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PubMed1980

[Serum prolactin levels during therapy of prostatic cancer with oestradiol-17 beta-undecylate and cyproterone acetate (author's transl)].

Sixteen patients aged from 50 to 79 years with inoperable prostatic cancer were allocated at random to treatment either with 300 mg cyproterone acetate at weekly intervals or with 100 mg oestradiol-17 beta-undecylate every month. Blood samples were taken before treatment and at monthly intervals during the 6-month period of treatment. Serum prolactin levels were determined by a double-antibody radioimmunoassay. Basal serum levels of prolactin were 7.76 +/- 4.84 ng/ml and 9.50 +/- 4.32 ng/ml in the two groups of patients before therapy with oestradiol-17 beta-undecylate or cyproterone acetate, respectively. These pretreatment serum prolactin levels were statistically indistinguishable. Serum prolactin levels did not rise significantly during the first 5 months of treatment with cyproterone acetate, although an increase in prolactin was found in the sixth months of therapy with the antiandrogen. On the other hand, oestradiol-17 beta-undecylate raised serum prolactin levels significantly already after one month of treatment and the mean values were significantly higher than in the antiandrogen-treated group. These data combine to suggest cyproterone acetate as a suitable alternative to oestrogens in the therapy of inoperable prostatic cancer.

Aged↗
PubMed1994

[Long-term therapy of central precocious puberty in girls with the gonadoliberin analog D-Trp-6-LHRH after prior therapy with cyproterone acetate].

A group of five girls with central precocious puberty (CPP) (four girls with idiopathic CPP and one girl with organically conditioned CPP) were treated for a mean period of 17 months (12-20 months) with an agonist of gonadoliberine (aGnRH) D-Trp-6-LHRH(Triptorelin), 60-100 micrograms/kg by the i.m. route, every four weeks. The calendar age (CA) of the girls was at the onset of aGnRH treatment 7.3 +/- 0.7 years, the bone age (BA) 9.6 +/- 1.0 years. Previously Cyproterone acetate treatment administered for an average period of 26 months (4-56 months) was gradually discontinued in the course of 12 weeks. After 12 months aGnRH treatment the growth rate slowed down from 8.1 #/- 2.1 to 6.2 +/- 1.7 cm/year (NS). The bone age increment per calendar year declined at the end of the first year of treatment from 1.7 +/- 0.8 to 0.94 +/- 0.4 (NS). Prediction of the adult height did not change in the course of one year (before aGnRH therapy 158.6 +/- 5.3 after one year's treatment 159.0 +/- 5.3 cm). In all girls premature maturing was arrested already during the original Cyproterone acetate treatment. With the exception of a single patient during aGnRH therapy progression was not recorded. In this girl with the idiopathic form of CPP the authors observed during regular Triptorelin administration, starting from the fourth month, clinical and biochemical manifestations of secondary therapeutic failure after termination of hitherto administered Cyproterone acetate treatment-"escape from treatment". Clinical and hormonal indicators improved after addition of Cyproterone acetate. This patient lacks typical symptoms suggesting McCune-Albright's syndrome.

Child↗
PubMed1991

Cyproterone acetate for severe hirsutism: results of a double-blind dose-ranging study.

OBJECTIVE: The objective was to determine if cyproterone acetate (CPA) therapy for hirsute women demonstrated a dose response. DESIGN: A double-blind dose-ranging study of the effect of 3 doses of cyproterone acetate for a period of 12 months. PATIENTS: Twenty-one hirsute women received the Dianette contraceptive pill (35 micrograms ethinyl oestradiol + 2 mg CPA, Schering Healthcare, UK), 20 received Dianette plus 20 mg CPA and 19 received Dianette plus 100 mg CPA: supplementary CPA was administered on days 1-10 of the birth control pill cycle as described by Hammerstein. MEASUREMENTS: Hair growth was measured using the clinical scale of Ferriman and Gallwey and by direct measurement of hair shaft diameter and linear growth of hair on the face, forearm, abdomen and thigh. RESULTS: Thirty-eight women completed 12 months therapy, eight withdrew due to side-effects and 14 were lost to follow-up. All three dose schedules produced significant reductions in clinical hair growth scores. This reduction was seen after 6 months with Dianette alone (P less than 0.005) and after 3 months with both the higher doses (P less than 0.01). There were no significant differences between the effect of different doses at any of the three-monthly time points. Hair diameter measurements were reduced by all doses after 12 months: face by 27*, 37, 37%*, forearm 5, 10, 8%*, abdomen 22*, 39*, 33%*, thigh 12, 24*, 30%* (median reductions (*P less than 0.01) for Dianette, D + 20 mg CPA and D + 100 mg CPA respectively). There were no significant reductions in daily linear growth rates. A comparison of the percentage reduction in hair shaft diameter at each site demonstrated no significant difference between doses, although the reductions by the three doses on the forearm, abdomen and thigh suggested a trend towards a dose response. CONCLUSIONS: We conclude that cyproterone acetate 2 mg daily appears to be as effective as higher doses in the therapy of hirsute women.

