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PubMed1985

Hormonal modulation in systemic lupus erythematosus. Preliminary clinical and hormonal results with cyproterone acetate.

We prospectively studied the effects of hormonal modulation using the antigonadotropic drug, cyproterone acetate (CA), in 7 female patients who had moderately active systemic lupus erythematosus. CA was taken orally at a mean daily dose of 50 mg for 21-33 months by 6 patients (9 months by the seventh patient) without any side effects. The number of clinical lupus exacerbations during CA treatment was lower than that during the corresponding pretreatment period (15 of 170 patient-months versus 27 of 156 patient-months; P less than 0.05), despite a reduction in the daily maintenance dose of corticosteroids or antimalarial drugs. Mean plasma testosterone levels were low initially and remained unchanged (0.66 +/- 0.31 to 0.59 +/- 0.23 nmoles/liter), whereas plasma estradiol decreased markedly (from 0.6 +/- 0 38 to 0.11 +/- 0.03 nmoles/liter), resulting in a significant reduction in the estradiol:testosterone ratio (from 1.19 +/- 0.68 to 0.23 +/- 0.12) and in the plasma concentration of the sex hormone-binding protein. Thus, cyproterone acetate induced improvement in clinical lupus activity in parallel with the expected lower estradiol:testosterone balance.

Adult↗
PubMed1980

Antagonistic effects of cyproterone acetate and oestradiol on the development of the fetal rat prostate gland induced by androgens in organ culture.

The influence of cyproterone acetate and 17beta-estradiol on the induction of the rat prostate gland by androgens has been investigated in organ culture. The gland develops from its "anlage," the urogenital sinus, as epithelial buds projecting from the urogenital epithelium into the surrounding mesenchyme. In 16.5-day-old male sinuses explanted in organ culture, testosterone or dihydrotestosterone induced such buds de novo; cyproterone acetate or 17beta-estradiol combined with the androgens competitively inhibit the bud formation in most explants. In contrast, in 18.5-day male sinuses both anti-androgens are ineffective, and prostatic buds develop. The difference in response suggests that in the older tissue, exposure to endogenous testosterone before explantation has already set in motion events leading to the differentiation of the gland that are irreversible.

Androgen Antagonists↗
PubMed2000

Cyproterone acetate and reversal of the impaired endometrial decidualization in streptozotocin-diabetic pseudopregnant rats.

Reproductive dysfunction in the female diabetic rat is associated with impaired hypothalamic-hypophyseal system, anovulation, insufficiency of ovarian steroidogenesis and spontaneous failure of pregnancy. Formation of decidua, the highly modified endometrium of pregnancy and pseudopregnancy could only be achieved when the uterus was sensitized by a sequence of oestrogen and progesterone. In this study, we examined whether the impaired expression of endometrial decidualization in the pseudopregnant rat is linked with diabetes-associated hypersecretion of testosterone. Rats were made pseudopregnant by sterile mating. Diabetes was induced by streptozotocin on day 1 p.c. Deciduogenic stimulus was given on day 5 p.c. Treatment of cyproterone acetate (10 mg kg(-1)) was scheduled from day 5 through day 9 p.c. Animals were killed on day 10 p.c, and the degree of endometrial decidual growth, plasma levels of oestradiol, progesterone, ACTH and testosterone were determined. Results showed that compared to controls there was a concomitant drop in endometrial decidual growth concurrently with impaired levels of oestradiol and progesterone in diabetic pseudopregnant rats. ACTH and testosterone levels were, however, profoundly elevated. Cyproterone acetate treatment in the diabetic pseudopregnant rat resulted in a simultaneous elevation of oestradiol and progesterone, which eventually helped the endometrial differentiation to decidua in the diabetic pseudopregnant rat parallel to controls. Present experimental data suggest that diabetes-associated impaired endometrial decidualization in the pseudopregnant rat is possibly caused by testosterone-induced oestrogen deficiency.

