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PubMed1989

Comparison of cyproterone acetate and danazol in the treatment of pelvic pain associated with endometriosis.

Twenty-three patients with laparoscopically diagnosed endometriosis and pelvic pain were allocated randomly to treatment with cyproterone acetate 27 mg plus ethinyl estradiol 0.035 mg/day (11 patients) or danazol 600 mg/day (12 patients). All women received treatment for 6 months, except for one in the cyproterone group who suspended treatment for nonmedical reasons and was excluded from analysis of the results. The clinical condition and pain symptoms were monitored in all patients for 1 year after treatment suspension. The intensity of pelvic pain at diagnosis, during treatment, and at follow-up was evaluated by a multidimensional verbal score and an analogue scale. At the end of treatment, a repeat laparoscopy was performed in those patients who agreed (four in the cyproterone group, five in the danazol group); the results showed a partial regression of endometriotic lesions in both groups, with no significant differences between them. Dysmenorrhea disappeared in all patients during treatment. At 6 months after suspension, dysmenorrhea recurred in 66% of the cyproterone group and 58% of the danazol group, and at 1 year in 89 and 92%, respectively. Intermenstrual pelvic pain improved markedly during treatment in both groups; 6 months after treatment withdrawal it was present in four cyproterone subjects and four danazol group patients, whereas after 1 year, only one woman in the danazol group did not have this symptom. Deep dyspareunia was less affected by treatment, and 6 months later had recurred in all the women.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
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of liver function tests should be mandatory in patients receiving high doses of cyproterone acetate; the drug should be withdrawn immediately if abnormal liver function tests are found.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↗
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↗
PubMed1991

Use of cyproterone acetate in prostate cancer.

Cyproterone acetate is a progestational antiandrogen with potent antigonadotropic activity that results in rapid suppression of serum testosterone. Used as a single agent, cyproterone acetate yields a total androgen blockade. It may be combined with low-dose diethylstilbestrol, orchiectomy, or LHRH agonists to improve, in theory, the results of such therapy. In clinical testing, cyproterone acetate has proved equivalent to diethylstilbestrol with markedly less toxicity. It is useful in conjunction with LHRH agonists, either transiently to block the flare phenomenon, or continuously to block peripheral androgen receptors; the necessity for this latter action has not yet been proved. Cyproterone acetate may afford transient objective improvement in patients not responding to other forms of hormone deprivation. Experience in this role is limited. The drug may be used to suppress the hot flushes associated with orchiectomy or LHRH agonist therapy. Cyproterone acetate induces local tumor regression; owing to its reversible effects, it is useful as neoadjuvant or adjuvant androgen withdrawal therapy in patients with lower-stage disease undergoing radical surgery or radiotherapy. Adverse effects are mostly those related to hormone withdrawal, namely, impotence, infertility, and lassitude. Gynecomastia and breast tenderness occur in less than 18% and cardiovascular complications in approximately 10% of treated men.

Androgen Antagonists↗
PubMed1988

Rat prostatic weight regression in reaction to ketoconazole, cyproterone acetate, and RU 23908 as adjuncts to a depot formulation of gonadotropin-releasing hormone analogue.

The effects of the s.c. administration of a depot formulation of the luteinizing hormone-releasing hormone (LHRH) analogue Zoladex were studied in normal male rats, alone and in combination with three drugs with "antiandrogenic" action (ketoconazole, cyproterone acetate, and RU 23908) on prostatic weight and on circulating hormone levels in order to investigate whether these antiandrogens might prevent the LHRH-A-induced initial increase in these parameters. These effects were compared with those caused by surgical castration. In addition the effects of the antiandrogens on the activity of the hypothalamic-pituitary-adrenal axis were investigated. The depot LHRH analogue caused an initial increase in ventral prostatic weight after 4 days but suppressed the prostatic and testicular weights, the pituitary luteinizing hormone (LH) content, and plasma LH and testosterone levels after 10 and 17 days. All three antiandrogenic drugs used prevented the initial LHRH analogue-induced rise in prostatic weight, while RU 23908 suppressed its weight after only 4 days. After 10 and 17 days cyproterone acetate and RU 23908 had a similar significantly greater suppressive effect on prostatic and testicular weights than the LHRH analogue alone, while the additive inhibitory effect of ketoconazole was smaller. Surgical castration suppressed prostatic weight significantly more after 4 days, while its effects after 10 and 17 days were similar to that exerted by the combination of LHRH-A and RU 23908. The antigonadotropic effect of cyproterone acetate and the indirect gonadotropin-stimulating effects of ketoconazole and RU 23908 were not recognized in rats simultaneously treated with the LHRH analogue and did not interfere with the LHRH analogue-induced rapid depletion of the pituitary LH content and the decrease in circulating LH and testosterone levels. The LHRH analogue stimulated circulating progesterone and suppressed 17-hydroxyprogesterone levels. Ketoconazole and cyproterone acetate caused disorders in the pituitary-adrenal axis via different mechanisms: ketoconazole caused adrenal hypertrophy with normal circulating corticosterone levels caused by a compensatory increase in ACTH secretion; while cyproterone acetate exerted glucocorticoid-like effects causing a depletion of the pituitary adrenocorticotropic hormone content, adrenal atrophy, and lowered corticosterone levels. The addition of RU 23908 did not change the LHRH agonist-induced changes in adrenocortical activity.(ABSTRACT TRUNCATED AT 400 WORDS)