Adolescent↗
PubMed1971

Testosterone action in the rat ventral prostate. The effects of diethylstilboestrol and cyproterone acetate on the metabolism of ( 3 H)testosterone and the retention of labelled metabolites by rat ventral prostate in vivo and in vitro.

Recent reports have indicated that the prior metabolism of testosterone by the secondary sexual tissues may be necessary for its androgenic effect. The effects of two anti-androgens, diethylstilboestrol and cyproterone acetate (17alpha-acetoxy-6-chloro-1,2alpha-methylenepregna-4,6-diene-3,20-dione) used in the chemotherapy of human prostatic carcinoma, have been examined on both the metabolism of testosterone and the retention of its metabolites by the rat ventral prostate gland. Cyproterone acetate was found to inhibit the retention of labelled metabolites of [(3)H]-testosterone by prostatic nuclei, both in vivo and in vitro. This inhibition appeared to be competitive. In contrast with its effect on nuclear retention of metabolites of testosterone, cyproterone acetate had no significant effect on the metabolism of [(3)H]testosterone by rat ventral prostate tissue. Diethylstilboestrol similarly had little effect on the metabolism of [(3)H]testosterone by prostatic tissue, although it did appear partially to inhibit its initial metabolism in all the incubation systems used. Diethylstilboestrol inhibited the nuclear retention of dihydrotestosterone when both [(3)H]testosterone and diethylstilboestrol were injected intraperitoneally in vivo, but had no effect on dihydrotestosterone retention when both testosterone and diethylstilboestrol were supplied directly to the prostate either in vivo or in vitro. It was concluded that if diethylstilboestrol has an anti-androgenic effect at the level of the target organ as distinct from its effect on androgen production by the testes, then it is probably due to a mechanism differing from that of cyproterone acetate.

Androgen Antagonists↗
PubMed1981

In vivo studies on the antiandrogenic effects of cimetidine versus cyproterone acetate in rats.

To investigate the antiandrogenic action of cimetidine in vivo, prostatic androgen uptake and metabolism, spermatogenesis, morphology of the prostate and testes, and plasma hormone levels were studied using Sprague-Dawley rats, and the results were compared with the effects of cyproterone acetate or castration. Cimetidine and cyproterone acetate caused significant reduction in the weights of the ventral prostate and testes. The changes of ventral prostate were accompanied by a dose-related epithelial atrophy. No adverse effect on spermatogenesis was observed after treatment with cimetidine at daily doses of 50 mg/kg or cyproterone acetate of 10 mg/kg. Although cimetidine treatment induced a significant decrease in plasma testosterone levels, the uptake of testosterone-3H and its conversion to DHT of the ventral prostate were not inhibited by cimetidine.

Androgen Antagonists↗
PubMed1981

The effects of orchiectomy, oestrogens and cyproterone-acetate on the antithrombin-III concentration in carcinoma of the prostate.

The incidence of thromboembolic complications is increased in patients with oestrogen-treated prostatic carcinoma. Because reduced antithrombin-III (AT-III) levels are associated with increased risk of thromboembolism we have determined AT-III concentrations during oestrogen therapy and other treatments. Forty-six patients with carcinoma of the prostate were allocated to either treatment with subcapsular orchiectomy, oestrogen administration, or cyproterone acetate, AT-III was determined before treatment, at 2 weeks and 2 months later. During oestrogen therapy there was a significant reduction in AT-III to 77% of the base-line value. No significant changes were found after orchiectomy. During cyproterone-acetate treatment there was a slight but significant increase in AT-III at 2 months. The reduction in AT-III could indicate an increased risk of thromboembolism during oestrogen treatment of patients with carcinoma of the prostate. On the other hand, the unchanged AT-III levels after orchiectomy and the increased levels during cyproterone acetate therapy could mean that the risk of thromboembolism is less with these two forms of treatment.

Aged↗
PubMed1987

The effect of cyproterone acetate on the growth of children with central precocious puberty.

