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PubMed1981

Effects of estrogen, orchidectomy, and cyproterone acetate on tissue fibrinolysis in patients with carcinoma of the prostate.

Twenty-six patients with carcinoma of the prostate were allocated to treatment by subcapsular orchidectomy, estrogen administration, or cyproterone acetate administration. Tissue fibrinolytic activity in skin biopsy specimens was estimated by a histochemical method before treatment was initiated and 2 and 8 weeks later. Orchidectomy caused no significant changes in the fibrinolytic activity. During estrogen therapy the fibrinolytic activity in skin was significantly reduced at 8 weeks. In the group given cyproterone acetate the activity was significantly increased at 8 weeks. In the group given cyproterone acetate the activity was significantly increased at 8 weeks. The reduction in fibrinolytic activity in skin could contribute to the increased risk of thromboembolism during estrogen treatment of patients with cancer of the prostate.

Aged↗
PubMed1994

[Acceptability, tolerance and quality of life impact of cyproterone acetate treatment in female hirsutism. Comparison of 2 protocols in combination with oral or transdermal estradiol].

67 women (aged 16-40) with hirsutism and/or other signs of hyperandrogenism (acne, androgenic alopecia, cycle disturbances) have been treated for one year with cyproterone acetate + estradiol. Patients have been randomly assigned to therapy with cyproterone acetate and estradiol valerate per or cyproterone acetate and transdermal estradiol. Acceptance, tolerance and effects on quality of life of this treatment have been assessed using a self questionnaire completed with questions for assessment for compliance. Among patients who have had a full course of treatment, 54 have fulfilled the end-of-study quality of life questionnaire. The queries allow calculation of a relational well-being score and of an emotional well-being score. The answers to the initial questionnaire show in a high percentage of patients emotional trouble (depressive state, anxiety, irritability) and disturbances in relational life. The hirsutism score has been found to be significantly correlated with anxious trouble but not with the global quality of life score. The treatment has resulted in a significant improvement in acceptance of being exposed to view (p < 0.01), self-assurance (p < 0.01) as well as emotional well-being score (p < 0.05), without any significant difference between the 2 therapeutics groups. Measurement of treatment acceptance with a visual analogic scale has been found globally very satisfactory by patients from the 2 groups. Compliance of treatment with transdermal estradiol turned out to be lesser in younger patients but is better in patients in whom emotional balance has been improved by therapy.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Cutaneous↗
PubMed1996

Treatment of endometriosis with cyproterone acetate. Preliminary report.

The objective of this work was to evaluate the effectiveness of cyproterone acetate for the treatment of endometriosis. Seven patients with dysmenorrhea due to endometriosis and idiopathic hirsutism were included. Endometriosis was laparoscopically classified as minimal in two cases, mild in two, moderate in two and severe in one patient. Cyproterone acetate was initiated at a daily dose of 10 mg orally for 20 days, followed by 10 days without medication. This sequence was repeated over a period of 6 months. Dysmenorrhea improved in all study subjects. Menstrual disorders were observed in all women, with oligomenorrhea in six patients and spotting in one. At the end of treatment, a second look laparascopy revealed minimal endometriosis in five patients and no evidence of the disease in the other two cases. Hirsutism was slightly reduced in two patients and without changes in the other five. These preliminary data disclose the possible therapeutic use of cyproterone acetate in endometriosis.

Administration, Oral↗
PubMedDate not supplied

[The effects of cyproterone acetate on plasma testosterone in the hirsute woman].

It seems that the principal antiandrogenic action of cyproterone acetate is on the site of the androgenic receptors. Since recent work proves that there is an action on plasma testosterone, we wanted to check in women with raised testosterone levels if cyproterone lowered these levels. The answer is : Yes. Observations seem to confirm that cyproterone acetate causes a significant lowering of plasma testosterone. The basic level of testosterone and the drop in blood levels of testosterone after the antiandrogenic action has occurring do not seem to be significantly different whether the virilism is caused by an adrenal mechanism or by an ovarian mechanism.

Adolescent↗
PubMed1998

Blockade of the in vitro effects of testosterone and erythropoietin on Cfu-E and Bfu-E proliferation by pretreatment of the donor rats with cyproterone and flutamide.

