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PubMedDate not supplied

Effects of cyproterone acetate on the reproductive tract and pituitary-gonadal axis of the golden hamster.

The effects of cyproterone acetate (CA) on the reproductive tract and serum levels of gonadotropins and testosterone in male golden hamsters exposed to long days, were studied. The daily injection of CA at 100 mg kg-1 body weight during 8 weeks reduced sperm count, both in caput and cauda epididymidis. The weight of epididymis and seminal vesicles were also reduced, while testicular weight and histology were not affected. Serum levels of testosterone and LH were increased 3.6 and 1.8 fold, respectively, above controls, while FSH was not affected by the treatment with CA. The absence of an inhibitory action of CA on the testis could be explained through an increase in LH stimulation, thus suggesting that in the golden hamster CA is devoid of progestagenic partial effects.

Animals↗
PubMed1978

Behavioural and physiological effects of testosterone propionate and cyproterone acetate in immature male domestic ducks, Anas platyrhynchos.

The behavioural and morphological effects of testosterone propionate and of the antiandrogen cyproterone acetate were studied in male domestic ducks. Testosterone was also measured by radioimmunoassay in the plasma of these birds to relate the behaviour to the actual circulating levels of hormone. Testosterone stimulates sexual behaviour but has few effects on social displays. There is no correlation between the individual variations of plasma testosterone and sexual behaviour.

Aggression↗
PubMed1977

The treatment of hirsutism with cyproterone acetate (an anti-androgen).

The rationale of anti-androgen treatment for hirsutism is explained. The results are presented of treatment with cyproterone acetate of idiopathic hirsutism or hirsutism associated with polycystic ovarian disease. Ten out of 14 patients showed a good response after six months treatment. The response was dramatic in two patients.

Adolescent↗
PubMed1979

Effect of cyproterone acetate (CA) on growth and endocrine function in precocious puberty.

16 girls with precocious puberty have been studied. Following low dosage cyproterone acetate (CA) therapy (mean daily dosage 65 mg/m2BSA) a beneficial effect on growth and skeletal maturation was observed. During high dosage therapy (150 mg/m2 per day) endocrinological studies were performed in 10 of these patients. There was no significant difference in HGH levels (insulin- and arginine-test), T3 and TSH values (TRH-test) between patients and controls, T4 concentration was significantly increased. Basal prolactin levels and prolactin response to TRH was definitely elevated. Oral glucose load and arginine infusion resulted in a significantly enhanced insulin release. There was a significant reduction in basal LH levels and an increase in FSH response to LH-RH. Basal and diurnal plasma cortisol values were markedly reduced and the cortisol release due to corticotrophin injection, lysinevasopressin (LVP) injection and insulin-hypoglycemia as well. A definite increase in basal ACTH levels was observed, during LVP- and insulin-hypoglycemia test ACTH concentrations were within or significantly above normal range. In our patients a primary adrenocortical insufficiency due to CA treatment was evident.

Arginine↗
PubMed1998

Environmental xenobiotics and the antihormones cyproterone acetate and spironolactone use the nuclear hormone pregnenolone X receptor to activate the CYP3A23 hormone response element.

The pregnenolone X receptor (PXR), a new member of the nuclear hormone receptor superfamily, was recently demonstrated to mediate glucocorticoid agonist and antagonist activation of a hormone response element spaced by three nucleotides (DR-3) within the rat CYP3A23 promoter. Because many other steroids and xenobiotics can up-regulate CYP3A23 expression, we determined whether some of these other regulators used PXR to activate the CYP3A23 DR-3. Transient co-transfection of LLC-PK1 cells with (CYP3A23)2-tk-CAT and mouse PXR demonstrated that the organochlorine pesticides transnonachlor and chlordane and the nonplanar polychlorinated biphenyls (PCBs) each induced the CYP3A23 DR-3 element, and this activation required PXR. Additionally, this study found that PXR is activated to induce (CYP3A23)2-tk-CAT by antihormones of several steroid classes including the antimineralocorticoid spironolactone and the antiandrogen cyproterone acetate. These studies reveal that PXR is involved in the induction of CYP3A23 by pharmacologically and structurally distinct steroids and xenobiotics. Moreover, PXR-mediated PCB activation of the (CYP3A23)2-tk-CAT may serve as a rapid assay for effects of nonplanar PCBs.

