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PubMed1998

Topical cyproterone acetate treatment in women with acne: a placebo-controlled trial.

OBJECTIVE: To evaluate the clinical and hormonal response of topically applied cyproterone acetate, oral cyproterone acetate, and placebo lotion in women with acne. DESIGN: Placebo-controlled, randomized study. SETTING: Patients were recruited from the Institute of Endocrine Cosmetics, Vienna, Austria. PATIENTS: Forty women with acne. INTERVENTIONS: Treatment with oral medication consisting of 0.035 mg of ethinyl estradiol and 2 mg of cyproterone acetate (n=12), 20 mg of topical cyproterone acetate lotion (n=12), and placebo lotion (n=16) was offered. Patients were assessed monthly for 3 months. MAIN OUTCOME MEASURES: Clinical grading according to acne severity and lesion counts as well as determinations of serum cyproterone acetate concentrations. RESULTS: After 3 months of therapy with topical cyproterone acetate, the decrease of mean facial acne grade from 1.57 to 0.67 was significantly better (P<.05) compared with placebo (which showed a change from 1.57 to 1.25), but not compared with oral medication (1.56 to 0.75) (P>.05). Lesion counts also decreased from 35.9 to 9.1 in the topical cyproterone acetate group compared with oral medication (45.4 to 15.5) (P>.05) and placebo (38.2 to 23.1) (P<.05). After topical cyproterone acetate treatment, serum cyproterone acetate concentrations were 10 times lower than those found after oral cyproterone acetate intake. CONCLUSIONS: The therapeutic effect of topically applied cyproterone acetate for acne treatment was clearly demonstrated. Topically applied sexual steroids in combination with liposomes are as effective as oral antiandrogen medication in acne treatment, while reducing the risk of adverse effects and avoiding high serum cyproterone acetate concentrations.

Acne Vulgaris↗
PubMed1986

Response of male acne to antiandrogen therapy with cyproterone acetate.

The antiandrogen cyproterone acetate, which is known to suppress sebum production, but is not a standard therapy, was given in combination with tetracycline to 63 young unmarried men who had failed to respond to 6 months' tetracycline therapy alone. Fifty-seven patients responded and the mean time to clearance was 5.2 months' therapy. The main side effects were nodular sub-nipple breast swellings, which occurred in 13 cases (21%). Such side effects were reversible and cleared after 3-4 months following cessation of therapy. Eighty-eight percent of patients relapsed within 3 months of discontinuing therapy.

Acne Vulgaris↗
PubMedDate not supplied

Chronopharmacokinetic behaviour of cyproterone acetate in rabbits.

Cyproterone acetate (CPA) is an antiandrogenic compound that shows a rhythmic toxicologic behaviour. The purpose of this study was to determine whether CPA pharmacokinetics in the rabbit were influenced by the administration time of day. Previously synchronised rabbits received a single intravenous dose of 4 mg kg(-1) of CPA at two hours after light onset (2 HALO) and 14 hours (14 HALO) after light onset. The drug concentration in plasma samples was determined by high performance liquid chromatography. The mean concentrations in plasma were significantly higher (P<0.05) in 2 HALO than in 14 HALO animals at five, 15 and 30 minutes after dosing. Both plasma concentration profiles were fitted to two-compartment open models. Mean A, Vc and Vss differed significantly between 2 and 14 HALO dosage (P<0.005). Temporal variations in plasma protein binding, drug distribution and in drug elimination may play an important role in explaining these results.

Animals↗
PubMed1984

Sexual maturation in male mice treated with cyproterone acetate from birth to puberty.

