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At least 19 recordsLinked to original sources
PubMed2000

Highly sensitive and specific time-resolved fluoroimmunoassay (TR-FIA) of cyproterone acetate and free cyproterone.

We have developed a non-isotopic TR-FIA for Cyproterone acetate and Cyproterone in plasma. Synthesis of the biotinylated tracers, biotinylated Cyproterone acetate, and Cyproterone, as well as the preparation of anti-Cyproterone acetate and anti-Cyproterone antisera are reported. The specificity of anti-Cyproterone acetate antiserum resulting from the coupling of link bridge (link bridge between steroid and BSA), on the 3-position on the steroid skeleton, allowed to carry out the Cyproterone acetate assay directly on extracted plasma (without chromatography). On the other hand Cyproterone assays require a purification step, including extraction plus chromatography, because the plasma Cyproterone acetate concentrations in Cyproterone acetate-treated women are 200 times higher than for Cyproterone. Theses plasma TR-FIA of Cyproterone acetate and Cyproterone presented the advantage of needing only small doses of radioactivity for recovery controls, and better practicability related to the only existing RIA described to date.

Acne Vulgaris↗
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↗
PubMed1977

Some effects of cyproterone and cyproterone acetate on the reproductive physiology of the male rat.

Male rats were treated with 5 or 20 mg cyproterone acetate/kg/day or 20 mg cyproterone/rat/day for 1, 2, 3, 4, or 5 weeks. There was some reduction in fertility with both compounds, the maximum effect occurring after 5 weeks with the higher dose of cyproterone acetate and after 2 weeks with cyproterone. A significant increase in testosterone levels was found after treatment with the high dose of cyproterone acetate by 1 week and with cyproterone by 2 weeks. Dose-dependent atrophy of the seminal vesicles occurred after treatment with cyproterone acetate; with cyproterone atrophy occurred at 1 and 2 weeks but approximated to control values at 3, 4 and 5 weeks. Epididymal weights were reduced with the high dose of cyproterone acetate but the low dose had little effect. Reduction in the weight of the testes was only observed after 5 weeks of treatment with the high dose of cyproterone acetate. Since plasma testosterone levels were not depressed below normal values, accessory sex organ regression evidently resulted from the local antiandrogenic action of the drugs. There was some indication of interference with the secretory and absorptive activity of the lining cells of the epididymis but in general treatment with either steroid caused only relatively small and variable changes in the composition of epididymal plasma.

Animals↗
PubMed1973

Androgen dynamics in vitro in the human prostate gland. Effect of cyproterone and cyproterone acetate.

Hyperplastic and adenocarcinomatous human prostatic tissue was superfused in vitro with radioactively labelled androst-4-ene-3,17-dione, testosterone and 5alpha-dihydrotestosterone (17beta-hydroxy-5alpha-androstan-3-one), with and without addition of the anti-androgens cyproterone and cyproterone acetate. Cyproterone competitively inhibited the entry of the androgens into the majority of the tissues, whereas cyproterone acetate increased this entry. These findings indicated that transport of androstenedione, testosterone and 5alpha-dihydrotestosterone into prostatic tissue is performed by a specific mechanism, possibly involving a carrier situated in the cell membrane. The extent of metabolism of the three androgens was also modified: formation of 5alpha-dihydrotestosterone from testosterone, and of the latter from androstenedione, was decreased by cyproterone and increased by the acetate. Acetate was more effective than cyproterone in decreasing the ;uptake' of the perfused androgens by the tissue; at the same time, it increased the androgen clearance from the tissue. As cyproterone acetate is the more potent of the two anti-androgens, the possibility that these findings in vitro are related to the different anti-androgenic potency exhibited by the two compounds in vivo is discussed. ;Uptake' of the two anti-androgens and the response to their action on androgen dynamics were similar in adenocarcinomatous and hyperplastic glands.

Acetates↗
PubMed1977

Isolation and identification of 15-beta-hydroxy cyproterone acetate as a new metabolite of cyproterone acetate in dog, monkey and man.

15-beta-hydroxy cyproterone acetate could be identified by thin layer chromatography, mass spectrum, NMR and IR spectrum as a major unconjugated metabolite of cyproterone acetate in plasma and urine of dog, monkey and man. This metabolite has been found to interferein the Mattingly method for the determination of 11-hydroxy-corticosteroids which suggests, that this method is inadequate in controling the adrenal function of subjects treated with cyproterone acetate.

Animals↗
PubMed1995

Identification of 3 alpha-hydroxy-cyproterone acetate as a metabolite of cyproterone acetate in the bile of female rats and the potential of this and other already known or putative metabolites to form DNA adducts in vitro.

Cyproterone acetate (CPA) is a synthetic steroid hormone used in the therapy of prostate cancer in men and different forms of acne and hirsutism in women. CPA has been shown by 32P-postlabeling analysis to bind covalently to hepatic DNA of rats in vivo and in vitro. A prerequisite for DNA adduct formation of CPA is metabolic activation of the drug to a reactive intermediate. In the present study bile was collected from [3H]CPA-treated female rats and, following chromatographic separation of bile extracts, fractions of the eluate were examined for the presence of reactive metabolites which were able to form adducts with calf thymus DNA in vitro. The formation of adducts was detected by 32P-postlabeling analysis. One major metabolite of CPA present in the bile extracts was isolated and, following a thorough structural elucidation by mass spectrometry and 1H-NMR, this metabolite was identified as 3 alpha-hydroxy-cyproterone acetate (3 alpha-OH-CPA). This metabolite was able to form the same major adduct in vitro which has been observed before in CPA-treated rats in vivo and in rat hepatocytes in vitro. A number of already known or putative metabolites of CPA were available as authentic standards and these were also examined for their propensity to form adducts in vitro. A positive result was obtained for 3-O-acetyl-cyproterone acetate, which formed the same major adduct as 3 alpha-OH-CPA. However, the presence of this putative metabolite in rat bile could not be demonstrated. Besides 3 alpha-OH-CPA, additional reactive metabolites of CPA were present in the bile extracts, however, since these were only minor components, their chemical structures could not be elucidated.

