Tisell L E, Salander H
Acta Endocrinol (Copenh). 1975 Feb;78(2):316-24. doi: 10.1530/acta.0.0780316.
Megestrol acetate (17alpha-acetoxy-6-dehydro-6-methylprogesterone), a synthetic steroid with high progestational activity, is used in oral contraceptives but also in the treatment of prostatic diseases in man. To investigate whether megestrol acetate has any androgenic properties the growth of the ventral and dorsolateral prostate, the coagulating glands and the seminal vesicles was studied morphologically in castrated rats treated with megestrol acetate and in non-treated castrated rats. The effect of megestrol acetate on the body weight, the levator ani muscle and the adrenals was also studied. Megestrol acetate was administered in daily doses of 0.02 mg, 0.2 mg, 2.0 mg or 20.0 mg for a period of 21 days. Megestrol acetate in the two higher doses retarded growth and gave a low weight for the levator ani muscle at autopsy indicating an anti-anabolic or catabolic action of megestrol acetate in high doses. Megestrol acetate in daily doses of 0.2, 2.0 and 20.0 mg caused an involution of the adrenal glands. After the two higher doses the weight of the adrenals amounted to only about a third of that of the untreated rats. Megestrol acetate in the lower doses had no demonstrable effect on the growth of the accessory reproductive glands. After the two higher doses of megestrol acetate some growth of the dorsal part of the dorsolateral prostate and of the coagulating glands was observed. Only the seminal vesicles exhibited complete morphological criteria of an androgenic stimulation and then only after the largest dose of megestrol acetate. The investigation shows that megesterol acetate has weak androgenic properties which are apparent at a dose per kg body weight approximately 200 times greater than that used in the treatment of prostatic diseases in man.
醋酸甲地孕酮（17α - 乙酰氧基 - 6 - 脱氢 - 6 - 甲基孕酮）是一种具有高孕激素活性的合成类固醇，用于口服避孕药，也用于治疗男性前列腺疾病。为了研究醋酸甲地孕酮是否具有任何雄激素特性，对用醋酸甲地孕酮治疗的去势大鼠和未治疗的去势大鼠的腹侧和背外侧前列腺、凝固腺和精囊的生长进行了形态学研究。还研究了醋酸甲地孕酮对体重、提肛肌和肾上腺的影响。醋酸甲地孕酮以每日0.02毫克、0.2毫克、2.0毫克或20.0毫克的剂量给药，持续21天。两种较高剂量的醋酸甲地孕酮会阻碍生长，尸检时提肛肌重量较低，表明高剂量的醋酸甲地孕酮具有抗合成代谢或分解代谢作用。每日剂量为0.2、2.0和20.0毫克的醋酸甲地孕酮会导致肾上腺萎缩。在两种较高剂量后，肾上腺重量仅约为未治疗大鼠的三分之一。较低剂量的醋酸甲地孕酮对附属生殖腺的生长没有明显影响。在两种较高剂量的醋酸甲地孕酮后，观察到背外侧前列腺的背侧部分和凝固腺有一些生长。只有精囊表现出雄激素刺激的完整形态学标准，而且只有在使用最大剂量的醋酸甲地孕酮后才出现。研究表明，醋酸甲地孕酮具有弱雄激素特性，其在每千克体重的剂量下表现明显，大约是用于治疗人类前列腺疾病剂量的200倍。
