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PubMed1976

Effects of an antiandrogen, cyproterone acetate, on the kidney of the three-spined stickleback (Gasterosteus aculeatus L.).

The fine structure of the kidney is studied in the sexually mature male three-spined stickleback after administration of an antiandrogen, cyproterone acetate. Under these conditions, the dedifferentiation of renal tubules is characterized by the same involutive processes as those induced by castration, with the difference that cyproterone acetate only begins to act after 14 days whereas after castration the first signs of involution are visible after 7 days. The ultrastructural modifications affect the nucleoli, the rough endoplasmic reticulum and the Golgi apparatus. They reflect an inhibition of the secretory process. The results obtained demonstrate that administration of cyproterone acetate to male sticklebacks has an inhibitory effect on renal target cells, apparently indistinguishable from the changes induced by lack of male sex hormone, and that this drug may be a valid substitute for castration in fish.

Animals↗
PubMed1980

Effect of cyproterone acetate on steroid-induced sexual behavior in adult ewes.

The inhibitory effect of cyproterone acetate on sexual behavior has been investigated in adult ovariectomized ewes treated with either testosterone propionate (10 mg/day) or estradiol benzoate (200 micrograms/day) to induce male activity and female receptivity simultaneously. Intra-muscular injections of 100 mg cyproterone acetate/day resulted in a rapid decrease in some of the male sexual responses after both testosterone and estradiol treatments, whereas the female reactions were eliminated by cyproterone acetate only when they had been induced by testosterone.

Animals↗
PubMed1979

Interaction of luteinizing hormone-releasing hormone, cyproterone acetate and arginine vasotocin on plasma levels of luteinizing hormone in intact and castrated adult male rats.

Treatment of unanesthetized castrated adult male rats every 3 h for 48 h with either 5 microgram of arginine vasotocin (AVT) and/or 1 microgram luteinizing hormone-releasing hormone (LRH) caused a significant inhibition of plasma levels of luteinizing hormone (LH) and compared to castrated control rats receiving diluent only. However, the intravenous (iv) injection of 1 microgram of AVT into urethane-anesthetized male rats which had been castrated for 0, 24 or 48 h did not affect plasma levels of LH at 10, 20 or 60 min following injection compared to their respective diluent-treated castrated control rats. Similarly, the iv injection of either 100 ng, 1 microgram or 10 microgram AVT was unable to acutely affect plasma levels of LH in intact male rats. Following the iv injection of 2 doses of 50 ng LRH spaced 1 h apart in anesthetized castrated male rats, 2 peaks of equal magnitude in plasma LH were noted. Castrated rats treated with 2 injections spaced 1 h apart of LRH + AVT had significantly higher plasma levels of LH than did rats treated with LRH alone. In subsequent studies, both AVT and arginine vasopressin were observed to augment the plasma response of LH to an injection of LRH whereas oxytocin had no effect. A single injection of AVT + LRH significantly augmented the plasma titers of LH compared to levels observed in LRH-treated control rats as did a second injection 1 h later. The administration of cyproterone acetate sc for 2 days by itself had no effect on plasma LH but in conjunction with LRH caused a marked rise in plasma LH compared to intact rats treated with LRH alone. AVT in combination with LRH and cyproterone acetate caused a significant elevation in plasma LH at 60 min post-injection when compared to plasma levels of rats treated with LRH alone or the combination of LRH and cyproterone acetate. It is concluded that acute intravenous injections of AVT augment the LH-releasing activity of LRH; chronic treatment for 48 h, however, with LRH + AVT leads to a significant depression of plasma LH perhaps due to an exhaustion of the releasable pool of LH in the anterior pituitary.

Animals↗
PubMed2000

Evaluation of efficacy, safety, and reversibility of combination regimen of cyproterone acetate and testosterone buciclate in bonnet monkey.

