Bhargava A S, Kapp J F, Poggel H A, Heinick J, Nieuweboer B, Günzel P
Arzneimittelforschung. 1981;31(6):1005-9.
The effect of oral administration of 17 alpha-acetoxy-6-chloro-1,2 alpha-methylene-4,6]pregnadiene-3,20-dione (cyproterone acetate, Androcur) on the adrenal function in male hypersexual subjects and in female rhesus monkey was investigated on the basis of cortisol and ACTH levels in serum or plasma and excretion of cortisol and 17-ketosteroids. In addition, cyproterone acetate and its main metabolite alcohol of the main metabolite were characterized for treatment of male hypersexual subjects and female rhesus monkeys did not reveal any signs of adrenal suppression. Cyproterone acetate and its metabolites gave on indication of any appreciable anti-inflammatory effect in the adjuvant edema test in rats. However, there was a general increase in the level of blood glucose and liver glycogen as well as a reduction in body weight and organ weight (spleen, thymus and adrenal) in rats, in which 15 beta-hydroxy cyproterone was slightly more active with the exception of adrenal weight tests. It can be concluded that adult man and rhesus monkey are much less sensitive, is so at all, to some corticosteroid-like activities of cyproterone acetate and its main metabolites than the rat.
基于血清或血浆中皮质醇和促肾上腺皮质激素(ACTH)水平以及皮质醇和17 - 酮类固醇的排泄情况,研究了口服17α - 乙酰氧基 - 6 - 氯 - 1,2α - 亚甲基 - 4,6]孕二烯 - 3,20 - 二酮(醋酸环丙孕酮,Androcur)对男性性欲亢进者和雌性恒河猴肾上腺功能的影响。此外,对醋酸环丙孕酮及其主要代谢产物的醇进行表征,用于治疗男性性欲亢进者和雌性恒河猴,未发现肾上腺抑制的任何迹象。在大鼠佐剂性水肿试验中,醋酸环丙孕酮及其代谢产物未显示出任何明显的抗炎作用。然而,大鼠的血糖和肝糖原水平普遍升高,体重以及器官重量(脾脏、胸腺和肾上腺)下降,其中15β - 羟基环丙孕酮除肾上腺重量试验外活性略高。可以得出结论,成年男性和恒河猴对醋酸环丙孕酮及其主要代谢产物的某些类皮质醇活性的敏感性远低于大鼠,甚至根本不敏感。