Comparison of the anti-androgen effects of cyproterone acetate and spironolactone on male-to-female transsexuals / 中华医学美学美容杂志

Objective:To compare the anti-androgenic effect of cyproterone acetate (CPA) and spironolactone (SPL) on male-to-female transsexuals.Methods:From January 2012 to September 2021, 185 male-to-female transsexuals (95 using CPA and 90 using SPL) who visited the Peking University Third Hospital and under stable medication for ≥3 months were enrolled, aged 16 to 40 (23±5) years. General information and laboratory indicators of the last visit were collected for a cross-sectional study.Results:The median doses of antiandrogens in the CPA group and SPL group were 25 mg/d and 80 mg/d, respectively. And the median dose of oral estradiol valerate in both groups was 2 mg/d. Testosterone level in the CPA group was significantly lower than the SPL group [0.7 (0.7-1.5) nmol/L vs. 13.2(6.7-18.4) nmol/L, U= 6 970.500, P<0.001]. The CPA group also had better subjective effects on testicular atrophy, erection decrease, body hair decrease, skin softening and figure feminization (all P<0.05). The prolactin level of CPA group was significantly higher than that of SPL group [21.5 (12.6-30.1) ng/ml vs. 11.9 (7.7-20.0) ng/ml, U= 2 053.500, P<0.001]. Conclusions:CPA has a more significant effect on lowering testosterone levels than SPL, and is better than SPL in terms of testicular atrophy, erection decrease, body hair decrease, skin softening and figure feminization, albeit with a potentially higher risk of hyperprolactinemia.

Effect of Shengxuening tablets combined with ethinylestradiol and cyproterone acetate on thickness of endometrium and hemoglobin levels in patients with endometrial polyps for transcervical resection of polyp / 国际中医中药杂志

Objective To investigate the effects of Shengxuening tablets combined with ethinylestradiol and cycloproterone acetate on endometrial thickness and hemoglobin level in patients with endometrial polyps for transcervical resection of polyp. Methods A total of 150 patients with hysteroscopic endometrial polypectomy were randomly divided into three groups, 50 in each group. The control group was treated with hysteroscopy endometrial polyp electrotomy, while the western medicine group was treated with ethinylestradiol and cycloprogesterone acetate tablets on the basis of the control group, and the combined group was treated with Shengxuening tablets on the basis of the western medicine group. The menstrual volume, endometrial thickness and hemoglobin levels were observed before treatment, at 3 month, 6 month and 12 month after treatment, and the clinical efficacy and recurrence during follow-up were evaluated. Results The total effective rate was 98.0％(49/50) in the combined group, 96.0％ (48/50) in the western medicine group, 86.0％ (43/50) in the control group. The total effective rate in the combined group and the western medicine group was significantly higher than that in the control group (χ2=6.643, P=0.036). The menstrual volume (F=28.096, 49.096, 33.303), endometrial thickness (F=11.214, 20.265, 63.947) in the three groups were significantly different after treatment (P<0.01), and which in the combined group were significantly lower than those in the western medicine group, menstrual volume at 36,12 after treatment (t value were 4.747, 2.244, 4.489, P<0.01); endometrial thickness at 3, 6, 12 month after treatment (t value were 3.293, 3.356, 5.293, P<0.01); there were significant differences in hemoglobin levels in the three groups (F=11.002, 8.662, 8.958, P<0.01), and which in the combined group was significantly higher than that in the western medicine group at 3,6,12 month after treatment (t value were 2.722, 2.074, 2.028, P<0.05). During the follow-up period, 2 cases (4.1％) recurred in the combined group, 3 cases (6.3％) recurred in the western medicine group and 9 cases (20.9％) recurred in the control group. The recurrence rate in the combined group or the western medicine group was significantly lower than that in the control group (χ2=6.775, P=0.034). There was no significant difference in the recurrence rate in the combined group and the western medicine group (χ2=0.211, P=0.646). Conclusions The Ethynestradiol and Cyproterone acetate combined with Shengxuening tablets could improve the curative effect, reduce menstrual volume and endometrial thickness, increase hemoglobin level and reduce recurrence rate in patients with endometrial polyps for transcervical resection of polyp.