A combination regimen of cyproterone acetate (CPA) and testosterone buciclate (TB) was evaluated for its contraceptive efficacy, safety, and reversibility in bonnet monkeys. Cyproterone acetate (5 mg in 0.2 mL of olive oil) injected daily for 180 days, in combination with 40 mg testosterone buciclate given i.m. on days 0, 60, and 120 in the monkeys of group II (n = 6) induced azoospermia in all animals by 120 days, which was maintained until day 210. By day 240 sperm concentration increased gradually and reached baseline values by day 330. When 5mg of cyproterone acetate was injected daily for a similar duration in combination with a higher dose (80 mg) of testosterone buciclate in the monkeys of group III (n = 6) on days 0, 60, and 120, uniform and consistent azoospermia could not be achieved and two animals remained oligozoospermic even after 180 days of treatment. Mean sperm concentration did not return to baseline values until the day that the study ended, i.e. day 330. In groups II and III serum testosterone levels were elevated (p <0.05) from days 9-120 except on day 150 and returned to near baseline values by day 330. Serum testosterone levels were higher in group III compared to group II. The sperm concentration and testosterone levels in control animals (group I; n = 6) showed fluctuations. Lipid profile and liver function parameters did not show significant changes in any group. The present data clearly indicate that administration of CPA and TB in proper dosage combination can provide an effective, safe, and reversible method of male contraception.

Animals↗
PubMed1997

Cyproterone acetate displaces opiate binding in mouse brain.

Drugs acting on androgen receptors modify opioid transmission in the central nervous system. To investigate a direct interaction, we studied whether the binding of [3H]diprenorphine to mouse brain membranes was modified by cyproterone acetate (progesterone derivative with antiandrogen activity), flutamide (non-steroidal antiandrogen), 5alpha-dihydrotestosterone and progesterone. Only cyproterone acetate inhibited [3H]diprenorphine binding (IC50 = (1.62 +/- 0.33) x 10(-6) M) without modifying its association rate. These results suggest that cyproterone acetate binds to opiate receptors independently of its classical androgenic intracellular receptor effect.

Androgen Antagonists↗
PubMed1997

An oral regimen of cyproterone acetate and testosterone undecanoate for spermatogenic suppression in men.

OBJECTIVE: To test the effectiveness, safety, and reversibility of the combined administration of cyproterone acetate and T undecanoate. DESIGN: Open clinical trial. SETTING: Healthy volunteers in an academic research environment. PATIENT(S): Eight healthy men, aged 25-42 years were selected. INTERVENTION(S): Cyproterone acetate, 12.5 mg, and T undecanoate, 80 mg, were administered orally twice daily for 16 weeks. MAIN OUTCOME MEASURE(S): Semen analyses every 2 weeks; physical examination, chemistries, hematology, prostatic-specific antigen, gonadotropins and T levels, and a questionnaire on sexual and behavioral function every 4 weeks. RESULT(S): In all subjects a profound suppression of spermatogenesis occurred; one subject became azoospermic, five subjects had sperm counts of < or = 3 x 10(6)/mL, and in two subjects sperm counts were 4 and 6 x 10(6)/mL in week 16. Sperm counts returned to baseline in all men after hormone administration was discontinued. No changes in metabolic parameters and total prostatic-specific antigen were detected. Hemoglobin and hematocrit decreased statistically significantly at week 16 of treatment and returned to baseline by week 12 of recovery. There was no change in sexual function or behavior. CONCLUSION(S): The oral administration of T undecanoate plus cyproterone acetate induces a profound suppression of spermatogenesis with no major adverse effects. These data suggest the feasibility of oral contraception in men.

Adult↗
PubMed1999

Oral contraceptives that contain ethinyl estradiol (0.035 mg) and cyproterone acetate (2 mg) inhibit leukocyte transmigration through endothelial cell monolayers.

OBJECTIVE: To investigate the influence of ethinyl estradiol and cyproterone acetate in oral contraceptives on leukocyte migration through endothelial cell monolayers. DESIGN: Experimental in vitro prospective study. SETTING: An academic research laboratory. INTERVENTION(S): Endothelial cells were cultured on microporous membranes to produce monolayers. Polymorphonuclear leukocytes were used in a previously described migration assay (n = 7). The amount of untreated polymorphonuclear leukocytes that migrated through untreated endothelial cell monolayers was used as a control and set at 100%. In addition, a leukocyte adhesion assay was used. MAIN OUTCOME MEASURE(S): Leukocyte adhesion to and transmigration through endothelial cell monolayers. RESULT(S): Ethinyl estradiol and cyproterone acetate inhibited the migration of polymorphonuclear leukocytes through endothelial cell monolayers significantly (67% +/- 6.4%) when both cell types were treated to simulate in vivo conditions. The adhesion assay produced similar results. CONCLUSION(S): Ethinyl estradiol and cyproterone acetate were identified as potent inhibitors of leukocyte migration through endothelial cell monolayers.

