|
| 1 | +--- |
| 2 | +title: 雌二醇在不同途径下的大致等效剂量 |
| 3 | +description: 许多人常咨询雌二醇在不同途径下的等效剂量。本页对此予以解惑。 |
| 4 | +author: Aly |
| 5 | +published: 2020-04-19 |
| 6 | +updated: 2022-11-29 |
| 7 | +translated: 2022-11-30 |
| 8 | +translators: |
| 9 | + - Bersella AI |
| 10 | +tags: |
| 11 | + - 雌激素 |
| 12 | + - 用药途径与剂量 |
| 13 | +trackHash: a1ecdfa409b2f259a36571f1867efd3d05925d6d |
| 14 | +--- |
| 15 | + |
| 16 | +## 译者按 {#notice} |
| 17 | + |
| 18 | +1. **<u>⚠免责声明：本文不构成任何医疗、处方建议。如有医疗需要，应于专业医师指导下进行。</u>** |
| 19 | +1. 因译者能力所限，部分术语之翻译或有纰漏，烦请指正。 |
| 20 | + |
| 21 | +-------- |
| 22 | + |
| 23 | +## 前言 {#preface} |
| 24 | + |
| 25 | +许多女性倾向跨性别者常就雌二醇在不同给药途径下的等效剂量进行咨询。本页将相关信息综合叙述，以便消解此类疑惑。 |
| 26 | + |
| 27 | +## 等效雌二醇剂量的表格 {#table-of-comparable-estradiol-dosages} |
| 28 | + |
| 29 | +下表展示了雌二醇在不同途径下的*等效剂量估计值*： |
| 30 | + |
| 31 | +<section class="box"> |
| 32 | + |
| 33 | +| 途径 | 低剂量 | 中等剂量 | 高剂量 | 超高剂量 | |
| 34 | +| --- | --- | --- | --- | --- | |
| 35 | +| [口服][wiki-743472c6]<sup>(1)</sup> | 2 mg/天 | 4 mg/天 | 8 mg/天 | 12 mg/天 | |
| 36 | +| [舌下][wiki-cfae5e37]或[面颊含服][wiki-5da4ee3a]<sup>b</sup> | 0.5–1 mg/天 | 1–2 mg/天 | 2–4 mg/天 | 3–6 mg/天 | |
| 37 | +| [透皮贴片][wiki-28597a32]<sup>c,d</sup> | 50–100 μg/天 | 100–200 μg/天 | 200–400 μg/天 | 300–600 μg/天 | |
| 38 | +| [透皮凝胶][wiki-84bc38cb]<sup>c</sup> | 1.5 mg/天 | 3 mg/天 | 6 mg/天 | 9 mg/天 | |
| 39 | +| [肌肉][wiki-e49191bf]或[皮下注射][wiki-6bca878c]<sup>e</sup> | 1 mg/周 | 2 mg/周 | 4 mg/周 | 6 mg/周 | |
| 40 | +| [皮下植入微球][wiki-1b0a2bc4] | 25 mg/六个月 | 50 mg/六个月 | 100 mg/六个月 | 150 mg/六个月 | |
| 41 | +| 雌二醇的大致平均水平 | 50 pg/mL<br>(184 pmol/L) | 100 pg/mL<br>(367 pmol/L) | 200 pg/mL<br>(734 pmol/L) | 300 pg/mL<br>(1101 pmol/L) | |
| 42 | +| 相近的[月经周期][wiki-df8b5b56] | [卵泡期][wiki-c8588b48] | 全周期 | [黄体期][wiki-ebaee44c] | [排卵期][wiki-d8cebda1] | |
| 43 | + |
| 44 | +(1) 按口服*雌二醇*计。2 mg 的[戊酸雌二醇][wiki-55cc0770]相当于 1.5 mg 的雌二醇<sup>([维基百科][wiki-08ebd67a])</sup>。\ |
| 45 | +(2) 据研究发现，舌下含服雌二醇的[生物利用度][wiki-f9e263a2]相当于口服的约 2-5 倍<sup>([维基百科][wiki-08ebd67a]; [Sam, 2021][s21-set])</sup>。\ |
| 46 | +(3) 透皮雌二醇可用于外生殖器，剂量远低于常规皮肤部位<sup>([Aly, 2019][a19-gea])</sup>。\ |
| 47 | +(4) 不同品牌的贴片所引起的雌二醇水平或各异<sup>([Rohr, Nauert, & Stehle, 1999][rns99]; [Langley et al., 2008][l08]; [Farahmand & Maibach, 2009][fm09]; [Langley et al., 2015][l15])</sup>。\ |
| 48 | +(5) 此为每周总注射剂量，适用于戊酸雌二醇、[环戊丙酸雌二醇][wiki-71ff8176]、[庚酸雌二醇][wiki-31e73858]与[苯甲酸雌二醇][wiki-3183b9f0]等[雌二醇酯][wiki-8b92d2c5]。上述成分的分子质量差别甚小<sup>([表格][wiki-tpl-bcfed1bc])</sup>，可忽略不计。各成分所适用的注射间隔不同，因此应通过调整注射间隔，使剂量与上表所示的周均剂量相当<sup>([Aly, 2021][a21-iema-if])</sup>。 |
| 49 | + |
| 50 | +</section> |
| 51 | + |
| 52 | +### 补充说明 {#notes} |
| 53 | + |
| 54 | +1. 上述剂量并不绝对，而只应视为粗略的参考值；其由多项不同研究的通用*模型* 得出，而这些研究的发现往往在个体间差异显著。而且，其假设雌二醇水平会按剂量呈线性或成比例的变化，但这并不一定属实。例如，有一项研究就发现口服雌二醇在高剂量下的生物利用度较低<sup>([Kuhnz, Gansau, & Mahler, 1993][kgm93])</sup>。 |
