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PubMed1987

Efficacy of low-dose oral contraceptives containing levonorgestrel, gestoden and cyproterone acetate.

The efficacy of low-dose oral contraceptives containing 30 micrograms or 35 micrograms ethinyl estradiol in combination with Levonorgestrel, gestoden (delta 15-Levonorgestrel) and cyproterone acetate was studied. Borderline doses for inhibition of ovulation were found to be approximately 50 micrograms for Levonorgestrel, 40 micrograms for gestoden and 1 mg for cyproterone acetate. These results were derived from the assay of luteinizing hormone, follicle-stimulating hormone, 17 beta-estradiol and progesterone serum levels during the daily treatment of a total of 47 female volunteers from day 5 through day 25 of their cycles. A combination of 30 micrograms ethinyl estradiol plus 75 micrograms Levonorgestrel or 75 micrograms gestoden resulted in complete inhibition of ovulation in each of the 20 subjects studied. Monitoring of hormone serum levels in 6 female volunteers with normal cycles during the administration of 35 micrograms ethinyl estradiol plus 2 mg cyproterone acetate showed inhibition of ovulation in all subjects studied during the first and third therapy cycle. One subject exhibited follicular maturation during the third treatment cycle as judged from the patterns of 17 beta-estradiol serum levels. Present data suggest that low-dose oral contraceptives containing Levonorgestrel, gestoden and cyproterone acetate are highly efficient in providing great contraceptive safety and do not support the previous notion that the kind of progestagen used is relevant for the degree of central inhibition.

Adolescent↗
PubMed1988

Prolonged influence of a neonatal cyproterone acetate treatment on renal androgen binding in mice.

To determine whether neonatal endogenous androgens influence adult renal androgen binding, newborn male mice were injected from 1 to 10 days of age with cyproterone acetate and newborn females with testosterone from 1 to 10 days and from 20 to 40 days of age. In controls, at adulthood, the total cellular androgen receptor content was significantly higher in males (1700 +/- 200 receptors per cell) than in females (1060 +/- 50) and, as expected, the nuclear receptor content was 12-fold higher in males. While the total number of receptors (1650 +/- 200 per cell) was unchanged in adult males neonatally treated with cyproterone acetate, their distribution between cytosol and nucleus was similar to that in control females despite normal circulating and renal testosterone levels. The nuclear receptors represented 50, 7 and 11% of the total receptors in control males, control females and cyproterone acetate-treated males, respectively. The very low levels of nuclear receptors present in the kidney of cyproterone acetate-treated males probably explain the decreased sensitivity of this organ to testosterone. The nuclear receptor accumulation measured in adult animals after a single injection of testosterone did not seem to be affected by neonatal hormonal manipulations.

Age Factors↗
PubMed1982

The effects of orchidectomy, estrogens, and cyproterone acetate on plasma testosterone, LH, and FSH concentrations in patients with carcinoma of the prostate.

The peripheral plasma concentrations of testosterone, luteinising hormone (LH) and follicle stimulating hormone (FSH) were determined in 46 patients (age 51-86 years) with cytologically confirmed prostatic carcinoma. Treatment consisted of subcapsular orchidectomy (15 cases) or estrogen medication (16 cases) or cyproterone acetate (15 cases). The determinations were made before and 2 weeks and 2 months after treatment was initiated. No correlation was found between the pretreatment levels of testosterone and gonadotrophins and the local extent of the primary tumor or the degree of malignancy. Nor was there any correlation between hormonal level, presence of metastases or patient age. Orchidectomy and estrogen medication both resulted in very low plasma testosterone levels, corresponding to 15% of the pretreatment values. This proportion was 28% in the group treated with cyproterone acetate. Orchidectomy was followed by significant increase in the levels of LH and FSH. Estrogen treatment resulted in suppression of the LH levels to 40% and of FSH to 14% of the pretreatment values. The corresponding decreases in response to cyproterone acetate were 65 and 35%. The results indicate that reduction in gonadotrophin secretion is the primary mechanism in the lowering of testosterone levels produced by treatment with estrogens or cyproterone acetate.

Aged↗
PubMed1981

Effect of cyproterone acetate on adenohypophysis of castrated mice.