Effects of Ethinylestradiol and Cyproterone Acetate Combined with Metformin on Ovulation Induction of Pa-tients with Polycystic Ovarian Syndrome / 中国药房

OBJECTIVE:To discuss the effect of Ethinylestradiol and cyproterone acetate tablet combined with metformin on ovulation induction of patients with polycystic ovarian syndrome(PCOS). METHODS:184 PCOS patients were randomly divided into control group(92 cases)and observation group(92 cases). Control group orally received 1 Ethinylestradiol and cyproterone ac-etate tablet in 5 d of menstruation,once a day,it stopped after 21 d,the next cycle of treatment was started on the 5th of with-drawal bleeding. Observation group additionally received 3 Metformin tablet,once a day,without drug withdrawal during menstrua-tion,and lasted for 3 menstrual cycles. After 3 menstrual cycles,all patients received ovulation induction treatment [(50-100 mg clomiphene was orally given from the 5th day of the 4th menstrual cycle,for 5 days,or 75-150 U postmenopausal gonadotropin by intramuscular injection,when the dominant follicle diameter was(19.0±2.0)mm,10 000 U human chorionic gonadotropin(HCG) was intramuscularly injected,the ovulation was continuously monitored and whether there was ovarian hyperstimulation syndrome (OHSS)was observed]. Body mass index(BMI),follicle estrogen(FSH),luteinizing hormone(LH),prolactin(PRL),estradiol (E2)and testosterone(T)before and after treatment,fasting plasma glucose(FPG),fasting insulin(FINS),insulin resistance in-dex(HOMA-IR),pregnancy rate,ovulation rate and the incidences of OHSS and adverse reactions in 2 groups were observed.RE-SULTS:Before treatment,there were no significant differences in the BMI,FSH,LH,PRL,E2,T,FPG,FINS and HOMA-IR between 2 groups(P>0.05). After treatment,BMI,LH,PRL,E2,T,FPG,FINS and HOMA-IR in observation group and LH, E2 and FINS in control group were significantly lower than before,and BMI,PRL,E2,T,FPG,FINS and HOMA-IR in observa-tion group were lower than control group,the differences were statistically significant(P0.05). CONCLUSIONS:Ethinylestradiol and cyproterone acetate combined with metfor-min can effectively improve insulin resistance of POCS patients,recovery sex hormone secretion,promote ovulation and improve pregnancy rate,with good safety.

The ovulation effect of ethinylestradiol and cyproterone acetate combined with metformin on obesity type polycystic ovary syndrome / 中国医师进修杂志

Objective To evaluate the ovulation effect of ethinylestradiol and cyproterone acetate combined with metformin on obesity type polycystic ovary syndrome (PCOS).Methods Sixty-two patients with obesity type PCOS were divided into 2 groups by random digits table method:control group (30 cases) was treated with letrozole;observation group (32 cases) was treated with letrozole after 3 months treated with ethinylestradiol and cyproterone acetate combined with metformin.The weight,body mass index (BMI),glycometabolism indexes [fasting plasma glucose (FPG),fasting insulin (FINS) and homeostasis model of assessment for insulin resistance index (HOMA-IR)],hormone [follicle-stimulating hormone (FSH),luteotrophic hormone (LH),estradiol (E2) and testosterone (T)] before and after treatment and ovulation rate and pregnancy rate were compared between 2 groups.Results There were no statistical differences in weight,BMI,FPG,FINS and HOMA-IR in control group between before treatment and after treatment (P ＞ 0.05).The indexes in observation group after treatment were significantly lower than those before treatment [(55.76 ± 2.69) kg vs.(64.42 ± 4.93) kg,(21.52 ± 1.43) kg/m2 vs.(25.74 ± 1.58) kg/m2,(4.46 ± 0.89) mmol/L vs.(5.69 ± 2.01) mmol/L,(12.24 ± 1.82) mU/L vs.(22.88 ± 2.06) mU/L,2.94 ± 1.76 vs.5.27 ± 1.18],there were statistical differences (P＜ 0.05).There were no statistical differences in FSH and E2 in 2 groups between before treatment and after treatment (P ＞ 0.05).There were no statistical differences in LH and T before treatment between 2 groups (P ＞ 0.05),but after treatment were significantly lower than before treatment [control group:(10.33 ±0.57) mU/L vs.(15.63 ± 1.32) mU/L and (1.22 ±0.96) μg/L vs.(2.21 ± 1.24) μ g/L;observation group:(9.07 ± 0.82) mU/L vs.(16.18 ± 1.24) mU/L and (0.71 ± 1.24) μ g/L vs.(2.43 ± 1.52) μ g/L],furthermore the observation group was lower,there were statistical differences (P ＜ 0.05).The ovulation rate and pregnancy rate in observation group were significantly higher than those in control group [78.12％(25/32) vs.53.33％(16/30) and 53.12％(17/32) vs.26.67％(8/30)],there were statistical differences (P ＜ 0.05).Conclusion Ethinylestradiol and cyproterone acetate combined with metformin is more effective on obesity type PCOS,which can improve the ovulation rate and pregnancy rate.

