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7α-甲基-去甲睾酮(MENT):男性避孕的最佳雄激素。

7 alpha-methyl-nortestosterone (MENT): the optimal androgen for male contraception.

作者信息

Sundaram K, Kumar N, Bardin C W

机构信息

Population Council, New York, N.Y. 10021.

出版信息

Ann Med. 1993 Apr;25(2):199-205. doi: 10.3109/07853899309164168.

Abstract

UNLABELLED

Many methods of contraception involve the use of drugs that affect the secretion of hormones essential for reproduction. Oestrogens and progestins have been used for contraction in women as inhibitors of gonadotrophin secretion and ovulation. Similarly, androgens must be used in methods of fertility control for men that block gonadotrophin secretion. Androgen supplementation currently involves large, frequent doses of testosterone esters that are associated with wide fluctuations of plasma testosterone levels. Hence, there is a need for an androgen preparation that provides appropriate, continuous replacement doses over long periods. To achieve this goal, 7 alpha-methyl-19-nortestosterone (MENT), a synthetic androgen that is considerably more potent than testosterone, is suitable. As a consequence, it is feasible to administer this androgen as a substitute for testosterone for 1 year by subdermal implants. Another important feature of MENT is that it does not undergo 5 alpha- reduction in prostate as does testosterone. As a consequence, a dose of MENT sufficient to maintain normal muscle mass and gonadotrophin secretion will not hyperstimulate the prostate because its action in this organ is not amplified as is that of testosterone. Thus, MENT can be administered to men with the assurance that it will be less prone to cause diseases of the prostate than testosterone.

CONCLUSIONS

(i) MENT is the first androgen that has a health benefit compared to testosterone; (ii) MENT will be promoted as one component of a two-implant system for male contraception, the other component being an implant that will release an LHRH analogue; (iii) MENT has potential uses in patients with a variety of disorders, including hypogonadism, prostatic hyperplasia and muscle wasting.

摘要

未标注

许多避孕方法涉及使用影响生殖必需激素分泌的药物。雌激素和孕激素已被用作女性避孕药物,作为促性腺激素分泌和排卵的抑制剂。同样,雄激素必须用于男性生育控制方法中,以阻断促性腺激素分泌。目前雄激素补充涉及大剂量、频繁注射睾酮酯,这会导致血浆睾酮水平大幅波动。因此,需要一种能在长时间内提供适当、持续替代剂量的雄激素制剂。为实现这一目标,7α-甲基-19-去甲睾酮(MENT)是一种合适的合成雄激素,其效力比睾酮强得多。因此,通过皮下植入物将这种雄激素作为睾酮替代品给药1年是可行的。MENT的另一个重要特征是,它不像睾酮那样在前列腺中发生5α-还原。因此,足以维持正常肌肉质量和促性腺激素分泌的MENT剂量不会过度刺激前列腺,因为其在该器官中的作用不会像睾酮那样被放大。因此,可以放心地将MENT给予男性,因为与睾酮相比,它不太容易引起前列腺疾病。

结论

(i)MENT是第一种与睾酮相比具有健康益处的雄激素;(ii)MENT将作为男性避孕双植入系统的一个组成部分得到推广,另一个组成部分是释放促性腺激素释放激素(LHRH)类似物的植入物;(iii)MENT在包括性腺功能减退、前列腺增生和肌肉萎缩在内的各种疾病患者中具有潜在用途。

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