We have examined the growth and skeletal maturation of 19 children (6 male, 13 female) with central precocious puberty. The aetiology in nine patients (5 male, 4 female) was secondary to a hypothalamic hamartoma. Six children (2 male, 4 female) received no treatment whereas 13 children (4 male, 9 female) were treated with cyproterone acetate in a mean dose of 68 mg/m2 per day (range, 34-260) for a mean duration of 4.5 years (range, 0.8-7.9). There was no significant difference between height SDS for bone age at the beginning and end of observation in either treated or untreated groups. No significant relationship between the mean dose of cyproterone acetate used and change in height SDS for bone age could be determined. We conclude that cyproterone acetate has no beneficial effect on the growth prognosis of children with central precocious puberty.

Body Height↗
PubMed1977

The LH and FSH responses to LH-releasing hormone (LH-RH) in girls with true precocious puberty treated with cyproterone acetate.

Ten girls with precocious puberty ranging in age from 7 to 10 7/12 years who were treated with oral cyproterone acetate on a long term basis, were subjected to LH-RH tests, prior to and 3 to 16 months after the institution of therapy. Cyproterone acetate was given in doses from 60 to 153 mg/m2, which proved to be clinically effective, as evidenced by the slowing down of sexual maturation. The basal levels of LH were found to be unaffected by therapy and corresponded to the pubertal stages of the individual girls. The peak increment of LH after LH-RH stimulation was markedly suppressed by the therapy. FSH secretion and its responsiveness to LH-RH was not affected by cyprotereone acetate. The basal levels of FSH were higher during therapy than before, but the peak FSH increment remained the same. An escape phenomenon in the LH peak response was evident in 2 patients upon retesting after prolonged therapy. It is possible that the antigonadotrophic action of cyproterone acetate is due to its progestational nature.

Child↗
PubMed1992

Effects of orchiectomy, alone or in combination with testosterone, and cyproterone acetate on exocrine pancreatic carcinogenesis in rats and hamsters.

The results of a previous 4-mo study in azaserine-treated rats and BOP-treated hamsters indicated that orchiectomy inhibited pancreatic growth and development of putative preneoplastic lesions in the exocrine pancreas of rats but not hamsters. This 12-mo study was carried out to investigate the effects of orchiectomy, alone and in combination with testosterone, and of treatment with cyproterone acetate on pancreatic carcinogenesis in azaserine-treated rats and BOP-treated hamsters. Treatment started 4 mo after injection of the carcinogen. In orchiectomized rats, pancreatic wt was lower than in controls, whereas pancreatic wt of orchiectomized rats treated with testosterone was similar to that of controls. Both orchiectomy and cyproterone acetate caused a decrease in body wt gain and had an inhibitory effect on pancreatic carcinogenesis. Testosterone treatment did not influence the inhibitory effects of orchiectomy on body wt gain and on pancreatic carcinogenesis. In hamsters, neither orchiectomy, alone or in combination with testosterone, nor cyproterone acetate (CA) affected pancreatic growth or pancreatic carcinogenesis. This study indicates that testosterone plays a minor role in the development of pancreatic tumors induced in rats by azaserine but not in that of pancreatic tumors induced in hamsters by BOP.

Animals↗
PubMed1988

Effects of cyproterone acetate, LHRH agonist and ovarian surgery in McCune-Albright syndrome with precocious puberty and galactorrhea.

We have studied the endocrinological pattern in a girl with McCune-Albright syndrome. The young patient showed: normal prepubertal serum levels of gonadotropins, fluctuating estrogen concentrations, which sometimes were similar to the levels in adult women of fertile age, hyperprolactinemia with galactorrhea, ovarian cysts. The effects of treatment with antiandrogen drug, cyproterone acetate, and of a LHRH agonist, buserelin (less than D-Ser[TBU(8)6-des-gly NH2.10 greater than LHRH ethylamide), were studied. Cyproterone acetate with or without buserelin did not fully suppress estradiol concentrations. On the other hand, surgical resection of these cysts resulted in both clinical and endocrinological remission. It is likely that in this case of McCune-Albright syndrome precocious puberty was a result of ovarian estrogen secretion, while pubertal activation of the hypothalamus-pituitary axis was absent. Hyperprolactinemia, which appeared after the beginning of the combined therapy with buserelin and cyproterone acetate, was probably due to the elevated estrogen levels.

Buserelin↗
PubMed1985

3H-cyproterone acetate: binding characteristics to human uterine progestagen receptors.

