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PubMed2001

Male osteoporosis associated with longterm cyproterone treatment.

A 58-year-old man with previous dorsal vertebral fractures was referred for continuing management of osteoporosis. He was treated in the past with cyproterone acetate for hypersexuality. There were no other risk factors for osteoporosis. A dual energy radiographic absorptiometry scan confirmed osteoporosis. Treatment with alendronate 10 mg/day improved bone density and back pain. Patients receiving longterm treatment with cyproterone might be at risk for developing osteoporosis and would benefit from regular bone density monitoring.

Alendronate↗
PubMed1979

Effect of short-term administration of cyproterone acetate on the reproductive tract histology, ovarian and serum cholesterol contents of female monkey (Presbytis entellus entellus).

Short courses of cyproterone acetate, a compound with progestational and antiandrogenic activities were administered to normally cycling female monkeys to investigate into the effects of cyproterone acetate on the reproductive tract. In little earlier follicular stage 20 mg of the drug daily for 30 days increased the cholesterol contents in the gonads. Serum cholesterol contents were slightly increased. When the reproductive tract was examined histologically, the gonads showed reduction in size, along with widespread degeneration of the young follicles as well as other growing follicles. Uterus showed progestational endometrial proliferation and sloughing of the vaginal productive tract.

Animals↗
PubMed2002

Cyproterone acetate-ethinyl estradiol treatment alters urinary 6-sulfatoxymelatonin excretion in hyperandrogenic women.

OBJECTIVES: To investigate melatonin production in hyperandrogenic women before and during treatment with cyproterone acetate and ethinyl estradiol (Diane 35). MATERIAL AND METHODS: We studied 10 women with late onset adrenal hyperplasia due to 21-hydroxylase deficiency (LOCAH) and 10 women with idiopathic hirsutism (IH). 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. RESULTS: At baseline, women with LOCAH had significantly higher serum testosterone, 17-hydroxyprogesterone (17OHP) and ACTH stimulated 17OHP values than IH and control women. Their aMT6s values (51.0+/-20.5 mg/24h) were significantly higher than the values in IH (34.3+/-7.1) and control women (30.5+/-6.5) (p< 0.001). Diane 35 treatment significantly decreased serum LH, FSH and testosterone levels and aMT6s values in LOCAH patients (29.8+/-16.6 mg/24h) (p<0.0001) in LOCAH patients. CONCLUSIONS: These results indicate that hyperandrogenic women with LOCAH have increased melatonin production. The normalization of aMT6s and testosterone values during cyproterone acetate-ethinyl estradiol treatment, suggest that sex steroids either directly or through the suppression of gonadotropin, modulate melatonin secretion in these patients.

Adolescent↗
PubMed2003

[Endocrine and metabolic effects of metformin in combination with compound cyproterone acetate in women with polycystic ovarian syndrome].

OBJECTIVE: To study the endocrinologic and metabolic effects of metformin in combination with compound cyproterone acetate (CPA) on patients with polycystic ovarian syndrome (PCOS). METHODS: A prospective study involved total 45 PCOS patients as group A and 20 non-PCOS infertility patients as control (group B). Complete baseline work-up including body mass index (BMI), waist/hip ratio (WHR), ferriman-Gallwey score (FGS), gonadotrophin, testosterone (T), sex hormone-binding globulin (SHBG), dehydroepiandrosterone sulfate (Ds), insulin (FI) and glucose tolerance test, were performed in all patients. Patients in group A were treated with CPA alone (group A1), metformin alone (group A2) or combination of CPA with metformin (group A3), respectively by randomization. At the end of 12-week therapy, subjects were re-evaluated and above parameters were measured. RESULTS: Women in group A had significant increases in BMI, WHR, FGS, luteinizing hormone (LH), T, FI, insulin resistance, and significantly decrease in high-density lipoprotein (HDL)-C comparing with the control group (P < 0.01). No significant difference among A1, A2 and A3 was found at baseline. LH, T, free testosterone (FT) were significant decreased from (13.9 +/- 5.9) IU/L, (2.1 +/- 0.8) nmol/L and (2.8 +/- 2.3) nmol/L respectively to (5.8 +/- 2.2) IU/L, (1.2 +/- 0.4) nmol/L and (0.8 +/- 0.5) nmol/L respectively and SHBG was significant increased from (99 +/- 42) nmol/L to (187 +/- 64) nmol/L in group A3, when compared with LH, T and FT from (13.8 +/- 7.6) IU/L, (2.2 +/- 1.1) nmol/L and (2.5 +/- 1.9) nmol/L respectively to (11.8 +/- 6.5) IU/L, (1.8 +/- 0.8) nmol/L and (1.7 +/- 1.0) nmol/L respectively and SHBG from (99 +/- 40) nmol/L to (120 +/- 51) nmol/L in group A2 (P < 0.05 approximately 0.001). HDL-C were significantly increased from (1.5 +/- 0.3) mmol/L to (1.8 +/- 0.3) mmol/L in group A3 comparing with HDL-C from (1.5 +/- 0.4) mmol/L to (1.6 +/- 0.4) mmol/L in group A1 (P < 0.001). CONCLUSIONS: The PCOS patients treated with metformin in combination with compound cyproterone acetate may be more effective in inhibiting hyperandrogen and hypersecretion of LH than metformin alone and more obvious in improving lipid profiles than CPA alone.

