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PubMed1978

Therapy of androgenetic sympatomatology with cyproterone acetate and ethinyl estradiol.

The effectiveness of therapy with cyproterone acetate and ethinyl estradiol was studied in 103 women. Acne and seborrhea responded best with 91.7 and 93.3% respectively, including complete and partial therapeutic success. For hirsutism complete remission and partial improvement were found in 75.3% of the treated women. Under therapy, body weight did not change in 51.9%, while 24.7% of the patients gained weight and 23.4% lost weight. The cycle length remained normal after therapy in 35.8%. Normalization or improvement was found in 54.7%. In 6.3% no improvement was noted after therapy and in 3.2% cycle irregularity developed in women with previous undisturbed pattern. According to BBT, improvement of the functional capacity of the reproductive system was found in 32.9% of the patients. Only 3% of the women studied demonstrated a deterioration. The 17-ketosteroid excretion was diminished in 35.3% after therapy and remained unchanged in 64.7%. The therapeutic regimen used for the study was well tolerated and good cycle control was obtained.

17-Ketosteroids↗
PubMed1993

The long-term effect of cyproterone acetate on growth in girls with idiopathic precocious puberty. Androcur Study Group in Japan.

To define the effect of cyproterone acetate (CPA) on statural growth, 25 girls with idiopathic precocious puberty who had been treated with CPA were studied retrospectively. The final height SDS was -1.12 +/- 1.16 (mean +/- SD). The daily CPA dose was negatively related to the final height SDS. We divided our subjects into two groups according to the daily CPA dose [low dose, 84.9 +/- 15.4 mg/m2 (n = 19) vs high dose, 135.8 +/- 17.1 mg/m2 (n = 6)]. In the low dose group, the difference of the final height SDS minus height SDS for bone age at the initiation of CPA treatment was 0.55 +/- 1.16 and final height SDS was -0.82 +/- 1.05. The final height was not significantly different from the target height in the low dose group subjects whose target heights were obtained. Since the increment of height age to the increment of bone age during the treatment was significantly less in the group needing and treated with high dose CPA, high doses of CPA may reduce growth velocity more than its suppressive effect on bone maturation. These results suggest that CPA has an effect on statural growth in girls whose clinical symptoms can be controlled with a low dose of CPA, although they have not been compared with final height in untreated Japanese girls.

Age Determination by Skeleton↗
PubMed1997

Cyproterone acetate monotherapy in advanced prostatic carcinoma.

Cyproterone acetate was given as monotherapy to 18 patients with advanced prostatic carcinoma at a weekly dose of 300 mg. Progression was observed in all of the patients; median time to progression was 35 months and median survival time was 48 months. Partial response, stabilization, progression and exitus rates by years also showed favourable results, as compared with other forms of therapy in advanced prostatic carcinoma.

Aged↗
PubMed2005

Effects of metformin combined with cyproterone acetate on clinical features, endocrine and metabolism of non-obese women with polycystic ovarian syndrome.

In order to explore the effects of metformin combined with cyproterone acetate (CPA) on the clinical features, endocrine and metabolism of the patients with polycystic ovarian syndrome (PCOS), 50 cases of non-obese PCOS were randomly subjected to CPA (CPA treatment group, n = 25) and CPA+ metformin (n = 25) treatment for 6 months. Before and after treatment the body mass index (BMI), waist : hip ratio (WHR), ovarian volume, serum gonadotrophin, androgen and sex hormone-binding globulin (SHBG) levels, and fasting lipid, glucose and insulin levels were measured. The results showed that all of the parameters in two groups were similar before treatment. After treatment for 6 months in the CPA+ metformin group, BMI and WHR were significantly decreased, while insulin sensitivity was significantly decreased as Compared with those before treatment. In CPA group, no significant changes were found before and after treatment. Combined use of CPA and metformin could result in the reduction of serum androstenedione and increases of serum SHBG levels as compared with the CPA treatment alone. It was concluded that combined use of CPA and metformin could improve the insulin sensitivity, and further suppress the hyperandrogenism in non-obese women with PCOS.

Adolescent↗
PubMed1980

Adaptive responses of rat liver to the gestagen and anti-androgen cyproterone acetate and other inducers. I. Induction of drug-metabolizing enzymes.