Pituitaries from castrated male mice injected with cyproterone acetate were examined ultrastructurally. LH gonadotrophs showed two types: (a) those containing a dilated RER, a hypertrophied Golgi, and decreased granular content; and (b) those presenting an electron lucent cytoplasm and a nonhypertrophied RER. Following cyproterone acetate treatment both LH cell types showed increased RER cisternal hypertrophy and absence of Golgi membranes. In LH type (a) gonadotroph-increased granular content was noted. No detectable alterations were noted in FSH gonadotrophs following cyproterone acetate treatment. Cyproterone acetate may have stimulated the synthesis of the protein component but inhibited the incorporation of the carbohydrate moiety and LH release.

Animals↗
PubMed1997

Investigation into the age-dependence of the pharmacokinetics of cyproterone acetate in healthy male volunteers.

OBJECTIVE: To investigate a possible age-dependence of the pharmacokinetics of cyproterone acetate following single oral administration. METHODS: Twenty eight healthy men between 22 and 74 years of age received a single oral dose of 100 mg cyproterone acetate. The pharmacokinetic parameters, area under the serum concentration-time curve, apparent volume of distribution, apparent clearance, terminal half-life and the concentration ratio of 15 beta-hydroxycyproterone acetate/cyproterone acetate were examined for possible age-dependence using regression analysis. RESULTS: The values of area under the serum level-time curve showed high interindividual variability and were not related to age. With regard to apparent clearance and volume of distribution, decreasing and increasing values, respectively, were observed with increasing age. There was also a clear dependence of the terminal half-life on age. Elderly men had values about two times higher (95 h) than men belonging to the younger age groups (45 h). The mean concentration ratio of 15 beta-hydroxycyproterone acetate/cyproterone acetate was 0.8 (0.3) and showed no age-dependent change. CONCLUSIONS: Apparent clearance and apparent volume of distribution of cyproterone acetate showed age-dependent changes. Combined, the two effects cause a clear age-dependence of the terminal half-life of cyproterone acetate. An age-related reduction in liver volume is thought to be mainly responsible for the decrease in hepatic clearance with age. Chronic daily administration of the drug to elderly men may therefore lead to somewhat higher steady-state concentrations in the serum than in young men receiving the same dose.

Administration, Oral↗
PubMed2005

Genotoxic potential of cyproterone acetate: a possible role of reactive oxygen species.

The genotoxicity of cyproterone acetate was studied in human lymphocytes using chromosomal aberrations (CAs), mitotic index (MI) and sister chromatid exchanges (SCEs) as a parameter. Cyproterone acetate was found to be genotoxic at 20 and 30 microM. To study the possible mechanism of the genotoxicity of cyproterone acetate, superoxide dismutase (SOD) and catalase (CAT) were used separately and in combination along with the 30 microM of cyproterone acetate at different doses. SOD treatment increases CAs, SCEs and decreases MI as compared to treatment with 30 microM CPA alone, at both of the tested doses. CAT treatment decreases the frequencies of CAs and SCEs and increases MI in both, as compared to treatment with 30 microM CPA alone, separately and in combination with SOD, suggesting a possible role of reactive oxygen species for the genotoxic damage.

Androgen Antagonists↗
PubMed2001

Risk of venous thromboembolism with cyproterone or levonorgestrel contraceptives.

Results of studies have shown that there is an excess risk of venous thromboembolism in users of oral contraceptives containing cyproterone compared with those containing levonorgestrel. We did a case-control study, in which we assessed the risk of idiopathic venous thromboembolism in women taking combined low-dose oestrogen oral contraceptives containing cyproterone (n=24401) or levonorgestrel (n=75000). We compared the 26 women in this population who had idiopathic venous thromboembolism with 144 matched controls. 12 individuals and 30 controls were taking contraceptives that contained cyproterone. Our results suggest that risk of venous thromboembolism is increased four-fold in women taking contraceptives containing cyproterone by comparison with those exposed to levonorgestrel.

Adult↗
PubMed2003

Effects of the antiandrogens, vinclozolin and cyproterone acetate on gonadal development in the Japanese medaka (Oryzias latipes).