Adult↗
PubMed2004

Fully automated method for the liquid chromatographic-tandem mass spectrometric determination of cyproterone acetate in human plasma using restricted access material for on-line sample clean-up.

A new automated method for the quantitative analysis of cyproterone acetate (CPA) in human plasma has been developed using on-line solid phase extraction (SPE) prior to the LC-MS/MS determination. The method was based on the use of a pre-column packed with internal-surface reversed-phase material (LiChrospher RP-4 ADS, 25 mm x 2 mm) for sample clean-up coupled to LC separation on an octadecyl silica stationary phase by means of a column switching system. A 30 microl plasma sample volume was injected directly onto the pre-column using a mixture of water, acetonitrile and formic acid (90:10:0.1 (v/v/v)) adjusted to pH 4.0 with diluted ammonia as washing liquid. The analyte was then eluted in the back-flush mode with the LC mobile phase consisting of water, methanol and formic acid (10:90:0.1 (v/v/v)). The dispensing flow rates of the washing liquid and the LC mobile phase were 300 microl min(-1). Medroxyprogesterone acetate (MPA) was used as internal standard. The MS ionization of the analytes was achieved using electrospray (ESI) in the positive ion mode. The pseudomolecular ionic species of CPA and MPA (417.4 and 387.5) were selected to generate daughter ions at 357.4 and 327.5, respectively. Finally, the developed method was validated according to a new approach using accuracy profiles as a decision tool. Very good results with respect to accuracy, detectability, repeatability, intermediate precision and selectivity were obtained. The LOQ of cyproterone acetate was 300 pg ml(-1).

Automation↗
PubMed2005

[Risking more freedom? Cyproterone acetate, sexual offenders and the German "Law on voluntary castration and other methods of treatment", 1960-1975].

Shortly after the fall of the National Socialist regime efforts were made in the Federal Republic of Germany to legislate anew on sterilisation and castration. For some experts, in particular sexologists and forensic psychiatrists in Hamburg, the question of the "treatment" of sexual offenders soon played a major role. In another research context an endocrinological substance showing anti-androgenic effects was synthesised in 1961 at the Schering AG in Berlin. In 1966 this substance, cyproterone acetate, was used for the first time to subdue the sexual drive. During parliamentary debates on a reintroduction of castration as a method of treatment for sexual deviations the advocates of cyproterone acetate succeeded in "inserting" their expertise into the "law on voluntary castration and other methods of treatment", which was adopted by the German Bundestag in January 1969. This paper discusses the interface between applied pharmacology, forensic psychiatry and sexology, and the politics leading to this law.

Cyproterone Acetate↗
PubMedDate not supplied

Effects of cyproterone acetate on the testicular function of bat (Rhinopoma kinneari Wroughton).

1-Cyproterone acetate administration (0.2 mg/day/animal for 25 days) caused widespread testicular necrosis. The lumen of the epididymides were devoid of spermatozoa. The RNA, protein, sialic acid and phosphatase enzyme activity of the testes were reduced. Serum transaminase enzyme activity was slightly changed. Haemoglobin, hematocrit, blood sugar, and blood urea levels were in the normal range. Regressed Leydig cell tissue and decreased production of RNA and sialic acid in the testes could be due to the antiandrogenic action produced by cyproterone acetate.

