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At least 19 recordsLinked to original sources
PubMed1979

Effects of cyproterone and cyproterone acetate on the adrenal gland in the rat: studies in vivo and in vitro.

Male Wistar rats were treated for three weeks with cyproterone (1.7 or 5.1 mg/day) or cyproterone acetate (2 or 6 mg/day). The adrenal weights of animals treated with either dose of cyproterone acetate were significantly less (P less than 0.001) than those of untreated animals. In contrast, the adrenal weights of animals treated with cyproterone did not differ from those of the controls. The concentrations of corticosterone in the plasma were significantly less (P less than 0.001) in both groups treated with cyproterone acetate compared with those of the controls; only the higher dose of cyproterone reduced the plasma concentration of corticosterone (P less than 0.001). Cyproterone acetate inhibited the rat adrenal 3beta-hydroxysteroid dehydrogenase-5-ene,4-ene-isomerase complex in vitro, with both pregnenolone and dehydroepiandrosterone as substrates. Analysis of the reaction rates suggested an uncompetitive mode of inhibition. These results suggest that in rats the antiandrogens cyproterone and cyproterone acetate may provoke adrenal insufficiency by inhibition of steroid biosynthesis. Furthermore, indirect evidence from the mass and morphology of the adrenal suggests that cyproterone acetate may also suppress production or secretion of ACTH by the pituitary gland.

Adrenal Glands↗
PubMed1977

Some effects of cyproterone and cyproterone acetate on the reproductive physiology of the male rat.

Male rats were treated with 5 or 20 mg cyproterone acetate/kg/day or 20 mg cyproterone/rat/day for 1, 2, 3, 4, or 5 weeks. There was some reduction in fertility with both compounds, the maximum effect occurring after 5 weeks with the higher dose of cyproterone acetate and after 2 weeks with cyproterone. A significant increase in testosterone levels was found after treatment with the high dose of cyproterone acetate by 1 week and with cyproterone by 2 weeks. Dose-dependent atrophy of the seminal vesicles occurred after treatment with cyproterone acetate; with cyproterone atrophy occurred at 1 and 2 weeks but approximated to control values at 3, 4 and 5 weeks. Epididymal weights were reduced with the high dose of cyproterone acetate but the low dose had little effect. Reduction in the weight of the testes was only observed after 5 weeks of treatment with the high dose of cyproterone acetate. Since plasma testosterone levels were not depressed below normal values, accessory sex organ regression evidently resulted from the local antiandrogenic action of the drugs. There was some indication of interference with the secretory and absorptive activity of the lining cells of the epididymis but in general treatment with either steroid caused only relatively small and variable changes in the composition of epididymal plasma.

Animals↗
PubMed1977

Isolation and identification of 15-beta-hydroxy cyproterone acetate as a new metabolite of cyproterone acetate in dog, monkey and man.

15-beta-hydroxy cyproterone acetate could be identified by thin layer chromatography, mass spectrum, NMR and IR spectrum as a major unconjugated metabolite of cyproterone acetate in plasma and urine of dog, monkey and man. This metabolite has been found to interferein the Mattingly method for the determination of 11-hydroxy-corticosteroids which suggests, that this method is inadequate in controling the adrenal function of subjects treated with cyproterone acetate.

Animals↗
PubMed1988

Pharmacokinetics of cyproterone acetate and its main metabolite 15 beta-hydroxy-cyproterone acetate in young healthy women.