Cell Adhesion↗
PubMed1980

Endocrine effects of cyproterone acetate in patients with prostatic cancer.

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

Aged↗
PubMed2005

Bicalutamide vs cyproterone acetate in preventing flare with LHRH analogue therapy for prostate cancer--a pilot study.

OBJECTIVE: To evaluate the efficacy of bicalutamide vs cyproterone acetate in preventing PSA flare (as a surrogate for tumour flare) for patients requiring luteinizing hormone-releasing hormone (LHRH) analogue therapy for prostate cancer. PATIENTS AND METHODS: In this pilot study, 40 men were randomized 1 : 1 to bicalutamide 50 mg o.d. or cyproterone acetate 100 mg t.i.d. 5 days prior to goserelin acetate and continued for 21 days thereafter. PSA, luteinizing hormone (LH), follicle-stimulating hormone (FSH) and testosterone were obtained before treatment and on days 6, 8, 10, 16, 21 and 28. Primary end point was PSA. Hormone profile and clinical features including urinary symptoms and bone pain were secondary end points. RESULTS: Both groups were equally matched apart from serum creatinine and ALP. The speed and magnitude of the percentage change in median PSA from baseline was increased for the CPA group but there was no statistically significant difference in the two groups. Although those receiving bicalutamide all showed a testosterone peak, this remained within the normal range. No difference in the frequency of drug-specific adverse events was found. None of the patients died or developed cord compression during the study period. CONCLUSION: Bicalutamide is able to suppress the initial PSA surge as effectively as cyproterone acetate albeit slightly delayed. A statement whether bicalutamide is equally good at preventing clinical flare cannot be made and should be assessed in an appropriately powered study.

Aged↗
PubMed2002

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

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

Aged↗
PubMedDate not supplied

Cyproterone acetate could counteract the benefits of estradiol valerate in oophorectomized cholesterol-fed rabbits.

OBJECTIVE: The administration of hormonal replacement treatment to women with an intact uterus needs to be supplemented with progestogenic compounds to avoid endometrial hyperplasia. However, progestins may cancel the beneficial effects of estrogens on the cardiovascular system. The goal of this study was to examine the effects of adding cyproterone acetate to estradiol (E(2))on aorta atherogenesis. DESIGN: Thirty-two cholesterol-fed New Zealand white rabbits were studied for 4 months. The animals underwent laparotomy and were randomly allocated to four groups. Twenty-four rabbits underwent bilateral ovariectomy, and the other eight were sham-operated (group S). The ovariectomized rabbits were allocated to three groups of eight animals each receiving E(2) valerate (group E), E(2) valerate plus cyproterone acetate (group EC), or placebo after sterilization (group C). RESULTS: After 4 months, the cholesterol-rich diet caused atherosclerotic aortic lesions in both treated groups that affected 17.91% +/- 10.19% and 28.16% +/- 7.97% of the aortic surface of groups E and EC, respectively, with a markedly lower aortic plaque size in group E than in groups C and S. Rabbits from group E (but not from group EC) had aortic cholesterol content significantly lower than rabbits from the sham-operated and control groups. CONCLUSION: E(2) valerate reduces aortic atheromatosis in cholesterol-fed, ovariectomized rabbits, and the addition of cyproterone acetate may neutralize this effect.

Analysis of Variance↗
PubMed1975

The LH response to LH releasing hormone in children with true isosexual precocious puberty treated with cyproterone acetate.

