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Treatment of advanced prostatic carcinoma with cyproterone acetate and orchiectomy--5-year follow-up.

We report the results from 106 patients with extracapsular (stage C) or widespread (stage D) prostatic cancer, who were treated with cyproterone acetate and orchiectomy and followed for 5 years. As controls we used 40 patients, chosen at random, with stage C and stage D cancer of the prostate gland who were treated with stilbestrol and orchiectomy. The survival rate is improved in patients treated with cyproterone acetate and orchiectomy compared to the patients treated with stilbestrol and orchiectomy. Treatment with cyproterone seems more effective in those patients with low-stage and low-grade prostatic cancer. The side effects of this therapy are less and milder than those described in estrogenic treatment alone or with orchiectomy.

Adult↗

Plasma lipoproteins during treatment with cyproterone acetate in men with prostatic carcinoma.

The incidence of cardiovascular disease is lower in women than in men, but is raised in men with prostatic cancer treated by estrogens. The antiandrogenic gestagenic drug, cyproterone acetate, is sometimes used instead of estrogens in the treatment of prostatic cancer. The cardiovascular risk associated with such hormonal treatment has been debated. Changes in plasma lipoproteins are related to the risk of cardiovascular disease and can be brought about by hormonal treatment. Plasma lipoproteins were therefore investigated during cyproterone acetate therapy in 15 men with prostatic cancer. Cholesterol (C), triglyceride, and phospolipid (PL) concentrations were determined in the very low density, low density (LDL), and high density lipoprotein (HDL) fractions. During treatment, mean body weight decreased by 1.2 and 1.9 kg after 2 and 8 weeks, respectively. The mean C concentration was lowered by 16%. The HDL C was reduced by a mean of 25%, and the LDL C decreased by means of 15% and 10%. The part of plasma C carried in the HDL fraction decreased slightly from 19 to 17% (mean) and the mean HDL C/LDL c quotient was lowered from 0.27 to 0.22. The mean PL concentration in plasma was decreased due to a mean reduction of HDL-PL by 17% and LDL Pl by 10%. A reduction of the HDL/LDL quotient implicates an increased risk for development of atherosclerotic diseases. However, it seems unlikely that a modest reduction in the HDL/LDL quotient, as obtained by cyproterone acetate, should have any great influence on the incidence of cardiovascular disease in elderly men with prostatic carcinoma.

Aged↗

Serum insulin-like growth factor I (IGF-I) and IGF-binding protein 3 levels are increased in central precocious puberty: effects of two different treatment regimens with gonadotropin-releasing hormone agonists, without or in combination with an antiandrogen (cyproterone acetate).

Central precocious puberty (CPP) is characterized by early activation of the pituitary-gonadal axis, which leads to increased growth velocity and development of secondary sexual characteristics. It is generally believed that gonadal sex steroids stimulate pulsatile GH secretion, which, in turn, stimulates insulin-like growth factor I (IGF-I) and IGF-binding protein 3 (IGFBP-3) production. However, little is known about GH, IGF-I, and IGFBP-3 serum levels in children with precocious puberty. Treatment of CPP by GnRH agonists has become the treatment of choice. However, the effect of long term treatment with GnRH in combination with an antiandrogen (cyproterone acetate) to block the possible effect of adrenal androgens has not previously been evaluated. We, therefore, studied 40 patients with idiopathic CPP that were treated for 24 months with either GnRH analog (Buserelin) in combination with cyproterone acetate (Androcur; n = 23) or with long acting GnRH analog (Decapeptyl Depot; n = 17). We found that serum IGF-I levels were increased before treatment in both groups (mean +/- SE, 446 +/- 35 and 391 +/- 35 micrograms/L; P < 0.0001, respectively) compared to those in normal age-matched prepubertal children. Similarly, IGFBP-3 levels were significantly elevated (4675 +/- 209 and 4305 +/- 162 micrograms/L, respectively; P < 0.0001) in the two groups. Treatment with GnRH analog in combination with cyproterone acetate significantly decreased height velocity and serum IGF-I and IGFBP-3 levels to normal levels after 2 yr of treatment (P < 0.0001). Serum IGF-I levels remained unchanged during monthly im treatment with long acting GnRH analog, whereas IGFBP-3 levels significantly increased during the first year of this treatment despite unmeasurable estradiol levels. Thus, in both groups, the molar ratio between IGF-I and IGFBP-3 (i.e. free biologically active IGF-I) declined concomitantly with a decrease in growth velocity. Serum levels of IGF-I and IGFBP-3 (expressed as the SD score for bone age), but not those of estradiol, correlated with height velocity before and during treatment (r = 0.34; P < 0.0001 and r = 0.24; P = 0.003, respectively). Six of the patients with a subnormal GH response to clonidine had similar IGF-I and IGFBP-3 serum levels and growth velocity compared to the other 34 girls with CPP and a normal GH response.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗

A morphological study on the effect of cyproterone acetate on human prostatic carcinoma.

