Up to the present only C17-alkylated testosterone- and androstenediolderivates have been used for oral androgen treatment. These steroids given in higher doses or for longer periods all have an inhibitory effect on gonadotrophin secretion of the hypophysis and on the testicular tissue. Investigations with Mesterolone (1-methyl-androstane-17β-ol-3-one), a new androgen, are described. Like other investigators we did not find any inhibitory effect on gonadotrophin-secretion and on the number of spermatozoa. We further showed that there is no effect on the testicular tissue when Mesterolone is given up to a total dose of 12 570 mg over 4 months. 17-ketosteroid excretion in the urine is increased by the metabolite 1α-methyl-androsterone. 17-ketogenic steroids are also increased, and this cannot be explained at present. There is no impairment of hepatic function. The androgenic effect of Mesterolone is good. The absence of inhibition of gonadotrophin-secretion by Mesterolone could be explained by the fact, that the ring A in the steroid molecule is saturated. This kind of steroid cannot be aromatized to oestrogens, which have the greatest inhibiting effect on the gonadotrophin-function of the hypophysis.
Treatment with Cyproterone 200 mg/d induced no increase of total gonadotrophins in normal subjects. Plasma testosterone was elevated during the period of treatment. An alteration in the ratio LH/FSH has been suggested.
Urinary 17-KS showed no uniform pattern, but 17-KGS were always significantly elevated during Cyproterone treatment. Seminal fluid examinations showed no effect of Cyproterone (100 and 200 mg/d, total dose 4.2–38.6 g within 9 months) on spermatogenesis in 6 adults with normal gonadal function. No increase of spermatogenesis has been observed under treatment with Cyproterone (100 mg and 200 mg/d, total dose 3.5–35.4 g within 8 months) in 7 patients with oligospermia. Over a period of 21 days no influence of Cyproterone (200 mg/d) has been observed on the function of adrenal cortex, concerning cortisol- and aldosterone production, on the carbohydrate and lipid metabolism and on liver function in 5 subjects.
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