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雌激素及孕激素类药

雌激素类药物可以分为三种:

  • 天然雌激素:体内分泌的主要包括雌二醇、雌酮和雌三醇。目前临床常用的多为它们的衍生物,如注射用长效雌激素苯甲酸雌二醇、戊酸雌二醇、环戊丙酸雌二醇以及口服有效的炔雌醇、炔雌醚等。这些药物常与孕激素组合用于避孕,并治疗绝经期综合征、老年性阴道炎等。它们的体内代谢过程类似于天然雌激素,且如妊马雌酮是作为补充治疗药的一种天然结合型雌激素。

  • 半合成雌激素:包括口服强效雌激素炔雌醇,其作用约为己烯雌酚的20倍;雌三醇的长效衍生物尼尔雌醇等。

  • 合成雌激素(非甾体雌激素):如临床上常用的非甾体合成雌激素药物己烯雌酚,以及氯烯雌醚等品种。

孕激素类药物是指具有与天然孕激素相似生理活性的药物总称。这类药物主要通过改变子宫组织以利于受精卵的转运、着床和发育,并能抑制排卵、影响子宫功能及乳腺发育。天然孕激素黄体酮由黄体周期性分泌,工业上可通过合成薯芋皂甙元及甾醇获得。人工改造的孕激素化合物分为两大类:一类是黄体酮衍生物17α-羟孕酮类药物,如甲孕酮(安宫黄体酮)、甲地孕酮、氯地孕酮以及长效注射剂己酸孕酮等;另一类是以19-乙炔睾酮为基本结构的19去甲睾酮类,包括炔诺酮、异炔诺酮和高诺酮等。