This study was focused on determining the effects of exposure to antiandrogens on the gonadal development of Japanese medaka (Oryzias latipes). Test compounds included the fungicide, vinclozolin and the clinical antiandrogen, cyproterone acetate. Newly hatched medaka were exposed to aqueous solutions of vinclozolin (2500 microg/l) and the vinclozolin fungicide formulation, Ronilan (1000 and 5000 microg/l) and cyproterone acetate (1 and 10 microg/l), for 3 months. Histological evaluation of the gonadal tissues of exposed fish indicated that the 5000 microg/l concentration of the vinclozolin formulation (Ronilan) induced a low incidence of intersex (i.e. testis-ova) and the 2500 microg/l concentration of vinclozolin-affected spermatogenesis in males. Also, the vinclozolin treatments induced moderate ovarian atresia. Cyproterone acetate also induced a low incidence of testis-ova, but in contrast to the vinclozolin treatment the amount of ovarian tissue in the testis-ova was equal to or greater than the amount of testicular tissue. In the cyproterone acetate treatments, both oogenesis and spermatogenesis were moderately inhibited at all test concentrations. The results of this study indicate that antiandrogens have the potential to alter testicular development and gametogenesis in fish. However, research is needed to determine the mechanisms by which antiandrogens affect fish.

Analysis of Variance↗
PubMed1998

Combination therapy with GH and cyproterone acetate does not improve final height in boys with non-GH-deficient short stature.

BACKGROUND AND OBJECTIVE: Recently, we reported that GH therapy without gonadal suppression (GS) decreased the final height of boys with non-GH-deficient short stature by decreasing the height standard deviation score (SDS) for bone age (BA) during puberty. Combination therapy with GH and GS has been reported to suppress bone maturation and improve final height in some cases. We evaluated the effects of combination therapy with GH and GS using cyproterone acetate on the final height of boys with non-GH-deficient short stature. PATIENTS: Fifty nine boys with non-GH deficient short stature were observed retrospectively until they reached their final height. The boys were divided into 3 groups: Group A consisted of 26 boys who were not treated with GH, group B consisted of 13 boys who were treated with GH alone, and group C consisted of 20 boys who were treated with combination therapy with GH and GS using cyproterone acetate. At the start of observation, the height SDS for BA and projected height were matched among these three groups. RESULTS: The mean +/- SDS of the final height for groups A, B, and C were 162.7 +/- 5.3 cm, 155.4 +/- 4.9 cm, and 161.9 +/- 3.2 cm, respectively. GH therapy did not affect the height SDS for BA during the prepubertal period. GH therapy without GS decreased the height SDS for BA during puberty in group B. Combination therapy with GH and cyproterone acetate increased the height SDS for BA between 12 and 14 years BA in group C. However, after GS therapy was discontinued at 14 years BA, the height SDS for BA gradually decreased and eventually reached the same value as that in group A. CONCLUSIONS: GH therapy during the prepubertal period did not improve the final height of boys with non-GH-deficient short stature. GH therapy without GS decreased pubertal height gain, resulting in reduced final height. Combination therapy with GH and GS using cyproterone acetate decelerated the bone maturation during puberty which might be accelerated by GH therapy, but did not improve the final height which might have been attained without treatment.

Androgen Antagonists↗
PubMedDate not supplied

Atmospheric pressure photoionization applied to quantitation of cyproterone acetate in human plasma.

Cyproterone acetate [6-chloro-1beta,2beta-dihydro-17alpha-hydroxy- 3'H-cyclopropa(1,2)-pregna-1,4,6-triene-3,20-dione acetate] is a powerful antiandrogen used in the treatment of women suffering from disorders associated with androgenization such as hirsutism and acne. A fast, sensitive, and robustness method is developed for the determination and quantitation of cyproterone acetate in human blood plasma by liquid chromatography coupled with tandem mass spectrometry. Cyproterone acetate is extracted from 0.2 mL human plasma by liquid-liquid extraction. The method has a chromatographic run of 4.5 min, using a C18 analytical column (100- yen 2.1-mm i.d.), and the linear calibration curve over the range is linear from 1 to 500 ng/mL (r2 > 0.994). The between-run precision, based on the relative standard deviation replicate quality controls, is 96.2% (3 ng/mL), 97.5% (120 ng/mL), and 99.1% (400 ng/mL). The between-run accuracy was +/- 2.7%, 3.1%, and 4.8% for the previously mentioned concentrations, respectively. The method is employed in a bioequivalence study of two tablet formulations of cyproterone acetate (100 mg).

Androgen Antagonists↗
PubMed1997

CD8+ lymphocytic pneumonitis in a patient receiving cyproterone acetate.