Efficacy of rosiglitazone combined with ethinylestradiol cyproterone on treatment of polycystic ovary syndrome / 中国医师进修杂志

Objective To observe the effect of rosiglitazone combined with ethinylestradiol cyproterone on treatment of polycystic ovary syndrome (PCOS).Methods Sixty-eight cases with PCOS combined with insulin resistance (experimental group) and 68 cases with PCOS combined without insulin resistance (control group) were selected.The patients in experimental group were given rosiglihtazone combined with ethinylestradiol cyproterone,the patients in control group were not given rosiglitazone.The level of seurm adiponectin and lepfin was measured before and after treatment in two groups,body mass index (BMI),Homeostasis model assessment of insulin resistance index (HOMA-IR) was calculated before and after treatment in two groups,and drug adverse reaction was observed.Results There was no significant difference in serum adiponeetin,leptin,BMI before treatment between two groups (P ＞ 0.05).HOMA-IR in experimental group was higher than that in control group (3.90 ± 0.87 vs.2.15 ± 0.62),and there was significant difference (P ＜ 0.05).BMI,leptin after treatment in experimental group and control group was decreased compared with that before treatment [experimental group:(25.41 ± 1.01) kg/m2 vs.(30.11 ± 1.51) kg/m2,(0.25 ± 0.08) μ g/L vs.(0.44 ± 0.11) p g/L; control group:(26.68 ± 1.12) kg/m2 vs.(30.55 ± 1.42) kg/m2,(0.23 ± 0.1 0) μ g/L vs.(0.39 ± 0.23) μ g/L],adponectin was increased compared with that before treatment [experimental group:(1.39 ± 1.10) μ g/L vs.(0.89 ± 0.15) μ g/L;control group:(1.42 ± 1.05) μ g/L vs.(0.91 ± 0.44) μ g/L],and HOMA-IR after treatment (2.09 ± 0.68) in experimental group was lower than that before treatment,and there was significant difference (P ＜ 0.05).There was no significant difference between two groups (P ＞0.05).Experimental group did not appear obvious drug adverse reaction in the process of treatment.Conclusion Ethinylestradiol cyproterone can improve metabolic disorders indicators,PCOS combined with insulin resistance should add rosiglitazone to improve insulin resistance.

The clinical research of ethinylestradiol and cyproterone acetate combined with metformin in patients with polycystic ovary syndrome / 中国医师进修杂志

Objective To explore the clinical efficacy of ethinylestradiol and cyproterone acetate (Diane-35) combined with mefformin in patients with polycystic ovary syndrome (PCOS).Methods One hundred and sixty patients with PCOS were divided into control group and observation group by random digits table method with 80 cases each.Patients in the control group were given Diane-35 only,while patients in the observation group were given Diane-35 combined with metformin.The triglycerides (TG),total cholesterol (TC),low density lipoprotein cholesterol (LDL-C),fasting insulin (FINS),fasting blood glucose (FBG),follicle-stimulating hormone (FSH),luteinizing hormone (LH) and testosterone (T) of patients in the two groups were measured before treatment and after treatment 6 months,the rates of pregnancy and abortion were recorded.Results TC,LDL-C,FINS,FBG,FSH,LHt and T of both the 2 groups after treatment decreased obviously than before treatment,and TG in observation group decreased obviously than before treatment,there were statistical differences (P ＜ 0.05).There was no statistical difference in TG in control group between before treatment and after treatment (P ＞ 0.05).After treatment,TG,FINS,FBG,LH in observation group were lower than those in control group [(1.0 ± 0.2) mmol/L vs.(1.6 ± 0.8) mmol/L,(15.2 ± 6.3) mU/L vs.(18.9 ± 6.2) mU/L,(4.5 ± 1.1) mmol/L vs.(5.1 ± 0.9) mmol/L,(6.3 ± 3.0) U/L vs.(7.4 ± 2.9) U/L],there were statistical differences (P ＜ 0.05).After treatment,the rate of pregnancy in observation group was higher than that in control group [61.2％(49/80) vs.42.5％(34/80)],there was statistical difference (x2 =5.633,P＜ 0.05).The rote of abortion in observation group was lower than that in control group [6.1％(3/49) vs.17.6％(6/34)],but there was no statistical difference (x2 =1.694,P ＞ 0.05).Conclusion The clinical effect of Diane-35 combined with metformin in patients with PCOS is better than Diane-35 only.

