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PubMed2006

Hepatotoxicity induced by cyproterone acetate: a report of three cases.

Cyproterone acetate (CPA) is a steroidal synthetic progestagen and anti-androgenic compound widely administered in prostate cancer which has been evidentially correlated with a severe hepatotoxic potency. Three male patients aged 78-83 years are presented, in whom severe hepatotoxic reactions emerged after CPA administration. Patients were treated with CPA at the doses of 200-300 mg/d for malignant prostate disease for 3-12 mo prior to the acute manifestation of the hepatic disease. Clinical features compatible with mixed hepatocellular and cholestatic liver disease including jaundice, white stools and dark urine, manifested in all three cases whereas encephalopathy and ascites were present in two of the patients. Other primary causes of hepatotoxicity (alcohol consumption and viral hepatitis) were also verified in two cases, and in those patients biopsy findings revealed the presence of cirrhotic lesions in liver parenchyma. Discontinuation of the therapeutic agent led to the amelioration of the clinical profile in all the patients whereas a patient died 40 d after hospital admission due to sepsis, despite acute liver disease improvement. The current article highlights the hepatotoxic potency of a widely administered therapeutic agent and illustrates the importance of clinical surveillance especially in patients with previous hepatic diseases. Three relevant cases are reported and a review of the published literature is made.

Aged↗

PubMed1983

[The mechanism of action of cyproterone acetate in the treatment of hirsutism].

Cyproterone acetate (CPA) in association with percutaneously offinistered estradiol has been used for the treatment of 150 hirsute patients for periods ranging from 6 months to 3 years. A spectacular clinical improvement ensued. Plasma testosterone (T) and androstenedione (A) fell from 69 +/- 24 to 33 +/- 8 and 210 +/- 103 to 119 +/- 25 ng/dl (mean +/- SD) respectively after 3 months of treatment and remained low thereafter. In contrast, T glucuronide (Tg) and 3 alpha-androstanediol (Adiol) remained high during the whole course of treatment: 37 +/- 9 and 115 +/- 43 micrograms/24 h respectively. In vitro T 5 alpha-reductase activity (5 alpha-R) in pubic skin decreased from 147 +/- 34 to 79 +/- 17 fmol/mg skin after 1 year of treatment. To elucidate the discrepancy between plasma and urinary androgens levels, T production rate (PR) and metabolic clearance rate (MCR) were measured with the constant infusion technique in 6 patients before and after 6 months of treatment. PR decreased from 988 +/- 205 to 380 +/- 140 micrograms/24 h (mean +/- SD). In contrast MCRT increased from 1275 +/- 200 to 1632 +/- 360 1/24 h; this increase in MCRT explains the striking plasma T concentration fall and the high TG and Adiol excretion relative to the decrease in PR. Antipyrine clearance rate (n = 8) increased from 36.3 +/- 5.2 to 51.5 +/- 7.4 ml/min whereas urinary/6 beta hydroxycortisol remained unchanged. In conclusion, CPA acts through several mechanisms:(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗

PubMed2000

[Long-term side-effects following cyproterone acetate containing therapy in gynecology].

It has been suggested that cyproterone acetate (CPA) has a mutagenic potency. It has been postulated that a threshold dosage of CPA has mutagenic effects, but in the same way data have been published documenting that a continuous low dosage of cyproterone acetate leads to a reduction of mutagenic episodes. Despite published data about higher levels of DNA adduct creations due to CPA an international multicentre study analysing 2,506 patients with 7,971 patient-years that used CPA could not find any liver cell cancers, even if due to epidemiological data 6 liver cell cancers should have occurred upon this study group. The present study deals with the evaluation of 57 women which received CPA in combination with EE2 11-13 years before. The daily dosage was 2 mg CPA in combination with 35 mg or 50 mg EE2. In Germany these drugs were registered under the name of Diane 35 or Diane 50. Long-term follow-up evaluation concerning side effects, especially the appearance of liver cell carcinomas, were the aim of this study. With the records of 32% (18/57) of the above mentioned patient group the following long-term follow-up side effects could be observed: 1) weight gain, 2) headache, 3) migraine, 4) gastrointestinal disorders, 5) mood affections/depressions, 6) oedema of the legs, 7) skin affections, 8) mastodynia. No benign liver tumor or liver cell carcinoma was detected upon our group of investigated patients. In conclusion we can affirm that the use of CPA in a dosage of 2 mg per day does not lead to serious side effects under long-term follow-up observation conditions and that it's use does not correlate with a higher appearance of liver cell carcinomas.