Cyproterone acetate was administered every 2 days from 1 to 39 days of age to male mice which were killed 24 h or 20 days after the last injection. Cyproterone acetate caused a significant reduction in the relative weights of the epididymis, vas deferens, seminal vesicle and preputial gland, which was still evident at 60 days after birth. Testicular and epididymal androgens (testosterone and dihydrotestosterone) and circulating LH and FSH concentrations were equal to or higher than those of controls at 60 days. Cyproterone acetate did not inhibit spermatogenesis but all males were infertile. The results suggest that the peripheral effects of testosterone are necessary, during early stages of sexual maturation, in order to obtain subsequent full development of the accessory sex organs.

Aging↗
PubMed1998

Antiandrogen withdrawal syndrome with cyproterone acetate.

OBJECTIVES: To determine whether the antiandrogen withdrawal syndrome occurs with the steroidal antiandrogen cyproterone acetate. METHODS: Cyproterone acetate was withheld in 12 patients with progressing androgen-independent metastatic prostate cancer. Eight patients had been receiving cyproterone acetate concomitant with androgen ablation, and in 4 patients it was prescribed after failure of androgen suppression. Time to response and to disease progression were defined by serum prostate-specific antigen (PSA) levels and imaging studies. RESULTS: PSA levels decreased in 5 of the 1 2 patients; in 4 of them (33%), the decrease exceeded 50%. The decline lasted a median of 24 weeks (range 9 to 37.8). All 5 patients had received initial concomitant exposure to androgen ablation and cyproterone acetate. CONCLUSIONS: We recommend that the steroidal antiandrogen cyproterone acetate be added to the list of agents capable of inducing antiandrogen withdrawal syndrome.

Aged↗
PubMed1980

Spermatogenesis and immune responsiveness to sheep red blood cells in guinea pigs treated with cyproterone acetate and testosterone.

The synthetic steroid antiandrogen, cyproterone acetate, and the androgen, testosterone isobutyrate, were injected subcutaneously into adult male and female guinea pigs of two outbred strains (laboratory coloured and albino Pirbright-Harley stocks). Cyproterone acetate was given as 1, 10 and 20 daily 5-mg doses (body-weight matched with immunosuppressively effective doses in mice) and as 30 doses of 15 micrograms/100 g b.w. (body-weight matched with those used in the long-term human male contraception), testosterone as 1 and 10 doses of 5 mg/100 g b.w. The guinea pigs of the two stocks used showed different sensitivity: with the same doses of CA albino guinea pigs compared to the coloured ones declined in weight, had lower viability, reduced thymus weight, diminished capacity for SRBC haemolysin formation, a lower testes weight and inhibited spermatogenesis. Both stocks reacted by similar lymphopoenia, however. Testosterone neither inhibited haemolysin formation nor produced lymphopoenia but induced a more marked reduction of thymus weight than did CA and, in addition, produced greater depletion of cortex lymphocytes in albino guinea pigs. The thymus of albino guinea pigs was more sensitive to testosterone than to cyproterone acetate. Sexual dimorphism was apparent in some criteria in albino guinea pigs following cyproterone acetate and testosterone. Cyproterone acetate in the lowest doses had no inhibitory effect on thymus or SRBC formation but also did not affect spermatogenesis in albino guinea pigs. The hitherto accepted classification of animal species according to which guinea pigs (and also man) belong to steroid-resistant species is discussed and questioned, and the potential risks of application of sexual steroids in male contraception are stressed.

Animals↗
PubMed1985

Permanent changes in the functional development of accessory sex organs and in fertility in male mice after neonatal exposure to cyproterone acetate.

Male mice were injected daily with cyproterone acetate for 10 consecutive days during one of the four following periods: 1-10 days, 11-20 days, 21-30 days or 31-40 days. At all stages studied cyproterone acetate caused a significant reduction in the relative weights of epididymis, vas deferens, preputial gland and seminal vesicle in males killed 24 h after the last injection; the androgen content (testosterone + dihydrotestosterone) of the accessory sex organs was also reduced but the differences were not always significant. Cyproterone acetate treatment from 1 to 10 days resulted in a definitive reduction in the relative weights of all accessory sex organs studied and when injected from 11 to 20 days in epididymis and vas deferens. When cyproterone acetate was injected after 20 days of age, the inhibition of sexual organ weights was reversible and at adulthood organs were normally developed. Cyproterone acetate treatment induced a high percentage of infertile males only when injected from 1 to 10 days. Spermatogenesis, androgen levels in plasma and accessory sex organs, and sexual behaviour were not affected in sterile males. These results suggest that the functional development of accessory sex organs can be permanently affected by short-term neonatal exposure to endogenous androgens.