Animals↗
PubMed1988

Pharmacokinetics of cyproterone acetate and its main metabolite 15 beta-hydroxy-cyproterone acetate in young healthy women.

Cyproterone acetate (CPA) and 15 beta-hydroxy-cyproterone acetate (15 beta-OH-CPA) have been quantitated in human plasma by a selective, automated HPLC assay in 8 young female subjects. Subjects received a single oral dose of 100 mg CPA and four weeks later, a single intramuscular dose of 300 mg CPA. Plasma levels in seven subjects could be evaluated pharmacokinetically. After intramuscular administration maximum CPA serum levels of 191 +/- 49 ng/ml were reached between 2 and 3 days. Postmaximal levels declined with a half-life of 4.3 +/- 0.7 days. After oral administration maximal serum levels of 255 +/- 110 ng/ml were measured between 2 and 3 h. CPA levels decayed biphasically with a terminal half-life of 3.6 +/- 1.3 days. Bioavailability after oral administration was nearly complete (88 +/- 20%). Metabolite levels were below CPA levels until 4 days (i.m.) and 6 h (p.o.) and exceeded CPA levels later on. 15 beta-OH-CPA levels declined with half-lives similar to those of corresponding CPA levels, indicating that terminal half-life of the metabolite in serum reflects its rate of formation rather than its rate of elimination. Areas under the metabolite serum level curves after intramuscular and oral administration were 10 to 15% higher than the corresponding areas for unchanged CPA. Since CPA and 15 beta-OH-CPA contribute to the antiandrogenetic efficacy there is good reason to assume that the intramuscular administration of CPA might be equally effective in the therapeutical use as the oral administration.

Administration, Oral↗
PubMed1981

Cyproterone acetate, testosterone, LH, FSH, and prolactin levels in plasma after intramuscular application of cyproterone acetate in patients with prostatic cancer.

Five patients with prostatic carcinoma (stages T3N0M0) were injected intramuscularly with 300 mg of cyproterone acetate (CPA) (Androcur-Depot) at weekly intervals. The concentrations of CPA, testosterone, LH, FSH, and prolactin in plasma after the first, third, and fifth injection were measured by specific radioimmunoassays. After five injections of Androcur-Depot, CPA levels were slightly higher than in previous determinations, suggesting that a balance between active substance release from the depot and excretion could be achieved after eight to twelve injections, with only slightly higher levels of active substance attained. Testosterone levels clearly were reduced after the first injection of CPA, but the lowest values were registered only after three injections. Plasma concentrations of FSH and LH were slightly diminished, whereas the prolactin level increased after CPA therapy.

Cyproterone↗
PubMed1982

Teratogenic effects of cyproterone acetate and medroxyprogesterone treatment during the pre- and postimplantation period of mouse embryos. II. Cyproterone acetate and medroxyprogesterone acetate treatment before implantation in vivo and in vitro.

The study was performed to investigate direct embryotoxic effects of maternal progestin treatment during the preimplantation period. In the first experiment pregnant mice received a single subcutaneous injection of either cyproterone acetate (CA) or medroxyprogesterone acetate (MPA) on day 2 of pregnancy (5-600 mg/kg). In a second experiment four-cell embryos were exposed to CA or MPA in vitro (3 or 30 micrograms/ml medium). Our results revealed: (1) After maternal treatment the number of live embryos was reduced after the highest CA dose. Development into blastocysts was inhibited in a dose-related manner after CA but not after MPA. The number of cells in morulae, blastocysts, and of the inner cell mass (ICM) of late blastocysts was not affected. (2) When morulae and blastocysts were cultured in vitro after maternal treatment, hatching, attachment, and trophoblast outgrowth were inhibited after high doses, but development and differentiation of the ICM were inhibited even after low doses. (3) Application of 30 micrograms/ml of CA or MPA in vitro was directly embryolethal. Three micrograms/ml did not affect development into blastocysts, but ICM development and differentiation were again inhibited during subsequent culture in hormone-free medium. (4) Qualitative protein synthesis was altered in morulae and blastocysts 24 hours after maternal CA treatment. According to our results high doses of progestins are embryotoxic before implantation, low doses have delayed effects on embryonic development that are particularly evident after implantation in vitro.

Animals↗
PubMedDate not supplied

Cyproterone acetate: I. Microquantity releasing device of cyproterone acetate and its failure in inducing functional sterility in male rats.

Prasad and his coworkers emphasized that microquantities of cyproterone acetate (CPA) when continuously available developed functional sterility in male rats by interfering the epididymal physiology. In our experimental rats either 2 or 3 capsules containing CPA as per the specification of Prasad were implanted subcutaneously and left for 300 and 250 days, respectively. Fertility test was made every month and it was observed that all the experimental animals were able to impregnate female rats throughout the experiment. Excepting the epididymis the weight of testes and other accessory glands did not differ from the controls in the animals which had 2 CPA capsules for 300 days; On the other hand, the animals which received 3 CPA capsules for 250 days showed significant reduction in weight of all the acessory glands including the testes.

Animals↗