Adult↗

PubMed1976

Fine structure of the testis and epididymis of rats treated with cyproterone acetate.

Adult male rats were administered the antiandrogen, cyproterone acetate, for 4, 8 or 12 weeks, and the histology and fine structure of the testis and several parts of the epididymis were studied. After treatment for 8 or 12 weeks, the testes of treated animals displayed a great reduction in the abundance of late spermatids. Necrotic cells, many of which were identified as cap-phase spermatids, were present in the seminiferous epithelium. Sertoli cells contained many large lipid droplets and lysosome-like structures with a content of cellular debris, including parts of spermatids. Leydig cells of treated rats were smaller than those of control animals at all the intervals studied. Sperm were absent from the lumen of the middle segment, or caput epididymidis, of severely affected specimens. In the terminal segment, or cauda epididymidis, the microscopic appearance varied in different regions. In the proximal part of the cauda epididymidis, the lumen was usually clear of sperm. The epithelium was tall and the light cells were very large and distended with many dense bodies resembling lysosomes. In contrast, in the distal part of the cauda epididymidis, the lumen was filled with sperm and debris, which appeared to be derived from germ cells. It is suggested that the light cells of the epididymal epithelium may have a role in clearing the lumen in the proximal part of the cauda epididymidis, in which they are particularly large and numerous. The results suggest that in the presence of cyproterone acetate, germ cells develop up to a cap-phase spermatids and then begin to undergo degeneration and death. This alteration may have an important role in the antifertility effect of the drug, but changes in the epididymis may contribute also.

Animals↗

PubMed1977

Effect of short-term cyclic administration of cyproterone acetate on pituitary-ovarian function in the human.

Short courses of cyproterone acetate, a compound with progestational and antiandrogenic activities, were administered to normally menstruating women during different phases of the menstrual cycle to suppress growth and maturation of the follicles and corpus luteum function. Postovulatory administration of 20 mg of the drug daily for 8 days to two women delayed menstruation by 4 to 6 days, followed by prolonged bleeding and short post-treatment cycles. Plasma levels of progesterone were suppressed temporarily during therapy, but increased immediately after cessation of treatment. Administration of 10 mg of the drug for 8 days during the early follicular phase to two women resulted in irregular bleeding, short cycles, and decreased plasma levels of progesterone throughout the cycle. Reduction of the dose to 2.5 mg during the early follicular phase in two other women also resulted in irregular cycles. When the 2.5-mg dose was administered to three women from the 8th to the 15th days of the cycle, vaginal bleeding and cycle length were normal. Plasma levels of luteinizing hormone and progesterone were suppressed during therapy. In one subject, cervical mucus was found to be hostile to sperm penetration in all three treatment cycles. The results indicate that, with cyclic administration of low doses of cyproterone acetate to women during the late follicular phase, it may be possible to interrupt pituitary-ovarian function, as well as sperm transport through the cervical mucus.

Body Temperature↗

PubMed1994

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

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

Adult↗

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↗

PubMed1989

The effect of cyproterone acetate on hair roots and hair shaft diameter in androgenetic alopecia in females.

