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PubMed1975

Effects of cyproterone acetate on uterine motility in rats.

The effect of cyproterone acetate, an antiandrogen, on uterine contractility when the compound is administered to rats during midpregnancy was investigated. Pregnant Wistar rats were given cyproterone acetate subcutaneously on Days 8-11 of gestation. The results indicate that cyproterone acetate, either directly or indirectly, inhibits uterine contractility, an effect that may explain the prolongation of the gestational period observed in all treated animals.

Animals↗

PubMed1979

Effects of cyproterone and cyproterone acetate on the adrenal gland in the rat: studies in vivo and in vitro.

Male Wistar rats were treated for three weeks with cyproterone (1.7 or 5.1 mg/day) or cyproterone acetate (2 or 6 mg/day). The adrenal weights of animals treated with either dose of cyproterone acetate were significantly less (P less than 0.001) than those of untreated animals. In contrast, the adrenal weights of animals treated with cyproterone did not differ from those of the controls. The concentrations of corticosterone in the plasma were significantly less (P less than 0.001) in both groups treated with cyproterone acetate compared with those of the controls; only the higher dose of cyproterone reduced the plasma concentration of corticosterone (P less than 0.001). Cyproterone acetate inhibited the rat adrenal 3beta-hydroxysteroid dehydrogenase-5-ene,4-ene-isomerase complex in vitro, with both pregnenolone and dehydroepiandrosterone as substrates. Analysis of the reaction rates suggested an uncompetitive mode of inhibition. These results suggest that in rats the antiandrogens cyproterone and cyproterone acetate may provoke adrenal insufficiency by inhibition of steroid biosynthesis. Furthermore, indirect evidence from the mass and morphology of the adrenal suggests that cyproterone acetate may also suppress production or secretion of ACTH by the pituitary gland.

Adrenal Glands↗

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↗

PubMed1981

Cyproterone acetate in the treatment of hirsutism.

Cyproterone acetate (100 mg daily on the 5th-14th days of the normal cycle) together with ethinyl estradiol (0.05 mg daily on the 5th-25th days) was used for the treatment of hirsutism in 23 women for six months. This treatment caused a significant decrease in the severity of the hirsutism after only three months, the effect being maximal after six months. Sixty per cent of our patients reported being subjectively satisfied with the results. A relapse occurred, however, within three months of the end of the treatment in half the patients. The serum testosterone was significantly decreased after three months of treatment, but the changes in serum testosterone did not follow the changes in the clinical picture of hirsutism, suggesting that one facet in the favorable action of cyproterone acetate is an inhibition of the action of androgen on target cells. Various side effects, such as nausea, headache, loss of libido and depression, were reported very frequently, which undoubtedly limits the large scale use of this treatment, at least with the doses used in this study.

Adult↗

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↗

PubMed1993

Lipoprotein levels following treatment with cyproterone acetate or LHRH analogues.

Fasting serum lipoproteins were measured in patients with carcinoma of the prostate. Twelve patients were on no hormonal treatment (Group 1). Fifteen were on cyproterone acetate (Group 3), 17 were on the long-acting LHRH analogue Zoladex (Group 4) and 11 on a combination of cyproterone acetate and Zoladex (group 5). In addition, 27 patients with benign urological disease were taken as controls (Group 2). In both groups in which cyproterone acetate was part of the treatment the total high density lipoprotein cholesterol levels were significantly lower than in the other groups. Patients on cyproterone acetate alone had significantly higher levels of very low density lipoprotein (VLDL) triglyceride levels than those not on cyproterone acetate. These results confirm changes in serum lipoprotein levels in patients taking cyproterone acetate and these changes may have potential adverse effects if the treatment is prolonged.

Cholesterol↗

PubMed1981

Spermatogenesis and SRBC haemolysin formation in various inbred mouse strains treated with cyproterone acetate.