Sixteen patients with prostatic carcinoma were treated with 200 mg of Cyproterone acetate daily. No other kind of hormonal treatment was given. Transrectal biopsies of the prostate were taken before the treatment was started, and at regular intervals afterwards. The treatment period lasted from 3 to 16 months, with an average of 9 months. A thorough examination of multiple sections from all specimens revealed no convincing signs of cellular involution. The study has demonstrated no specific or significant atrophic changes following Cyproterone acetate therapy. Some possible explanations regarding the effect of Cyproterone acetate on human malignant prostatic tissue are discussed.

Adenocarcinoma↗

Effects on bone mass of two oral contraceptives containing ethinylestradiol and cyproterone acetate or desogestrel: results of a 2-year follow-up.

BACKGROUND: There are conflicting data about the effects of oral contraceptives on bone mass in young women. Moreover, amenorrheic women may also be affected to varying degrees by osteopenia. Both conditions (oral contraceptive use and amenorrhea) are not infrequent in women during their reproductive years. AIM: To evaluate the safety for bone mass of two oral contraceptives, one containing cyproterone acetate and the other containing desogestrel. METHODS: A total of 67 women between 19 and 29 years of age were studied. Of these women, 35 were selected to receive an oral contraceptive containing 35 mg ethinylestradiol and 2 mg cyproterone acetate. A second group of 32 women received an oral contraceptive containing 30 mg ethinylestradiol and 150 mg desogestrel for 2 years. Immediately before and after the 12th and 24th months of therapy, bone mineral density was assessed by dual X-ray absorptiometry, and hormonal profiles and Ferriman-Gallwey scores were evaluated. RESULTS: After the 2-year follow-up, all subjects showed regular cycles, no pregnancies, and no changes in bone mass density. In addition, hirsute subjects showed a decrease of almost 42% in hirsutism scores. CONCLUSION: Oral contraceptives containing cyproterone acetate or desogestrel in the studied doses have no deleterious effects on bone marrow.

Adult↗

Contraceptive and therapeutic effectiveness of two low-dose ethinylestradiol and cyproterone acetate regimens in the treatment of hirsute patients.

OBJECTIVE: To compare the effectiveness of two very low-dose ethinylestradiol and cyproterone acetate regimens in the treatment of hirsutism. PATIENTS: Eighteen hirsute women were randomized into two different regimens of cyproterone acetate and ethinylestradiol in a reverse sequential pattern: group 1 (0.28 mg ethinylestradiol monthly), group 2 (0.32 mg ethinylestradiol monthly). Both groups received 12.5 mg/day cyproterone acetate for the first 10 days of treatment each month. MAIN OUTCOME MEASURES: Hirsutism scores were measured according to the Ferriman and Gallwey scoring system and side-effects and complications were recorded during the 6 months of therapy. Ovulation was monitored by radioimmunoassay of estradiol, follicle stimulating hormone (FSH), luteinizing hormone (LH) and progesterone levels. The pituitary response was studied using a gonadotropin releasing hormone test. RESULTS: Hirsutism scores decreased significantly in both groups at the end of the 6 months (-30%). All patients were anovulatory, as documented by the reduction of the LH, FSH, estradiol and progesterone levels. Pretreatment basal LH and FSH levels were higher than LH and FSH levels during the treatment. Side-effects were observed only occasionally with some differences between the two therapeutic regiments. CONCLUSION: Both treatments greatly improve hirsutism, reduce clinical problems and side-effects, guarantee both anovulation and contraceptive effectiveness and afford an optimal control of the menstrual cycle.

Adult↗

Effect of cyproterone acetate on the action and metabolism of testosterone in the mouse kidney.

Cyproterone acetate given alone or in combination with testosterone propionate or 5alpha-dihydrotestosterone to castrated male mice does not exhibit an antiandrogenic action on the kidney. It functions rather as a slightly renotropic hormone, even potentiating the renotropic activity of androgens. The administered amount of cyproterone acetate to intact males or castrates supplemented with androgens, however, decreased dramatically the weight of seminal vesicles and of spleen. Cyproterone acetate treatment of the animals influences in vitro the testosterone to androstenedione conversion but not the activity of 5alpha-reductase in the mouse kidney slices.