Adrenocorticotropic Hormone↗
PubMed1986

Testosterone-induced DNA synthesis in cultured rat ventral prostate. I. Effects of cyproterone acetate.

Testosterone-induced DNA synthesis in cultured rat ventral prostate was evaluated as an in vitro model for screening the direct effects of anticancer agents on prostatic growth. Optimal conditions for this bioassay, particularly the concentration of testosterone, were established using the inhibitory effects of cyproterone acetate on testosterone-induced 125iododeoxyuridine (I-UdR) uptake as an index of DNA synthesis inhibition. Using 4 X 10(-7) M testosterone, only the highest concentration (X 10(-5) M) of cyproterone acetate inhibited I-UdR uptake and histological observations indicated that this was due to a non-specific cytotoxic effect. In contrast, cyproterone acetate had a dose-dependent inhibitory effect on the proliferative response to 4 X 10(-9) M testosterone. Cyproterone acetate (4 X 10(-7) M) combined with 4 X 10(-9) M testosterone exerted an inhibitory effect on I-UdR uptake and caused epithelial atrophy indicative of androgen deprivation. The results are consistent with similar in vivo studies and confirm the hypothesis that cyproterone acetate acts by directly antagonising testosterone action at the target tissue level. Thus, this in vitro method provides a useful model for screening the direct effects of antiprostatic drugs.

Androgen Antagonists↗
PubMed1981

Effect of cyproterone acetate and its metabolites on the adrenal function in man, rhesus monkey and rat.

The effect of oral administration of 17 alpha-acetoxy-6-chloro-1,2 alpha-methylene-4,6]pregnadiene-3,20-dione (cyproterone acetate, Androcur) on the adrenal function in male hypersexual subjects and in female rhesus monkey was investigated on the basis of cortisol and ACTH levels in serum or plasma and excretion of cortisol and 17-ketosteroids. In addition, cyproterone acetate and its main metabolite alcohol of the main metabolite were characterized for treatment of male hypersexual subjects and female rhesus monkeys did not reveal any signs of adrenal suppression. Cyproterone acetate and its metabolites gave on indication of any appreciable anti-inflammatory effect in the adjuvant edema test in rats. However, there was a general increase in the level of blood glucose and liver glycogen as well as a reduction in body weight and organ weight (spleen, thymus and adrenal) in rats, in which 15 beta-hydroxy cyproterone was slightly more active with the exception of adrenal weight tests. It can be concluded that adult man and rhesus monkey are much less sensitive, is so at all, to some corticosteroid-like activities of cyproterone acetate and its main metabolites than the rat.

17-Ketosteroids↗
PubMed2002

Cyproterone acetate versus a continuous monophasic oral contraceptive in the treatment of recurrent pelvic pain after conservative surgery for symptomatic endometriosis.

OBJECTIVE: To evaluate the efficacy and safety of cyproterone acetate versus an oral contraceptive in the treatment of endometriosis-associated recurrent pelvic pain. DESIGN: Randomized controlled trial. SETTING: Academic center. PATIENT(S): Ninety women with recurrent moderate or severe pelvic pain after conservative surgery for symptomatic endometriosis. INTERVENTION(S): Six months of continuous treatment with oral cyproterone acetate, 12.5 mg/d, or an oral contraceptive containing ethinyl estradiol, 0.02 mg, and desogestrel, 0.15 mg. MAIN OUTCOME MEASURE(S): Degree of satisfaction with therapy. RESULT(S): Six patients in the cyproterone acetate arm and nine in the oral contraceptive arm withdrew because of side effects (n = 9), treatment inefficacy (n = 4), or loss to follow-up (n = 2). At 6 months, dysmenorrhea, deep dyspareunia, and nonmenstrual pelvic pain scores were substantially reduced, and significant improvements were observed in health-related quality-of-life, psychiatric profile, and sexual satisfaction; no major between-group differences were seen. Subjective and metabolic side effects were limited. According to an intention-to-treat analysis, 33 of 45 (73%) of patients in the cyproterone acetate group and 30 of 45 (67%) in the oral contraceptive group were satisfied with the treatment received. CONCLUSIONS: Both cyproterone acetate and a continuous monophasic oral contraceptive were effective, safe, and inexpensive therapy for recurrent pain after conservative surgery for endometriosis.