Erythropoietin is obligatory to support the terminal proliferation and differentiation of erythroid cells but it is not the only agent in modulating red cell production. Previously, we have shown that Testosterone enhances erythropoiesis, at least in part, by increasing renal erythropoietin production. Testosterone may also influence directly the behavior of the erythroid progenitor cells increasing erythroid stem cell proliferation. To gain further insight into the role of testosterone in regulation of erythropoiesis and its interactions with erythropoietin, we studied the effect of testosterone and erythropoietin, using clonal cultures of erythropietic progenitors, to observe CFU-E and late and early BFU-E colonies proliferation from bone marrow cells of donor rats pretreated for 2 days with the androgen antagonists cyproterone (10 mg/kg/day) and flutamide (160 mg/kg/day). Specific nuclear receptors for testosterone were demonstrated in marrow erythroid cells. Then, erythroid progenitors may come with their androgen receptors blocked by pretreatment. Cultures were prepared using the methylcellulose technique containing a standard dose of erythropoietin (250 mU/ml) or testosterone (10(-7)M). Results obtained demonstrate that testosterone produced a significant stimulation on CFU-E and BFU-E colony formation. A dose effect correlation was apparent. Testosterone enhances proliferation of late BFU-E more than CFU-E and produce only a slight augmentation of early BFU-E. As expected, erythropoietin markedly stimulate all erythroid colony growth, mainly CFU-E. The effects of testosterone were completely abolished in cultures from bone marrow cells of rats pretreated with cyproterone and flutamide. Activation of the specific androgen nuclear receptors in erythroid cells appears to be necessary for testosterone to develop the erythropoietic effect. Surprisingly, the effects of erythropoietin on erythroid colonies proliferation were also completely blocked by pretreatment with flutamide and partially blocked by pretreatment with cyproterone. Right now, we do not have a satisfactory explanation regarding inhibition of the effects of erythropoietin by pretreatment to marrow donor rats with the androgen antagonists. In conclusion, we postulate triggering late BFU-E cells, a marrow erythropoietin responsive cell population, into active cell cycle, as well as by increasing blood erythropoietin concentration.

Androgen Antagonists↗
PubMed1999

Long-term sequential treatment with combined estradiol valerate and cyproterone acetate in early postmenopause.

BACKGROUND: We sought to evaluate the long-term safety and efficacy of cyclic combined estradiol valerate and cyproterone acetate. METHODS: A six-year, single center, open study was performed of forty-eight recently postmenopausal women. We evaluated biochemical markers of bone turnover, bone mineral content, bone mineral density, serum lipids, climacteric symptoms, and bleeding throughout the six-year period. Ultrasound evaluation of the endometrium was performed yearly for the first two years. RESULTS: Markers of bone turnover were decreased over the study period, while bone mineral content and density remained unchanged. High density lipoprotein cholesterol levels were increased with unchanged blood pressure over the six years. Menopausal symptoms showed significant improvements within 6 months. Endometrial scan results never required hysteroscopic evaluation. CONCLUSION: Sequentially combined estradiol valerate and cyproterone acetate can be used for an indefinite number of years in women with recent natural menopause. Cyproterone acetate provides adequate endometrial protection and cycle control while allowing estradiol valerate to exert its positive effects on lipid profile, bone metabolism, and climacteric symptoms.

Cyproterone Acetate↗
PubMed1977

Effect of short-term cyclic administration of cyproterone acetate on pituitary-ovarian function in the human.

Short courses of cyproterone acetate, a compound with progestational and antiandrogenic activities, were administered to normally menstruating women during different phases of the menstrual cycle to suppress growth and maturation of the follicles and corpus luteum function. Postovulatory administration of 20 mg of the drug daily for 8 days to two women delayed menstruation by 4 to 6 days, followed by prolonged bleeding and short post-treatment cycles. Plasma levels of progesterone were suppressed temporarily during therapy, but increased immediately after cessation of treatment. Administration of 10 mg of the drug for 8 days during the early follicular phase to two women resulted in irregular bleeding, short cycles, and decreased plasma levels of progesterone throughout the cycle. Reduction of the dose to 2.5 mg during the early follicular phase in two other women also resulted in irregular cycles. When the 2.5-mg dose was administered to three women from the 8th to the 15th days of the cycle, vaginal bleeding and cycle length were normal. Plasma levels of luteinizing hormone and progesterone were suppressed during therapy. In one subject, cervical mucus was found to be hostile to sperm penetration in all three treatment cycles. The results indicate that, with cyclic administration of low doses of cyproterone acetate to women during the late follicular phase, it may be possible to interrupt pituitary-ovarian function, as well as sperm transport through the cervical mucus.

Body Temperature↗
PubMed1977

The influence of combined cyproterone acetate-ethinyl oestradiol therapy on serum levels of dehydroepiandrosterone, androstenedione, and testosterone in hirsute women.