Twenty female patients suffering from androgenetic alopecia were treated during one year with 50 micrograms ethinyloestradiol plus 2 mg cyproterone acetate and additional 20 mg cyproterone acetate on days 5-20 of the menstrual cycle. The control group consisted of eight untreated female patients with androgenetic alopecia. The parameters used to evaluate therapeutic results were trichogram, hair shaft diameter of full anagen and number of hairs measuring less than 40 microns. Hair roots were epilated from two locations of the scalp: fronto-cranial and left temporal (reference point). The trichogram of the fronto-cranial scalp region showed an increase of anagens as well as a decrease of telogens. These changes were statistically highly significant. Further, there was a decrease of dysplastic/dystrophic forms. The left temporal scalp region showed no significant differences. The mean hair shaft diameter of full anagen (n = 8) increased, while the number of hairs measuring less than 40 microns (n = 8) decreased. The last two findings showed no statistically significant differences. The therapeutic results warrant the conclusion that cyproterone acetate seems to be effective in androgenetic alopecia in women.

Adolescent↗

PubMed1991

[Cyproterone acetate in the treatment of girls with central precocious puberty].

Cyproterone acetate (Androcur, Schering Co) was administered within the range of recommended doses to seven girls with central premature puberty. During the investigation period, on average within 1.8 years, in all girls regression of the premature development of sex signs and gonads occurred, as well as normalization of the vaginal cytology. The growth rate corresponded to that of girls of similar calendar age, while there was progress of bone maturation. The growth prognosis deteriorated on average by 3.7 cm per year, during the whole investigation period by as much as 5.1 cm. Cyproterone acetate did not meet the demands of adequate comprehensive treatment of children with central premature puberty.

Androgen Antagonists↗

PubMed1993

Synaptonemal complex studies in male mice treated with cyproterone acetate or with testosterone.

Male mice were injected either with cyproterone acetate (CyAc) or with testosterone enanthate (TE) separately or in combination with estradiol benzoate (E2B) from the neonatal period on or during adulthood. Neonatally treated animals were killed on d28 or d60, whereas all treated adults were killed on d60. Synaptonemal complexes (SCs) were analyzed under the electron microscope. Various SC anomalies were recorded. The frequency of SC alterations was higher in neonatally treated mice injected with E2B alone or in combination with CyAc (range 9.6-23.7%) than in those injected separately with TE or CyAc (range 2-3.9%). In treated neonates, combination of CyAc and E2B treatment increased the prevalence of synaptic impairments (range 11-23.5%). However, whenever TE was added to E2B treatment a significant reduction of these impairments was observed (range 11-2.4 and 23.7-9.7% respectively). In treated adult mice the prevalence of SC anomalies was low (range 2.4-3.1%) whatever hormone was injected. Furthermore, the combination of estradiol with CyAc had no increasing effect on the induction of synaptic alterations. In E2B-treated animals, those injected during the neonatal period were more susceptible than those treated in adulthood. In mice injected separately with TE or CyAc such a difference of sensitivity between neonates and adults was not noticeable. This work demonstrates that testosterone deficiency is partly responsible for E2B-induced SC alterations. However, inhibition of testosterone action at the level of testicular target cells, such as that resulting from administration of cyproterone acetate, is less harmful to the synaptic process of meiosis.

Animals↗

PubMed1988

Suitability of cyproterone acetate in the treatment of osteoporosis associated with athletic amenorrhea.

The effectiveness of the antiandrogenic agent cyproterone acetate (CA) in its contraceptive form (2 mg CA + 50 micrograms ethinyl estradiol) in the treatment of osteoporosis associated with athletic amenorrhea was studied in seven high-performance athletes. Four women with similar characteristics served as controls. Their mean age was 21.9 years +/- 3.9. Training was started at a mean age of 14.0 years +/- 2.0. The mean training intensity expressed as kilometers run per week was 35 +/- 15. Mineral density was primarily affected by the hypoestrogenic status of these athletes (= 22 pg/ml +/- 8.8 in the midluteal phase). All participants showed low serum progesterone (= 2.85 ng/ml +/- 2.10) and LH profiles (= 5.6 mlU/ml +/- 0.8) during the midluteal phase. Cyproterone acetate was administered for 8 months to treat the increased bone loss in seven women athletes. Vertebral density appeared to be increased with 9.5% +/- 2.45% (mean +/- SD) while cortical base mineral content measured at the radius was not significantly changed. Our results demonstrate that cyproterone acetate administered in combination with estrogens provides a suitable therapeutic agent in the management of osteoporosis due to a hypoestrogenic status. This treatment could substitute other contraceptive agents. Moreover, women with the most severe estrogen deficiency showed a more pronounced reaction to this therapy.