中文名称 英文名称 CAS号 化学式 结构式图片
—— [(2S,3S,5R,15R,16S)-15-Acetyl-9-chloro-2,16-dimethyl-6-oxo-15-pentacyclo[9.7.0.02,8.03,5.012,16]octadeca-7,9-dienyl] acetate 57-38-5 C24H29ClO4
[(2S,3S,5R,15R,16S)-15-Acetyl-9-chloro-2,16-dimethyl-6-oxo-15-pentacyclo[9.7.0.02,8.03,5.012,16]octadeca-7,9-dienyl] acetate
—— (8R,9S,13S,14S,17R)-17-acetyl-17-hydroxy-13-methyl-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one 2137-18-0 C20H28O3
(8R,9S,13S,14S,17R)-17-acetyl-17-hydroxy-13-methyl-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one
—— β-Oestradiol-3-benzoat 50-50-0 C25H28O3
β-Oestradiol-3-benzoat
—— 3-Benzoyloxy-oestra-1,3,5(10)-trien-17β-ol 50-50-0 C25H28O3
3-Benzoyloxy-oestra-1,3,5(10)-trien-17β-ol
—— 3-methoxy-(17β<i>H</i>)-19-nor-pregna-1,3,5(10)-trien-20-yn-17-ol 72-33-3 C21H26O2
3-methoxy-(17β<i>H</i>)-19-nor-pregna-1,3,5(10)-trien-20-yn-17-ol
—— (17α)-3-methoxy-19-norpregna-1,3,5(10)-triene-20-yn-17-ol 72-33-3 C21H26O2
(17α)-3-methoxy-19-norpregna-1,3,5(10)-triene-20-yn-17-ol
—— mestranol 72-33-3 C21H26O2
mestranol
—— 3-Hydroxy-17β-valeryloxy-oestratrien-(1,3,5(10)) 979-32-8 C23H32O3
3-Hydroxy-17β-valeryloxy-oestratrien-(1,3,5(10))
—— Ethisterone 434-03-7 C21H28O2
Ethisterone
—— estra-1,3,5(10)-triene-3,16β,17α-triol 50-27-1 C18H24O3
estra-1,3,5(10)-triene-3,16β,17α-triol
—— estra-1,3,5(10)-triene-3,16α,17β-triol 50-27-1 C18H24O3
estra-1,3,5(10)-triene-3,16α,17β-triol
—— estra-1,3,5(10)-triene-3,16β,17β-triol 50-27-1 C18H24O3
estra-1,3,5(10)-triene-3,16β,17β-triol
—— estriol 50-27-1 C18H24O3
estriol
—— estra-1,3,5(10)-triene-3,16α,17α-triol 50-27-1 C18H24O3
estra-1,3,5(10)-triene-3,16α,17α-triol
—— (2S,3S,5R,15R,16S)-15-acetyl-9-chloro-15-hydroxy-2,16-dimethylpentacyclo[9.7.0.02,8.03,5.012,16]octadeca-7,9-dien-6-one 2098-66-0 C22H27ClO3
(2S,3S,5R,15R,16S)-15-acetyl-9-chloro-15-hydroxy-2,16-dimethylpentacyclo[9.7.0.02,8.03,5.012,16]octadeca-7,9-dien-6-one
—— estradiol 50-28-2 C18H24O2
estradiol
—— estra-1,3,5(10)-triene-3,17β-diol 50-28-2 C18H24O2
estra-1,3,5(10)-triene-3,17β-diol
—— β-estradiol 50-28-2 C18H24O2
β-estradiol
—— estra-1,3,5(10)-triene-3,17α-diol 50-28-2 C18H24O2
estra-1,3,5(10)-triene-3,17α-diol
—— 19-nor-pregna-1,3,5(10)-trien-20-yne-3,17-diol 57-63-6 C20H24O2
19-nor-pregna-1,3,5(10)-trien-20-yne-3,17-diol
—— 17α-ethynyl-estradiol 57-63-6 C20H24O2
17α-ethynyl-estradiol
—— (+/-)-lumiestrone 53-16-7 C18H22O2
(+/-)-lumiestrone
—— 3-hydroxy-estra-1,3,5(10)-trien-17-one 53-16-7 C18H22O2
3-hydroxy-estra-1,3,5(10)-trien-17-one
—— DL-8-Isooestron 53-16-7 C18H22O2
DL-8-Isooestron
—— progesterone 57-83-0 C21H30O2
progesterone
—— 14β.17β<i>H</i>-pregnene-(4)-dione-(3.20) 57-83-0 C21H30O2
14β.17β<i>H</i>-pregnene-(4)-dione-(3.20)
—— pregn-4-ene-3,20-dione 57-83-0 C21H30O2
pregn-4-ene-3,20-dione
—— 21-Methyl-Δ9-10-norprogesteron 34184-77-5 C22H30O2
21-Methyl-Δ9-10-norprogesteron
—— 17alpha-Hydroxy-19-norprogesterone caproate 1253-28-7 C26H38O4
17alpha-Hydroxy-19-norprogesterone caproate
—— Estradiol-benzoat 50-50-0 C25H28O3
Estradiol-benzoat
—— progesterone 57-83-0 C21H30O2
progesterone
—— diethylstilbestrol 56-53-1 C18H20O2
diethylstilbestrol
—— Aragest 71-58-9 C24H34O4
Aragest
—— 13-Methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,16,17-triol 50-27-1 C18H24O3
13-Methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,16,17-triol
—— 3-(Cyclopentyloxy)estra-1(10),2,4-triene-16,17-diol 1169-79-5 C23H32O3
3-(Cyclopentyloxy)estra-1(10),2,4-triene-16,17-diol
—— 3-hydroxy-7,13-dimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-one 10448-96-1 C19H24O2
3-hydroxy-7,13-dimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-one
—— Devocin 72-33-3 C21H26O2
Devocin
—— Colprone 977-79-7 C23H32O2
Colprone
—— ethisterone 434-03-7 C21H28O2
ethisterone
—— Aethinyl-oestradiol 57-63-6 C20H24O2
Aethinyl-oestradiol
—— 16alpha,17-(Isopropylidenedioxy)progesterone 4968-09-6 C24H34O4
16alpha,17-(Isopropylidenedioxy)progesterone
—— Ogyline 848-21-5 C20H22O2
Ogyline