The synthetic steroid antiandrogen cyproterone acetate (CA) was administered subcutaneously to adult male mice of the inbred strains B10, B10.D2, B10.BR and C57BL/6 either as a single dose of 1 mg or as 10 daily doses of 0.5 mg. At 48 h after a single dose of CA, the thymus and spleen weights were markedly reduced and the morphology of the thymus was changed (depletion of cortex lymphocytes) in some strains. At 6 h and at 12 days after the 10th dose of CA, thymuses in males of all strains were markedly diminished with a histologically apparent involution affecting the cortex, as well as the medulla and reticuloepithelial tissue. Spleen weights in males of some strains were also significantly lower. SRBC haemolysin titres at 12 days after the 10th dose and spermatogenesis at 6 h and at 12 days after the 10th dose were significantly decreased in males of all strains; in none of the males was sterility produced by the CA doses used, however, Indications of the strain differences could only be seen in the onset and duration of the damage to the spleen and the corresponding decrease in haemolysin formation. The importance of the consequences of short-term administration of CA is discussed in terms of potential risks for long-term administration of CA in the regulation of male fertility.

Animals↗

PubMed1996

Comparative study of DNA repair induced by cyproterone acetate, chlormadinone acetate and megestrol acetate in primary cultures of human and rat hepatocytes.

Cyproterone acetate (CPA), a synthetic progestin recently found to induce genotoxic effects in hepatocytes from female rats and from humans of both genders, and two structural analogues, chlormadinone acetate (CMA) and megestrol acetate (MGA), have been compared for their capacity to induce DNA repair synthesis as measured by quantitative autoradiography. Exposure of primary human hepatocytes for 20 h to concentrations of CPA, CMA and MGA ranging from 2 to 50 microM induced positive responses in cultures from donors of both genders and the amounts of DNA repair elicited by the three progestins were similar. Under the same experimental conditions substantial differences were observed in the amounts of DNA repair elicited by the three progestins in primary hepatocytes from female rats, their potency decreasing in the following order CPA > CMA > MGA, and the three compounds failed to induce DNA repair in hepatocytes from male rats. These results, which agree with previous findings, suggest that for these sex steroids extrapolation to humans of results obtained in rats might be questionable.

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↗

PubMed1985

Acne: double blind clinical and laboratory trial of tetracycline, oestrogen-cyproterone acetate, and combined treatment.

Since the recent introduction of a drug regimen containing 2 mg of the antiandrogen cyproterone acetate and 50 micrograms ethinyl-oestradiol (Diane; oestrogen-cyproterone acetate) several uncontrolled reports have extolled the benefits of this drug. Double blind studies, however, are lacking. Sixty two patients with moderate or moderately severe acne were therefore included in a double blind trial of treatment for six months comparing tetracycline alone, oestrogen-cyproterone acetate alone, and a combination of these agents. Sebum excretion rates and bacterial counts were measured before, during, and after treatment, at the same time as a clinical assessment was made. At six months the acne (as assessed by overall grade) had improved by 68% in the antibiotic treated group and by 74% in the oestrogen-cyproterone treated group. The group given a combination of both agents improved by 82%, which was significantly better (p less than 0.025) than the improvement in the tetracycline treated patients. No significant difference was found between the groups given oestrogen-cyproterone alone and the combined treatment. The sebum excretion rate was suppressed by 25% in the patients in both groups receiving oestrogen-cyproterone but not in the group given antibiotics alone. Oestrogen-cyproterone acetate is as effective as antibiotics in treating acne in women, and adding antibiotics offers no advantage over using oestrogen-cyproterone on its own, although in this study the combination was more effective than tetracycline alone at six months.

Acne Vulgaris↗

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↗

PubMed1979

Effect of cyproterone acetate on the reproductive system of the female rat. A histological review.

Effects of cyproterone acetate, a synthetic steroidal compound, on the reproductive organs of female rats have been investigated. This agent caused reduction of ovarian weights indicative of suppression of pituitary gonadotrophins. Oestrogenic nature of cyproterone acetate was investigated in intact and ovariectomized rats taking uterine weight and vaginal keratinization as an index of oestrogenicity. Cyproterone acetate in ovariectomized animals induced vaginal keratinization and increased the uterine weights. These effects were parallel to the effect of oestradiol dipropionate in ovariectomized animals, thus indicating oestrogenic activity of cyproterone acetate. We may conclude that the above compound caused antifertility effects due to its oestrogenic nature at the dose level of 2 mg/alternate day in rats when the compound was administered subcutaneously.