Age Factors↗
PubMed1973

Androgen dynamics in vitro in the human prostate gland. Effect of cyproterone and cyproterone acetate.

Hyperplastic and adenocarcinomatous human prostatic tissue was superfused in vitro with radioactively labelled androst-4-ene-3,17-dione, testosterone and 5alpha-dihydrotestosterone (17beta-hydroxy-5alpha-androstan-3-one), with and without addition of the anti-androgens cyproterone and cyproterone acetate. Cyproterone competitively inhibited the entry of the androgens into the majority of the tissues, whereas cyproterone acetate increased this entry. These findings indicated that transport of androstenedione, testosterone and 5alpha-dihydrotestosterone into prostatic tissue is performed by a specific mechanism, possibly involving a carrier situated in the cell membrane. The extent of metabolism of the three androgens was also modified: formation of 5alpha-dihydrotestosterone from testosterone, and of the latter from androstenedione, was decreased by cyproterone and increased by the acetate. Acetate was more effective than cyproterone in decreasing the ;uptake' of the perfused androgens by the tissue; at the same time, it increased the androgen clearance from the tissue. As cyproterone acetate is the more potent of the two anti-androgens, the possibility that these findings in vitro are related to the different anti-androgenic potency exhibited by the two compounds in vivo is discussed. ;Uptake' of the two anti-androgens and the response to their action on androgen dynamics were similar in adenocarcinomatous and hyperplastic glands.

Acetates↗
PubMed1985

Comparison of the antiandrogenic/androgenic activities of flutamide, cyproterone acetate and megestrol acetate.

Flutamide is approximately 2-fold more potent than cyproterone acetate in reversing the stimulatory effect of dihydrotestosterone (DHT) on ventral prostate weight. Even at the highest dose of cyproterone acetate, prostate weight remains 40% above control while flutamide completely reverses the stimulatory action of DHT, thus suggesting some partial androgenic activity of cyproterone acetate. Megestrol acetate, on the other hand, is devoid of any antiandrogenic activity and it even increases the stimulatory effect of DHT on prostate weight. While flutamide completely reverses the inhibitory effect of DHT on plasma LH levels in castrated animals, cyproterone acetate reverses the value of this parameter by only 30% while megestrol acetate further inhibits plasma LH levels at all the doses used. Both cyproterone acetate and megestrol acetate inhibit adrenal weight to approximately 25% of control, thus indicating their glucocorticoid activity. As direct measure of androgenic activity, cyproterone acetate and megestrol acetate increased prostate weight in castrated animals by 60 and 100%, respectively (P less than 0.01) while flutamide had no effect. The present data show that cyproterone acetate and megestrol acetate, in addition to their well-known progestational and glucocorticoid action, have intrinsic androgenic activity. Since it is the only compound having pure antiandrogenic activity, flutamide provides the best scientific arguments for its successful use for the treatment of androgen-sensitive diseases.

Adrenal Glands↗
PubMed2003

Cyproterone acetate for hirsutism.