Cyproterone acetate (CPA) and 15 beta-hydroxy-cyproterone acetate (15 beta-OH-CPA) have been quantitated in human plasma by a selective, automated HPLC assay in 8 young female subjects. Subjects received a single oral dose of 100 mg CPA and four weeks later, a single intramuscular dose of 300 mg CPA. Plasma levels in seven subjects could be evaluated pharmacokinetically. After intramuscular administration maximum CPA serum levels of 191 +/- 49 ng/ml were reached between 2 and 3 days. Postmaximal levels declined with a half-life of 4.3 +/- 0.7 days. After oral administration maximal serum levels of 255 +/- 110 ng/ml were measured between 2 and 3 h. CPA levels decayed biphasically with a terminal half-life of 3.6 +/- 1.3 days. Bioavailability after oral administration was nearly complete (88 +/- 20%). Metabolite levels were below CPA levels until 4 days (i.m.) and 6 h (p.o.) and exceeded CPA levels later on. 15 beta-OH-CPA levels declined with half-lives similar to those of corresponding CPA levels, indicating that terminal half-life of the metabolite in serum reflects its rate of formation rather than its rate of elimination. Areas under the metabolite serum level curves after intramuscular and oral administration were 10 to 15% higher than the corresponding areas for unchanged CPA. Since CPA and 15 beta-OH-CPA contribute to the antiandrogenetic efficacy there is good reason to assume that the intramuscular administration of CPA might be equally effective in the therapeutical use as the oral administration.

Administration, Oral↗
PubMedDate not supplied

Cyproterone acetate: I. Microquantity releasing device of cyproterone acetate and its failure in inducing functional sterility in male rats.

Prasad and his coworkers emphasized that microquantities of cyproterone acetate (CPA) when continuously available developed functional sterility in male rats by interfering the epididymal physiology. In our experimental rats either 2 or 3 capsules containing CPA as per the specification of Prasad were implanted subcutaneously and left for 300 and 250 days, respectively. Fertility test was made every month and it was observed that all the experimental animals were able to impregnate female rats throughout the experiment. Excepting the epididymis the weight of testes and other accessory glands did not differ from the controls in the animals which had 2 CPA capsules for 300 days; On the other hand, the animals which received 3 CPA capsules for 250 days showed significant reduction in weight of all the acessory glands including the testes.

Animals↗
PubMed1985

Acne: double blind clinical and laboratory trial of tetracycline, oestrogen-cyproterone acetate, and combined treatment.

Since the recent introduction of a drug regimen containing 2 mg of the antiandrogen cyproterone acetate and 50 micrograms ethinyl-oestradiol (Diane; oestrogen-cyproterone acetate) several uncontrolled reports have extolled the benefits of this drug. Double blind studies, however, are lacking. Sixty two patients with moderate or moderately severe acne were therefore included in a double blind trial of treatment for six months comparing tetracycline alone, oestrogen-cyproterone acetate alone, and a combination of these agents. Sebum excretion rates and bacterial counts were measured before, during, and after treatment, at the same time as a clinical assessment was made. At six months the acne (as assessed by overall grade) had improved by 68% in the antibiotic treated group and by 74% in the oestrogen-cyproterone treated group. The group given a combination of both agents improved by 82%, which was significantly better (p less than 0.025) than the improvement in the tetracycline treated patients. No significant difference was found between the groups given oestrogen-cyproterone alone and the combined treatment. The sebum excretion rate was suppressed by 25% in the patients in both groups receiving oestrogen-cyproterone but not in the group given antibiotics alone. Oestrogen-cyproterone acetate is as effective as antibiotics in treating acne in women, and adding antibiotics offers no advantage over using oestrogen-cyproterone on its own, although in this study the combination was more effective than tetracycline alone at six months.

Acne Vulgaris↗
PubMed1976

Cyproterone-mediated stimulation of delta-aminolevulinic acid synthetase in chick embryo liver cells.