The availability of tritium labeled cyproterone acetate (CPA) facilitated the systematic investigation of the binding characteristics of this compound for human uterine progesterone receptors (PgR). The binding parameters of 3H-CPA are compared to those of 3H-R5020 and 3H-progesterone. The rate constants of association (k1M-1sec-1) to PgR were 7.8 X 10(3) for 3H-R5020, 4.5 X 10(4) for 3H-progesterone and 4.0 X 10(4) for 3H-CPA. The rate constants of dissociation (k-1, sec-1) were 3.6 X 10(-5) for 3H-R5020, 21.3 X 10(-5) for 3H-progesterone and 17.8 X 10(-5) for 3H-CPA. The Kd-values (M), as obtained by titration analysis and subsequent Scatchard plot analysis were 1.2 X 10(-9) for 3H-R5020, 6.0 X 10(-9) for 3H-progesterone and 5.2 X 10(-9) for 3H-CPA. On sucrose density gradient analysis binding in the 3.5, 5 and 8 S area could be observed using 3H-R5020. For 3H-progesterone and 3H-CPA binding was exclusively found in the 5 S area. The specificity of the steroid binding site of PgR is identical for 3H-R5020 and 3H-CPA. The order of potency of binding for various competitors decreases identically for both radioactive ligands: R5020 less than progesterone less than R1881 less than CPA less than dihydrotestosterone less than dexamethasone less than cyproterone less than 15 beta-OH-cyproterone. CPA resembles progesterone very closely in its binding characteristics to human uterine PgR.

Binding, Competitive↗
PubMed1990

Inhibition of spermatozoa maturation in rhesus monkey by cyproterone acetate.

The morphology of spermatozoa from the initial segment, caput, corpus and cauda epididymides of normal and cyproterone acetate-treated animals was studied using light and scanning electron microscopy to understand the changes taking place during spermatozoa maturation. A progressive and significant decrease in the percentage of spermatozoa that retained the cytoplasmic droplet and a shift in its position from proximal end of the midpiece to its distal end were seen during epididymal transit; these events were inhibited in cyproterone acetate-treated animals. A large percentage of spermatozoa from the initial segment and the caput epididymides showed coiling of the spermatozoa tail which involved the midpiece, principal piece and the endpiece. The percentage of spermatozoa that showed the coiled tail decreased; a gradual straightening of the spermatozoa tail with less complex types of coiling was also seen during epididymal transit. Cyproterone acetate reversed these changes occurring during maturation. These results indicate that spermatozoa maturation in the rhesus monkey, occurring between the corpus and cauda epididymides, is an androgen-dependent event.

Androgens↗
PubMed1990

Anti-masculinizing action of estradiol and cyproterone acetate: regulation of a protein fraction with phospholipase-A2 stimulatory and masculinizing activities.

Recently we have identified a protein fraction (55-63 K) from male and testosterone-exposed female mouse genital tract, which stimulates phospholipase A2 (PLA2) and induces masculine differentiation in an undifferentiated mouse genital explant, suggesting a role of this protein in the action of testosterone. In the current study we have further investigated the role of this protein by determining whether anti-masculinizing agents, namely, estradiol and cyproterone acetate, have any effect on the production of this protein. The results described here indicate that a protein fraction containing PLA2 stimulatory activity was present in both control male and estradiol- or cyproterone acetate-exposed male fetal genital tract. However the specific activity of the PLA2-stimulatory protein was significantly higher in the control males than in the experimental males. We did not find any major difference in the behavior of this protein fraction in various chromatographic steps except that in CM-sepharose column; the PLA2-stimulatory activity from the male preparation was eluted in two overlapping peaks with 0.3 and 0.25 M NaCl and that from the treated males was eluted only with 0.25 M NaCl. The SDS-gel analysis of this protein fraction revealed a doublet band (55 and 63 K) in control samples and primarily a 63 K band in experimental samples. The protein fraction from all these sources showed a significant difference in their biological activity. The control male preparation induced Wolffian duct whereas the estradiol sample was completely ineffective and the cyproterone acetate sample was partially effective in inducing Wolffian duct. Thus, it appears that the protein fraction has a role in the masculinizing action of testosterone.

Animals↗
PubMed1988

The combination of cyproterone acetate and low dose diethylstilbestrol in the treatment of advanced prostatic carcinoma.