Adolescent↗

PubMed1986

Paradoxical effects of the anti-androgen cyproterone acetate on lipid and lipoprotein metabolism.

The effects on fasting serum lipids of the potent anti-androgen, cyproterone acetate (CA) and the oestrogen, ethinyl oestradiol (EO) given both alone and in combination were examined in women acting as their own controls. Cyproterone acetate alone caused significant reductions in total cholesterol, high density lipoprotein subfraction 2 cholesterol (HDL2) and low density lipoprotein cholesterol (LDL). Ethinyl oestradiol alone significantly increased triglycerides, HDL and HDL2 and reduced LDL, and there was also a significant increase in the HDL/LDL and HDL2/LDL ratios. The two steroids were administered in combination according to a reverse sequential regime. The 28-day treatment cycle thus included Phase A during which both drugs were given followed by Phase B when EO alone was given. Triglycerides rose significantly in Phases A and B to the same extent as for the group taking EO alone. High density lipoprotein cholesterol was unchanged but HDL2 was reduced in both phases and this effect could not be overcome by increasing the dose of oestrogen. Low density lipoprotein cholesterol fell and the HDL/LDL ratio rose during the two Phases and these changes were significant during Phase A. The effects of EO demonstrated in this study are consistent with previous reports. Cyproterone acetate, however, has properties conventionally ascribed to both synthetic androgens (e.g. lowering of HDL2) and oestrogens (e.g. lowering of LDL). The limitations of the terms androgenic and oestrogenic activity in relation to their conventional associations with changes in lipid and lipoprotein levels are discussed.

Acne Vulgaris↗

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↗

PubMed1979

A morphological study on the effect of cyproterone acetate on human prostatic carcinoma.

Sixteen patients with prostatic carcinoma were treated with 200 mg of Cyproterone acetate daily. No other kind of hormonal treatment was given. Transrectal biopsies of the prostate were taken before the treatment was started, and at regular intervals afterwards. The treatment period lasted from 3 to 16 months, with an average of 9 months. A thorough examination of multiple sections from all specimens revealed no convincing signs of cellular involution. The study has demonstrated no specific or significant atrophic changes following Cyproterone acetate therapy. Some possible explanations regarding the effect of Cyproterone acetate on human malignant prostatic tissue are discussed.

Adenocarcinoma↗

PubMed1998

Contraceptive and therapeutic effectiveness of two low-dose ethinylestradiol and cyproterone acetate regimens in the treatment of hirsute patients.

OBJECTIVE: To compare the effectiveness of two very low-dose ethinylestradiol and cyproterone acetate regimens in the treatment of hirsutism. PATIENTS: Eighteen hirsute women were randomized into two different regimens of cyproterone acetate and ethinylestradiol in a reverse sequential pattern: group 1 (0.28 mg ethinylestradiol monthly), group 2 (0.32 mg ethinylestradiol monthly). Both groups received 12.5 mg/day cyproterone acetate for the first 10 days of treatment each month. MAIN OUTCOME MEASURES: Hirsutism scores were measured according to the Ferriman and Gallwey scoring system and side-effects and complications were recorded during the 6 months of therapy. Ovulation was monitored by radioimmunoassay of estradiol, follicle stimulating hormone (FSH), luteinizing hormone (LH) and progesterone levels. The pituitary response was studied using a gonadotropin releasing hormone test. RESULTS: Hirsutism scores decreased significantly in both groups at the end of the 6 months (-30%). All patients were anovulatory, as documented by the reduction of the LH, FSH, estradiol and progesterone levels. Pretreatment basal LH and FSH levels were higher than LH and FSH levels during the treatment. Side-effects were observed only occasionally with some differences between the two therapeutic regiments. CONCLUSION: Both treatments greatly improve hirsutism, reduce clinical problems and side-effects, guarantee both anovulation and contraceptive effectiveness and afford an optimal control of the menstrual cycle.