Adrenocorticotropic Hormone↗
PubMed1980

Influence of cyproterone acetate and estradiol on cell kinetics in the sebaceous gland of the golden hamster ear.

The cell kinetics of the sebaceous gland of the hamster ear were analysed in untreated animals, in animals treated with cyproterone acetate, and in animals treated with estradiol. Both active substances lead to a reduction in the size of the sebaceous gland (measurement with the integration plate), to a reduction of mitoses (colcemide method), to a reduction in the 3H-thymidine labelling index, to a prolongation of the S-phase (double labelling technique with 3H- and 14C-thymidine), and to a decrease in the number of cells labelled with 3H-thymidine which remain in contact with the basal lamina of the sebaceous gland 6 days after application of the isotope. The results indicate that, like cyproterone acetate, estradiol reduces the effect of androgens on cell kinetics in the sebaceous gland under the test conditions chosen, even if in an entirely different way.

Androgen Antagonists↗
PubMed1977

Effects of cyproterone acetate and carboxylic acid derivatives on the sebaceous glands of the Syrian hamster.

The Syrian hamster ear model was used to study effects of the anti-androgen cyproterone acetate and of the anti-lipogenic compound 17beta-carboxylic acid methyl ester and its ethyl ester. The steroid derivatives were applied topically in a 1-2% concentration or given systemically. Response of sebaceous gland was measured by means of cell proliferation (3H-TdR autoradiography) and by gland size (histoplanimetry). Cyproterone acetate significantly reduced the labelling and the planimetric value, both topically and systemically. The carboxylic acid derivatives, which block the 5alpha-reductase were ineffective. The new animal model is a sensitive and suitable means to study inhibition of sebum production.

Androgen Antagonists↗
PubMed1993

Double-blind placebo crossover study of cyproterone acetate in the treatment of the paraphilias.

Cyproterone acetate is a powerful antiandrogen used in the treatment of the paraphilias for at least a decade. Studies have reported it effective in reducing the recidivism rates of sexual crimes perpetrated by men. It acts through competitive inhibition of the androgen receptors blocking the effects of testosterone and dihydrotestosterone. Systematic clinical study of its effectiveness and its clinical effects on sexual behavior is lacking, however. In the current study 19 paraphilic men who had also recidivated in a variety of sexual crimes were treated with cyproterone acetate and placebo in a double-blind crossover design. The use of active drug was associated with a significant reduction of some aspects of sexual behavior, particularly sexual fantasies. There were also significant effects on levels of circulating sex hormones and some effects on physiological measurements and self-reports of sexual arousal.

Adult↗
PubMed1977

Radioprotective effects of cyproterone acetate.

The pretreatment of irradiated mice by cyproterone acetate had a better radioprotective effect in comparison with orchidectomy, although the weight of the thymus was lower in the cyproterone acetate group. The radioprotective mechanisms involved in both cases were discussed.

Animals↗
PubMed1998

Comparison of cyproterone acetate plus ethinyl estradiol and finasteride in the treatment of hirsutism.

The aim of this study was to compare the clinical efficacy and safety of low dose cyproterone acetate-estrogen combination (Diane) and the 5 alpha-reductase inhibitor finasteride in the treatment of hirsutism. Fourty-two women with hirsutism were included in the study. Twenty-one patients treated with cyproterone acetate (CPA) 2 mg and ethinyl estradiol (E) 35 micrograms daily on days 5-25 of the menstrual cycle, 21 with finasteride 5 mg daily. Hirsutism score, hormone levels, multiscreen blood chemistry and side effects were evaluated at three-monthly intervals for 9 months. A significant decrease in hirsutism score as compared to baseline was observed after 9 months with either CPA + E (Diane) (mean +/- SE, 15.81 +/- 1.19 vs 8.38 +/- 1.21) or finasteride treatment (17.81 +/- 1.05 vs 10.86 +/- 0.91) (p < 0.0005). The reductions in hirsutism scores (mean% +/- SE) were 14.23 +/- 2.29 vs 19.77 +/- 2.22 (p < 0.05) at 3, 40.23 +/- 4.58 vs 29.49 +/- 2.69 (p < 0.02) at 6 and 50.99 +/- 4.13 vs 39.87 +/- 3.30 (p < 0.02) at 9 months in CPA + E and finasteride groups, respectively. No significant changes were observed in hormone levels during finasteride treatment. Serum free testosterone significantly decreased at the third month of treatment, and remained suppressed for the duration of treatment in CPA + E group. DHEAS levels also decreased significantly after 6 and 9 months of therapy with CPA + E. SHBG significantly increased during CPA + E treatment. We conclude that both drugs are effective and well tolerated, but CPA + E appears to be more effective than 5 alpha-reductase inhibitor finasteride in long-term treatment of hirsute women. Diane is also a cost-effective drug.