Tratamento hormonal da acne baseado em evidências / Hormonal treatment of acne based on evidence

Este trabalho de revisão apresenta o tratamento hormonal da acne baseado em evidências. O trabalho resume a clínica, a classificação, a fisiopatologia e a etiologia da acne. A avaliação de estudos selecionados mostrou que o tratamento hormonal da acne deve ser complementado por tratamento cosmiátrico, e não está indicado para gestantes ou mulheres com planos de engravidar. A primeira escolha para esse tratamento são os contraceptivos hormonais orais, pois são efetivos e seguros para tratamento da acne e também para anticoncepção. Após tempo estabelecido, se o resultado for insatisfatório, outro medicamento, como acetato de ciproterona ou espironolactona, deve ser adicionado. A finasterida é o medicamento indicado para acne de origem idiopática, e a flutamida apresenta efeitos colaterais significativos, não constituindo indicação segura até o momento.

This review shows the hormonal treatment of acne. The review summarizes the clinical aspects, classification, physiopathology and etiology of the acne. The evaluation of selected papers showed that hormonal treatment of acne with hormones has to be complemented by esthetics treatment and is not prescribed for pregnant women or those who want to get pregnant. The first choice of treatment is the hormonal oral contraceptive one, because it is effective and safe for treatment of acne and also for contraception. After an established period with unsatisfactory results, other medicines, such as ciproterone acetate or spironolactone, can be added. The finasteride is prescribed for idiopathic acne and flutamide has many relevant side effects and is also not safe.

Clinical assessment of ethinylestradiol and cyproterone acetate in menstrual irregularities of hyper-androgenic origin / Avaliação clínica do uso de duas preparações de etinilestradiol e acetato de ciproterona em menstruação irregular de origem hiperandrogênica

We report on the results of a double-blind, randomized, controlled clinical trial comparing two preparations of ethinylestradiol and cyproterone acetate in the treatment of women of reproductive age presenting menstrual irregularities of hyper-androgenic origin. After obtaining informed consent, subjects were randomized to a 4-month treatment period consisting of one daily dose of 0.035mg ethinylestradiol + 2mg cyproterone acetate. The treatment regimen cycle consisted of one pill, once daily for 21 days, followed by a 7-day pill-free period. We compared the efficacy of two presentations of the drug combination after each treatment cycle (Visits 2, 3, 4, and 5) in establishment and maintenance of menstrual regulation, intensity of menstrual flow, and dysmenorrhea, as well as a comparison of the two presentations in terms of Global Satisfaction and Drug Satisfaction assessments performed by the patients and the investigating physician. At each study visit, drug compliance and use of concomitant medications, as well as incidence, severity and duration of adverse events were recorded. A total of 86 subjects were randomized to treatment, with 43 subjects in each treatment group. At Visit 2 and each subsequent visit, all patients in both treatment groups reported an episode of withdrawal bleeding during the 7-day hormone-free period. We observed a statistically significant (p<0.0001) decrease in the incidence of dysmenorrhea at each study visit in relation to the pretreatment assessment. There was a significant reduction (p<0.0001) in the number of subjects reporting intermenstrual bleeding at each study visit in both treatment groups. Global Satisfaction scores by the patient and physician increased significantly at each successive study visit in both treatment groups. There were no clinically significant changes in vital signs, weight, and body mass index throughout the study period in either group. The number of subjects reporting adverse events at each visit did not vary between treatment groups. The combined oral contraceptive pill containing ethinylestradiol and cyproterone acetate was found to be both effective and safe in the menstrual irregularities of hyper-androgenic origin (amenorrhea, dysmenorrhea, and intermenstrual bleeding) assessed in this study.