Animals↗
PubMed1978

[Serum concentrations of prolactin, growth hormone, and alpha-fetoprotein under long-term administration of an oral contraceptive containing cyproterone acetate (author's transl)].

Serum prolactin, growth hormone, and alpha-fetoprotein were determined in women taking a new oral contraceptive, consisting of 2 mg cyproterone acetate and 50 microgram of ethinylestradiol. Because these women were suffering from acne vulgaris they were taking this contraceptive containing a gestagen with antiandrogenic activity. Prolatin and growth hormone were determined because both may favour the development and the growth of mammary tumors and because their secretion may be stimulated by estrogenic compounds. Alpha-fetoprotein is a marker of hepatocellular carcinoma, which may be associated with long-term use of oral contraceptives. During one year of treatment with cyproterone acetate and ethinylestradiol there was a continuous rise of serum concentrations of prolactin. However, this rise did not exceed the normal range. In contrast, serum concentrations of growth hormone did not change significantly. Serum alpha-fetoprotein levels remained below the detection limit of the method.

Acne Vulgaris↗
PubMed1996

Radioimmunological analysis of cyproterone acetate in human serum. Comparison with a gas chromatographic/mass spectrometric method and influence of each method on the outcome of a bioequivalence trial.

Cyproterone acetate (CAS 427-51-0, CPA) is a steroid hormone with antiandrogenic and progestogenic properties, which has been used in the therapy of prostate carcinoma in men, and for the treatment of severe acne and hirsutism in women. The aim of the present study was to compare two equally sensitive analytical methods, a radioimmunoassay (RIA) and a gas chromatographic/mass spectrometric method (GC/MS), for the quantitative determination of CPA in human serum samples and to assess their suitability for bioequivalence trials. To this end, serum samples which had been collected during a study on the bioequivalence oaf two CPA-containing formulations (Androcur 100 and Androcur 50) were analysed using both methods. Basic pharmacokinetic parameters, like Cmax, tmax, t1/2 and AUC were calculated from each data set and corresponding parameters were compared by statistical methods. A comparison of the drug concentration-time curves obtained with both analytical methods revealed that in particular at later sampling times (48 to 120 h post dose) concentration values generated by RIA were slightly higher by about 20-40% than those measured with GC/MS. This indicates the presence of cross-reacting metabolite(s), most likely the 15 beta-hydroxy-cyproterone acetate. Accordingly, the values of Cmax, AUC(0-120 h) and AUC were overestimated by the RIA method by about 10-20%, 5% and 10%, respectively. However, there was a high correlation between corresponding parameters derived from RIA and GC/MS analysis. Although AUC values were slightly overestimated with the RIA method was used, this had no influence on the decision about bioequivalence because the mean ratio of the target variables Cmax and AUC was not affected. The variance of the pharmacokinetic parameters which is relevant for the bioequivalence test were even lower for RIA based values than those calculated after GC/MS analysis. In conclusion, it was found that although the GC/MS method is superior to RIA in terms of specificity, both methods were equally suited to demonstrate the bioequivalence of the two CPA-containing formulations. Thus, in future studies of this kind, the more simple RIA may be used instead of GC/MS.

Adult↗
PubMed1976

[Pharmacokinetics of cyproterone acetate in normal subjects after i.m. and oral application (author's transl)].

Sixteen volunteers were given cyproterone acetate-2'-14C (6-chloro-17-hydroxy-1alpha,2alpha-methylene-pregna-4,6-diene-3,20-dione acetate; Androcur¿) in single doses of between 2 and 12 mg i.m. and p.o. in 19 investigations. The plasma radioactivity was then determined at suitable intervals. Urine and faeces were collected quantitatively for 12 days. After oral administration the highest concentrations in plasma were found 1--4 h after administration. The mean amounts were 2--3% of the administered dose in the plasma volume. Plasma concentrations of more than half the highest values were measured for a period of 2--8 h. Cyproterone acetate was eliminated from the body with a half-life of about 1 1/2 days for men and about 2 days for women. After oral administration in single doses of 2--12 mg the compound was almost completely absorbed.