| 55 | +1. 上述为大致*等效或相当* 的剂量，不一定与临床上通常或推荐的剂量一致。例如，雌二醇注射剂的剂量通常会高于其它途径、形式的雌二醇<sup>([Aly, 2021][a21-iema-if])</sup>。 |
| 56 | +1. 上述剂量基于总雌二醇暴露量（而非雌激素疗效）而定。已知性激素水平随时间的差异会改变性激素制剂的效力<sup>([Aly, 2021][a21-iema-ee])</sup>。然而，由于相关数据与分析缺乏，此影响因子并未在上表中予以考虑。\ |
| 57 | + 无论如何，此影响因子应与某些会引起雌二醇水平大幅波动的给药途径有关——例如，舌下含服与短效注射剂。 |
| 58 | +1. 雌二醇透皮喷雾剂已经面市，其品牌为 Lenzetto。有一项针对已绝经妇女的研究发现，在一周试用不同剂量 Lenzetto 的过程中，雌二醇水平分别为 6 pg/mL（治疗前的稳态）、13 pg/mL（一次/天，即 1.53 mg/天）、19 pg/mL（两次/天，即 3.06 mg/天）以及 26 pg/mL（三次/天，即 4.59 mg/天）<sup>([Morton et al., 2009][m09]; [图表][wikimedia-e25492c0])</sup>。\ |
| 59 | + 据此，雌二醇透皮喷雾剂显然仅可达到较低的雌二醇水平，故应不适用于女性倾向跨性别者。目前尚无更高剂量的数据（即每日四次以上），因此其未被上表纳入。 |
| 60 | + |
| 61 | +## 补充讨论 {#discussion} |
| 62 | + |
| 63 | +作为参考，顺性别[绝经前][wiki-cb3c3c03]妇女在正常[月经周期][wiki-df8b5b56]内的综合平均雌二醇水平约为 100 pg/mL，而在[黄体期][wiki-ebaee44c]（周期后半段）内则有约 150 pg/mL<sup>([图表][wikimedia-a3bd615d]; [图表][wikimedia-5320e33c]; [Aly, 2018][a18-intro])</sup>。一个周期（即一个月）内所分泌的雌二醇总量平均约为 6 mg<sup>([Rosenfield et al., 2008][r08]; [Aly, 2018][a18-intro])</sup>。\ |
| 64 | +由于雌二醇酯的结构原因（*含戊酸等基团——译者注*），其雌二醇含量较少；在用于注射时，其需要稍高的剂量来确保与（*顺性别妇女*）内源性分泌的总量相当<sup>([表格][wiki-tpl-bcfed1bc])</sup>。 |
| 65 | + |
| 66 | +需要指出，各形式与途径的雌二醇所引起的雌二醇水平，在个体间差异显著。例如，某些人使用口服途径时仅有较低的雌二醇水平，另一些人使用透皮途径也仅有较低雌二醇水平；相反，某些人经透皮或注射途径会有较高的血清水平。从 [Aly (2021)][a21-iema-vbi] 的文章可见有关个体间差异（甚至是使用注射剂时）的数据。\ |
| 67 | +由于个体间的雌二醇水平有别，不同人群所适用的剂量往往并不一致。应通过验血来按需调整剂量。\ |
| 68 | +还需指出，某些途径所引起的雌二醇水平随时间会有大幅变动；例如舌下或面颊含服<sup>([图表][wiki-tpl-c63bb3fc]; [图表][wikimedia-85f78f54]; [Sam, 2021][s21-set])</sup>，以及肌肉或皮下注射<sup>([图表][wiki-tpl-4caa745e]; [Aly, 2021][a21-iema])</sup>。在如此大的波动下，在用药后不同时间点测得的雌二醇水平会有极大差别（如达峰时和达到谷底时）。 |
| 69 | + |
| 70 | +对于尚未进行、或未打算进行[性腺切除术][wiki-c71cb1a7]的女性倾向跨性别者，可使用较高至非常高的雌二醇剂量来达到对睾酮水平的高度抑制效果。上表的“高剂量”平均可将睾酮水平抑制约 90%，至 50 ng/dL 左右<sup>([维基百科][wiki-e2089aa4]; [Aly, 2018][aw18-intro-gs])</sup>。因此，其通常用于雌二醇单药疗法（即仅用雌二醇、无抗雄激素制剂的疗法）。\ |
| 71 | +接受性腺切除术之后，便无需抑制睾酮了，此时可仅使用较低剂量（如“中等剂量”）的雌二醇。\ |
| 72 | +当与抗雄激素制剂（包括[醋酸环丙孕酮][wiki-5cafcc7a]、[比卡鲁胺][wiki-bb37b2c5]、或[促性腺激素释放激素激动剂][wiki-3fb787cd]/[拮抗剂][wiki-c3bddcb0]）合用时，高剂量雌二醇并非必需。 |
| 73 | + |
| 74 | +## 资料来源 {#sources} |
| 75 | + |
| 76 | +- Kuhl, H. (2005). Pharmacology of estrogens and progestogens: influence of different routes of administration. *Climacteric*, *8*(Suppl 1), 3–63. \[DOI:[10.1080/13697130500148875][k05]] \[[PDF][k05-pdf]] |
| 77 | +- Bruni, V., & Pampaloni, F. (2019). Hormone Replacement Therapy in Premature Ovarian Insufficiency. In Berga, S. L., Genazzani, A. R., Naftolin, F., & Petraglia, F. (Eds.). *Menstrual Cycle Related Disorders* (pp. 111–142). Cham: Springer. \[DOI:[10.1007/978-3-030-14358-9\_10][bp19]] |
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| 79 | +- Pharmacokinetics of estradiol. (2020, August 29). In *Wikipedia*. \[[URL][archive-e7edb9ae]] |