Adult↗
PubMed2003

Use of cyproterone acetate, finasteride, and spironolactone to treat idiopathic hirsutism.

OBJECTIVE: To compare the effectiveness of cyproterone acetate, finasteride, and spironolactone in the treatment of idiopathic hirsutism. DESIGN: Prospective randomized clinical study. SETTING: University hospital. PATIENT(S): Forty-one women (median age, 21 years [range, 18-34 years]) with idiopathic hirsutism who had requested to use an oral contraceptive. INTERVENTION(S): Patients were randomly assigned to receive cyproterone acetate (12.5 mg/d for the first 10 days of the cycle), finasteride (5 mg/d), or spironolactone (100 mg/d) for 12 months. Follow-up was done at the end of therapy. MAIN OUTCOME MEASURE(S): Ferriman-Gallwey score before treatment, at 6 and 12 months of treatment, and 1 year after the end of treatment, and androgenic profile before and after treatment. RESULT(S): At the end of therapy, the Ferriman-Gallwey score decreased by 38.9%, 38.6%, and 38.5% in patients who used cyproterone acetate, finasteride, and spironolactone, respectively. One year after therapy, the Ferriman-Gallwey score of patients who used spironolactone was significantly lower (6.74 +/- 1.41) than that of patients who used either cyproterone acetate (7.92 +/- 1.08), or finasteride (9.08 +/- 0.99). The androgenic profile did not change significantly during treatment. CONCLUSION(S): In patients with idiopathic hirsutism, the short-term results of treatment with cyproterone acetate, finasteride, and spironolactone are similar, but spironolactone is effective for a longer time.

17-alpha-Hydroxyprogesterone↗
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↗
PubMed1998

Tissue distribution of sex steroids: concentration of 17beta-oestradiol and cyproterone acetate in selected organs of female Wistar rats.

The tissue distribution of 17beta-oestradiol and cyproterone acetate was investigated after intravenous and intragastric administration to female Wistar rats by measuring the time course of the concentration of the sex steroids in plasma, liver, kidney, brain, and heart by radioimmunoassay. Test substances were administered intravenously in doses of 0.1 mg/kg each and intragastrically in doses of 10 mg/kg (17beta-oestradiol) and 0.1 mg/kg (cyproterone acetate) corresponding to the expected oral bioavailability. Tissue distribution was assessed within each mode of administration by AUCorgan/AUCplasma-quotients (Q-values), and between both routes of administration by F-values representing (bio- and organ availability) and R-values, which express the organ load after intragastric compared to intravenous administration if the same amount of drug has been made bioavailable in the plasma after both routes (for explanation see next page). The absolute bioavailability of 17beta-oestradiol after intragastric administration of 10 mg/kg was ca. 8%. The oestradiol liver load after intragastric administration was about 20 times higher than after intravenous administration, whereas the drug load of other organs was independent of the administration route. Cyproterone acetate was completely bioavailable after intragastric administration in a dose of 0.1 mg/kg. Cyproterone acetate levels and AUC-values in all organs investigated were higher when compared to the plasma with highest levels in the liver. The organ distribution of cyproterone acetate including the drug liver load was independent of the route of administration.

Androgen Antagonists↗
PubMed2001

Acute hepatitis induced by cyproterone acetate.

OBJECTIVE: To report a case of acute hepatitis resulting from the use of cyproterone acetate, an adjuvant treatment for prostate cancer. CASE SUMMARY: An 87 year-old white man, admitted to surgery for prostate cancer, received cyproterone acetate 300 mg/d orally and developed acute hepatitis, which initially was diagnosed clinically. A liver biopsy showed changes suggestive of acute cholestatic hepatitis. Cyprotorone was stopped immediately, and the patient was subsequently treated with corticosteroids. He then improved rapidly. DISCUSSION: Cyproterone acetate is thought to be well tolerated, but some authors have reported severe hepatic reactions, in particular acute hepatitis, fatal fulminant hepatic failure, and hepatocellular carcinoma. The above-mentioned hepatotoxicity represents an idiosyncratic drug reaction, probably due to the hepatomitogen action of cyproterone, causing an increase of hepatocytes expressing placental glutathione S-transferase, which are considered preneoplastic elements. CONCLUSION: This case suggests the possibility of hepatotoxicity from cyproterone.

Adenocarcinoma↗
PubMed1979

Plasma levels of active ingredients after single and repeated administration of a new oral contraceptive containing 2 mg of cyproterone acetate and 50 micrograms of ethinyl estradiol (DIANE) to five young women.