Treatment of female Wistar rats with cyproterone acetate (CPA) was shown to cause pronounced increases of hepatic microsomal monooxygenase activity towards the following substrates: ethylmorphine (EM), aminopyrine (AP), benzphetamin (BPA) and benzo[a]pyrene (BP). Minor increases were seen using p-nitroanisole (pNA) and aniline (AN). Monooxygenase activity reached maximal levels within 24 h. The effects were dose-dependent, the threshold dose being about 4 mg/kg, and were reversible within 6 days. The results of comparative studies with several 'classical' microsomal enzyme inducers, i.e. pregnenolone-(16 alpha)-carbonitrile (PCN), phenobarbital (PB), alpha-hexachlorocyclohexane (alpha-HCH) and 3-methylcholanthrene (3-MC) suggest that CPA belongs to the PCN-type and alpha-HCH to the phenobarbital type of inducers. In male rats CPA induced only moderate increases of monooxygenase activities which can be explained by decreased testosterone scretion due to anti-gonadotropic effect of CPA.

Adaptation, Physiological↗
PubMed1980

Adaptive responses of rat liver to the gestagen and anti-androgen cyproterone acetate and other inducers. II. Induction of growth.

Treatment of female Wistar rats with cyproterone acetate (CPA) leads to considerable enlargement of the liver. The organ content of water, dry mass, protein, RNA, and DNA increased in parallel with the enlargement; only lipid accumulation showed a slight excess. The changes were maximal after treatment for 3 days and increased in a dose-dependent manner, the threshold dose being 5--10 mg CPA/kg DNA synthesis was strongly enhanced after a lag phase of 12--14 h; a maximal rate of synthesis was attained after 18--24 h. The number of parenchymal cells involved in DNA synthesis and mitosis were increased up to 20-fold. Sinusoidal cells participated only slightly in the growth process, and their number decreased relative to the number of parenchymal cells. These results indicate that CPA induces (presumably adaptive) liver growth essentially by parenchymal hyperplasia; of the model inducers used for comparison only pregenolone-16 alpha-carbonitrile (PCN) produced a similarly strong hyperplastic response while liver enlargement elicited by a alpha-hexachlorocyclohexane (alpha-HCH), phenobarbital (PB) and 3-methylcholanthrene (3-MC) was partly or exclusively due to hypertrophy. Liver growth was also observed in male rats treated with CPA, but was less pronounced in this sex. After discontinuation of treatment, liver enlargement and the increase of DNA regressed partially within 1--3 weeks; this regression seemed to be due to sequestration of old cells which were not involved in replication after CPA treatment. The relationship between induction of liver growth by CPA and hepatoma formation in rats is discussed.

Adaptation, Physiological↗
PubMed1980

Adaptive responses of rat liver to the gestagen and anti-androgen cyproterone acetate and other inducers. III. Cytological changes.

Treatment of rats with cyproterone acetate (CPA) induces liver growth. Intact hepatocytes and cell nuclei were isolated from enlarged livers and their volumes or diameters were determined by electronic and microscopic methods. No changes in mean hepatocyte volume or ploidy were observed. However, there was a marked fall in the frequency of binuclear hepatocytes (from 43% to 7%) and a concomitant increase of nuclear ploidy. This effect probably resulted from CPA-induced replication of binuclear hepatocytes. The total number of hepatocytes replicating in response to CPA was estimated on the basis of these data and was found to be up to 75% of all parenchymal cells. Similar cytological changes were observed in the liver after treatment with pregnenolone-16 alpha-carbonitrile (PCN) and, to a lesser extent, with alpha-hexachlorocyclohexane (alpha-HCH). In contrast, physiological liver growth in adolescent rats was characterized by only small changes in binuclearity and nuclear ploidy, and by increases of cellular ploidy. Thus, ploidy analyses may be a useful tool to characterize the type of growth stimulation. Following discontinuation of treatment the cytological changes induced by CPA or alpha-HCH were not reversible in a matter of 3 weeks.

Adaptation, Physiological↗
PubMed1978

Sex hormone binding globulin: binding capacity and studies on the binding of cyproterone acetate and other steroids.

Sex hormone binding globulin in blood is quantitated by ammonium sulphate precipitation technique with two radioactive ligands, [3H]testosterone and [3H5dihydrotestosterone. Plasma levels in normal men, normal women, women taking oral contraceptives containing oestrogens, and pregnant women are presented, measured with both ligands. Binding experiments with these ligands and several competing steroids show marked differences in displacement ability. For cyproterone acetate 100-500 ng per tube is required to obtain even a slight displacement of the radioactive ligands.

Contraceptives, Oral, Hormonal↗
PubMedDate not supplied

Maintenance of sexual behavior in castrate male SW mice using the anti-androgen, cyproterone acetate.

