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PubMed1982

Effects of cyproterone acetate and oestradiol benzoate on the rat testis. Morphometric study after treatment over 35 days.

The testes of juvenile and adult rats were subjected to a histomorphometric and ultramorphometric examination after a 5-week cyproterone acetate and oestradiol benzoate treatment respectively. In the cyproterone acetate animals only minor changes of spermatogenesis are found in contrast to the oestradiol benzoate ones. The juvenile rats were not differing from those in the control group. In the older rats a reduction of the spermatocytes area portion in the basal zone of seminiferous epithelium can be proven. Oestradiol benzoate leads to an arrest of spermatogenesis at the stage of spermatocytes or the early spermatids respectively. At the same time the median diameter of seminiferous tubulus and the total area of seminiferous epithelium has considerably decreased in comparison to the treatment with anti-androgen. By the applied method an influence of the two substances on the spermatogonia was not recognizable.

Age Factors↗
PubMed2003

Effects of estradiol, cyproterone acetate, tibolone and raloxifene on uterus and aorta atherosclerosis in oophorectomized cholesterol-fed rabbits.

BACKGROUND: Different hormonal replacement regimens are used for treating climacteric complaints; however, not all of them have the same clinical profile. Cardiovascular disease (CVD) is a major health problem and tibolone, raloxifene, estradiol (alone or with cyproterone acetate) have been added to cholesterol-fed rabbits to study atherosclerosis. METHODS: A total of 48 cholesterol-fed New Zealand white rabbits were studied for 4 months. Forty rabbits underwent bilateral ovariectomy and the other eight were sham operated (group S). The ovariectomized rabbits were allocated to five groups of eight animals each receiving tibolone (Group T, 6 mg/day), raloxifene (R, 35 mg/day), estradiol valerate (E, 3 mg/day), estradiol valerate plus cyproterone acetate (EC, 3+0.5 mg/day, respectively), and no treatment for the control group (C). The sham group received no treatment too. RESULTS: After 4 months the percentage of the extent of atherosclerosis in the aorta was 30.4% in C group, 24.5% in S group, 10.2% in T group, 30.3% in R group, 17.9% in E group and 28.1% in EC group (P<0.05 T vs. C, R, EC). The aortic cholesterol content compared with aortic weight was 8.55 microg/mg in C group, 11.97 microg/mg in S group, 1.86 microg/mg in T group, 3.82 microg/mg in R group, 2.86 microg/mg in E group and 5.24 microg/mg in EC group (P<0.05 T vs. EC, C, S; R vs. C, S; E vs. C, S). Uterine weights in grams were: 1.89 (C group), 2.24 (S), 7.38 (T), 1.94 (R), 9.92 (E), and 5.94 (EC); P<0.05 (C, S, R, vs. T, E, EC; T vs. E; EC vs. T, E). CONCLUSION: Our study showed a decrease in the extent of aortic atherosclerosis in oophorectomized cholesterol-fed rabbits treated with tibolone or estradiol, and a decrease in aortic cholesterol content in rabbits treated with tibolone, raloxifene and estradiol. However, rabbits treated with tibolone showed an increased uterine weight, which is contrary to that observed in humans.

Animals↗
PubMed2003

Effects of estradiol alone or in combination with cyproterone acetate on carotid artery pulsatility index in postmenopausal women.

OBJECTIVES: The incidence of cardiovascular disease (CVD) increases dramatically with the loss of ovarian function. Observational studies indicate that the risk of CVD may be reduced by up to 50% in postmenopausal women who take estrogen replacement therapy. Estrogen therapy reduces internal carotid artery pulsatility index (PI). The improvement in carotid PI following HRT has been proposed as a marker of the cardioprotective effect of estrogen therapy. Cyclical progesterone addition to ERT partially antagonizes the reduction on the carotid artery PI. As progesterone, androgens has been shown to decreases arterial vasodilatation and carotid PI. To our knowledge no information is available regarding the effect of CPA addition on the carotid artery PI in women taking estrogen replacement therapy. METHODS: We recruited a total of 30 women in postmenopause for at least 12 months and were in good health. Fifteen women were postmenopausal following surgical bilateral oophorectomy for benign condition. Fifteen postmenopausal women received estradiol valerate for 21 days and CPA (1 mg) for 10 days for 3 months (Group E/CPA). Ovarectomized women (n=15) received estradiol hemihydrate (2 mg) for 3 months (Group E). The main factor investigated was PI, an indicator of impedence to blood flow down stream. Doppler US were performed before the start and at the end of the therapy. RESULTS: The mean reductions respect to basal values were 11.5% in women treated with E and 10.8% in women treated with E/CPA. No significant difference was found between treatment values. CONCLUSIONS: The results of the present study demonstrate that cyproterone acetate addition to E do non-antagonize the effect of estrogen on carotid artery PI. The present study demonstrate that both estradiol hemihydrate and estradiol valerate plus cyproterone acetate lead to similar improvement in carotid artery; through this mechanism both treatments could potentially reduce the incidence of cerebrovascular disease in postmenopausal women.