BACKGROUND: Hirsutism is a distressing and relatively common endocrine problem in women which may prove difficult to manage. Cyproterone acetate, an anti-androgen, is frequently used to treat hirsutism, usually in combination with ethinyl estradiol. OBJECTIVES: The objective of this review was to investigate the effectiveness of cyproterone acetate alone, or in combination with ethinyl estradiol, in reducing hair growth in women with hirsutism secondary to ovarian hyperandrogenism. SEARCH STRATEGY: The Cochrane Menstrual Disorders and Subfertility Group trials register was searched (last search - 4 June 2002). The Cochrane Menstrual Disorders and Subfertility Group register is based on regular searches of MEDLINE (1966 to 2002), EMBASE (1980 to 2002), CINAHL (1982 to 2002), PsycINFO (1987 to 2002) and CENTRAL (Issue 2, 2002 of the Cochrane Library) the handsearching of several journals and conference proceedings, and searches of several key grey literature sources. All publications of randomised controlled trials of cyproterone acetate with or without estrogen versus placebo or other drug therapies for hirsutism were identified. SELECTION CRITERIA: All randomised controlled studies comparing:- cyproterone acetate to placebo- cyproterone acetate with ethinyl estradiol to placebo- cyproterone acetate with ethinyl estradiol to cyproterone acetate alone- cyproterone acetate (with or without estradiol) to other medical therapies for treatment of hirsutism. DATA COLLECTION AND ANALYSIS: Eleven studies were identified which fulfilled the inclusion criteria. Nine randomised studies were included in the review, and two were excluded because of insufficient information. Only one study had more than 100 women included in the analysis. The major outcomes included: subjective improvement in hirsutism, changes in Ferriman Gallwey scores, changes in linear hair growth and hair shaft diameter, alterations in endocrine parameters, side effects to treatment, withdrawals during therapy MAIN RESULTS: There were no clinical trials comparing cyproterone acetate alone with placebo. There was one small study comparing cyproterone acetate in combination with ethinyl estradiol to placebo. In this study there was a significant subjective reduction in hair growth with cyproterone acetate therapy, although the confidence limits were large. There were no studies comparing cyproterone acetate alone with cyproterone acetate in combination with ethinyl estradiol to treat hirsutism. In studies where cyproterone acetate was compared to other drug modalities (ketoconazole, spironolactone, flutamide, finasteride, GnRH analogues) no difference in clinical outcome was noted. There were, however, endocrinological differences in androgen and estrogen levels between different drug therapies. There were insufficient data to assess differences in side effects between women treated with cyproterone acetate and other medical therapy. REVIEWER'S CONCLUSIONS: Cyproterone acetate combined with estradiol results in a subjective improvement in hirsutism compared to placebo. Clinical differences in outcome between cyproterone acetate and other medical therapies were not demonstrated in the studies included in this review. This may be because of the small size of the studies, lack of standardized assessment and lack of objective determinants of improvement in hirsutism. The endocrinological effects of the different drug therapies reflect the mode of action. Larger carefully designed studies are needed to compare efficacy and safety profiles between drug therapies for hirsutism.

Androgen Antagonists↗
PubMed2003

Glucocorticoid receptor antagonism by cyproterone acetate and RU486.

The steroid compound cyproterone acetate was identified in a high-throughput screen for glucocorticoid receptor (GR) binding compounds. Cyproterone (Schering AG) is clinically used as an antiandrogen for inoperable prostate cancer, virilizing syndromes in women, and the inhibition of sex drive in men. Despite its progestin properties, cyproterone shares a similar pharmacological profile with the antiprogestin mifepristone (RU486; Roussel Uclaf SA). The binding affinities of cyproterone and RU486 for the GR and progesterone receptor were similar (K(d), 15-70 nM). Both compounds were characterized as competitive antagonists of dexamethasone without intrinsic transactivating properties in rat hepatocytes (K(i), 10-30 nM). In osteosarcoma cells, RU486 revealed a higher potency than cyproterone acetate to prevent responses to dexamethasone-induced GR transactivation and NF kappa B transrepression. Upon administration to Sprague-Dawley rats, both compounds were found to be orally bioavailable and to inhibit transactivation of liver GR. Molecular docking of cyproterone acetate and RU486 into the homology model for the GR ligand binding domain illustrated overlapping steroid scaffolds in the binding pocket. However, in contrast to RU486, cyproterone lacks a bulky side chain at position C11 beta that has been proposed to trigger active antagonism of nuclear receptors by displacing the C-terminal helix of the ligand-binding domain, thereby affecting activation function 2. Cyproterone may therefore inhibit transactivation of the GR by a molecular mechanism recently described as passive antagonism. New therapeutic profiles may result from compounds designed to selectively stabilize the inactive and active conformations of certain nuclear receptors.