The present study was designed to test the hypothesis that cyproterone acetate (C) might selectively block the actions of dihydrotestosterone (D) and via this action, function as an anti-androgen in male sexual behavior. Sexually experienced male SW mice, a strain previously shown to respond to D following castration, were divided randomly into six groups. Beginning on the day after castration, animals received SC injections for 21 days of either testosterone (T), (D), (C), (T+C), (D+C) or vehicle (V). C was found to significantly reduce seminal vesicle and body weights in all androgen treated groups. There was no evidence to support the contention that C selectively blocks the action of D. To the contrary, in sex tests C maintained palpations, thrust mounts, with intromissions and mounts with ejaculations. Indeed, only animals receiving C alone or in combination with T and D exhibited ejaculations throughout the testing. These results suggest that in the SW mouse, C can work like an androgen in the maintenance of male sexual behavior.

Animals↗
PubMed1978

Effect of several androgens, cyproterone acetate or estrogen-progesterone on the prolactin-releasing activity of arginine vasotocin in castrated male rats.

Intravenous (iv) administration of 5 microgram of arginine vasotocin (AVT) into urethane-anesthetized, castrated male rats had no effect on plasma prolactin titers as compared to the rise in prolactin levels observed in intact AVT-treated rats. However, when castrated rats were first treated for two days with 2.5 mg/day of testosterone propionate and then challenged with a 5-microgram dose of AVT, the prolactin surge values obtained were comparable to those seen in intact AVT-treated rats. Conversely, treatment of intact rats for two days with 25 mg/day of the anti-androgen, cyproterone acetate, blocked the prolactin-releasing activity of AVT. In a separate experiment, treatment of castrated rats for two days with 2.5 mg/day of testosterone, androsterone or 50 microgram of estradiol benzoate and 25 mg progesterone, completely restored the prolactin-releasing activity of AVT. Similar treatment with 2.5 mg/day of androstenedione or dihydrotestosterone was without effect in restoring this response to AVT. It is concluded that the presence of gonadal steroids is essential to the action of AVT in provoking the release of prolactin in urethane-anesthetized male rats.

Androgens↗
PubMed2004

Effects of a model androgen (methyl testosterone) and a model anti-androgen (cyproterone acetate) on reproductive endocrine endpoints in a short-term adult mummichog (Fundulus heteroclitus) bioassay.

A short-term gonadal recrudescence bioassay using the mummichog (Fundulus heteroclitus) was employed to examine the consequences of environmentally relevant and pharmacological exposures (1-1000 ng/l) of the androgen, 17alpha-methyl testosterone (MT), and the anti-androgen, cyproterone acetate (CA), on reproductive endocrine endpoints. Recrudescing male (GSI = approx. 2%) and female (GSI = approx. 10%) fish were exposed to graded concentrations of MT and CA for 7 or 14 days. In the first experiment (7-day exposure), MT concentrations of 250 or 1000 ng/l decreased circulating testosterone (T) and estradiol (E(2)) in female fish, and 11-ketotestosterone (11-KT) in male fish. Plasma T, 11-KT and E(2) were decreased following CA exposure (250 and 1000 ng/l). Gonadal steroid biosynthetic capacity was also inhibited in both sexes after exposure to MT or CA, as evidenced by decreased in vitro production of T and E(2). In experiment 2 (14-day exposure), exposures to lower MT and CA concentrations (1, 10 and 100 ng/l) resulted in decreased plasma T, with females showing greater sensitivity than males. Both 11-KT and E(2) were significantly reduced beginning at 10 ng/l MT. In vitro gonadal T production was impaired at 100 ng/l MT in both males and females while 1 ng/l CA caused a significant decrease in female fish. In experiment 2, in vitro E(2) production was decreased in females at all concentrations of MT and CA, while only 100 ng/l reduced 11-KT synthesis in males. Plasma vitellogenin (Vtg) was reduced in females exposed to 1000 ng/l (experiment 1) and 100 ng/l (experiment 2) MT, while CA did not alter plasma Vtg at any concentration. This bioassay has the potential to be used to assess the possible consequences in estuarine fish of exposure to environmental anti/androgens.

Androgen Antagonists↗
PubMed2006

Sex steroids in the female zebrafish (Danio rerio). Effects of cyproterone acetate and leachate-contaminated sediment extract.