| 80 | +- Template:Estrogen dosages for menopausal hormone therapy. (2020, October 2). In *Wikipedia*. \[[URL][wiki-tpl-1dfbcc52]] |
| 81 | +- Taboada, M., Santen, R., Lima, J., Hossain, J., Singh, R., Klein, K. O., & Mauras, N. (2011). Pharmacokinetics and pharmacodynamics of oral and transdermal 17β estradiol in girls with Turner syndrome. *The Journal of Clinical Endocrinology & Metabolism*, *96*(11), 3502–3510. \[DOI:[10.1210/jc.2011-1449][t11]] |
| 82 | +- Armston, A., & Wood, P. (2002). Hormone replacement therapy (oestradiol-only preparations): can the laboratory recommend a concentration of plasma oestradiol to protect against osteoporosis? *Annals of Clinical Biochemistry*, *39*(3), 184–193. \[DOI:[10.1258/0004563021902107][aw02]] |
| 83 | +- Simon, J. A., & Snabes, M. C. (2007). Menopausal hormone therapy for vasomotor symptoms: balancing the risks and benefits with ultra-low doses of estrogen. *Expert Opinion on Investigational Drugs*, *16*(12), 2005–2020. \[DOI:[10.1517/13543784.16.12.2005][ss07]] \[[表格][imgur-2d4c7930]] |
| 84 | +- Farahmand, S., & Maibach, H. I. (2009). Transdermal drug pharmacokinetics in man: Interindividual variability and partial prediction. *International Journal of Pharmaceutics*, *367*(1–2), 1–15. \[DOI:[10.1016/j.ijpharm.2008.11.020][fm09]] |
| 85 | +- Baker, V. L. (1994). Alternatives to Oral Estrogen Replacement: Transdermal Patches, Percutaneous Gels, Vaginal Creams and Rings, Implants, and Other Methods of Delivery. *Obstetrics and Gynecology Clinics of North America*, *21*(2) \[*Primary Care of the Mature Woman*], 271–297. \[DOI:[10.1016/S0889-8545(21)00629-X][b94]] \[[PDF][b94-pdf]] |
| 86 | +- Aly (2021). An Informal Meta-Analysis of Estradiol Curves with Injectable Estradiol Preparations. *Transfeminine Science*, injectable-e2-meta-analysis. \[[URL][a21-iema]] |
| 87 | + |
| 88 | +<!-- 维基百科内容 --> |
| 89 | +[wiki-08ebd67a]: https://en.wikipedia.org/wiki/Estradiol_valerate#Oral_administration |
| 90 | +[wiki-1b0a2bc4]: https://en.wikipedia.org/wiki/Pharmacokinetics_of_estradiol#Subcutaneous_implantation |
| 91 | +[wiki-1c6b5107]: https://en.wikipedia.org/wiki/Interindividual_variability |
| 92 | +[wiki-28597a32]: https://en.wikipedia.org/wiki/Pharmacokinetics_of_estradiol#Transdermal_patches |
| 93 | +[wiki-3183b9f0]: https://en.wikipedia.org/wiki/Estradiol_benzoate |
| 94 | +[wiki-31e73858]: https://en.wikipedia.org/wiki/Estradiol_enantate |
| 95 | +[wiki-3fb787cd]: https://en.wikipedia.org/wiki/Gonadotropin-releasing_hormone_agonist |
| 96 | +[wiki-55cc0770]: https://en.wikipedia.org/wiki/Estradiol_valerate |
| 97 | +[wiki-5cafcc7a]: https://en.wikipedia.org/wiki/Cyproterone_acetate |
| 98 | +[wiki-5da4ee3a]: https://en.wikipedia.org/wiki/Pharmacokinetics_of_estradiol#Buccal_administration |