Tratamento hormonal do hirsutismo baseado em evidências / Evidence-based hormonal treatment of hirsutism

A revisão de estudos baseados em evidências mostra o melhor tratamento hormonal para o hirsutismo. Inicialmente, resumiu-se a fisiologia do pelo, caracterizou-se o hirsutismo, suas variantes e suas causas. Revelou-se que o tratamento hormonal do hirsutismo deve ser complementado pelo tratamento cosmético e não deve ser indicado para mulheres grávidas ou que desejam engravidar. A primeira opção é o contraceptivo hormonal oral, seguro para contracepção e eficaz para tratamento do hirsutismo. Após tempo estipulado, não ocorrendo resposta satisfatória, associar acetato de ciproterona ou espironolactona. A finasterida é indicada para hirsutismo idiopático e a flutamida, devido aos efeitos colaterais, ainda não é opção segura

An evidence-based review shows the best hormonal treatment of hirsutism. This paper summarized the physiology of the hair, characterized the hirsutism, its variants and etiologies. The study revealed that hormonal treatment of hirsutism has to be complemented by esthetic treatment, and it is not recommended for pregnant women or for those who want to get pregnant. The first option is hormonal oral contraceptive, which is safe for contraception and effective for treatment of hirsutism. After a established period of treatment, if good results do not occur, the association of cyproterone or spironolactone is recomended. Finasteride is the treatment of idiopathic hirsutism, and flutamide is not a safe option due to its side effects

Effects of ethinylestradiol and cyproterone acetate on endocrine metabolism in non-obese women with polycystic ovary syndrome / 上海交通大学学报（医学版）

Objective To investigate the effects of ethinylestradiol and cyproterone acetate tablets(Diane-35)on endocrine metabolism in non-obese women with polycystic ovary syndrome(PCOS). Methods Fifty-three non-obese patients with PCOS were assigned to the 6-month treatment with Diane-35.Body mass index(BMI),waist to hip ratio(WHR),F-G score and acne score were recorded before treatment and at the end of the third and sixth cycle after treatment.Serum total testosterone,follicle stimulating hormone(FSH),luteinizing hormone(LH),LH/FSH,fast plasma glucose,fast insulin and insulin resistance index(HOMA-IR)were obtained at early follicular phase and at the end of the third and sixth month.Results There was no significant change in BMI and WHR after treatment.Compared with those before treatment.F-G score,acne score,serum total testosterone,LH and LH/FSH were significantly decreased at two time points after treatment (P<0.05).BMI and HOMA-IR in patients with insulin resistance were significantly higher at the end of the sixth cycle after treatment than those before treatment(P<0.05). Conclusion Diane-35 can improve hyperandrogenism in non-obese patients with PCOS.However,Diane-35 may aggravate insulin resistance in those with insulin resistance.

A case of fulminant hepatic failure due to cyproterone acetate in a patient with cryptogenic liver cirrhosis / 대한내과학회지

Cyproterone acetate is an antiandrogenic drug that has been used in prostatic cancer. The drug is thought to be well-tolerated but has hepatotoxic effects. An 89 year-old man treated with cyproterone acetate 300 mg/d for prostatic cancer presented with a hepatotoxic reaction. Toxic hepatitis was diagnosed and cyproterone acetate was stopped immediately. The patient was treated with supportive management and a corticosteroid, but he died 28 days after administration due to liver failure. A liver biopsy performed after his death revealed the presence of acute hepatitis with cirrhosis. Underlying cirrhosis was not suspected before his death. Ultimately, the case was diagnosed as fulminant hepatic failure due to cyproterone acetate with underlying cryptogenic liver cirrhosis. This case and current literature highlight the hepatotoxic potential of cyproterone acetate and illustrate the importance of clinical surveillance, especially in patients with unrecognized liver disease.