In Molnbyggen, a leachate-contaminated lake in Sweden, effects on the reproductive system of perch included a decreased frequency of sexually mature female perch, reduced gonadosomatic index and decreased plasma levels of androstenedione and testosterone, but the contaminants responsible for these effects have not yet been identified. A biomarker-directed fractionation approach could be used to narrow the search for the compound(s) responsible for the adverse effects in Molnbyggen female perch. Thus, it is important to develop and test a suitable biomarker, which can be used in this type of approach. We evaluated if decreased concentrations of sex steroids could work as an in vivo end-point in female zebrafish fed an organic extract of bottom sediments from Molnbyggen. The responsiveness of zebrafish to endocrine alteration was evaluated using a positive control substance, cyproterone acetate (CA), which is known to inhibit steroid biosynthesis. After the 21-day exposure period the concentrations of testosterone (T) and estradiol (E2) were successfully determined by HRGC/HRMS in whole-body homogenates of individual fish. Median T concentrations were 1.7pmol/g fish in controls and were decreased after exposure both to CA (0.55pmol/g fish) and Molnbyggen sediment extract (1.2-1.3pmol/g fish). Median E2 concentrations were 5.3pmol/g fish in controls and were decreased after CA exposure (2.3pmol/g fish) and after exposure to Molnbyggen sediment extract (4.0-4.5pmol/g fish). This suggests that sex steroid concentrations in zebrafish are responsive to endocrine alteration and indicates that compounds with endocrine altering potency are present in Molnbyggen sediments.

Androgen Antagonists↗
PubMed2005

Cyproterone acetate affects protamine gene expression in the testis of adult male rat.

The temporal effects of oral administration of cyproterone acetate (CPA), a progestational androgen receptor blocker, were studied on the fertility of adult male rat sires, at a dose of 20 mg kg-1 day-1 after 15 days of gavage. The treatment reduced the fertility and weights of accessory sex glands, without altering the serum levels of luteinizing hormone, follicle-stimulating hormone (FSH) and testosterone (T). Sperm counts were significantly reduced after treatment. Several changes were evident in caput epididymal sperm chromatin in treated rats. The in vitro decondensation rates of sperm chromatin and total fluorescent acridine orange (AO) dye uptake were enhanced. The fluorescent AO dye uptake by the double- and single-stranded sperm chromatin increased. The uptake of thiol-specific monobromobimane fluorescent dye by sperm chromatin was significantly reduced. Sperm of treated rats exhibited hypoprotamination. Protamine levels in the testis were significantly reduced after treatment. Androgen-binding protein (ABP) expression was significantly reduced in testis after treatment. A slight but significant increase was observed in cyclic AMP immunoexpression in testis after treatment. The expression and levels of transition proteins 1 (TP1) and 2 (TP2) as well as cyclic AMP response element modulator protein-tau were maintained at control levels in the testis of treated rats. The present study reports that androgen receptor occupation by CPA preferentially reduces the levels of spermatidal protamine in testis and spermatozoa involved in nuclear chromatin condensation. It is inferred that ABP could be mediating the effects of T in modulating the sequential expression of TPs and protamines during nuclear chromatin condensation. It is likely that indirect effects of T involve its aromatization in spermatids.

Androgen Antagonists↗
PubMed2005

Combined use of metformin and ethinyl estradiol-cyproterone acetate in polycystic ovary syndrome.

OBJECTIVE: The aim of our study was to compare the effect of metformin applied independently to the effect of metformin used in combination with oral contraceptive containing ethinyl estradiol (EE) and cyproterone acetate (CA). STUDY DESIGN: This prospective, open clinical study lasted 6 months and included 30 women with PCOS, divided in two groups of 15 women each. Group 1 received 850 mg metformin twice a day and group 2 in which Diane35 was added to the same treatment only during the first 2 months of the investigation. Serum levels of testosterone, immune reactive insulin (IRI), sex hormone binding globulin (SHBG), dehydroepiandrosterone sulfate (DHEAS) and lipid metabolism parameters were measured before the treatment, on the third and sixth month. Free androgen index (FAI) and HOMA-IR were calculated. Body mass index (BMI) and waist-to-hip ratio (WHR) were assessed at baseline and at the end of therapy. RESULTS: Much better and faster decrease in the level of testosterone and free androgen index in group with combined use of metformin and Diane35 was established, without deterioration of the anthropometric and biochemical indices and insulin sensitivity. CONCLUSION: The combination of metformin with intermittent application of Diane35 is an appropriate alternative for the pathogenic influence and clinical improvement of the symptoms of androgen excess in cases with PCOS.

Adult↗
PubMed2004

Metastatic prostate cancer treated by flutamide versus cyproterone acetate. Final analysis of the "European Organization for Research and Treatment of Cancer" (EORTC) Protocol 30892.