Serum levels of dehydroepiandrosterone, androstenedione, and testosterone in hirsute women suffering from either idiopathic hirsutism or the polycystic ovary syndrome were determined before and during treatment with cyproterone acetate combined with ethinyl oestradiol. During this treatment the hirsutism decreased markedly. In untreated hirsute women serum dehydroepiandrosterone levels do not differ from those in normal women and do not change during therapy; androstenedione levels are higher than normal and decrease markedly during treatment, and the testosterone levels are elevated compared to normals, with a considerable overlap, and show only a tendency to decrease. There is no correlation between dehydroepiandrosterone and androstenedione levels or between androstenedione and testosterone levels in the serum of untreated hirsute women. After 12-14 months of cyproterone acetate-ethinyl oestradiol therapy a linear correlation is found between dehydroepiandrosterone and androstenedione levels. This can be explained by the relatively higher contribution of the peripheral conversion of dehydroepiandrosterone to androstenedione to the occurrence of lower androstenedione levels. The linear correlation between androstenedione and testosterone after treatment, also found in normal women, indicates the restoration of the role of androstenedione as the major peripheral precursor of testosterone.

Adolescent↗
PubMed1969

Androgen accumulation andbinding to macromolecules in seminal vesicles: inhibition cyproterone.

Cyproterone reduces the accumulation of testosterone and dihydrotestosterone in seminal vesicles 30 minutes after intravenous administration of tritiated testosterone to castrated rats. Testosterone, added in vitro, binds to macromolecules from the supernatant fraction of the seminal vesicle homogenates; this interaction is antagonized competitively by cyproterone. Cyproterone may diminish androgenic effects by competition for binding molecules.

Animals↗
PubMed1982

Cyproterone acetate in advanced male breast cancer.

Three male patients of 55, 63 and 71 years of age, with metastatic breast cancer, were treated with cyproterone acetate. Two patients showed complete remission, one lasting 21 months, another 51+ months and a third achieved partial remission lasting 9 months. These results suggest that cyproterone acetate may be useful in the treatment of advanced male breast cancer.

Aged↗
PubMed1992

The position of cyproterone acetate (CPA), a steroidal anti-androgen, in the treatment of prostate cancer.

Cyproterone acetate is a steroidal anti-androgen that blocks the androgen-receptor interaction and reduces serum testosterone through its weak anti-gonadotropic action. It can be regarded as the only anti-hormone that causes complete androgen blockade as monotherapy. Many animal experiments and several clinical phase II and phase III trials have demonstrated that it deserves a place in the endocrine therapy of advanced prostate cancer, particularly for those patients who find orchidectomy unacceptable and who do not have known cardiovascular risks. Additionally, cyproterone acetate can be used safely to prevent disease flare when a luteinizing hormone releasing hormone analog is the drug of choice and to suppress hot flashes in response to LHRH agonists or after orchidectomy.

Androgen Antagonists↗
PubMed1985

On the site of action of the anti-adrenal steroidogenic effect of cyproterone acetate.

Cyproterone acetate (CA) inhibited 1-24 ACTH (50 ng/l)-stimulated cortisol production by dispersed guinea-pig adrenal cells in a dose-related manner. Inhibition occurred over the range 10(-6) to 5 X 10(-5) moles/l. The concentration of drug which induced 50% inhibition was 4.6 X 10(-6) moles/l. The sites of action of this anti-steroidogenic effect have been established. Dispersed adrenal cells were challenged with the cortisol precursor steroids (all at 10(-5) moles/l) pregnenolone (Pe), 17 alpha hydroxypregnenolone (17-OH Pe), 17 alpha-hydroxyprogesterone (17-Po), and 11 deoxycortisol or 1-24 ACTH (100 ng/1) in the absence and presence of increasing concentrations of CA (10(-5) to 10(-4) moles/l). In the absence of drug, the steroid precursors or ACTH provoked cortisol secretion greater than 10-fold that secreted by cells incubated in their absence. ACTH-stimulated cortisol secretion was inhibited greater than 68% at concentrations of CA greater than 10(-5) moles/l. CA (10(-5) moles/l) had no significant effect on steroid-stimulated cortisol production when the delta 4, 3 ketosteroids 17-OH Po and 11-deoxycortisol were used, but depressed secretion by greater than 61% (P less than 0.001) when the delta 5 3 beta hydroxysteroids (Pe, 17-OH Pe) were employed. Increasing CA concentrations to 10(-4) moles/l had little effect on cortisol secretion provoked by 11-deoxycortisol, but significantly (P less than 0.05) depressed cortisol secretion stimulated by 17-OH Po. These results suggest that the major site of action of CA is delta 5, 3 beta hydroxysteroid dehydrogenase (3 beta-HSD) with a secondary effect on 21-hydroxylase activity. To confirm these findings cortisol secretion provoked by 17, 21, dihydroxypregnenolone (17, 21 diOH Pe) and 21 deoxycortisol (21-DOC) was measured in the absence and presence of increasing concentrations of CA. At the lowest concentration of CA (5 X 10(-6) moles/l), cortisol secretion provoked by 17, 21 diOH Pe was inhibited by 28% (P less than 0.01) whereas secretion provoked by 21-DOC was not significantly affected. At the highest concentration of CA (10(-4) moles/l), the relative inhibition was 80% for 17, 21 diOH Pe and 38% for 21-DOC. We conclude that cyproterone acetate inhibits adrenal steroidogenesis at both 3 beta-HSD and 21-hydroxylase, the degree of inhibition being more pronounced at 3 beta-HSD.