3-Oxo-5-alpha-Steroid 4-Dehydrogenase↗

[The effectiveness of oral cyproterone acetate in combination with ethinylestradiol in acne tarda of the facial type].

BACKGROUND: Cyproterone acetate is a potent antiandrogen with strong progestational activity. In combination with ethinyloestradiol, it has been shown to be of clinical benefit to women displaying signs of androgenization, such as acne, seborrhoea and hirsutism. In addition, this combined oestrogen/progestogen preparation provides effective contraceptive protection. OBJECTIVE: The aim of this open-label, multicentre study was to determine the efficacy and tolerability of a preparation containing cyproterone acetate and ethinyloestradiol in women with various grades of facial acne. PATIENTS: A total of 890 women aged from 15 to 50 years with grade I-IV facial acne according to the classification of Plewig and Kligman, participated in the study. METHODS: Patients received six cycles of a preparation containing 2 mg cyproterone acetate and 0.035 mg ethinyloestradiol (EE/CPA). Changes from baseline counts of individual acne lesions (open and closed comedones, papules, pustules, nodes and cysts) were monitored together with the simultaneous presence of seborrhoea and hirsutic signs. Reductions in the number of all and individual lesions were classified as: 75-100%, "very good"; 50-75%, "good"; 25-50%, "moderate"; < or = 25%, "absence of therapeutic effect". Body weight and blood pressure were recorded throughout the study. Adverse events and reasons for premature withdrawal from treatment were documented. RESULTS: A "good" or "very good" therapeutic response (i.e. reduction in the total lesion count of > 50%) was seen in 82.8% (95% CI 80.1-85.5) of patients after six cycles of EE/CPA. A similar response was achieved in the different grades of acne with a significant decrease in the number of all lesions throughout the study (p < 0.05). A greater than 50% reduction in open and closed comedones, papules, pustules, nodes and cysts was observed in 75.6%, 80.0%, 88.4% and 85.1% of patients, respectively. By the end of the study, 64.3% of women displayed a lower grade of acne and only 4.9% experienced exacerbation of the condition. EE/CPA was well tolerated, with only 3.4% of patients discontinuing treatment because of adverse events. The majority of events were described as mild, and their incidence declined as the study progressed. No clinically significant changes in blood pressure and body weight were recorded. CONCLUSION: EE/CPA is an effective treatment for acne of all grades and all types of lesion. The preparation is well tolerated and would appear to be an appropriate treatment for women with these symptoms of androgenization.

Acne Vulgaris↗

beta-glucuronidase activity is elevated in the rat harderian gland after bromocriptine but decreased after cyproterone acetate treatment or castration. Postcastrational effects on the ultrastructure of the gland.

OBJECTIVE: To investigate the effect of castration, bromocriptine and cyproterone acetate treatment on lysosomal hydrolytic enzymes and ultrastructure of the rat Harderian gland. METHODS: Groups of rats were subjected to the treatment by bromocriptine, cyproterone acetate and castration. Harderian glands were dissected from each experimental animal cut into small pieces and immediately stored in liquid nitrogen. Only those from castrated animals were fixed in Karnovsky fluid and processed for electron microscopy. The activity of acid phosphatase and ss-glucuronidase were estimated by kits from Sigma (St. Louis, Mo, USA). Semi-thin sections were stained with 1-% toluidine blue and ultra-thin sections with uranyl acetate and counter-stained with lead citrate. The examination was performed by Joel JEM-1200 EX II electron microscope. RESULTS: The treatment of male rats with the prolactin release inhibitor bromocriptine induced a significant increase in ss-glucuronidase activity. On the contrary, such activity was significantly decreased after treatment with the testosterone receptor antagonist cyproterone acetate as well as after castration. However, these treatments did not alter the activity of lysosomal acid phosphatase. Castration induced dramatic changes mostly in type A cells such as the appearance of lipid vacuoles with irregular forms and the predomination of smooth endoplasmic reticulum (SER) throughout the cytoplasm. The most dramatic postcastrational change was the degeneration of the mitochondria. These changes in type A cells might be due to the uneven distribution of the testosterone receptors in the rat Harderian gland, which are more numerous in type A cells. CONCLUSIONS: the gland physiology is responsive to alteration in circulating prolactin and testosterone levels.