Administration, Oral↗
PubMed1983

Cyproterone acetate and the treatment of hirsutism.

Forty-two women with hirsutism completed 12 months of treatment with cyproterone acetate and ethinyl oestradiol given in a reverse sequential regimen. A highly significant improvement was recorded in the whole group using the Ferriman and Gallwey scoring system. Ten patients recorded a poor response whereas 19 recorded a good or very good result. Patients from groups with polycystic ovarian disease and idiopathic hirsutism recorded equally beneficial responses. Fasting plasma triglycerides rose significantly after 12 months. Other lipids were largely unaffected although a small fall in high density lipoprotein-cholesterol was detected at mid-cycle. No other biochemical abnormalities were found. Circulating levels of testosterone and 17 hydroxyprogesterone were suppressed during treatment. Side-effects were not prominent. This appears to be a very useful medication for a clinical problem which hitherto has been difficult to treat.

Androgen Antagonists↗
PubMed1976

Alterations in the fine structure of the prostate and seminal vesicle of rats treated with cyproterone acetate.

Young adult male rats were treated with daily injections of 10 mg of cyproterone acetate for periods up to 16 weeks. Samples of the ventral prostate and the seminal vesicle were studied with the light and electron microscopes. Alterations visible with the light microscope included decreases in cell size, cytoplasmic basophilia, the size of the nucleolus, and the amount of luminal secretory material. Ultrastructural changes in the epithelium of both glands involved mainly the organelles that participate in the formation of secretions. Large declines were observed in the abundance of rough endoplasmic reticulum, size of the Golgi apparatus, and number of secretory vacuoles. Lipid droplets accumulated in the seminal vesicle epithelium, and lysosomes were numerous in both glands. Changes were first observed microscopically in the seminal vesicle after one week and in the prostate after two or three weeks. Maximal development of the alteration occurred after treatment for approximately eight weeks.

Animals↗
PubMed1980

Use of low-dosage oral cyproterone acetate as a male contraceptive.

To ascertain the effects of low-dosage cyproterone acetate (CPA) on the reproductive and endocrine functions of normal men, 25 volunteers were given CPA 0, 5 or 10 mg daily over 16 weeks, preceded by 12 weeks pretreatment observation and followed by 24 weeks posttreatment follow-up. CPA caused a decrease in sperm concentration, percentage motility, proportion of normal sperm and ability of the sperm to penetrate a column of cervical mucus in most patients. In addition, circulating testosterone, estradiol, LH and FSH levels were significantly reduced during treatment. All these changes reverted to the pretreatment level upon drug withdrawal. These findings suggest that firstly, although low dosage CPA was able to induce changes in seminal analyses, azoospermia was present in only one out of 15 subjects exposed to the drug. Secondly, the marked decrease in androgen levels associated with CPA treatment renders CPA unsuitable as a single entity agent for long-term male contraception.

Adult↗
PubMed1980

Transfer of cyproterone acetate to the milk of lactating women.

Cyproterone acetate (CPA) was administered in a dose of 50 mg to 6 lactating women delivered by caesarean section. All women had to discontinue breast feeding the day before treatment. Prior to, and 3 and 9 hours after ingestion of the drug, plasma and milk specimens were taken. Total daily milk volume was recorded. Concentration of CPA in plasma and milk was determined by RIA. The plasma levels of CPA were in the range of 65 - 450 ng/ml at 3 h and 76 - 270 ng/ml after 9 hours. The respective concentrations in milk were 16 - 260 ng/ml (3 h) and 55 - 130 ng/ml (9 h). The plasma/milk ratio of drug concentration varied between 1.1 and 9.3 (3 h) and 0.6 and 2.9 (9 h). The mean of all values amounted to 2.8 +/- 2.3. Taking into account a daily milk production of 1050 +/- 230 ml, 0.2% of the dose administered (range: 0.06 - 0.41 % of dose) would have been transferred to the newborn. Use of the CPA-containing oral contraceptive DIANER (2 mg of CPA + 50 microgram of ethinyl estradiol) by nursing women would therefore result in the transfer of 1 microgram/kg to the child.