Androgen Antagonists↗
PubMed1986

[Inhibition of ovulation with 35 micrograms of ethinyl estradiol and 2 mg of cyproterone acetate (Diane 35)].

In the study reported here the ovulation inhibition dose for cyproterone acetate was determined. Experiments showed that the ovulation inhibition dose is 1 mg of cyproterone acetate, administered daily. Results proved that the cyproterone acetate dose cannot be reduced when cyproterone acetate is combined with ethinyl estradiol. However, the objective of this study was to determine whether it is possible to reduce the estrogen dose to 35 micrograms when the common combination of 2 mg cyproterone acetate and ethinyl estradiol is being used. After a control menstruation cycle, 2 mg cyproterone acetate and 35 micrograms ethinyl estradiol were administered daily to six women with normal menstruation. Drug administration began on Day 5 and ended on Day 25. During the control cycle, the first treatment cycle, and the third treatment cycle, LH, FSH, 17 beta estradiol, progesterone, testosterone, prolactin, and SHGB were examined daily. Cervix score and karyopyknosis index were determined at the same time. In addition, antithrombin III was examined during the control cycle and during the third treatment cycle. Present results show that ovulation inhibition is possible with dose reduction of ethinyl estradiol to 35 micrograms, combined with 2 mg of cyproterone acetate. Increase in SHBG and reduction in testosterone serum level point to an additional antiandrogenic effect of cyproterone acetate, aside from its cellular effect. The combined preparation discussed here does not bring about any changes in antithrombin III values. Results permit the conclusion that ovulation inhibition is insured with a reduction of the daily estrogen dose from 50 micrograms to 35 micrograms.

Adult↗
PubMed1981

Oestrogenic activity of cyproterone acetate in female mice.

Effects of cyproterone acetate, a synthetic steroidal compound, on the reproductive organs of female mice 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 animals taking uterine weight, vaginal keratinization and other biochemical oestrogen sensitive parameters. Cyproterone acetate in ovariectomized animals induced vaginal keratinization increase in uterine weight and uterine protein, RNA, glycogen and sialic acid contents. These effects were parallel to the effects of oestradiol dipropionate in ovariectomized animals, thus indicating oestrogenic activity of the compound.

Animals↗
PubMed1990

Severe hepatitis caused by cyproterone acetate.

A case of severe acute hepatitis caused by cyproterone acetate in a 71 year old man with prostatic carcinoma is reported with a review of the literature on hepatic reactions to this drug. The association between the use of cyproterone acetate and liver abnormalities is poorly documented. This is the fourth published report of adverse hepatic reaction to cyproterone acetate and it substantiates other evidence that cyproterone acetate is potentially hepatotoxic. Monitoring of liver function tests should be mandatory in patients receiving high doses of cyproterone acetate; the drug should be withdrawn immediately if abnormal liver function tests are found.

Adenocarcinoma↗
PubMed1980

Endocrine effects of cyproterone acetate in patients with prostatic cancer.

Cyproterone acetate was given to patients with stages C and D prostatic cancer and its effect on endocrine parameters was studied. At a daily oral dose of 100 mg. cyproterone acetate induced marked reduction in the size and consistency of tumor, while it caused moderate suppression of serum luteinizing hormone, follicle-stimulating hormone and testosterone levels. Elevation of serum prolactin levels was observed after treatment with cyproterone acetate but was to a lesser degree than that caused by estrogens.