Adult↗

PubMed1977

The LH and FSH responses to LH-releasing hormone (LH-RH) in girls with true precocious puberty treated with cyproterone acetate.

Ten girls with precocious puberty ranging in age from 7 to 10 7/12 years who were treated with oral cyproterone acetate on a long term basis, were subjected to LH-RH tests, prior to and 3 to 16 months after the institution of therapy. Cyproterone acetate was given in doses from 60 to 153 mg/m2, which proved to be clinically effective, as evidenced by the slowing down of sexual maturation. The basal levels of LH were found to be unaffected by therapy and corresponded to the pubertal stages of the individual girls. The peak increment of LH after LH-RH stimulation was markedly suppressed by the therapy. FSH secretion and its responsiveness to LH-RH was not affected by cyprotereone acetate. The basal levels of FSH were higher during therapy than before, but the peak FSH increment remained the same. An escape phenomenon in the LH peak response was evident in 2 patients upon retesting after prolonged therapy. It is possible that the antigonadotrophic action of cyproterone acetate is due to its progestational nature.

Child↗

PubMed1992

The importance of adequate serum ferritin levels during oral cyproterone acetate and ethinyl oestradiol treatment of diffuse androgen-dependent alopecia in women.

OBJECT: To evaluate the treatment with cyproterone acetate and ethinyl oestradiol of diffuse androgen-dependent alopecia in women. DESIGN: Twenty women were treated for a period of 12 months in a reverse sequential regimen employing cyproterone acetate (CPA, 50 mg once daily from Day 5 to Day 15) and ethinyl oestradiol (EE2, 30 micrograms once daily from Day 5 to Day 24 of the menstrual cycle), and 20 were left untreated and acted as controls. Half of each group had serum ferritin concentrations above or below 40 micrograms/l. PATIENTS: Forty Caucasian premenopausal women aged between 18 and 47 years, presenting with diffuse androgen-dependent alopecia, were enrolled into this study. MEASUREMENTS: Hair variables were assessed initially by the unit area trichogram and again in the same sites 12 months later. Biochemical investigations were performed before treatment and after 3, 6, and 12 months. RESULTS: In the treated group, a significant (P less than 0.01) mean increase in total hair density (hair/cm2) and meaningful hair density (non-vellus hair/cm2) was found in patients in whom the serum ferritin was above, but not below 40 micrograms/l. However, in the control group a significant (P less than 0.05) mean decrease in total hair density and meaningful hair density was observed after 12 months. No correlation between serum ferritin levels and the degree of hair loss within this group could be established. CONCLUSION: Patients treated with the anti-androgen cyproterone acetate and ethinyl oestradiol respond best when serum ferritin is above 40 micrograms/l.

Adolescent↗

PubMed1981

In vivo studies on the antiandrogenic effects of cimetidine versus cyproterone acetate in rats.

To investigate the antiandrogenic action of cimetidine in vivo, prostatic androgen uptake and metabolism, spermatogenesis, morphology of the prostate and testes, and plasma hormone levels were studied using Sprague-Dawley rats, and the results were compared with the effects of cyproterone acetate or castration. Cimetidine and cyproterone acetate caused significant reduction in the weights of the ventral prostate and testes. The changes of ventral prostate were accompanied by a dose-related epithelial atrophy. No adverse effect on spermatogenesis was observed after treatment with cimetidine at daily doses of 50 mg/kg or cyproterone acetate of 10 mg/kg. Although cimetidine treatment induced a significant decrease in plasma testosterone levels, the uptake of testosterone-3H and its conversion to DHT of the ventral prostate were not inhibited by cimetidine.

Androgen Antagonists↗