Androgen Antagonists↗
PubMed2004

Neoadjuvant hormone treatment with leuprolide acetate depot 3.75 mg and cyproterone acetate, before radical prostatectomy: a randomized study.

OBJECTIVES: To assess the effect of neoadjuvant hormone treatment before radical prostatectomy on: tumor/prostate volume, prostate-specific antigen (PSA) and testosterone levels, surgical margin status and tumor stage, and the ease of surgery following treatment. METHODS: Patients with clinically localized prostatic carcinoma were randomized to receive leuprolide acetate depot 3.75 mg once a month for 3 months and cyproterone acetate 300 mg once a week for 3 weeks prior to surgery (group A). A control group of patients had surgery without any pretreatment (group B). RESULTS: 167 patients were evaluated for the efficacy parameters. In group A, 31% of patients had a reduction in tumor/prostate volume following hormone therapy. PSA and testosterone levels were significantly reduced (p = 0.0001) in patients in group A compared to basal values. Centralized histopathological data evaluated in 145 patients (group A and 75 group B) showed that more patients in group B had tumors at stages T3A and T3B than in group A; this difference was close to significance (p = 0.057). Positive surgical margins were more common in group B (60% of patients) compared to group A (39% of patients). Similarly lymph node involvement was more common in group B compared to group A (11 versus 3%). There was little difference between the 2 study groups for the other surgical parameters assessed (ease of dissection, duration of surgery, blood loss). CONCLUSIONS: Neoadjuvant hormone therapy before radical prostatectomy has some effects in the treatment of prostate cancer. However, long-term follow-up of patients is needed to assess the impact of this therapy on morbidity and mortality.

Adenocarcinoma↗
PubMed1980

Histophysiological effects of an antiandrogen (cyproterone acetate) on the testis of the frog Rana temporaria.

An attempt was made to study the effects of cyproterone acetate (CA), an antiandrogen, on the testicular activity of the frog Rana temporaria, employing histological and histochemical methods. Each treated frog received a total dose of 4 mg during the period of 4 weeks. Light-microscopic examinations revealed that CA blocked the formation of spermatids and mature sperms; however, the early stages of spermatogenesis, i.e. proliferation and development of spermatogonia and spermatocytes, remained unaffected. CA caused interstitial tissue disruption and degeneration, and led to the shrinkage of Leydig cells; the drug stopped the production of lipoidal material in the interstitial tissues. Also, a loss of testicular weight was documented in the frogs treated with CA.

Animals↗
PubMed1979

Effect of cyproterone acetate acutely administered on the pituitary-testicular axis.

The effect of cyproterone acetate (CA) on the pituitary-testicular axis was studied in 6 healthy men. A dose of 300 mg of CA was administered orally in the early morning, after 3 h blood samples were collected using a multiple sample technique. Testosterone (T) levels were decreased by CA in all subjects (p 0.01), LH in all (p less than 0.01) but one whereas 17-hydroxyprogesterone did not show any significant variation. In vitro, using an equilibrium dialysis, CA displaced T from plasma-binding proteins in males at 37 degrees C. The role of testosterone-binding globulin on the effects of CA on the pituitary-testicular axis remains to be clarified.

Adolescent↗
PubMed1992

Final height attainment and gonadal function in girls with precocious puberty treated with cyproterone acetate.