Acid Phosphatase↗

[Effects of a sequential combination of estradiol valerate and cyproterone acetate on the functional properties of the arterial wall in menopausal women].

Several studies have shown that estrogen replacement therapy protects postmenopausal women against coronary artery disease. This protective effect has been ascribed to the hormone's effect on serum lipids, as well as a direct action on the vascular wall. Concurrent administration of a progestin to protect women from the risk of endometrial hyperplasia may alter the protective effects of estrogen. The aim of this study was to assess the evolution of the endothelial function in postmenopausal women given a sequential combination of oral 2 mg estradiol valerate for 11 days, followed by 2 mg estradiol valerate associated with 1 mg cyproterone acetate for ten days (Climène). Each 21-day sequence was followed by a seven-day treatment-free interval. The women received a three-month treatment course. Thirty-one healthy postmenopausal women participated in the study (median age: 51 years; range: 45-59 years). Flow-mediated dilatation (FMD), a reflection of endothelium-dependent vasomotor function, increased from 8.47% at baseline (range: 4.57-11.02%) to 9.64% (range: 7.07-13.12%) at the end of the first treatment cycle; i.e., a 15% increase over baseline (P < 0.0001). FMD further increased after three treatment cycles to 10.59% (range: 8.09-15.22%); i.e., a 28.6% increase over baseline (P < 0.0001). FMD at the end of the first combined sequence or after the 11 days of estradiol only were similar (delta = 0.25%; range: -2.31-5.81%; not significant). In conclusion, in postmenopausal women, a three-month sequential treatment combining estradiol valerate and estradiol valerate plus cyproterone acetate (Climène) has beneficial effects on endothelial function as demonstrated by the evolution of the FMD. There was no decrease in the effect of estradiol on FMD when cyproterone acetate was added to estradiol.

Arteries↗

Comparison of the effect on acne with a combiphasic desogestrel-containing oral contraceptive and a preparation containing cyproterone acetate.

OBJECTIVE: To investigate the effect of a combiphasic oral contraceptive containing ethinylestradiol and desogestrel (combiphasic EE/DSG) on acne, compared with a preparation containing ethinylestradiol and cyproterone acetate (EE35/CPA). METHODS: An open, randomized, group-comparative, multicenter study was carried out, with 172 women randomized to treatment with either combiphasic EE/DSG (25 microg desogestrel and 40 microg ethinylestradiol for 7 days followed by 125 microg desogestrel and 30 microg ethinylestradiol for 15 days) or EE35/CPA (2.0 mg cyproterone acetate and 35 microg ethinylestradiol for 21 days). Assessments were performed at pretreatment and after cycles 3 and 6. RESULTS: The number of comedones, papules, pustules and nodules significantly decreased in both groups over the 6-month study. Compared with pretreatment (= 100%), the relative numbers of comedones, papules, pustules and nodules at cycle 6 significantly decreased to 37%, 38%, 19% and 12.5% in the combiphasic EE/DSG group and to 24%, 36%, 17% and 1% in the EE35/CPA group, respectively. All reductions were statistically significant (p < or = 0.003) at both cycles 3 and 6, except for nodules at cycle 6 with combiphasic EE/DSG, which probably resulted from differences between the treatment groups at baseline. There were no statistically significant differences between the two treatments. In both groups, the majority of women with severe acne shifted to a less severe acne category. CONCLUSIONS: Combiphasic EE/DSG progressively reduced the number and severity of acne lesions during the six cycles of treatment. The reduction in acne with the combiphasic oral contraceptive was comparable to a preparation containing the antiandrogen cyproterone acetate.

Acne Vulgaris↗

Cyproterone, norethindrone, medroxyprogesterone and levonorgestrel are less potent local human growth hormone and insulin-like growth factor I secretion stimulators than progesterone in human breast cancer explants expressing the estrogen receptor.