Peripheral plasma from five young women was analyzed for cyproterone acetate and ethinyl estradiol during a period of 96 hours duration after single oral intake of a coated tablet of DIANE (2 mg of cyproterone acetate + 50 micrograms of ethinyl estradiol), and during a treatment cycle of 21 days during which the formulation was given daily. Radioimmunoassays were utilized for quantifications. A maximum concentration of 11.0 +/- 3.4 ng of cyproterone acetate/ml plasma was found 1.6 +/- 0.6 hours after a single administration of DIANE. Postmaximal disposition took place in two phases with half-lives of 1.9 +/- 0.6 hours and 2.2 +/- 0.2 days. The maximum level of 0.08 +/- 0.03 ng of ethinyl estradiol/ml plasma was found 1.6 +/- 0.6 hours after such single administration. Following commencement of a daily oral intake of DIANE a steady state was reached by the 5th to 8th days, during which 24 hours after each dose cyproterone acetate concentrations were found to be 2.4 +/- 0.7 times higher than at the corresponding time after a single administration. Accordingly, after the first third of the 21 day treatment cycle an almost constant plasma level was reached indicating an equilibrium of intake and elimination. Except for a change in the mean terminal half life after multiple dosing, there was evidently no change in the kinetics of cyproterone acetate. No pointers to an accumulation of ethinyl estradiol upon daily administration of DIANE could be found.

Adult↗
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↗
PubMed1979

Effect of cyproterone acetate on the genital organs of female rats.

Effects of cyproterone acetate, a synthetic steroidal compound, on the reproductive organs of female rats have been investigated. This agent causes reduction in 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 oestrogen sensitive biochemical 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 effect of oestradiol dipropionate in ovariectomized animals, thus indicating oestrogenic activity cyproterone acetate. The histological and biochemical parameters lead to the conclusion that cyproterone acetate possessed antifertility property due to its inherent oestrogenic nature.

Adrenal Glands↗
PubMed1986

Comparison of diethylstilbestrol, cyproterone acetate and medroxyprogesterone acetate in the treatment of advanced prostatic cancer: final analysis of a randomized phase III trial of the European Organization for Research on Treatment of Cancer Urological Group.

Patients with previously untreated category T3 to T4 Mo or Ml prostatic cancer were allocated randomly to receive 250 mg. cyproterone acetate per day, a loading dose of 500 mg. medroxyprogesterone acetate intramuscularly 3 times weekly for 8 weeks followed by 100 mg. orally twice daily, or 1 mg. diethylstilbestrol 3 times daily in a phase III trial (protocol 30761) performed by the genitourinary tract cooperative group of the European Organization for Research on the Treatment of Cancer. Of 236 patients entered 210 were eligible: 75 received cyproterone acetate, 71 medroxyprogesterone acetate and 64 diethylstilbestrol. Local and distant tumor response, time to progression, survival and toxicity were assessed. Patients treated with medroxyprogesterone acetate had a less favorable course with a shorter duration of survival and time to progression than those treated with the other 2 drugs. There was no significant difference between diethylstilbestrol and cyproterone acetate. Cardiovascular side effects were reported more often in patients treated with diethylstilbestrol than in those treated with cyproterone acetate but severe and lethal cardiovascular toxicity was relatively low in all groups. Other side effects were negligible. Further studies are required to establish the influence of effective hormonal treatment upon survival.

Aged↗
PubMed1986

Effect of a new topically active antiandrogen (RU 38882) on the rat sebaceous gland: comparison with cyproterone acetate.

RU 38882 is a new antiandrogen. When given by subcutaneous or oral route, RU 38882 is about 25 times less potent than cyproterone acetate. However, when applied topically to the intact rat skin, RU 38882 (0.25-25 mg/rat/day for 5 days or 3 weeks) decreases, in a dose-related manner, the volume density of the smooth endoplasmic reticulum vesicles of the differentiating cells of the sebaceous gland, a structure directly involved in sebum lipid synthesis. Under these conditions RU 38882 is about 100 times more potent than cyproterone acetate and unlike cyproterone acetate, does not modify the prostate weight. The lack of efficacy of cyproterone acetate on the sebaceous gland could be due to its partial androgenic activity while RU 38882, under these conditions, acts as a pure antiandrogen which inhibits the nuclear androgen-receptor translocation.

Administration, Topical↗
PubMed1980

[Bioavailability of cyproterone acetate after oral and intramuscular application in men (author's transl)].

Cyproterone acetate was administered orally and intramuscularly to 5 male patients. The level of the active substance in plasma was monitored at intervals during the period of application using radioimmunoassay specific for cyproterone acetate. The areas under the drug level curves were similar after oral and intramuscular application of cyproterone acetate when taking into consideration the different doses used. Accordingly, cyproterone acetate is not dependent upon a "first-pass" effect. The bioavailability of the active substance was complete following oral application.

Administration, Oral↗