Thirty-four girls with precocious puberty (27 idiopathic, 6 cerebral, 1 McCune-Albright syndrome) were treated with cyproterone acetate (CPA) for 1.2-8.4 years (3.71 +/- 0.31; mean +/- SEM) at a daily dosage of 66-150 mg/m2 (103.7 +/- 6.2). The mean chronological age (CA) and bone age at the beginning of treatment were 5.99 +/- 0.31 and 8.6 +/- 0.39 years, respectively, and 9.78 +/- 0.19 and 12.44 +/- 0.22 years, respectively, at the end of therapy. At the last evaluation, mean CA was 14.23 +/- 0.4 years, and 32 girls had reached final height. The control group consisted of 10 girls with idiopathic precocious puberty who, at their parents' request, were not treated. Mean CA at the onset of pubertal signs was 6.05 +/- 0.25 years. All patients had reached final height at the time of the last observation. There was no significant difference between final height of treated (152.43 +/- 1.36 cm) and untreated (149.55 +/- 1.99 cm) girls. Final height was significantly lower than target height in both treated (155.08 +/- 0.92 cm; p < 0.025) and untreated (156.45 +/- 1.29 cm; p < 0.0005) patients, but the mean height of treated patients is nearer to target height than that of untreated ones. A positive correlation was found between final height and target height both in treated (p < 0.005) and untreated (p < 0.05) patients. After the discontinuation of CPA treatment all girls resumed the progressive course of puberty.(ABSTRACT TRUNCATED AT 250 WORDS)

Body Height↗
PubMed1997

Final height of girls with central precocious puberty, untreated versus treated with cyproterone acetate or GnRH analogue. A comparative study with re-evaluation of predictions by the Bayley-Pinneau method.

This study was designed to determine the benefit of therapy on final height (FHt) in girls with central precocious puberty (CPP). A total of 102 patients were evaluated--28 untreated, 26 treated with cyproterone acetate (CyA), and 48 treated with GnRH analogue (GnRHA)-and their achieved FHt was compared to the respective target height (THt). Of the untreated girls, half (14/28) had a slow course of puberty and reached THt +/- 0.5 SD (FHt 160.2 +/- 7.1, THt 159.5 +/- 6.6 cm); the other half (14/28) had an accelerated course of puberty with a FHt well below THt (FHt 150.8 +/- 4.3, THt, 159.2 +/- 5.9 cm) and in most cases (14/28) below the height-SDS of both parents. The treated girls (both regimens) reached THt above (CyA group: FHt 157.8 +/- 5.1, THt 156.8 +/- 5.1 cm; GnRHA group: 159.6 +/- 6.3, THt 157.7 +/- 5.7 cm). We conclude that without treatment the FHt of girls with CPP may be significantly compromised and that therapy is more beneficial if started before bone age exceeds 12 years. Our data also showed that for final height predictions in CPP the Bayley and Pinneau tables for average children should be used, regardless of the advanced bone age of the patients.

Administration, Oral↗
PubMedDate not supplied

Tamoxifen or cyproterone acetate in combination with buserelin are ineffective in patients with pancreatic adenocarcinoma.

Experimental evidence and preliminary clinical data suggest a responsiveness of pancreatic adenocarcinoma to sex hormones and LH-RH agonists. In this study, we investigated the effect of the antiestrogen tamoxifen and the antiandrogen cyproterone acetate in combination with the LH-RH agonist buserelin in 9 patients with unresectable pancreatic adenocarcinoma. In all patients the disease was progressive under this therapeutic regimen. In conclusion, complete androgen blockade and antiestrogens in combination with LH-RH agonist cannot be recommended in patients with widespread pancreatic adenocarcinoma.

Adenocarcinoma↗
PubMed1980

Effect of cyproterone acetate orally on hair density and diameter and endocrine factors in women with idiopathic hirsutism.

The effect of oral cyproterone acetate on hair density and diameter was studied in a clinically homogeneous group of 11 women with idiopathic hirsutism. Therapy was continued for 12 cycles of treatment. Hair density and mean hair diameter on the chin and left upper leg were measured before, immediately after and 3 months after therapy. Generally, the effect of treatment consisted of a quantitative reduction of both parameters, but the effect was not permanent after termination of therapy. Concurrently, the possible influence on plasma androgen was studied. No significant differences were found between the concentrations of plasma testosterone, dehydroepiandrosterone and androstenedione before and after treatment.