5-alpha Reductase Inhibitors↗
PubMed1999

Cirrhosis in a child with hypothalamic syndrome and central precocious puberty treated with cyproterone acetate.

UNLABELLED: Before the advent of gonadotropin-releasing-hormone analogues, cyproterone acetate (CPA) had been widely prescribed for the treatment of precocious puberty. Although it is usually well tolerated, liver toxicity has been recognized as a complication of its long-term use. We report the occurrence of cirrhosis in a 10-year-old boy with hypothalamic syndrome and precocious puberty who was treated with CPA for over 50 months. Despite discontinuation of the medication, the liver disease progressed. The patient died of sepsis and multiorgan failure at the age of 14 years. This is the first paediatric report of substantial liver damage and liver toxicity progressing to cirrhosis associated with CPA treatment. CONCLUSION: Prolonged cyproterone acetate treatment may induce cirrhosis. Monitoring of liver function both during treatment and for several months after discontinuation of therapy is recommended.

Adolescent↗
PubMed1980

Cyproterone acetate and seminal vesicles in the regulation of male fertility.

The effect of continuous release of microquantities of cyproterone acetate from subcutaneously implanted silastic capsules on the fertility of surgically manipulated seminal vesicles of rat has been studied. The experimental animals showed infertility for 3 weeks, as a consequence of removal of seminal plasma, following which normal fertility returns as efficiently as that operated control. However, a significant decrease in weight of the testes and epididymides, were recorded. It appears that seminal vesicles can synthesize seminal plasma even at very low levels of androgen in the presence of cyproterone acetate.

Animals↗
PubMed1987

Effects of the antiandrogens cyproterone acetate and flutamide on male reproductive behavior in a lizard (Anolis sagrei).

This study examined the effects of the antiandrogens cyproterone acetate (CA) and flutamide (F) on male reproductive behavior in the lizard Anolis sagrei. Reproductively active males were implanted with subcutaneous pellets of either CA, F, or placebo (P). Pellets delivered CA and F at a constant rate of 0.1 mg/day. Three weeks after implantation, males were tested with stimulus males and two days later with stimulus females. Cyproterone acetate inhibited aspects of male aggressive and sexual behavior, and reduced testis weight and size of the renal sex segment. Plasma testosterone (T) levels in CA-treated males were not significantly different than those of P-treated males. Flutamide did not inhibit aggressive or sexual behavior, but did decrease testis weight as well as the size of the renal sex segment. Plasma T levels were significantly higher in F-treated males than in P-treated males. These data suggest that CA, an antiandrogen with antigonadotropic activity, may be used to inhibit reproductive behavior in male lizards.

Aggression↗
PubMed1976

Metabolism of testosterone by the epididymis and ventral prostate of rat and its inhibition by cyproterone acetate.