OBJECTIVES: This trial was designed to compare the efficacy of Flutamide (FLU) versus Cyproterone acetate (CPA) in men with metastatic prostate cancer and favourable prognostic factors. The primary endpoint of the trial was overall survival, disease specific survival, time to progression and side effects were secondary endpoints. The results pertaining to sexual function were already reported [Br J Cancer 82(2) (2000) 283]. MATERIAL AND METHODS: The trial was designed to detect a 50% improvement in median overall survival with 80% power. At the time of the present report, the trial provides 88% power to detect the planned difference of 50% with a 2-sided Logrank test and 80% power to detect a difference of 43% in median survival. RESULTS: 310 patients were randomized to treatment by FLU (250 mg t.i.d. p.o.) or CPA (100 mg t.i.d. p.o.). Of the 310 patients, 12 (3.9%) were ineligible. The baseline characteristics of the two groups were similar except for age which was significantly younger in the CPA group and for the presence of soft tissue metastases which were absent in the FLU group and present in 6 patients in the CPA group. The median follow-up was 8.6 years, 245 patients died, 158 (64.5%) of prostate cancer. There was no significant difference between the treatment arms with respect to overall survival, specific survival nor time to progression. Side effect profiles were studied and found to be more favourable for CPA overall and in particular with respect to gynecomastia, diarrhea and nausea. CONCLUSIONS: The trial shows no significant differences in efficacy between Flutamide and CPA monotherapy. The number of patients who died of prostate cancer up to this time is insufficient for a definitive analysis of specific survival. Erectile function and sexual activity are not preserved with FLU but decay slowly with both antiandrogens, toxicity is more pronounced with FLU.

Aged↗
PubMed2004

Finasteride versus cyproterone acetate-estrogen regimens in the treatment of hirsutism.

OBJECTIVES: To compare the clinical and hormonal effects of finasteride and a combination regimen of cyproterone acetate (CPA) plus ethinyl estradiol (EE2) in the treatment of hirsutism. METHODS: Forty hirsute women were enrolled in a prospective randomized trial. Twenty-nine had polycystic ovary syndrome (PCOS) and 11 had idiopathic hirsutism. Patients were randomly treated with finasteride (5 mg/day; n=20) or CPA plus EE2 [CPA (25 mg/day on days 5-14) plus EE2 (20 microg/day on days 5-25) n=20] for 9 months. Main outcome measurement was a reduction in hair growth. Hirsutism score and hormone levels were measured at the beginning and at the end of the study. The student t-test and Mann-Whitney U tests were used for analysis of the data. RESULTS: The modified Ferriman-Gallwey scores for hirsutism decreased significantly at the end of the study from a mean+/-SD of 23.7+/-4.4 to 11.3+/-1.5; P=<0.001 in finasteride group and from 22.3+/-4.2 to 11.4+/-1.2; P=<0.001 in CPA plus EE2 group. Improvement of hirsutism induced by the two treatment methods was similar (47.6 % vs. 51.1%; P=0.2). Treatment with CPA plus EE2 significantly decreased serum total and free T, A, DHEAS, and DHT and increased SHBG levels. Finasteride significantly increased total T but reduced DHT levels. CONCLUSION: Finasteride and CPA plus EE2 are equally effective in decreasing hirsutism, despite significantly different effects on serum hormone levels.

Adolescent↗
PubMed2004

Development and validation of a high-performance liquid chromatographic method for the determination of cyproterone acetate in human skin.

In the framework of a preliminary study on the transdermal penetration of cyproterone acetate (CPA), a simple and rapid procedure involving an extraction step coupled to a HPLC-UV determination has been developed for the separation and quantification of CPA in the two main skin layers-epidermis and dermis-after local application. The separation of epidermis and dermis layers was carefully carried out by means of a sharp spatula after skin immersion in heated water at 65 degrees C. The two skin layers were then treated separately according to the same process: (1) sample homogenization by vibration after freezing with liquid nitrogen in a Mikro-Dismembrator; (2) CPA extraction with methanol after addition of the internal standard (betamethasone dipropionate); (3) centrifugation; (4) evaporation of a supernatant aliquot; (5) dissolution of the dry residue in methanol and addition of water; (6) centrifugation; (7) injection of a supernatant aliquot into the HPLC system. The separation was achieved on octadecylsilica stationary phase using a mobile phase consisting in a mixture of acetonitrile and water (40:60 (v/v)). The method was then validated using a new approach based on accuracy profiles over a CPA concentration range from 33 to 667 ng/ml for each skin layer. Finally, the method was successfully applied to the determination of CPA to several skin samples after topical application of different gel formulations containing CPA.

Chromatography, High Pressure Liquid↗