The aim of the present study was to compare the ability of natural progesterone and synthetic progestins to stimulate local growth hormone (GH) and insulin-like growth factor I (IGF-I) secretion by breast cancer explants. Explants obtained during surgery were divided according to their estrogen/progesterone receptor phenotype - ER(+)PR(-); ER(+)PR(+); ER(-)PR(+) - as determined by immunocytochemistry. Natural progesterone (10(-5) mol/l) and synthetic progestins (cyproterone acetate (5 x 10(-7) mol/l), norethindrone (10(-5) mol/l), medroxyprogesterone acetate (10(-7) mol/l), and levonorgestrel (10(-7) mol/l) were tested in vitro for their ability to induce secretion of proliferation-promoting agents such as human GH (hGH) and IGF-I. All hormone-dependent breast cancer cell types responded to progesterone stimulation with increased local hGH secretion, while in the non-malignant tissue this effect was observed only in PR(+) cells. Moreover, progesterone in only PR(+) cells in vitro stimulated local IGF-I secretion by both malignant and non-malignant tissue. Medroxyprogesterone and levonorgestrel increased GH secretion by both malignant and non-malignant ER(-)PR(+) breast cancer explants, while cyproterone stimulated it only in non-malignant tissue. None of the synthetic progestins tested in this experiment exerted an effect on GH secretion by both malignant and non-malignant tissue of ER(+) breast cancer explants. The present data additionally showed that, apart from cyproterone, which increased IGF-I secretion in the same manner as progesterone by both malignant and non-malignant ER(-)PR(+) breast explants, other progestins tested had either no effect on IGF-I local secretion or decreased it. Medroxyprogesterone and levonorgestrel induced a decrease in IGF-I secretion noted in ER(+) explants of non-malignant tissue and in malignant ER(-)PR(+) breast tissue. All progestins tested decreased IGF-I secretion by malignant ER(+)PR(+) explants. Taken together, the tested synthetic progestins widely used as oral contraceptives and in hormone replacement therapy were less potent than progesterone in inducing secretion of proliferation-promoting agents such as hGH and IGF-I in ER-containing breast tissue. Despite the lack of confirmation of the link between the use of progestins and breast cancer risk, patients should be informed that the use of certain estrogen/progestin preparations is of no influence on breast cancer risk while others may increase it.

Breast↗

[Cyproterone acetate: cardiovascular tolerance].

Cyproterone acetate, characterised by its antiandrogen and antigonadotrophin actions, is indicated in the treatment of advanced prostatic cancer. It can be used alone or in combination with surgical or chemical castration. This paper reviews the literature concerning the cardiovascular safety of this drug. Metabolic studies evaluating the impact of cyproterone acetate on lipids and certain clotting parameters indicate the absence of any harmful effects on these cardiovascular risk factors. The two trials conducted by the EORTC (30761 and 30 762) demonstrated that the cardiovascular safety of cyproterone acetate was better than that of diethylstilboestrol. Cardiovascular adverse effects were reported in less than 5% of cases. This figure was confirmed by a large number of published studies. A comparable incidence of cardiovascular complications was also observed in series of patients treated by orchidectomy, LHRH agonists and/or pure antiandrogens. It is difficult to formally demonstrate the responsibility of antihormonal treatment in this elderly population in which ischaemic heart disease and cerebral vascular accidents are frequent causes of death.

Cardiovascular Diseases↗

Determination of cyproterone acetate in plasma samples by high-performance liquid chromatography.

A rapid and sensitive high-performance liquid chromatographic method for the determination of cyproterone acetate in human plasma has been developed. The chromatographic separation was performed on an analytical mbondapak C8 column (125 yen 4.6 mm, i.d) with an isocratic mobile phase consisting of methanol-water (62.38 v/v). Using ultra violet detection at 282 nm, the detection limit for cyproterone acetate in plasma was 10 ng/ml. The calibration curve was linear over the concentration range 50-160. 0 ng/ml. Cyproterone was isolated from plasma by liquid-liquid extraction and the recovery was about 90% for plasma. The inter-day and intra-day assay coefficients of variation were found to be less than 10%.

Androgen Antagonists↗

[Cyproterone acetate improves beta-cell function in postmenopausal women with diabetes mellitus type 2].