In cultured chick embryo liver cells, cyproterone and cyproterone acetate, synthetic anti-androgenic steroids, were found to be potent inducers of mitochondrial delta-aminolevulinic acid (ALA) synthetase, the rate-limiting enzyme in the heme biosynthetic pathway. Both steroids produced a detectable increase in enzyme activity at 5 muM and a maximal stimulation, 36-fold for cyproterone and 29-fold for cyproterone acetate, at 55 muM. The dose-response curves of the steroids differed, however, in that cyproterone acetate produced a greater mean stimulation of the enzyme at concentrations less than approximately 25 muM, whereas, at higher concentrations, cyproterone was the more effective inducer. Increased activity of ALA synthetase was not apparent until about 12 hours after the addition of cyproterone, and maximal activity was not achieved until 20-24 hours. The induction of ALA synthetase by these anti-androgens was prevented by actinomycin D, cordycepin, anisomycin, cycloheximide, and puromycin. These results suggest that new RNA and protein synthesis are necessary for enzyme induction. The cyproterone-mediated induction of the enzyme was inhibited 50% by 2 muM heme, the putative physiological inhibitor of ALA synthetase. These antiandrogens, unlike other potent steroid inducers of this enzyme in chick embryo liver, do not possess either a 5beta-pregnane or 5beta-androstane nucleus. The stimulation of hepatic ALA synthetase represents the first example of a direct effect of these steroids on enzyme induction.

5-Aminolevulinate Synthetase↗
PubMed1990

[Therapy of hirsutism in females with adrenal enzyme defects of steroid hormone biosynthesis: comparison of dexamethasone with cyproterone acetate].

In patients with adrenal hirsutism or enzyme deficiencies in steroidogenesis, elevated adrenal androgens could be normalized by dexamethasone. We were interested to see if dexamethasone would be as effective as cyproterone acetate in treating hirsutism in selected patients with adrenal pathogenesis. Therefore 28 patients with hirsutism of adrenal origin or enzyme deficiency were treated cyclically either with cyproterone acetate and ethinylestradiol (2 mg cyproterone acetate + 0.035 mg ethinyl-estradiol days 1-21, +10 mg cyproterone acetate days 1-15) (n = 15) or with 0.25-0.5 mg dexamethasone daily at 10 pm (n = 13). In the dexamethasone group there was a significant drop in dehydroepiandrosterone and dehydroepiandrosterone sulfate levels within 9 months, but there was a diminution in hirsutism in only four women (31%); in four out of seven menstrual irregularities decreased. In the cyproterone acetate group hirsutism diminished significantly in 66% (n = 10) without suppression of adrenal androgens. Weight gain occurred in a few cases in both groups; other side effects developed in 33% in the cyproterone acetate group. Preselection of patients with hirsutism is useful with respect to diagnosis; adrenal pathogenesis should not generally indicate dexamethasone treatment of hirsutism unless there is a desire for pregnancy, because cyproterone acetate is a more powerful agent in reducing hair growth.

3-Hydroxysteroid Dehydrogenases↗
PubMed1976

[Bioavailability and pharmacokinetics of 14C-cyproterone acetate after administration as a 50-mg tablet (author's transl)].

Four male volunteers were each given a 50 mg oral dose of methylene-14C-labelled cyproterone acetate in a formulation largely identical to the commercial preparation Androcur Tablets. A further 3 volunteers were each given 10 mg of the 14C-labelled compound by intramuscular injection. Plasma samples were obtained and urine and faeces collected quantitatively from each volunteer up to 10 days post administration. 1. Absorption of the 50 mg of cyproterone acetate administered in the form of Androcur Tablets was largely complete. 2. The maximal plasma level of 400 +/- 40 ng cyproterone acetate equivalents/ml of plasma, calculated from the 14C activity, was found 3,8 +/- 0,5 hours after oral administration. By 10 hours post administration the plasma level had declined with a half-life of 7,9 +/- 2,5 hours (distribution and elimination). The fictitious distribution volume assignable to this process amounted to 140 +/- 40% of body weight. Plasma 14C-activity then decreased with a half-life of 1,8 +/- 0,2 days, which was consistent with elimination. 3. The labelled substance was almost completely extractable from plasma and could be separated by chromatography into 2 fractions of about equal size: cyproterone acetate and one metabolite. 4. Orally administered cyproterone acetate was eliminated with a half-life of 1,6 +/- 0,1 days. By 10 days post administration 33 +/- 6% of the dose had been detected in urine and 60 +/- 8% in faeces. Up to this time total elimination amounted to 93 +/- 5% of the dose. 5. After intramuscular injection of 10 mg of cyproterone acetate the half-life for absorption from the muscular depot was 7,0 +/- 0,2 hours. Between 2 and 10 days post administration there was a uniform decrease in plasma level and urinary elimination with half-life of 2,3 +/- 0,1 days and 2,1 +/- 0,2 days respectively. By the end of the trial 34 +/- 5% of the dose had been eliminated with urine and 57 +/- 6% with faeces.