Cardiovascular Diseases↗
PubMed2001

Different methods for the determination of gestodene, and cyproterone acetate in raw material and dosage forms.

Four new precise accurate and selective methods have been developed for the determination of gestodene (I) and cyproterone acetate (II). The first method (A) depends on reaction of (I) and (II) with isoniazide in an acid medium and the colored products were measured at 378 and 400 nm, respectively. The second method (B) depends on the reaction of (I) and (II) with tetrazolium blue in an alkaline medium and the colored products were measured quantitatively at 515 and 520 nm, respectively. The optimum conditions for the analysis were studied. Both methods determined gestodene (I) in concentration range from 4 to 24 microg ml(-1) with mean percentage recoveries 99.54%+/-1.20 and 99.63%+/-1.89 for method A and B, respectively. For cyproterone acetate, the concentration ranges were 4-36 and 8-40 microg ml(-1) with mean percentage recoveries 99.94%+/-1.19 and 99.23%+/-2.00 for methods A and B, respectively. The third method (C) depends on the quantitative evaluation of (I) and (II) densitometrically using dichloroethane:methanol:water (95:5:0.2) as mobile phase and the chromatogram were scanned at 247 and 281 nm, respectively. Method (C) determines (I) and (II) in concentration ranges from 0.2 to 1.6 and 0.1-0.7 microg microl(-1) using Hamilton syringe 10 microl, with mean percentage recoveries 99.94%+/-1.19, and 99.82%+/-1.75, respectively. The fourth method (D) is a first derivative one depends on measuring the D(1) value at 303 nm for (II) only in concentration range 10-20 microg ml(-1) with mean percentage recoveries 99.95%+/-1.49.

Acne Vulgaris↗
PubMed2003

Fully automated method for the liquid chromatographic determination of cyproterone acetate in plasma using restricted access material for sample pre-treatment.

A new fully automated method for the quantitative analysis of an antiandrogenic substance, cyproterone acetate (CPA), in plasma samples has been developed using on-line solid-phase extraction (SPE) prior to the determination by reversed-phase liquid chromatography (LC). The automated method was based on the use of a precolumn packed with an internal-surface reversed-phase packing material (LiChrospher RP-4 ADS) for sample clean-up coupled to LC analysis on an octadecyl stationary phase using a column-switching system. A 200-microL volume of plasma sample was injected directly on the precolumn packed with restricted access material using a mixture of water-acetonitrile (90:10, v/v) as washing liquid. The analyte was then eluted in the back-flush mode with the LC mobile phase which consisted of a mixture of phosphate buffer, pH 7.0-acetonitrile (54:46, v/v). The elution profiles of CPA and blank plasma samples on the precolumn and the time needed for analyte transfer from the precolumn to the analytical column were determined. Different compositions of washing liquid and mobile phase were tested to reduce the interference of plasma endogenous components. UV detection was achieved at 280 nm. Finally, the developed method was validated using a new approach, namely the application of the accuracy profile based on the interval confidence at 90% of the total measurement error (bias+standard deviation). The limit of quantification of cyproterone acetate in plasma was determined at 15 ng mL(-1). The validated method should be applicable to the determination of CPA in patients treated by at least 50 mg day(-1).

Androgen Antagonists↗
PubMed1999

Fatal fulminant hepatic failure due to cyproterone acetate.

Cyproterone acetate is a normally well-tolerated drug that is used widely for the treatment of prostatic carcinoma. Liver toxicity due to its use is not well known. We describe two cases of fatal fulminant hepatitis related to the use of cyproterone acetate.