Adult↗
PubMed1980

Treatment of hirsutism, acne and alopecia with cyproterone acetate.

Cyproterone acetate, combined with ethinyl estradiol, was administered to 60 women (mean age: 25 years) suffering from hirsutism, acne and alopecia for 3--39 months. The rate of success was 94% for acne, 85% for hirsutism and 55% for alopecia. These results are comparable to those already reported. No correlation was found between the degree of the disease or plasma levels of testosterone, androstenedione, respectively urinary 17-cetosteroids, and the effectiveness of the treatment. Side effects were rare and identical in frequency and nature to those encountered during treatment with estrogen-containing contraceptives.

17-Ketosteroids↗
PubMed1977

Treatment of acne vulgaris with cyproterone acetate and ethinyl estradiol.

The results obtained with low-dosage treatment with 2 mg cyproterone acetate and 0.05 mg ethinyl estradiol in 10 women with moderate to severe acne are reported. Eight of these patients showed a very good response, one a moderate response, and one showed no improvement after 3 months. In four patients the administration of antibiotics could be discontinued, and in most of the other patients the dose could be reduced. Three patients discontinued this treatment, two because of side effects and one because of lack of improvement.

Acne Vulgaris↗
PubMed1996

An open randomized comparative study of an oral contraceptive containing ethinyl estradiol and cyproterone acetate with and without the GnRH analogue goserelin in the long-term treatment of hirsutism.

A multicenter randomized study was carried out to compare the efficacy of combined therapy with a GnRH analog (goserelin) + an oral contraceptive (OC) containing ethinyl estradiol and cyproterone acetate and same OC alone in the treatment of severe hirsutism. The effect of these two therapies was assessed in a subjective and an objective evaluation of hair growth. According to the subjective evaluation, judged by physician and patient. 95% of patients obtained a partial response. The objective response was assessed by measuring the mean diameter of hair from 3 different areas and 1 control area. The decrease in hair diameter compared to pretreatment was statistically significant for both treatments, mainly for the abdomen and face. The difference between the two groups did not reach statistical significance. Therefore, we assume that OC alone remains the treatment of choice for hirsutism. However, the addition of the GnRH analog to OC needs further investigation and could be justified for patients with no response to standard monotherapy.

Acne Vulgaris↗
PubMed1980

The effect of cyproterone acetate and orchiectomy on metastases from prostatic cancer.

We have studied 38 patients with previously untreated, widespread prostatic cancer, who were submitted to therapy with cyproterone acetate and orchiectomy. 70% of patients with symptoms have shown subjective improvement. Moreover, it was possible to observe the regression, stabilization or progression of metastases in 32, 50 and 18% of the cases, respectively. We conclude that such therapy is effective in the initial treatment of metastatic prostate cancer and can be continued under radiographic control until the appearance of new metastases. At this point radiotherapy and alkylating agents may be effective.

Adult↗
PubMed1996

Cyproterone acetate in the treatment of advanced prostatic cancer: retrospective analysis of liver toxicity in the long-term follow-up of 89 patients.

Cyproterone acetate (CPA) was the first steroidal antiandrogen used for the treatment of prostatic cancer. In recent studies CPA has been linked with DNA adduct formation and increased DNA repair synthesis in vitro, suggesting an increased risk for the development of hepatic malignancies. To assess liver-toxic and carcinogenic effects, 89 patients who received CPA 50 mg/day p.o. over 4 (range 2-152 months) years for prostatic cancer treatment were retrospectively evaluated. 22 patients (28.2%) showed elevated liver enzyme concentrations. In none of the 89 patients alpha-fetoprotein serum levels were elevated. In no case hepatocellular carcinoma has been observed, and in no case CPA administration was discontinued due to side effects. Considering the life expectancy of patients with advanced prostatic cancer and the long-term and high-dose exposure to CPA necessary to possibly induce liver tumors, it appears highly unlikely that CPA treatment may account for a substantial number of liver carcinomas in such patients.

Aged↗