Fourteen girls and one boy with isosexual precocious puberty were submitted to LHRH stimulation tests, during and without therapy with cyproterone acetate. In addition, fourteen girls with isosexual precocious puberty not receiving any therapy were tested and served as controls. It was found that cyproterone acetate induces suppression of the responsiveness of the pituitary gland to secrete LH on LHRH stimulation. Daily oral therapy was found to be more effective than the regimen of intramuscular depot injections. These findings demonstrate that cyproterone acetate has an antigonadotrophic effect.

Administration, Oral↗
PubMed1975

Cyproterone acetate: a study involving two volunteers with idiopathic hirsutism.

Two female volunteers, of menstrual age, with severe idiopathic hirsutism were treated for eight cycles and fifteen cycles respectively with cyproterone acetate 50 mg twice daily on days 5-14 of the cycle. In all but one cycle, ethinyl oestradiol in a dose of 50 mug daily from day 5 to 21 was given in addition. Cyproterone acetate when given alone abolished the mid-cycle LH surge. Combined therapy with cyproterone acetate and ethinyl oestradiol produced a significant improvement in both patients' hirsutism and was accompanied by a marked reduction in the urinary excretion of LH, FSH and androgens and by a fall in plasma testosterone. However, the clinical benefit derived from this drug was due principally to its action as a peripheral antiandrogen.

Adult↗
PubMed1980

The effect of cyproterone acetate on serum testosterone, LH, FSH, and prolactin in male sexual offenders.

The anti-androgen, cyproterone acetate, was administered in a dose of 100 mg/day to eight adult male sexual offenders for 21-31 days. Serum testosterone fell to subnormal levels within 7 days and remained low for 6-28 days after treatment was stopped. The fall in testosterone was accompanied by a fall in serum luteinizing hormone (LH) and follicle stimulating hormone (FSH), and a rise in serum prolactin. All subjects experienced a decrease in libido and in frequency of masturbation. The probable mechanisms of action of cyproterone acetate are discussed, as is its potential role in the management of sexual offenders. These studies suggest that measurement of serum testosterone could be used as an index of compliance in sexual offenders treated with cyproterone acetate who are released on parole.

Adult↗
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↗
PubMed1980

Treatment of advanced prostatic cancer with parenteral cyproterone acetate: a phase III randomised trial.

Forty-two patients with previously untreated T3/4 N1-4 MO/1 prostatic adenocarcinoma were treated with either cyproterone acetate (n = 21; 300 mg intramuscularly per week) or oestradiol undecylate (n = 21; 100 mg intramuscularly per month) after extensive staging which included open skeletal biopsy and pelvic lymphadenectomy in some cases. Subjective and objective parameters as well as signs of drug toxicity were recorded regularly. Evaluation after 6 months showed cyproterone acetate to be more effective in the following respects: (1) the significantly different castration effect as judged by plasma testosterone, (2) the objective voiding pattern and tumour response, with regression of palpable and histologically evaluable local tumour in 16 of 21 patients, and (3) side effects and untoward reactions. Thus cyproterone acetate is suggested as a valuable alternative in the treatment of advanced prostatic cancer.

Adenocarcinoma↗
PubMed1977

Radioimmunological determination of cyproterone acetate.

A sensitive and specific radioimmunoassay for cyproterone acetate in serum has been developed. Antiserum was raised in rabbits by immunization with a conjugate of cyproterone acetate-11 alpha-hemisuccinate and bovine serum albumin. Radioactive tracers with high specific activities were synthesized by coupling the hemisuccinate with [3H]-tyrosine methyl ester of [125I]-iodohistamine. Competition studies with substances structurally related to cyproterone acetate have revealed that the structures of ring A and B are mainly responsible for binding to the antibody.

Antibody Specificity↗
PubMed1996

Testotoxicosis proved by immunohistochemical analysis and successfully treated with cyproterone acetate.

We present a case of testotoxicosis diagnosed on the basis of immunohistochemical investigation of the testis. The patient was treated with the antiandrogen cyproterone acetate at a dose of 70-130 mg/m2/day. Clinical and biochemical features are consistent with the diagnosis of testotoxicosis. The long-term experience with cyproterone acetate had been generally satisfactory. There are, to our knowledge, no reports on cyproterone acetate treatment of testotoxicosis.

Age Factors↗