Menopause is associated with two main risk factors for the development of type 2 diabetes mellitus--impaired beta-cell insulin secretion and insulin resistance. Physiologically estrogens improve carbohydrate metabolism, but this is not the case with different progestogens. The aim of the present study was to evaluate the effect of Cyproterone acetate (a progestogen with antiandrogenic activity) on insulin secretion, peripheral insulin sensitivity, lipid parameters and parameters of oxidative stress. Seven type 2 diabetic females, of mean age 55.4 +/- 4.7 years and mean BMI 30.8 +/- 9.39 kg/m2, in menopause for average 5 years, in good borderline glycaemic control (mean HbAic 7.8%), with dyslipidaemia, normal parameters of calcium and phosphate metabolism and with osteopenia (T-score < 88%) were enrolled in the study. They were treated with Estradiol valerate + Cyproterone acetate (Climen, Schering) for three months. Phases of insulin secretion--first phase (FPIS), second phase (SPIS) and AUC for FPIS and SPIS were assessed during IVGTT. Insulin sensitivity was determined with the manual method of euglycaemic hyperinsulinaemic clamp technique. The postmenopausal diabetic women in the present study were with overweight and obesity; they did not increase their body weight during HRT and even decreased it by mean 0.7%. Insulin secretion improved after Climen--FPIS increased by 16% and SPIS by 44%. Insulin sensitivity increased by 15%; triglycerides decreased by 16% and HDL-cholesterol increased by 27%. Total antioxidant capacity of the serum (TAOK) increased by 7%. The favourable effect on the pathophysiological mechanisms improved metabolic control--HbAic was reduced by mean 3% after 3 months. In conclusion, our results suggest that HRT with the progestogen Cyproterone acetate (Climen) should be preferred in postmenopausal type 2 diabetic females with predominant beta-cell insulin secretion defect.

Blood Glucose↗

The efficacy of topical cyproterone acetate alcohol lotion versus placebo in the treatment of the mild to moderate acne vulgaris: a double blind study.

Acne is an inflammatory condition of the pilosebaceous unit. One of the essential factors for development of acne lesions is increased sebum excretion that is promoted by androgen. It is shown that oral cyproterone acetate significantly reduces the sebum excretion. In this study we evaluated the efficacy of cyproterone acetate alcohol lotion (CAAL) in the treatment of the mild to moderate acne vulgaris. This was a randomized double-blind clinical trial performed on 86 female patients with mild to moderate acne. They were randomly divided into 3 groups and were treated with 0.5 percent CAAL (n = 30), 1 percent CAAL (n = 13) and placebo (n = 43). They were followed every 15 days for a period of 45 days. Response to treatment was evaluated by the total acne lesions counting (TLC) and acne severity index (ASI) and was analyzed statistically by SPSS program. The efficacy of treatment on TLC was maximum for 1 percent CAAL (90 % reduction in TLC)(P value = 0.000). CAAL at 0.5 percent was able to reduce TLC as high as 80.8 percent during 6 weeks followup. The efficacy of placebo was determined to be 38.5 percent. Regarding TLC, 1 percent CAAL was 2.33 times more effective than placebo. CAAL at 0.5 percent was 2.09 times more effective than placebo in this respect. The efficacy of treatment on ASI was maximum for 1 percent CAAL (88 % reduction in ASI)(P value = 0.000). CAAL at 0.5 percent reduced ASI as much as 79.5 percent during 6 weeks of followup. The efficacy of placebo was calculated to be 9.8 percent in reduction of ASI . Regarding ASI, 1 percent CAAL was 8.97 times more effective than placebo. CAAL at 0.5 percent was 8.06 times more effective than placebo. Regarding the results of this study, we suggest the use of cyproterone acetate alcohol lotion as one of the main treatments for mild-moderate acne in female patients and as an adjuvant treatment for moderate to severe acne vulgaris.

Acne Vulgaris↗

[Adrenal reactivity to prolonged-action ACTH in hirsute women treated with 50 mg of cyproterone acetate combined with percutaneous estradiol].

A prolonged-action Synacthen (R) test (1 mg.i.m. was performed in 14 hirsute women before and 6 months after instituting combined treatment with cyproterone acetate (50 mg/day/21 days) and percutaneous estradiol (3 mg during the last 10 days of cyproterone acetate administration). Determination of blood cortisol and precursors of cortisol--plasma androgens--was carried out to evaluate possible modification of adrenal enzymatic activity. At the used doses, cyproterone acetate failed to influence adrenal reactivity to synthetic ACTH or the enzymatic activities of 21-hydroxylase and 17-beta-reductase in vivo.

Administration, Cutaneous↗

Effects of cyproterone and tamoxifen upon the hair waves in mice.

The effects of cyproterone and of tamoxifen citrate upon the hair waves were studied in normal and castrated C57 mice. Cyproterone (1 mg/day) had no effect upon the hair waves in normal male mice and produced a slight inhibition of the diffuse growth induced by their castration. Tamoxifen citrate (1 mg/day) had no effect upon the hair waves in normal female mice and produced a marked inhibition (0.2 to 1 mg/day) upon the diffuse hair growth induced by their castration. The differences between the effects of castration and the effect of these drugs can be explained in the case of cyproterone by a slight agonistic androgenic effect and in the case of tamoxifen citrate by a marked agonistic estrogenic effect upon the hair follicles in mice.

Animals↗