Aged↗
PubMed1977

Some effects of cyproterone and cyproterone acetate on the reproductive physiology of the male rat.

Male rats were treated with 5 or 20 mg cyproterone acetate/kg/day or 20 mg cyproterone/rat/day for 1, 2, 3, 4, or 5 weeks. There was some reduction in fertility with both compounds, the maximum effect occurring after 5 weeks with the higher dose of cyproterone acetate and after 2 weeks with cyproterone. A significant increase in testosterone levels was found after treatment with the high dose of cyproterone acetate by 1 week and with cyproterone by 2 weeks. Dose-dependent atrophy of the seminal vesicles occurred after treatment with cyproterone acetate; with cyproterone atrophy occurred at 1 and 2 weeks but approximated to control values at 3, 4 and 5 weeks. Epididymal weights were reduced with the high dose of cyproterone acetate but the low dose had little effect. Reduction in the weight of the testes was only observed after 5 weeks of treatment with the high dose of cyproterone acetate. Since plasma testosterone levels were not depressed below normal values, accessory sex organ regression evidently resulted from the local antiandrogenic action of the drugs. There was some indication of interference with the secretory and absorptive activity of the lining cells of the epididymis but in general treatment with either steroid caused only relatively small and variable changes in the composition of epididymal plasma.

Animals↗
PubMed1995

Accumulation and persistence of DNA adducts of the synthetic steroid cyproterone acetate in rat liver.

Cyproterone acetate (CPA) is a synthetic steroid which is widely used in antiandrogenic and gestagenic drugs. We have recently shown that CPA induces DNA adducts in cultured rat hepatocytes and in rat liver (1). In the present investigation, we studied the persistence and accumulation of CPA-derived DNA adducts in the liver of rats using the 32P-postlabeling technique. To study the persistence of CPA-DNA adducts, rats were treated with a single oral dose of 10 (female rats) or 100 mg CPA/kg body wt (male rats). Four DNA adducts were detected in the liver of both gender. In female rats, maximal total DNA adduct levels of 3.40 +/- 0.04 adducts/10(6) nucleotides were observed after 1 week. Eleven weeks later, 40% of the adducts determined after 1 week were still detectable. In male rats, maximal hepatic DNA adduct levels of approximately 98 +/- 3/10(9) nucleotides were attained after 2 weeks. The adduct level decreased during the following 4 weeks to approximately 40% of the earlier observed maximal level. To study the accumulation of the CPA-DNA adducts, rats were treated daily with a low oral dose of 50 micrograms CPA/kg body wt for 42 days. During this treatment period, the level of the four adducts increased continuously from approximately 10 to approximately 380 adducts/10(9) nucleotides in the liver of female rats. DNA adducts were formed at much lower levels in male rats; only one type of DNA adduct was detectable, the level of which increased to approximately 6 adducts/10(9) nucleotides after 42 days. In conclusion, CPA induces DNA adducts in rat liver; binding of the steroid is much higher in female compared to male rats. The CPA-DNA adducts show a high persistence and as a consequence of their long half life, CPA-DNA adducts accumulate significantly in the liver of rats.

Androgen Antagonists↗
PubMed2002

Shortness of breath: an uncommon side-effect of cyproterone acetate in the treatment of androgenetic alopecia.

Cyproterone acetate is indicated for treatment of acne, hirsutism, seborrhea, and androgenetic alopecia in females. In general this medication is well tolerated in standard doses. Shortness of breath has been previously reported in men with prostatic carcinoma, receiving high-dose (200 mg/day) treatment with cyproterone acetate. We report a 66-year-old lady taking 50 mg/day of cyproterone acetate for biopsy proven androgenetic alopecia, who developed this unusual complication of shortness of breath. To our knowledge it has not been previously reported in women undergoing treatment for androgenization.

Aged↗