3-Hydroxysteroid Dehydrogenases↗
PubMed1988

Effects of cyproterone acetate plus ethinylestradiol low dose on plasma androgens and lipids in mildly hirsute or acneic young women.

The purpose of this study was to compare, by a randomized double-blind study, involving 30 women with either acne or mild hirsutism, the effects on plasma androgens and lipoproteins, of two hormonal preparations used in acne and ensuring reliable contraception, namely DianeR (cyproterone acetate 2 mg and ethinylestradiol 50 micrograms per pill - D-50) and Diane 35 (cyproterone acetate 2 mg and ethinylestradiol 35 micrograms per pill - D-35). Both drugs, used over a 6-month period (treatment cycle of 21 days with a pill-free interval of 7 days), induced an impressive decrease of free testosterone levels and of 5 alpha-androstane-3 alpha, 17 beta-diol-glucuronide, a parameter of peripheral androgen formation; also dehydroepiandrosterone sulfate levels decreased significantly. Except for an increase of both total T and dihydrotestosterone and as well as for a more important increase in SHBG levels during treatment with D-50, consequences of its more pronounced estrogen dominance in comparison to D-35, the effects of both drugs on androgen levels were similar. The effects on lipids were characterized by a non-significant increase of total cholesterol and a significant increase of HDL-C, HDL2-C and Apo-Al lipoproteins, which were somewhat more pronounced during D-50 treatment. Triglycerides increased significantly during D-50 but hardly during D-35 treatment, whereas HDL-C/LDL-C increased similarly during treatment with either drug. It is concluded that, being as efficient as D-50 in treatment of acne and hirsutism and taking into account its reliable contraceptive effects, without unfavourable effects, as far as atherogenesis is concerned, on plasma lipids, D-35 is to be preferred over D-50.

Acne Vulgaris↗
PubMed1991

Endometrial patterns during danazol and cyproterone acetate treatment for endometriosis: structural and ultrastructural study.

We studied the endometrial structure and ultrastructure in serial biopsies from 16 patients with endometriosis treated with danazol (n = 9) or the combination cyproterone acetate plus ethinyl estradiol (n = 7) for 6 months. Biopsies were performed before and at 3 and 6 months of treatment. The material obtained was studied by light (LM), scanning (SEM) and transmission electron microscopy (TEM). A morphometric analysis was performed evaluating three morphometric and three stereologic indices. The results indicate that danazol had a progestational effect on endometrial glands and stroma, associated with a marked hypotrophy of the mucosa. The cyproterone acetate/ethinyl estradiol combination induced progressive atrophy of the endometrium with an increase in the stromal component and a reduction of glandular tissue.

Adult↗
PubMed1983

Cyproterone acetate prevents translocation of the androgen receptor in the rat prostate.

The translocation of the androgen receptor in prostatic tissue has been studied under the influence of different ligands (testosterone, methyltrienolone and cyproterone acetate) in vivo and in vitro. Nuclear and cytoplasmic androgen receptors were estimated using an exchange assay with [3H]methyltrienolone ( [3H]R1881) 1 h and 16 h after injection in castrated rats of either 100 micrograms testosterone (T), 10 mg cyproterone acetate (CA) or the combination of T and CA. Within 1 h after T administration, nuclear receptor levels increased with a concomitant depletion of cytosol receptors. In the CA-treated rats nuclear receptor levels were not different from those of control castrated animals and there was no depletion of cytosol receptors. The combined treatment of T and CA resulted in a partial depletion of cytosol receptors and a simultaneous increase of nuclear receptors. The absence of an increase in nuclear androgen receptors in CA-treated animals cannot be explained by a delay in translocation, because even 16 h after CA injection, only a very small number of nuclear receptors were detectable. Incubation of minced prostatic tissue with [3H]CA or [3H]R 1881 resulted in receptor translocation only in the R1881 incubations and confirmed the in vivo results. Competition studies with different steroids and cytosol receptor (non-activated, 8S form in low salt gradient) or nuclear receptor (activated 3.6S form in high salt gradient) of prostatic tissue show that CA can compete with R1881 for specific androgen-binding sites with a similar relative binding affinity for both receptor preparations. The present results provide evidence that CA prevents translocation of the androgen receptor to the nucleus, although CA can be bound with similar affinities to the nuclear receptor and the cytoplasmic receptor. We propose that the anti-androgenic action of CA involves an inhibition of receptor translocation.