| 99 | +[wiki-6bca878c]: https://en.wikipedia.org/wiki/Pharmacokinetics_of_estradiol#Subcutaneous_injection |
| 100 | +[wiki-71ff8176]: https://en.wikipedia.org/wiki/Estradiol_cypionate |
| 101 | +[wiki-743472c6]: https://en.wikipedia.org/wiki/Pharmacokinetics_of_estradiol#Oral_administration |
| 102 | +[wiki-84bc38cb]: https://en.wikipedia.org/wiki/Pharmacokinetics_of_estradiol#Transdermal_gel |
| 103 | +[wiki-8b92d2c5]: https://en.wikipedia.org/wiki/Estrogen_ester |
| 104 | +[wiki-99d5ef20]: https://en.wikipedia.org/wiki/Molecular_weight |
| 105 | +[wiki-bb37b2c5]: https://en.wikipedia.org/wiki/Bicalutamide |
| 106 | +[wiki-c3bddcb0]: https://en.wikipedia.org/wiki/Gonadotropin-releasing_hormone_antagonist |
| 107 | +[wiki-c71cb1a7]: https://en.wikipedia.org/wiki/Gonadectomy |
| 108 | +[wiki-c8588b48]: https://en.wikipedia.org/wiki/Follicular_phase |
| 109 | +[wiki-cb3c3c03]: https://en.wikipedia.org/wiki/Menopause#Premenopause |
| 110 | +[wiki-cfae5e37]: https://en.wikipedia.org/wiki/Pharmacokinetics_of_estradiol#Sublingual_administration |
| 111 | +[wiki-d8cebda1]: https://en.wikipedia.org/wiki/Ovulation |
| 112 | +[wiki-df8b5b56]: https://en.wikipedia.org/wiki/Menstrual_cycle |
| 113 | +[wiki-e2089aa4]: https://en.wikipedia.org/wiki/Pharmacodynamics_of_estradiol#Antigonadotropic_effects |
| 114 | +[wiki-e49191bf]: https://en.wikipedia.org/wiki/Pharmacokinetics_of_estradiol#Intramuscular_injection |
| 115 | +[wiki-ebaee44c]: https://en.wikipedia.org/wiki/Luteal_phase |
| 116 | +[wiki-f9e263a2]: https://en.wikipedia.org/wiki/Bioavailability |
| 117 | +[wiki-tpl-1dfbcc52]: https://en.wikipedia.org/w/index.php?title=Template:Estrogen_dosages_for_menopausal_hormone_therapy&oldid=981467870 |
| 118 | +[wiki-tpl-4caa745e]: https://en.wikipedia.org/wiki/Template:Hormone_levels_with_estradiol_esters_by_intramuscular_injection |
| 119 | +[wiki-tpl-bcfed1bc]: https://en.wikipedia.org/wiki/Template:Structural_properties_of_selected_estradiol_esters |
| 120 | +[wiki-tpl-c63bb3fc]: https://en.wikipedia.org/wiki/Template:Hormone_levels_with_sublingual_estradiol |
| 121 | +[wikimedia-5320e33c]: https://commons.wikimedia.org/wiki/File:Estradiol_levels_with_LC-MS-MS_during_the_normal_menstrual_cycle_in_women.png |
| 122 | +[wikimedia-85f78f54]: https://commons.wikimedia.org/wiki/File:Estradiol_levels_during_therapy_with_0.25_mg_buccal_estradiol_in_postmenopausal_women.png |
| 123 | +[wikimedia-a3bd615d]: https://commons.wikimedia.org/wiki/File:Estradiol_levels_across_the_normal_menstrual_cycle_in_women.png |
| 124 | +[wikimedia-e25492c0]: https://commons.wikimedia.org/wiki/File:Estradiol_levels_with_estradiol_transdermal_spray_\(brand_name_Lenzetto\)_in_postmenopausal_women.png |
| 125 | + |