The metabolism of 3H-testosterone by the epididymis and accessory organs of adult male rats exposed continuously to microdoses of cyproterone acetate from subcutaneous capsules were studied. The major metabolite of 3H-testosterone in the epididymis, vas deferens and ventral prostate of control rat was dihydrotestosterone while the formation of androstanediol by these tissues was low. The highest percentage of DHT was formed by the ventral prostate and cauda epididymis. In rats exposed to cyproterone acetate for four months, the conversion of testosterone to DHT was inhibited in all the tissues but maximally in the ventral prostate and cauda epididymis. In these rats, the secretory function of the ventral prostate was normal while that of the epididymis was markedly decreased. These data are discussed based on the differential thresholds of androgens required to regulate the functions of the accessory organs.

Animals↗
PubMed1977

The effect of testosterone and cyproterone acetate on the concentration of gamma-aminobutyric acid in brain areas of aggressive and non-aggressive mice.

Mice which had been housed in groups were introduced into the home cages of isolated mice and the aggressive defensive behaviour assessed. The grouped mice were chronically treated with testosterone, cyproterone acetate or arachis oil. The concentration of GABA was determined in 10 regions following the last behavioural assessment. The grouped mice which were treated with testosterone or with the anti-androgen, cyproterone acetate, were subjected to fewer aggressive attacks by the isolated mice thatn the grouped controls. The concentration of GABA in particular brain areas appears to depend on the degree of aggressive behaviour exhibited, the type of environment into which the mouse is introduced, the hormone treatment, and the housing conditions.

Aggression↗
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↗
PubMed1987

Post-heparin plasma hepatic lipase activity as predictor of high-density lipoprotein response to progestogen therapy: studies with cyproterone acetate.

Cyproterone acetate (CPA) was administered to 13 menstruating women from day 14 to day 27 of the cycle at a dose of 5 mg/day. Serum lipoprotein lipid levels and postheparin plasma lipase activity were determined on day 27 of the cycle before treatment and during two treatment cycles. No significant changes were observed in hepatic lipase activity or in very-low-density (VLDL) or low density lipoprotein (LDL) concentrations. However, analysis of high-density-lipoprotein (HDL) subfractions by precipitation demonstrated a significant reduction in HDL2 cholesterol (-24%, P less than 0.05) during cyproterone acetate treatment. It is suggested that this change is related to oestrogen deficiency induced by inhibition of luteinizing hormone (LH) secretion.

Adult↗
PubMed1995

Does vitamin D3 have negative effects on serum levels of lipids? A follow-up study with a sequential combination of estradiol valerate and cyproterone acetate and/or vitamin D3.

The effects of four different treatment schedules on serum lipid concentrations were studied for 1 year in 402 postmenopausal women in the Kuopio Osteoporosis Study. The women were randomized to four treatment groups: A, Sequential combination of estradiol valerate and cyproterone acetate (Climen); B, Vitamin D3, 300 IU/day; C, Climen+Vitamin D3, D, placebo. In group A, serum concentrations of total cholesterol (Chol) decreased by 4.8% in 6 months and by 6.2% in 12 months (P < 0.001), but in group C the decrease was only 2.9% in 6 months (P < 0.05) and 3.4% in 12 months (P < 0.01). The decline of total-Chol in group A was accounted for by the 6.8% to 7.5% decrease in LDL-Chol levels (P < 0.001). The decrease of LDL-Chol in group C was statistically non-significant. Use of vitamin D3 (group B), increased serum Chol by 2.7% (6 months), P < 0.05 and by 2.1% (12 months) and the increases were the result of the 6.0% to 6.2% increase in LDL-Chol levels in 6 and 12 months, respectively (P < 0.001). Serum concentrations of HDL-Chol and TG remained relatively stable in all groups. No correlations were found between LDL-Chol, 25-OH-D3 and 1,25(OH)2-D3 levels in group B. Our results confirm the beneficial effect of estradiol valerate and cyproterone acetate on the lipid profile. In contrast, vitamin D3 had a negative influence on this profile by increasing serum concentrations of LDL-Chol.(ABSTRACT TRUNCATED AT 250 WORDS)

Cholecalciferol↗
PubMed1995

Influence of two hormone replacement therapy regimens, oral oestradiol valerate and cyproterone acetate versus transdermal oestradiol and oral dydrogesterone, on lipid metabolism.