A large number of drugs can induce pulmonary disease. We report the case of a female patient who was receiving cyproterone acetate for severe hirsutism. After 4 months of cyproterone therapy, she had dyspnea, pulmonary infiltrates, and a restrictive ventilatory defect. Bronchoalveolar lavage showed CD8+ lymphocytosis as well as increased neutrophils and eosinophils, a profile highly suggestive of an iatrogenic process. The patient showed no other significant clinical or biologic abnormality. Symptoms and functional abnormalities disappeared after withdrawal of cyproterone and reappeared after its reintroduction. This suggests that cyproterone acetate, a substance used to treat hirsutism and prostate cancer and in the composition of certain oral contraceptives, can be added to the list of drugs that may cause lymphocytic pneumonitis.

Adult↗
PubMed1979

Effect of cyproterone acetate on the reproductive system of the female rat. A histological review.

Effects of cyproterone acetate, a synthetic steroidal compound, on the reproductive organs of female rats have been investigated. This agent caused reduction of ovarian weights indicative of suppression of pituitary gonadotrophins. Oestrogenic nature of cyproterone acetate was investigated in intact and ovariectomized rats taking uterine weight and vaginal keratinization as an index of oestrogenicity. Cyproterone acetate in ovariectomized animals induced vaginal keratinization and increased the uterine weights. These effects were parallel to the effect of oestradiol dipropionate in ovariectomized animals, thus indicating oestrogenic activity of cyproterone acetate. We may conclude that the above compound caused antifertility effects due to its oestrogenic nature at the dose level of 2 mg/alternate day in rats when the compound was administered subcutaneously.

Animals↗
PubMed1987

Parenteral and oral cyproterone acetate treatment in severe hirsutism.

In the present study a parenteral treatment regimen with cyproterone acetate was compared with the high dose peroral administration in patients with severe hirsutism. Two groups consisting of 10 patients each performed treatment with either 100 mg cyproterone acetate perorally for the first 10 days of the menstrual cycle or received a monthly implant of 300 mg cyproterone acetate intramuscularly applied on the first day of each cycle. In addition, contraception was performed with Diane in both patient groups. 9 treatment cycles were followed by a posttreatment period of 3 months. Hair parameters and serum androgens were monitored regularly. No significant differences of testosterone, androstenedione, dehydroepiandrosterone-sulfate and prolactin serum levels became evident between both cyproterone acetate regimens. Measurements of facial hair diameters revealed a better reduction for the parenteral application. Also the improvement of dermatological parameters was more prominent in the parenteral treatment group. The good effects of a medium dose parenteral application against higher dose peroral treatment thus was documented. The lack of significant differences of androgenic suppression in both regimens turns up the question if different metabolism at the cellular level may be responsible for that phenomenon.

Administration, Oral↗
PubMed1996

A prospective, randomised study to compare goserelin acetate (Zoladex) versus cyproterone acetate (Cyprostat) versus a combination of the two in the treatment of metastatic prostatic carcinoma.

A prospective randomised study was performed to test the hypothesis that total androgen ablation, achieved by combining an LHRH analogue, goserelin acetate (Zoladex), with an antiandrogen, cyproterone acetate (Cyprostat), is more effective than conventional monotherapy in delaying the time to progression of metastatic prostatic cancer. 525 patients were recruited at 18 UK centres between May 1986 and January 1989, 175 patients being allocated to each arm. Patients were clinically and biochemically assessed at 1, 2, 3, 6, 9 and 12 months after initiation of therapy and then every 6 months until a maximum duration of 48 months. There was no statistically significant difference in terms of median time to progression between the combination treatment arm and either monotherapy arm, although there was a statistically significant difference between goserelin acetate alone and cyproterone acetate alone, in favour of goserelin acetate (p = 0.016). All treatment regimens were well tolerated and cyproterone acetate reduced both tumour flare reactions and hot flushes in patients receiving goserelin acetate. It is concluded that total androgen ablation using cyproterone acetate (300 mg/day) and goserelin acetate (3.6 mg every 28 days) confers no advantage in terms of time to progression, to conventional monotherapy, but can reduce certain side effects caused by LHRH analogue treatment alone.

Adenocarcinoma↗
PubMed1981

Effect of cyproterone acetate on pituitary-adrenocortical function in man.