Aged↗
PubMed1979

[Contraception in androgenised women with a low-dose cyproterone-acetate containing one-phase preparation (author's transl)].

101 hirsute women received Diane, a combination of 2 mg cyproterone acetate and 50 micrograms ethinyl oestradiol per capsule, from the fifth to twenty-fifth day during a total of 1105 cycles. The treatment was satisfactory in 96% of women with acne, 84% with androgenic alopecia, 79% with seborrhoea, and 50% of those with mild or moderate hirsutism. The effectiveness of treating hirsutism or alopecia depended on its severity and duration. There was no correlation between various measures of androgen levels before and during treatment and the clinical results. Side effects were similar to those after contraceptive one-phase preparations, both in kind and incidence. None of the women became pregnant. Diane is thus the drug of choice in hormonal contraception of patients with acne, seborrhoea, androgenic alopecia or mild hirsutism. It is also suitable in the follow-up or interval management of high-dose cyproterone acetate treatment of severe hirsutism, in order to maintain the effect obtained with lower hormone doses.

Acne Vulgaris↗
PubMed2004

Urinary 6-sulfatoxymelatonin excretion in hyperandrogenic women: the effect of cyproterone acetate-ethinyl estradiol treatment.

Evidence for a relationship between melatonin and the reproductive hormones in humans is based on observations of abnormal melatonin secretion in clinical disorders of the pituitary-gonadal axis. The aim of this study was to investigate melatonin production in hyperandrogenic women before and during treatment with cyproterone acetate and ethinyl estradiol (Diane 35). Twelve women with polycystic ovary syndrome (PCOS), 10 women with idiopathic hirsutism (IH), and 10 women with late onset adrenal hyperplasia due to 21-hydroxylase deficiency (LOCAH) were studied. Patients were treated with Diane 35 for four months. Fasting blood samples for the determination of luteinizing hormone (LH), follicle-stimulating hormone (FSH), testosterone and dihydroepiandrosterone sulfate (DHEAS) and 24-hour urine collections for the determination of 6-sulfatoxymelatonin (aMT6s) excretion were obtained from all patients at baseline and after 4 months of treatment. Results were compared with those obtained in 15 control women. At baseline, women with PCOS and LOCAH had significantly higher testosterone and aMT6s values than women with IH and controls. Diane 35 treatment significantly decreased testosterone, LH, FSH and aMT6s values in PCOS and LOCAH patients compared with pretreatment values. These results indicate that hyperandrogenic women with PCOS and LOCAH have increased melatonin production. The decrease in aMT6s excretion together with reduced serum LH, FSH, DHEAS and testosterone values during treatment with cyproterone acetate-ethinyl estradiol, suggest that sex steroids either directly or through the suppression of gonadotropins, modulate melatonin secretion in these patients.

Adrenal Hyperplasia, Congenital↗
PubMed1994

[Serum hormones before and during therapy with cyproterone acetate and spironolactone in patients with androgenization].

The effect of cyproterone acetate (CPA) and spironolactone (SPL) on the serum androgen concentrations of premenopausal women with symptoms of hyperandrogenism were investigated in a total of 39 women. The observation period was 12 months. CPA was administered according to the Hammerstein regimen: cyproterone acetate (CPA) [Androcur] 100 mg/die 5.-14. day of the cycle; ethinylestradiol (EE) [Progynon C]: 40 mg/die 5.-25. day of the cycle; Spironolactone (SPL) was given in a dosage of 100 mg/die from day 1.-21. of the cycle. During the therapy with CPA a significant decrease of total testosterone (61%), free testosterone (78%), LH (48%) and 17 alpha-Hydroxyprogesterone (72%) was observed; during the medication with spironolacton only a significant decrease of 5 alpha-dihydrotestosterone (81%), which could not be seen during CPA use, was observed. Serum concentrations of total testosterone, free testosterone, LH and 17 alpha-Hydroxyprogesterone remained unchanged. DHA and DHAS did not change during neither medication. Since peripheral androgens were not suppressed by SPL the positive therapeutical effect of SPL can be explained by the antiandrogenic effect at the level of the receptor. A disadvantage of spironolacton is the lack of contraceptive efficacy. In cases where contraindication for oral contraceptives are present SPL can be considered as a good alternative to CPA. The suppressive effect of CPA/EE on total testosterone, LH addition to the antivulatory effect makes it the preferable medication for hyperandrogenemic patients with polycystic changes of the ovaries (PCOD).