Animals↗

PubMed1987

Parenteral and oral cyproterone acetate treatment in severe hirsutism.

In the present study a parenteral treatment regimen with cyproterone acetate was compared with the high dose peroral administration in patients with severe hirsutism. Two groups consisting of 10 patients each performed treatment with either 100 mg cyproterone acetate perorally for the first 10 days of the menstrual cycle or received a monthly implant of 300 mg cyproterone acetate intramuscularly applied on the first day of each cycle. In addition, contraception was performed with Diane in both patient groups. 9 treatment cycles were followed by a posttreatment period of 3 months. Hair parameters and serum androgens were monitored regularly. No significant differences of testosterone, androstenedione, dehydroepiandrosterone-sulfate and prolactin serum levels became evident between both cyproterone acetate regimens. Measurements of facial hair diameters revealed a better reduction for the parenteral application. Also the improvement of dermatological parameters was more prominent in the parenteral treatment group. The good effects of a medium dose parenteral application against higher dose peroral treatment thus was documented. The lack of significant differences of androgenic suppression in both regimens turns up the question if different metabolism at the cellular level may be responsible for that phenomenon.

Administration, Oral↗

PubMed1976

[Bioavailability and pharmacokinetics of 14C-cyproterone acetate after administration as a 50-mg tablet (author's transl)].

Four male volunteers were each given a 50 mg oral dose of methylene-14C-labelled cyproterone acetate in a formulation largely identical to the commercial preparation Androcur Tablets. A further 3 volunteers were each given 10 mg of the 14C-labelled compound by intramuscular injection. Plasma samples were obtained and urine and faeces collected quantitatively from each volunteer up to 10 days post administration. 1. Absorption of the 50 mg of cyproterone acetate administered in the form of Androcur Tablets was largely complete. 2. The maximal plasma level of 400 +/- 40 ng cyproterone acetate equivalents/ml of plasma, calculated from the 14C activity, was found 3,8 +/- 0,5 hours after oral administration. By 10 hours post administration the plasma level had declined with a half-life of 7,9 +/- 2,5 hours (distribution and elimination). The fictitious distribution volume assignable to this process amounted to 140 +/- 40% of body weight. Plasma 14C-activity then decreased with a half-life of 1,8 +/- 0,2 days, which was consistent with elimination. 3. The labelled substance was almost completely extractable from plasma and could be separated by chromatography into 2 fractions of about equal size: cyproterone acetate and one metabolite. 4. Orally administered cyproterone acetate was eliminated with a half-life of 1,6 +/- 0,1 days. By 10 days post administration 33 +/- 6% of the dose had been detected in urine and 60 +/- 8% in faeces. Up to this time total elimination amounted to 93 +/- 5% of the dose. 5. After intramuscular injection of 10 mg of cyproterone acetate the half-life for absorption from the muscular depot was 7,0 +/- 0,2 hours. Between 2 and 10 days post administration there was a uniform decrease in plasma level and urinary elimination with half-life of 2,3 +/- 0,1 days and 2,1 +/- 0,2 days respectively. By the end of the trial 34 +/- 5% of the dose had been eliminated with urine and 57 +/- 6% with faeces.

Administration, Oral↗

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↗

PubMed1997

Changes in expression of CCAAT/enhancer binding protein alpha (C/EBP alpha) and C/EBP beta in rat liver after partial hepatectomy but not after treatment with cyproterone acetate.

