系列副作用与风险。
作为选择性 AR 拮抗剂,比卡鲁胺本身并不会使睾酮分泌量或水平降低,反而会使其升高;因为其会中断 AR 对促性腺激素分泌的负反馈调节,而(多出来的促性腺激素)会对性腺的睾酮分泌进行补偿性正调节<sup>([维基][wiki234-iohl])</sup>。而比卡鲁胺仍可阻断多出来的这部分睾酮的效力;事实上,其基本不会让睾酮增至超过其阻断能力的水平<sup>([维基][wiki173-pd]; [Aly, 2019][AW19-BD])</sup>。此外,如若将比卡鲁胺与一种适当剂量的抗促性腺激素制剂(如雌二醇)结合使用,则会让睾酮水平增幅减缓、以至无增幅<sup>([维基][wiki234-iohl]; [维基][wiki245-tht])</sup>。\
而前列腺癌的发生率会因女性倾向跨性别者的激素治疗引起雄激素缺少而显著下降,不过该风险未完全消除,仍有发生的可能<sup>([de Nie et al., 2020][NIE20])</sup>。[前列腺][wiki297]不会随[阴道再造术][wiki105]而摘除,因此即使在术后也需对前列腺癌进行监测。\
[睾丸癌][wiki298]已知不对激素敏感;在接受激素治疗的女性倾向跨性别者当中,其发生率并不会提高<sup>([Bensley et al., 2021][BENS21]; [de Nie et al., 2021][NIE21]; [Jacoby et al., 2021][J21])</sup>。
而前列腺癌的发生率会因女性倾向跨性别者的激素治疗引起雄激素缺少而显著下降,不过该风险未完全消除,仍有发生的可能<sup>([de Nie et al., 2020][DN20])</sup>。[前列腺][wiki297]不会随[阴道再造术][wiki105]而摘除,因此即使在术后也需对前列腺癌进行监测。\
[睾丸癌][wiki298]已知不对激素敏感;在接受激素治疗的女性倾向跨性别者当中,其发生率并不会提高<sup>([Bensley et al., 2021][BENS21]; [de Nie et al., 2021][DN21]; [Jacoby et al., 2021][J21])</sup>。
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