Recent literature (1973-1976) suggests suppression of pituitary-adrenal function in patients (eg with pubertas praecox) who are treated with cyproterone acetate in high doses for prolonged periods. Therefore we investigated in our metabolic ward the effects of administration of 200 mg cyproterone acetate per day during 20 days to 4 healthy male volunteers. Baseline plasma cortisol and ACTH levels, repeated diurnal plasma cortisol and ACTH profiles and the results of tetracosactide (Synacthen) stimulation tests and single-dose metyrapone (Metopiron) tests proved to be comparable before, during and after treatment. Moreover, a slight gradual increase in urinary cortisol excretion during the observation period indicated that cyproterone acetate in the given dose during 20 days certainly does not reduce the pituitary-adrenal function of 4 healthy male volunteers. Long-term administration (during 1 to 7 years) of the combination of cyproterone acetate and ethinyloestradiol did not suppress serum levels of cortisol, prolactin, thyroxine and TSH in 18 female patients with hirsutism and/or acne.

Adrenocorticotropic Hormone↗
PubMed1996

Comparison of flutamide and cyproterone acetate in the treatment of hirsutism: a randomized controlled trial.

The objective of this study was to compare the efficacy of flutamide and cyproterone acetate in the treatment of hirsutism. Twenty-two women with idiopathic hirsutism were randomized to receive either flutamide or cyproterone acetate. Each patient underwent a complete gynecological examination as well as an endocrinological profile and hematological, hepatic and renal function analyses. Hirsutism scores were determined using a modified Ferriman-Gallwey scoring system. These tests were then repeated at 3 and 9 months of therapy. Eleven patients received 250 mg of flutamide twice daily and 11 patients received 100 mg of cyproterone acetate on days 5-14 of the menstrual cycle. Ferriman-Gallwey scores were decreased significantly in both groups at the end of 9 months. There was a trend towards a better response with flutamide, that did not achieve significance. Another significant difference was the increased sex hormone-binding globulin in both groups. A statistically significant decrease was also observed for the levels of testosterone on both drugs. No subject withdrew from the study due to a side-effect. The data suggest that both flutamide and cyproterone acetate were similarly effective in treatment of hirsutism, and that the pure antiandrogen flutamide is a safe, well-tolerated and effective alternative in treatment.

Adolescent↗
PubMed1975

Effect of antiandrogen cyproterone acetate on the action of testosterone on mouse kidney.

The loss of endogenous testosterone in castrated male mice leads to a marked decrease in seminal vesicle and kidney tissue weight. 21 days' administration of exogenous testosterone abolished the effect of castration on the seminal vesicles and kidney tissue. The antiandrogen cyproterone acetate produced significant changes in the target tissue for androgens, i.e. in the seminal vesicles. In every case it blocked the action of both exogenous and endogenous testosterone on the seminal vesicles, but failed to block the "renotropic" action of testosterone, expressed as relative kidney weight. Contrary to its effect on the seminal vesicles, it did not influence relative kidney weight in normal animals. It likewise did not block the effect of exogenous testosterone on kidney tissue. The mechanism of the action of cyproterone acetate in androgen-dependent tissues is known to consist in inhibition of androgen binding to specific cell receptors in the target tissues. Some of the specific androgen receptors in mouse kidney are evidently different in character from those in the accessary sex glands, that being the reason why cyproterone acetate has an antiandrogenic, but not an antirenotropic effect. In agreement with experiments on rats, adrenal weight also decreases in mice after the administration of cyproterone acetate.

Animals↗
PubMed1977

Estrogenic and antifertility effect of cyproterone acetate in female gerbils, meriones hurriane Jerdon.

Effects of cyproterone acetate, a steroidal synthetic compound, on the reproductive organs of female gerbils have been investigated. This agent causes reduction of ovarian weights indicative of suppression of pituitary gonadotrophins. Estrogenic nature of cyproterone acetate was investigated in intact and ovariectomized gerbils taking uterine weight, vaginal keratinization and glycogen contents are parameters of estrogenic action. Cyproterone acetate in ovariectomized gerbils induced vaginal keratinization, increase in uterine weight, protein, RNA, glycogen and sialic acid contents of uterus, thus indicating an estrogenic activity. The histological and biochemical parameters lead to the conclusion that cyproterone acetate possesses estrogenic properties.

Animals↗