Administration, Oral↗
PubMed1975

Metabolism and mode of action of androgens in target tissues of male rats. V. Uptake and metabolism of cyproterone acetate and its influence on the uptake and metabolism of testosterone and 5alpha-dihydrotestosterone in target organs and peripheral tissues.

In order to get more information on the mode of action of anti-androgens, two series with low but biologically active doses of cyproterone acetate were started. In the first experiments 12 mug of [3H]cyproterone acetate was injected intravenously into adult rats castrated 3 days before treatment. Thirty min after injection the radioactivity uptake in the target organs and other tissues was measured. The metabolites were separated by thin layer chromatography. A large pool of radioactivity could be shown in the liver. Thin layer chromatography revealed that in this pool cyproterone acetate had been converted by more than 80% to one metabolite. In blood plasma, too, the metabolite accounted for the major part of radioactivity. When compared to skeletal muscle, the prostate, seminal vesicles, and m. bulbocavernosus and m. levator ani accumulated more radioactivity. Within 30 min unchanged cyproterone acetate was retained selectively thus showing its relative high affinity to target organs. In a second experimental series, adult castrated male rats were given 10 mug of cyproterone acetate intravenously 30 min before the injection of [3H]testosterone or [3H]5alpha-dihydrotestosterone. Under this condition androgen uptake in target tissues was reduced to about 70% of the control values. The data parallel the results of in vivo studies on cytosol receptor displacement of androgens by cyproterone acetate. In agreement with previous investigators no significant influence of the anti-androgen on androgen metabolism was observed. The importance of the findings concerning the mode of anti-androgen action is discussed.

Adipose Tissue↗
PubMed1989

Comparison of cyproterone acetate and danazol in the treatment of pelvic pain associated with endometriosis.

Twenty-three patients with laparoscopically diagnosed endometriosis and pelvic pain were allocated randomly to treatment with cyproterone acetate 27 mg plus ethinyl estradiol 0.035 mg/day (11 patients) or danazol 600 mg/day (12 patients). All women received treatment for 6 months, except for one in the cyproterone group who suspended treatment for nonmedical reasons and was excluded from analysis of the results. The clinical condition and pain symptoms were monitored in all patients for 1 year after treatment suspension. The intensity of pelvic pain at diagnosis, during treatment, and at follow-up was evaluated by a multidimensional verbal score and an analogue scale. At the end of treatment, a repeat laparoscopy was performed in those patients who agreed (four in the cyproterone group, five in the danazol group); the results showed a partial regression of endometriotic lesions in both groups, with no significant differences between them. Dysmenorrhea disappeared in all patients during treatment. At 6 months after suspension, dysmenorrhea recurred in 66% of the cyproterone group and 58% of the danazol group, and at 1 year in 89 and 92%, respectively. Intermenstrual pelvic pain improved markedly during treatment in both groups; 6 months after treatment withdrawal it was present in four cyproterone subjects and four danazol group patients, whereas after 1 year, only one woman in the danazol group did not have this symptom. Deep dyspareunia was less affected by treatment, and 6 months later had recurred in all the women.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1990

Severe hepatitis caused by cyproterone acetate.

A case of severe acute hepatitis caused by cyproterone acetate in a 71 year old man with prostatic carcinoma is reported with a review of the literature on hepatic reactions to this drug. The association between the use of cyproterone acetate and liver abnormalities is poorly documented. This is the fourth published report of adverse hepatic reaction to cyproterone acetate and it substantiates other evidence that cyproterone acetate is potentially hepatotoxic. Monitoring of liver function tests should be mandatory in patients receiving high doses of cyproterone acetate; the drug should be withdrawn immediately if abnormal liver function tests are found.

Adenocarcinoma↗