OBJECTIVE: To compare the influence on lipid metabolism of two discontinuous, sequentially combined hormone replacement therapy (HRT) regimens. STUDY DESIGN: In an open, randomized study in 60 women, a full lipid profile including Lp(a) and liver function tests were assessed in a fasting state at the end of treatment cycles 6 and 12. Group A was treated with 2 mg oestradiol valerate (days 1-21) sequentially combined with 1 mg cyproterone acetate (days 12-21); group B was treated with a patch releasing 50 micrograms oestradiol daily, twice a week (3 weeks), sequentially combined with 20 mg dydrogesterone (days 12-21) orally. Statistical analysis by two-sided one-way analysis of covariance (covariable is baseline) for adjusted means of lipid parameters and rank transformation analysis for lipoprotein(a) (Lp(a)) was performed. RESULTS: Both groups were statistically comparable. The trial was completed by 45 subjects. Protocol violations occurred in 3 cases. Twelve subjects, equally divided between the groups, dropped out mainly because of adverse reactions. Both treatments were equally effective in the treatment of climacteric complaints. Liver function tests during the treatment period were normal in both groups. In group A, a statistically significant (P < 0.05) decrease versus baseline was observed in the serum levels (adjusted means) of the following parameters after 6 and 12 treatment cycles: total cholesterol (TC)-5% and -7%, respectively; low-density lipoprotein cholesterol (LDL-C) -13% and -14%, respectively; low-density lipoprotein cholesterol/high-density lipoprotein cholesterol ratio (LDL-C/HDL-C ratio) -16% and -18%, respectively. Triglycerides (TG) levels were significantly increased by 28% and nearly significantly (P = 0.07) by 25% after 6 and 12 treatment cycles, respectively. In group B, all lipid parameters (with the exception of apolipoprotein A-II which was significantly decreased after 12 treatment cycles) remained unchanged during therapy. Statistically significant differences for all aforementioned variables were found between the groups after 6 and 12 treatment cycles, respectively, with the exception of TC after 12 treatment cycles. After 6 treatment cycles, Lp(a) was decreased significantly (-18%) in group A as compared with baseline; after 12 months the decrease was -17% without reaching statistical significance. In group B, Lp(a) showed a slight but not statistically significant tendency to increase by 2% and 12% after 6 and 12 treatment cycles, respectively. Differences between both groups did not reach the level of significance. CONCLUSION: In this randomized, comparative study, a sequentially combined oral HRT regimen consisting of oestradiol valerate (2 mg daily on days 1-21) and cyproterone acetate (1 mg daily on days 12-21), induced a lipid pattern and probably also a change in Lp(a) levels, which is generally viewed to be more beneficial with regard to the prevention of cardiovascular disease than the lipid pattern induced by a sequentially combined regimen of transdermal 17 beta-oestradiol (50 micrograms twice weekly during three weeks) and oral dydrogesterone (20 mg daily on days 12-21).

Administration, Cutaneous↗
PubMed1979

The role of antiandrogenic action in cyproterone acetate-induced morphologic and biochemical changes in human semen.

Following the daily administration of 10 mg of cyproterone acetate to three normal fertile human volunteers for 12 to 16 weeks, there was a marked decrease in the count, motility, and cervical mucus-penetrating ability of spermatozoa, with a concomitant increase in abnormal and immature forms. The levels of seminal acid phosphatase and glycerylphosphoryl choline were also significantly decreased. Subsequently, concurrent daily administration of 75 mg of mesterolone increased the count, motility, and cervical mucus-penetrating ability of spermatozoa and stimulated the seminal biochemical constituents. The results indicate that the effects of a low dose of cyproterone acetate are due mainly to peripheral androgen deprivation.

Acid Phosphatase↗