BACKGROUND/AIMS: The proliferation rate of adult rat liver is normally very low. It is markedly enhanced during compensatory regeneration, e.g. after partial hepatectomy, or after administration of certain growth promoters, e.g. cyproterone acetate. These two types of liver cell proliferation appear to differ, since the expression of immediate early genes is induced during compensatory regeneration but not after cyproterone acetate treatment. The transcription factor C/EBP alpha, which has been associated with hepatocyte differentiation and growth arrest, is suppressed during compensatory regeneration. In contrast, C/EBP beta, associated with acute phase reaction, is increased during regeneration. We have investigated the effects of the liver growth promoter cyproterone acetate on the hepatic expression of C/EBP alpha and C/EBP beta. METHODS: Adult male rats received either cyproterone acetate treatment or were subjected to partial hepatectomy. Livers were obtained at different time intervals for measurement of C/EBP alpha and C/EBP beta mRNA with solution hybridization/RNAse protection assay, and C/EBP alpha and C/EBP beta content with immunoblotting. RESULTS: The levels of both C/EBP alpha and C/EBP beta mRNA and the corresponding immunoreactivities were unchanged 2-48 h after injection of cyproterone acetate. The levels of C/EBP alpha mRNA and immunoreactivity were significantly suppressed 10-18 h and 18-26 h after partial hepatectomy, respectively. The levels of C/EBP beta mRNA and immunoreactivity were enhanced during compensatory regeneration 2 h after partial hepatectomy. CONCLUSIONS: Liver cell proliferation during regeneration, but not in response to cyproterone acetate treatment, is associated with changes in C/EBP alpha and C/EBP beta expression. This further supports the notion that changes in expression of transcription factors during liver growth in vivo are dependent on the growth inducer.

Animals↗

PubMed1997

Investigation into the age-dependence of the pharmacokinetics of cyproterone acetate in healthy male volunteers.

OBJECTIVE: To investigate a possible age-dependence of the pharmacokinetics of cyproterone acetate following single oral administration. METHODS: Twenty eight healthy men between 22 and 74 years of age received a single oral dose of 100 mg cyproterone acetate. The pharmacokinetic parameters, area under the serum concentration-time curve, apparent volume of distribution, apparent clearance, terminal half-life and the concentration ratio of 15 beta-hydroxycyproterone acetate/cyproterone acetate were examined for possible age-dependence using regression analysis. RESULTS: The values of area under the serum level-time curve showed high interindividual variability and were not related to age. With regard to apparent clearance and volume of distribution, decreasing and increasing values, respectively, were observed with increasing age. There was also a clear dependence of the terminal half-life on age. Elderly men had values about two times higher (95 h) than men belonging to the younger age groups (45 h). The mean concentration ratio of 15 beta-hydroxycyproterone acetate/cyproterone acetate was 0.8 (0.3) and showed no age-dependent change. CONCLUSIONS: Apparent clearance and apparent volume of distribution of cyproterone acetate showed age-dependent changes. Combined, the two effects cause a clear age-dependence of the terminal half-life of cyproterone acetate. An age-related reduction in liver volume is thought to be mainly responsible for the decrease in hepatic clearance with age. Chronic daily administration of the drug to elderly men may therefore lead to somewhat higher steady-state concentrations in the serum than in young men receiving the same dose.

Administration, Oral↗

PubMed2005

Simultaneous determination of cyproterone acetate and ethinylestradiol in tablets by derivative spectrophotometry.

Derivative spectrophotometry offers a useful approach for the analysis of drugs in multi-component mixtures. In this study a third-derivative spectrophotometric method was used for simultaneous determination of cyproterone acetate and ethinylestradiol using the zero-crossing technique. The measurements were carried out at wavelengths of 316 and 226 nm for cyproterone acetate and ethinylestradiol respectively. The method was found to be linear (r2>0.999) in the range of 0.5-6 mg/100 ml for cyproterone acetate in the presence of 35 microg/100 ml ethinylestsradiol at 316 nm. The same linear correlation (r2>0.999) was obtained in the range of 10-80 microg/100 ml of ethinylestradiol in the presence of 2 mg/100 ml of cyproterone acetate at 226 nm. The limit of determination was 0.5 mg/100 ml and 10 microg/100 ml for cyproterone acetate and ethinylestradiol respectively. The method was successfully applied for simultaneous determination of cyproterone acetate and ethinylestradiol in pharmaceutical preparations without any interferences from excipients.

Calibration↗