Adult↗
PubMed2005

Effectiveness of cyproterone acetate in achieving castration and preventing luteinizing hormone releasing hormone analogue induced testosterone surge in patients with prostate cancer.

PURPOSE: To our knowledge this study represents the first analysis monitoring the efficacy of cyproterone acetate (CPA) monotherapy for achieving castrate testosterone levels prior to administering a luteinizing hormone-releasing analogue (LHRHA) for treating prostate cancer in the prostate specific antigen (PSA) era. MATERIALS AND METHODS: Patients with untreated locally advanced or metastatic prostate cancer were recruited prospectively. Treatment involved a 28-day course of oral cyproterone acetate and LHRHA depot injection on day 14. Patients had serum PSA, luteinizing hormone and testosterone monitored at intervals during a 56-day period. RESULTS: A total of 15 patients with a mean age of 74 years completed the study. Near castrate serum testosterone was achieved on day 7 (mean +/- 95% CI 83.38 +/- 17.87 ng/dl). There was a significant testosterone increase after LHRHA administration on day 14 compared with the level of 160.23 +/- 36.60 ng/dl on day 16 (p <0.01). Serum luteinizing hormone mirrored testosterone, increasing from a mean of 4.93 +/- 0.61 to 15.4 +/- 6.12 nmol/l after LHRHA administration (p <0.01). Mean serum PSA demonstrated a decrease from 199.25 +/- 6.12 microg/l at day 0 to 43.77 +/- 33.08 microg/l by day 56. There was no increase in serum PSA after LHRHA administration. CONCLUSIONS: Two weeks of priming with CPA does not eliminate the surge in serum testosterone (testosterone flare) upon LHRHA administration but the testosterone increase does not exceed pretreatment levels. Furthermore, 2 weeks of CPA may not offer a benefit over 1 week in lowering serum testosterone. Finally, there is no increase in serum PSA when LHRHA is administered after priming with CPA.

Aged↗
PubMedDate not supplied

Effects of cyproterone acetate on spontaneous contractility of the rat epididymis.

The spontaneous contractility of the rat epididymis was recorded in vivo and the effects of cyproterone acetate were studied. At 7 days after cyproterone acetate daily administration the records of the epididymal contractility did not show significant differences from the records obtained in control animals. On the contrary, in animals injected during 11 days the amplitude and frequency of epididymal contractions showed a significant decrease, and this activity completely ceased at 14 days of treatment.

Animals↗
PubMedDate not supplied

Contractile behaviour of rat seminal vesicle after gonadectomy, testosterone replacement and cyproterone treatment.

The effects of bilateral gonadectomy, testosterone replacement and cyproterone acetate treatment on seminal vesicle contractions were studied in rats in order to contribute new data on the role of androgens in the spontaneous motility of the seminal vesicle. In gonadectomized-testosterone treated rats the glands exhibited a spontaneous rhythmic activity similar to that of entire animals. The seminal vesicles of gonadectomized as well as of cyproterone treated rats also contracted spontaneously but the contractions showed a smaller amplitude. Such decrease could be related with the well-known atrophy and reduction in the number of smooth muscle cells occurring in seminal vesicles after castration. The results reported in this paper suggest that androgens are not required for the normal spontaneous activity of seminal vesicles.

Animals↗
PubMed1976

Testosterone metabolism in benign prostatic hypertrophy: in vivo studies of gestonorone caproate and cyproterone acetate.

18 patients with obstructive benign prostatic hypertrophy were studied. A 5-day treatment with gestonorone caproate (200 mg daily and 200 mg on alternate days) and cyproterone acetate (300 mg daily) suppressed the plasma LH and serum LH levels. Subsequently, H3-testosterone was injected intravenously and its elimination from plasma and uptake and metabolism in the BPH tissue studied. The elimination of total radioactivity and H3-testosterone from plasma was not altered after the 3 treatment regimens as compared to the control group. The uptake of total radioactivity into BPH tissue and its intraprostatic metabolism particularly to dihydrotestosterone was significantly suppressed in the patients with daily injections of gestonorone. Cyproterone acetate and gestonorone caproate on alternate days did not cause this effect.

Aged↗
PubMed1976

Cyproterone acetate in treatment of precocious puberty.