Effects of Metformin Combined with Cyproterone Acetate on Clinical Features, Endocrine and Metabolism of Non-obese Women with Polycystic Ovarian Syndrome / 华中科技大学学报（医学）（英德文版）

In order to explore the effects of metformin combined with cyproterone acetate (CPA) on the clinical features, endocrine and metabolism of the patients with polycystic ovarian syndrome (PCOS), 50 cases of non-obese PCOS were randomly subjected to CPA (CPA treatment group, n=25) and CPA+metformin (n= 25) treatment for 6 months. Before and after treatment the body mass index (BMI), waist: hip ratio (WHR), ovarian volume, serum gonadotrophin, androgen and sex hormone-binding globulin (SHBG) levels, and fasting lipid, glucose and insulin levels were measured. The results showed that all of the parameters in two groups were similar before treatment. After treatment for 6 months in the CPA+ metformin group, BMI and WHR were significantly decreased, while insulin sensitivity was significantly decreased as compared with those before treatment. In CPA group, no significant changes were found before and after treatment. Combined use of CPA and metformin could result in the reduction of serum androstenedione and increases of serum SHBG levels as compared with the CPA treatment alone. It was concluded that combined use of CPA and metformin could improve the insulin sensitivity, and further suppress the hyperandrogenism in non-obese women with PCOS.

Intermittent Androgen Deprivation(IAD) with Cyproterone Acetate Monotherapy for Prostate Cancer: A preliminary report / 대한비뇨기과학회지

PURPOSE: The purpose of this study was to evaluate the feasibility of using IAD, as a steroidal antiandrogen (cyproterone acetate) monotherapy, for prostate cancer. MATERIALS AND METHODS: A total of 43 prostate cancer patients (Stage A to C in 27, D1 in 2 and D2 in 14) were reviewed. Androgen deprivation, with cyproterone acetate (200-300mg P.O/day), was continued until a serum prostate specific antigen (PSA) nadir was maintained for at least 3 months. Medication was then discontinued until the serum PSA reached a predetermined level. This cycle of treatment was repeated until there was a continual increase in the PSA irrespective of the medication. RESULTS: The mean observation period was 10.5 months, ranging from 4 to 28 months. In seven of the 43 patients, there was treatment failure before entering the off-treatment period of the 1st cycle. 17 of the remaining 36 patients completed the on-treatment during cycle 1, with a median time to PSA nadir of 4 months. Seven patients completed cycle 1, with a median time off-treatment of 5 months (43% of the treatment cycle). Nineteen patients are still in the on-treatment intervals and 10 in the off-treatment intervals of their first cycles. Two patients completed the on-treatment of the 2nd cycle, with a median time to PSA nadir of 2.5 months. During the off-treatment interval, most patients reported an improvement in the symptoms associated with androgen suppression. CONCLUSIONS: IAD, using cyproterone acetate monotherapy, is a feasible alternative for continuous androgen deprivation in the treatment of prostate cancer. It also results in the reduction of toxicity, cost of treatment and possibly a delay in the tumor progression.

Do thyroid and testis modulate the effects of pineal and melatonin on haemopoietic variables in Clarias batrachus.

Involvement of pineal and its major hormone, melatonin, in the process of erythropoiesis in a freshwater catfish, Clarias batrachus has been investigated. The study was conducted during four phases, namely preparatory phase, spawning phase, postspawning phase and late postspawning phase of its annual reproductive cycle. During each phase a fish received either melatonin injections or subjected to pinealectomy. In addition, each fish in all the groups, received either iopanoic acid or cyproterone acetate or vehicle in the morning or late afternoon. Results clearly indicate that melatonin stimulates the rate of erythropoiesis in Clarias batrachus. It appears that the extent of stimulation depends upon the phase of the annual reproductive cycle. However, in general, the pineal- or melatonin-induced modulation of blood variables is gonad dependent and thyroid seems to play a time of the day dependent subtle role.

Biological and clinical research on male reproduction and fertility regulation.

Biological and clinical research on male reproduction and fertility regulation carried at the National Institute of Health and Family Welfare over the past 17 years has been highlighted in this review. Areas of research covered pertains to hormones in relation to sperm maturation and transport; fertilizing ability of spermatozoa under different experimental conditions; agents producing functional sterility; seasonal variations in primate reproduction; male infertility including semen biochemistry, differential diagnosis between obstructive and non-obstructive azoospermia and hormone therapy; vasectomy, reversible vasocclusion and vasanastomosis; and the use of cyproterone acetate and testosterone enanthate in male rhesus monkey and human volunteers for reversible contraception.