Cyproterone acetate is a steroidal antiandrogen with weak progestational activity that results in the partial suppression of pituitary gonadotropin. We demonstrate that the associated decrease in serum testosterone is more complete and prolonged if cyproterone acetate (200 mg. daily) is combined with a low dose of diethylstilbestrol (0.1 mg. daily). The effectiveness of the combination in the treatment of prostatic carcinoma was investigated in 51 patients with stage D2 malignancy. From an initial concentration of 360 +/- 23 ng. per dl. (mean +/- standard error), serum testosterone decreased to 56 +/- 5 ng. per dl. after 1 week and reached a plateau of approximately 30 ng. per dl. after 2 months. This was accompanied by a decrease in serum prostatic acid phosphatase from a mean starting concentration of 43 +/- 11 ng. per ml. to a low of 3 +/- 1 ng. per ml. at 12 months; the proportion of normal values increased from 10 to 80 per cent. A complete response was observed in 7 patients (13 per cent), partial response in 35 (69 per cent) and stable disease in 8 (16 per cent), yielding an over-all objective response rate of 98 per cent (1980 National Prostatic Cancer Project criteria). The actuarial median time to progression was 17 months and the median survival time was 23.5 months. In 26 patients who subsequently had signs of progressive carcinoma the relapse rate in bone (85 per cent) far exceeded that in nonskeletal sites (23 per cent). The incidence of cardiovascular toxicity was 12 per cent. These results indicate that cyproterone acetate and low dose diethylstilbestrol may be co-administered to achieve a synergistic and potent androgen withdrawal effect in the treatment of advanced prostatic carcinoma.

Acid Phosphatase↗
PubMed1983

Cyproterone acetate in treatment of post-orchidectomy hot flushes. Double-blind cross-over trial.

12 patients with troublesome hot flushes after orchidectomy (as a primary treatment for prostatic carcinoma) were treated with cyproterone acetate or placebo in a double-blind cross-over trial. The frequency of hot flushes was significantly reduced during the three weeks that cyproterone acetate (100 mg three times a day) was given. 5 patients complained of lassitude while on cyproterone acetate, but in none was it necessary to discontinue treatment.

Aged↗
PubMed1988

Suitability of cyproterone acetate in the treatment of osteoporosis associated with athletic amenorrhea.

The effectiveness of the antiandrogenic agent cyproterone acetate (CA) in its contraceptive form (2 mg CA + 50 micrograms ethinyl estradiol) in the treatment of osteoporosis associated with athletic amenorrhea was studied in seven high-performance athletes. Four women with similar characteristics served as controls. Their mean age was 21.9 years +/- 3.9. Training was started at a mean age of 14.0 years +/- 2.0. The mean training intensity expressed as kilometers run per week was 35 +/- 15. Mineral density was primarily affected by the hypoestrogenic status of these athletes (= 22 pg/ml +/- 8.8 in the midluteal phase). All participants showed low serum progesterone (= 2.85 ng/ml +/- 2.10) and LH profiles (= 5.6 mlU/ml +/- 0.8) during the midluteal phase. Cyproterone acetate was administered for 8 months to treat the increased bone loss in seven women athletes. Vertebral density appeared to be increased with 9.5% +/- 2.45% (mean +/- SD) while cortical base mineral content measured at the radius was not significantly changed. Our results demonstrate that cyproterone acetate administered in combination with estrogens provides a suitable therapeutic agent in the management of osteoporosis due to a hypoestrogenic status. This treatment could substitute other contraceptive agents. Moreover, women with the most severe estrogen deficiency showed a more pronounced reaction to this therapy.

Adolescent↗
PubMed1990

Reduced serum vitamin B12 levels during oral cyproterone-acetate and ethinyl-oestradiol therapy in women with diffuse androgen-dependent alopecia.

In a group of healthy, non-vegetarian females currently being treated for diffuse androgen-dependent alopecia with 50 or 100 mg of oral cyproterone acetate for 11 days and 30 or 40 micrograms of ethinyl oestradiol for 20 days of the menstrual cycle, significant decreases in mean serum vitamin B12 (P less than 0.0001), haemoglobin (P less than 0.003) and haematocrit (P less than 0.004) values, were observed after 6 months. Serum folic acid, red-cell folate and mean cell volume remained unchanged within the normal range during this time. All patients responded to oral cyanocobalamin, or intramuscular injections of hydroxocobalamin. In patients with baseline serum vitamin B12 levels below 350 ng/l, we would suggest prophylactic cyanocobalamin concurrent with cyproterone-acetate-ethinyl-oestradiol (CPA EE2) therapy. Studies involving other dose regimens of CPA EE2 (Dianette) or cyproterone acetate alone (Androcur, Cyprostat), may require evaluation of the vitamin B12 status if treatment is to be given for periods of longer than 3 months.

Administration, Oral↗
PubMed1983

Indirect evidence that the action of cyproterone acetate on the skin is due to a metabolite.

Cyproterone acetate, applied as 1% solution in ethanol or isopropyl myristate, did not decrease the sebum excretion rate (SER) when applied to forehead skin of patients with acne, although SER is decreased when the drug is given systemically. The probable explanation is that cyproterone acetate owes its local action to a metabolite formed systemically. The present study shows this is unlikely to be the 17 beta-hydroxy cyproterone acetate.

Acne Vulgaris↗