Twenty-nine children (23 girls, 6 boys) with precocious puberty were treated with cyproterone acetate for various periods of time ranging from 6 months to 3 years 4 months. They received an oral dose ranging from 70-150 mg/m2 per day, or an intramuscular depot injection once a fortnight or once a month at a dose ranging from 107-230 mg/m2. Both forms of therapy were found to suppress the signs of sexual maturation, but the oral form proved to be superior. Only the younger patients with a bone age under 11 years showed a beneficial effect upon linear growth and bone maturation. No side effects were noted, but additional advantageous effects upon behaviour and sociability were. It is concluded that at present cyproterone acetate by mouth is the drug of choice in the treatment of precocious puberty. The treatment should be initiated as early as possible to attain maximum benefit.

Administration, Oral↗
PubMed1981

Effect of cyproterone acetate on adrenocortical function in children with precocious puberty.

Seven children with precocious puberty were treated with cyproterone acetate and their adrenal function studied. In each child the drug caused significant adrenal hypofunction which was secondary to adrenocorticotrophic hormone suppression. None of these children had clinical evidence of adrenal hypofunction and it is assumed that the drug has glucocorticoid-like properties. Children receiving cyproterone acetate should carry information to warn doctors of this effect since they may require steroid cover during illness.

Adrenal Cortex↗
PubMed1998

Maximum androgen blockade using LHRH agonist buserelin in combination with short-term (two weeks) or long-term (continuous) cyproterone acetate is not superior to standard androgen deprivation in the treatment of advanced prostate cancer. Final analysis of EORTC GU Group Trial 30843. European Organization for Research and Treatment of Cancer (EROTC) Genito-Urinary Tract Cancer Cooperative Group.

This is the final analysis of EORTC GU Group Trial 30843 in which the treatment of advanced, metastatic prostate cancer with a combination of the LHRH agonist buserelin (nasal spray) and cyproterone acetate (Androcur), either continuously of only during the first 2 weeks, was compared with orchidectomy. There was no significant difference between the three arms as far as response rate, time to progression (subjective and objective) and duration of survival are concerned. Retrospective stratification according to the most important prognostic factors did not change the conclusions. Possible reasons for the difference with trial 30853, which used the same entry criteria but compared goserelin and flutamide with orchidectomy, are discussed. Reasons for using cyproterone acetate in combination treatment are the prevention of flare of the disease after LHRH agonists only and the prevention/reduction of toxicity in the form of hot flushes.

Acid Phosphatase↗
PubMed1977

Kinetics of 3H-testosterone and 3H-dihydrotestosterone metabolism in patients with benign prostatic hypertrophy. Effect of cyproterone acetate.

The response of 3H-testosterone and 3H-dihydrotestosterone to the administration of cyproterone acetate (CA) over a period of 5 days was investigated. Both tracers were injected intravenously in patients with benign prostatic hypertrophy. Blood was withdrawn for up to 5 h. Benign prostatic hypertrophy tissue was obtained by transurethral resection. Nine patients served as controls. Eleven patients received 300 mg CA intramuscularly. Cyproterone acetate suppressed testosterone and FSH, but not LH. 3H-testosterone was cleared more rapidly from plasma in the patients given CA presumably due to increased metabolism in the liver. 3H-dihydrotestosterone, however, remained virtually uninfluenced. Moreover, CA did not significantly alter the 3H-testosterone and 3H-dihydrotestosterone uptake and metabolism within prostatic tissue.

Aged↗
PubMed1978

The effect of cyproterone acetate on the pituitary-adrenal axis in hirsute women.

The functioning of the hypothalamo-pituitary-adrenal axis was assessed in 10 adult women with idiopathic hirsutism treated for 2 weeks with the anti-androgen cyproterone acetate in a dose of 50 mg b. d. daily and in 4 patients treated for at least 3 months. Basal plasma ACTH and cortisol levels and the cortisol response to 8 h ACTH infusion were comparable before and during short-term treatment. The plasma ACTH and cortisol responses to insulin induced hypoglycaemia before and during anti-androgen therapy also were of the same order of magnitude. In the 4 patients treated for at least 3 months also no suppressive effect of the anti-androgen on basal plasma cortisol levels was observed. From these data the conclusion seems warranted that short-term cyproterone acetate treatment in the given dose not significantly influences pituitary-adrenal function in adult women with idiopathic hirsutism.

Adolescent↗