| 126 | +<!-- 站内资源 --> |
| 127 | +[s21-set]: https://transfemscience.org/articles/sublingual-e2-transfem/ |
| 128 | +[aw18-intro-gs]: https://transfemscience.org/articles/transfem-intro/#gonadal-suppression |
| 129 | +[a21-iema-vbi]: https://transfemscience.org/articles/injectable-e2-meta-analysis/#variability-between-individuals |
| 130 | +[tfsci-8092b611]: https://transfemscience.org/about/#aly |
| 131 | +[a19-gea]: https://transfemscience.org/articles/genital-e2-application/ |
| 132 | +[a21-iema]: https://transfemscience.org/articles/injectable-e2-meta-analysis/ |
| 133 | +[lc92-pdf]: https://files.transfemscience.org/pdfs/Lobo%20&%20Cassidenti%20\(1992\)%20-%20Pharmacokinetics%20of%20Oral%2017%20%CE%B2-Estradiol.pdf |
| 134 | +[a21-iema-if]: https://transfemscience.org/articles/injectable-e2-meta-analysis/#insights-for-clinical-guidelines-and-dosing-recommendations |
| 135 | +[b94-pdf]: https://files.transfemscience.org/pdfs/Baker%20\(1994\)%20-%20Alternatives%20to%20Oral%20Estrogen%20Replacement.%20Transdermal%20Patches,%20Percutaneous%20Gels,%20Vaginal%20Creams%20and%20Rings,%20Implants,%20and%20Other%20Methods%20of%20Delivery.pdf |
| 136 | +[a21-iema-ee]: https://transfemscience.org/articles/injectable-e2-meta-analysis/#estradiol-exposure-and-potency |
| 137 | +[a18-intro]: https://transfemscience.org/articles/transfem-intro/#normal-hormone-levels |
| 138 | + |
| 139 | +<!-- 文献链接 --> |
| 140 | +[archive-e7edb9ae]: https://web.archive.org/web/20200829215330/https://en.wikipedia.org/wiki/Pharmacokinetics_of_estradiol |
| 141 | +[fm09]: https://doi.org/10.1016/j.ijpharm.2008.11.020 |
| 142 | +[rns99]: https://doi.org/10.1016/S0378-5122\(99\)00039-0 |
| 143 | +[b94]: https://doi.org/10.1016/S0889-8545\(21\)00629-X |
| 144 | +[m09]: https://doi.org/10.1177/0091270009339187 |
| 145 | +[bp19]: https://doi.org/10.1007/978-3-030-14358-9_10 |
| 146 | +[l08]: https://doi.org/10.1111/j.1464-410X.2008.07583.x |
| 147 | +[k05]: https://doi.org/10.1080/13697130500148875 |
| 148 | +[l15]: https://doi.org/10.1016/j.maturitas.2015.02.320 |
| 149 | +[aw02]: https://doi.org/10.1258/0004563021902107 |
| 150 | +[ss07]: https://doi.org/10.1517/13543784.16.12.2005 |
| 151 | +[t11]: https://doi.org/10.1210/jc.2011-1449 |
| 152 | +[lc92]: https://scholar.google.com/scholar?cluster=6161874457522650604 |
| 153 | +[r08]: https://scholar.google.com/scholar?cluster=9979206541205334235 |
| 154 | +[k05-pdf]: https://hormonebalance.org/images/documents/Kuhl%2005%20%20Pharm%20Estro%20Progest%20Climacteric_1311166827.pdf |
| 155 | +[imgur-2d4c7930]: https://imgur.com/a/6fgJkAQ |
| 156 | +[lc92-pubmed]: https://pubmed.ncbi.nlm.nih.gov/1548642/ |
| 157 | +[kgm93]: https://pubmed.ncbi.nlm.nih.gov/8240460/ |
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