Androgen Antagonists↗
PubMed1986

Effects of different doses of cyproterone acetate (CA) on preputial gland structure and activity in intact male mice.

The preputial is an androgen-dependent structure which appears to be used in pheromonal signalling in rats and mice. The structure of representative glands from intact oil injected male laboratory TO strain mice was contrasted with tissue from intact counterparts treated with the anti-androgen cyproterone acetate (CA). Sixteen days of an i.m. application of a modest range of CA doses (0.5, 1.0 and 2.0 mg/day given as oily solutions) and a variety of control treatments were used to assess influences on the structure and function of the preputial. The glands of intact male mice treated with oil were well-developed and actively secreting with parenchymatous acini at different stages of maturation. Such glands are generally highly Sudanophilic, with the lipophilic stain concentrated in acini in frozen sections and many acini are compressed by their neighbours to assume irregular shapes. Wax and frozen preputial sections from intact subjects treated with 0.5 or 1.0 mg CA were, in contrast, less well-developed and had fewer and smaller lipid droplets. Treatment of counterparts with 2 mg CA reduced acinar number and diameter in both wax and frozen sections with a concomitant increase in the proportion of connective tissue. The data confirm that this anti-androgen antagonizes the androgen secreted by the testis and adrenal cortex in terms of its expression of function on the preputial gland. These data provide further evidence that cyproterone acetate's suppressive actions on murine aggression are primarily via its ability to depress the secretion of odour cues that facilitate attack.

Animals↗
PubMed1987

Decrease of serum testosterone by cyproterone acetate accompanied by an unexpected increase of calcitonin secretion capacity.

The interaction between testosterone and calcitonin secretion capacity was studied in 9 patients with prostatic cancer. Treatment with the antiandrogenic agent cyproterone acetate resulted in an expected decrease in serum testosterone but an unexpected and unexplained increase in calcitonin secretion capacity. The previous statement that a positive correlation between sex hormones and calcitonin secretion capacity can be recognized probably requires revision. This unexpected effect of cyproterone acetate had possible additive beneficial advantages for treatment, such as bone mass sparing and its analgesic effect.

Aged↗
PubMed1987

Metastatic cancer of the prostate managed with buserelin versus buserelin plus cyproterone acetate.

We recruited 71 previously untreated patients with metastatic prostatic carcinoma to 2 separate consecutive prospective phase 2 studies done by the same group of investigators according to the same protocols in which only the treatment regimens differed. Of the patients 58 were treated with the luteinizing hormone-releasing hormone analogue buserelin alone (0.4 mg. 3 times daily intranasally) and 13 were treated with buserelin combined with cyproterone acetate, a potent antiandrogen (50 mg. 3 times daily orally). The objective of the study was to investigate the efficacy, safety and tolerability of the medication used during at least 12 months by studying adequate endocrine parameters, the rate and duration of response, as well as the rate of progression and possible side effects. All endocrine parameters were studied in 1 laboratory. Modified response criteria of the National Prostatic Cancer Project were used. The endocrine studies showed an effective suppression of plasma testosterone to castration levels by buserelin after an initial increase during the first 2 weeks. Luteinizing hormone and follicle-stimulating hormones were lowered significantly and could not be re-stimulated by the intravenous application of luteinizing hormone-releasing hormone. There was no correlation of plasma testosterone with response and progression. However, a significant correlation existed between higher basal cortisol levels at entry, and after 3 and 6 months, and progression. Response is reported for all patients at the 12-month interval and did not seem to differ among treatment groups. The rate of progression after all patients had been treated for 1 year was 37.9 per cent in the buserelin group and 41 per cent in the buserelin plus cyproterone acetate group. Three early deaths occurred in the buserelin group. Except for impotence, only mild side effects were noted. Our study shows that treatment of metastatic prostatic cancer by means of the luteinizing-hormone-releasing hormone analogue buserelin is safe and effective. The results obtained are compatible with those obtained by castration. In our study a superiority of total androgen withdrawal over testicular suppression alone could not be shown.

Buserelin↗