Adult↗
PubMed1990

Long-term treatment with the combination ethinylestradiol and cyproterone acetate in polycystic ovary syndrome.

This study evaluates the effect of therapy over a long period of time (36 cycles without interruption) with the monophasic combination containing 0.035 mg of ethinylestradiol and 2 mg of cyproterone acetate (EE35-CPA) on hormonal and clinical parameters of 66 patients with polycystic ovary syndrome (PCOS). During the administration of the pill a significant decrease in the LH/FSH ratio and in adrenal and ovarian androgens has been observed, as well as a significant increase of the Sex Hormone Binding Globulin (SHBG). The progressive decrease of the total androgenic activity explains the clinical results that have been obtained: at the 36th cycle of therapy acne disappeared in 100% of the cases, seborrea in 76.4% and hirsutism in 75%. Our results underline the need for a continuous administration without interruption of the pill with CPA in patients with clinical hyperandrogenic symptoms.

Acne Vulgaris↗
PubMed1977

Estrogen-induced sexual receptivity and localization of 3H-estradiol in brains of female mice: effects of 5 alpha-reduced androgens, progestins and cyproterone acetate.

Sexual receptivity induced in ovariectomized CD-1 mice with chronic daily administration of estradiol benzoate (E2 B) was blocked by concurrent administration of the 5 alpha-reduced androgen, dihydrotestosterone (DHT). Receptivity was restored in these females with progesterone-, but not with dihydroprogesterone-priming 6 hr prior to testing. Delaying the DHT injections until 12 hr after the E2 B injections greatly reduced its inhibitory properties. Receptivity in E2 B-primed females was also blocked by concurrent treatment with cyproterone acetate and 3 alpha-, but not 3 beta-adrostanediol. Pretreatment with DHT, or 3 alpha- or 3 beta-androstanediol failed to consistently affects 3H-estradiol accumulation in crude nuclear and supernatant fractions from brain and pituitary.

20-alpha-Dihydroprogesterone↗
PubMed1998

Low dose of cyproterone acetate and testosterone enanthate for contraception in men.

After a control phase, 10 normal men received cyproterone acetate (CPA) at a dose of 25 mg/day (CPA-25; n=5) or 12.5 mg/day (CPA-12.5; n=5) plus testosterone enanthate (TE) 100 mg/week, for 16 weeks. Throughout the study sperm counts were performed every 2 weeks, and luteinizing hormone (LH), follicle stimulating hormone (FSH), testosterone, biochemical and haematological tests were performed every 4 weeks. All five men in group CPA-25 and three men in group CPA-12.5 achieved azoospermia. One man in group CPA-25 was azoospermic by week 12 of hormone administration, but had a sperm count of 0.1 x 10(6)/ml at week 16. Time to azoospermia was 9.0+/-1.3 and 8.7+/-0.7 weeks in groups CPA-25 and CPA-12.5 respectively. Gonadotrophins were decreased by week 4 of hormone administration, remained around the minimum detectability of the assay for the duration of hormone administration and returned to baseline after stopping hormone administration. Testosterone values did not change. No change in any biochemical parameters was found. Haematological parameters were decreased at week 16 of hormone administration and returned to baseline after stopping hormone administration. In conclusion, these results suggest that an hormonal regimen consisting of testosterone plus a progestin with anti-androgenic properties holds promise as an effective, safe and reversible male contraceptive.

Adult↗
PubMed1982

Cyproterone acetate in the treatment of acne vulgaris in adult females.

22 adult females with therapy-resistant acne vulgaris were treated for 12 months with Diane, a drug containing cyproterone acetate and ethinylestradiol. Treatment was withdrawn in 7 patients because of side-effects of lack of of effect. In the remaining 15 patients, the treatment had extremely promising results, from 70 to 90% improvement of the acne. In a remarkably high number of patients, the androgen production, measured by the urinary excretion of fractional 17-ketosteroids, was elevated. None of these patients had signs of endocrinological diseases, in particular no cases of hirsutism of Stein-Leventhal syndrome were found. The current concept of the course of acne is that the conversion in the skin of testosterone to dehydrotestosterone is increased. The finding of an elevated urinary excretion of androgenic substances in this group of acne patients indicates that the pathogenesis is far more complicated.

17-Ketosteroids↗