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7α-甲基-19-去甲睾酮可维持性腺功能减退男性的性行为和情绪。

7Alpha-methyl-19-nortestosterone maintains sexual behavior and mood in hypogonadal men.

作者信息

Anderson R A, Martin C W, Kung A W, Everington D, Pun T C, Tan K C, Bancroft J, Sundaram K, Moo-Young A J, Baird D T

机构信息

Medical Research Council Reproductive Biology Unit, Center for Reproductive Biology, Edinburgh, Scotland.

出版信息

J Clin Endocrinol Metab. 1999 Oct;84(10):3556-62. doi: 10.1210/jcem.84.10.6028.

Abstract

The synthetic steroid 7alpha-methyl-19-nortestosterone (MENT) is a potent androgen that is resistant to 5alpha-reductase. It thus has decreased activity at the prostate and may have advantages over testosterone-based regimens in long term treatment or as part of a male contraceptive. Administration to eugonadal men results in suppression of gonadotropins, but its ability to support androgen-dependent behavior has not been investigated. For sustained release administration, MENT acetate was used, because its diffusion characteristics were more suitable for use in implants. However, upon release the acetate is rapidly hydrolyzed, and MENT is the biologically active moiety in circulation. We studied the effects of MENT on sexual interest and activity, spontaneous erection, and mood states in comparison with testosterone enanthate (TE) in 20 Caucasian and Chinese hypogonadal men recruited in Edinburgh and Hong Kong (n = 10 in each center). Outcomes were measured using a combination of daily diaries, semistructured interviews, and questionnaires. Nocturnal penile tumescence (NPT) was also recorded in the Edinburgh group. After withdrawal of androgen replacement treatment (wash-out phase) for a minimum of 6 weeks, subjects were randomized to two groups in a cross-over design. Drug treatment regimens were of 6-week duration and consisted of two implants, each containing 115 mg MENT acetate, inserted s.c. into the upper arm and removed after 6 weeks and two injections of TE (200 mg, i.m.) 3 weeks apart. MENT treatment resulted in stable plasma MENT concentrations of 1.4 +/- 0.1 nmol/L after 3 weeks and 1.3 +/- 0.1 nmol/L after 6 weeks (mean +/- SEM; all men). Nadir testosterone concentrations were 3.6 +/- 0.6 nmol/L at the end of the wash-out phase and 9.4 +/- 0.6 nmol/L 3 weeks after each injection. There were no differences in hormone concentrations between centers. There were no adverse toxicological effects. There were only minor differences between the two treatments. Both MENT and TE treatment resulted in significant increases in sexual interest and activity, spontaneous erection (both by self-report and NPT measurement), and increases in positive moods, with decreases in negative moods in the Edinburgh group. In the Hong Kong group, both treatments increased waking erection, with a trend toward increased sexual interest and activity. Mood states appeared to be less affected during the wash-out phase than in Edinburgh men and showed no significant response to either treatment. These results demonstrate that MENT has similar effects on sexual activity and mood states as testosterone in hypogonadal men. As NPT is a physiological androgen-dependant outcome, these data provide further evidence for the androgenicity of MENT. The lack of detected effect of either androgen in Hong Kong men other than on waking erection illustrates the importance of the cultural context of symptomatology and its measurement. The appropriate dose of MENT remains to be determined, but these results support its development as a potential androgen replacement therapy.

摘要

合成类固醇7α-甲基-19-去甲睾酮(MENT)是一种强效雄激素,对5α-还原酶具有抗性。因此,它在前列腺的活性降低,在长期治疗或作为男性避孕药的一部分时,可能比基于睾酮的治疗方案具有优势。给予性腺功能正常的男性会导致促性腺激素受到抑制,但其支持雄激素依赖性行为的能力尚未得到研究。对于缓释给药,使用了MENT醋酸盐,因为其扩散特性更适合用于植入物。然而,释放后醋酸盐会迅速水解,MENT是循环中的生物活性部分。我们在爱丁堡和香港招募的20名白种人和中国性腺功能减退男性中(每个中心10名),研究了MENT与庚酸睾酮(TE)相比,对性兴趣和活动、自发勃起以及情绪状态的影响。使用每日日记、半结构化访谈和问卷相结合的方式来测量结果。爱丁堡组还记录了夜间阴茎勃起(NPT)情况。在至少停用雄激素替代治疗6周(洗脱期)后,受试者采用交叉设计随机分为两组。药物治疗方案为期6周,包括两个植入物,每个植入物含有115 mg MENT醋酸盐,皮下插入上臂,6周后取出,以及两次间隔3周的TE注射(200 mg,肌肉注射)。MENT治疗3周后血浆MENT浓度稳定在1.4±0.1 nmol/L,6周后为1.3±0.1 nmol/L(均值±标准误;所有男性)。洗脱期结束时睾酮最低浓度为3.6±0.6 nmol/L,每次注射后3周为9.4±0.6 nmol/L。各中心之间激素浓度无差异。未观察到不良毒理学效应。两种治疗之间只有微小差异。MENT和TE治疗均导致性兴趣和活动、自发勃起(通过自我报告和NPT测量)显著增加,爱丁堡组的积极情绪增加,消极情绪减少。在香港组,两种治疗均增加了清醒时的勃起,性兴趣和活动有增加趋势。与爱丁堡男性相比,香港男性在洗脱期情绪状态似乎受影响较小,且对任何一种治疗均无显著反应。这些结果表明,MENT对性腺功能减退男性的性活动和情绪状态的影响与睾酮相似。由于NPT是一种生理性雄激素依赖性结果,这些数据为MENT的雄激素性提供了进一步证据。除了对清醒时勃起的影响外,在香港男性中未检测到两种雄激素的其他效应,这说明了症状学及其测量的文化背景的重要性。MENT的合适剂量仍有待确定,但这些结果支持其作为一种潜在的雄激素替代疗法的开发。

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