Aim: To study the effect of testosterone undecanoate (TU) injection on spermatogenesis in rats. Methods:Twenty adult SD rats received vehicle or TU (8 mg/kg, 19 mg/kg or 625 mg/kg) injection, im, every 15 days for 60d...Aim: To study the effect of testosterone undecanoate (TU) injection on spermatogenesis in rats. Methods:Twenty adult SD rats received vehicle or TU (8 mg/kg, 19 mg/kg or 625 mg/kg) injection, im, every 15 days for 60days, and another 38 animals received similar treatments for 130 days with half of them undergoing a recovery phase of120 days (5 rats for each treatment). At the end of the treatment, testes were removed and the diameter of the seminif-erous tubules and the number of late elongated spermatids (steps 15-19) per testis were estimated with stereologicalmethods as a measure of the spermatogenic efficiency. Results: Low dose (8 mg/kg) TU treatment virtually hadno effect on spermatogenesis. A dose of 19 mg/kg slightly suppressed spermatogenesis 60 days after treatment, and se-vere suppression occurred after another 70 days of dosing. Spermatogenesis was completely recovered at the end of therecovery phase. Large dose (625 mg/kg) TU treatment did not significantly affect spermatogenesis and was well toler-ated by animals. Conclusion: TU injection reversibly suppresses spermatogenesis in rats.展开更多
Testosterone (T) as a compound for treatment of T deficiency has been available for almost 70 years, but the pharmaceutical formulations have been less than ideal. Traditionally, injectable T esters have been used f...Testosterone (T) as a compound for treatment of T deficiency has been available for almost 70 years, but the pharmaceutical formulations have been less than ideal. Traditionally, injectable T esters have been used for treatment, but they generate supranormal T levels shortly after the 2-3 weekly injection interval. T levels then decline very rapidly, becoming subnormal during the days preceding the next injection. The rapid fluctuations in plasma T are subjectively experienced as disagreeable. T undecanoate (TU) is a new injectable T preparation with a considerably better pharmacokinetic profile. After two initial injections separated by a 6-week interval, the following intervals between two injections are generally 12 weeks, eventually amounting to a total of four injections per year. Plasma T levels with this preparation are nearly always in the range of normal men, as are its metabolic products estradiol and dihydrotestosterone (DHT). It reverses the effects of hypogonadism on bone and muscle and metabolic parameters, and on sex functions. It is suitable for male contraception. Its safety profile is excellent because of the continuous normalcy of plasma T levels. No polycythemia has been observed and no adverse effects on lipid profiles. Prostate safety parameters are well within reference limits. TU is a valuable treatment option of androgen deficiency.展开更多
Aim: To study the anti-spermatogenic mechanism of supra-physiological doses of testosterone undecanoate (TU).Methods: Twenty fertile adult men received four intramuscular injections of TU at monthly intervals, 1000 mg...Aim: To study the anti-spermatogenic mechanism of supra-physiological doses of testosterone undecanoate (TU).Methods: Twenty fertile adult men received four intramuscular injections of TU at monthly intervals, 1000 mg uponadmission and 500 mg for the subsequent injections. The apoptotic germ cells in the semen were studied under light mi-croscope with tenninal deoxynucleotidyl tmnsferase-mediated dUTP-biotin nick end labeling (TUNEL) and Wright-Giem-sa staining methods. Results: After treatment, the sperm density and the number of spermatogenic cells in the semenwere significantly decreased ( P < 0.01), while the apoptotic ratios of spermatocytes and spermatids increased significantly( P <0.01) as compared with the pretreatment levels. Apoptosis was found to be augmented in the whole series of castoffspennatogenic cells. Conclusion: Besides its suppressive effect on spermatogenesis through a negative feed-backmechanism, TU enhances apoptosis of spermatogenic cells, which may be an additional mechanism of its anti-spermato-genic activity. ( Asian J Androl 1999 Sep; 1: 155 - 158)展开更多
Objective To investigate possible causes resulting in the differences in the spermatogenesis suppression on individual treated with levonorgestrel (LNG) implants and testosterone undecanoate (TU) injectableMethods Tot...Objective To investigate possible causes resulting in the differences in the spermatogenesis suppression on individual treated with levonorgestrel (LNG) implants and testosterone undecanoate (TU) injectableMethods Totally 21 Chinese male volunteers were given treatment with LNG implants (four rods, 75 mg/rod) and intramuscular injection of TU (500 mg,bimonthly for 3 times). According to the effects of treatment, they were divided into two groups, namely, azoospermia group (group A) and oligozoospermia group (group O). Then seminal FSH, LH, T and estradiol (E2) were determined by immunoenzymetric assay, while seminal and serum dihydrotachysterol (DHT) and serum sex hormone binding globulin (SHBG) were by radioimmunoassay, and seminal transferrin (Tf) by scatter turbidimetry assay.Results Seminal FSH, LH and serum DHT, SHBG, FTI (T/SHBG ×100) levels were significantly lower in group A than in group O, while higher seminal concentrations ofE2 were observed in azoospermia group.Conclusion The differences in the spermatogenic suppression in Chinese men might be attributed to different rate of peripheral androgen metabolism, variations in serum SHBG levels, 5á-reductase activity and individual aromatase activity during LNG plus TU administration. In addition, seminal sex hormones might be more sensitive indexes to assess the extent of feedback inhibition on hypothalamus-pituitary-testis with exogenous testosterone plus progestogen in the efficacy hormone male contraceptive trials.展开更多
The mechanism of antifertility effect of testosterone undecanoate on male rat was investigated. Eight 12-week old rats were injected with 20 mg/kg of testosterone undecanoate at bi--week intervals for 3 months. As com...The mechanism of antifertility effect of testosterone undecanoate on male rat was investigated. Eight 12-week old rats were injected with 20 mg/kg of testosterone undecanoate at bi--week intervals for 3 months. As compared to that in the 10 control rafs, the sperm density in testis rete fluid of the treatment rats declined by 7%, the motility of sperm from epididymis cauda reduced to 6%. While the testosterone level in serum increased to 255 %, the testosterone level in testis rete fluid decreased to 55%. All of these differences were significant. The androgen receptor gene expression in the testis and epididymis was suppressed in the treatment group. The decrease in output of the sperm and sperm motility of epididymis cauda may be due to the reduced testosterone production by Leydig cells and suppression of androgen receptor gene expression in testis and epididymis.展开更多
BACKGROUND Non-alcoholic fatty liver disease(NAFLD)is highly prevalent in people with diabetes with no available treatment.AIM To explore the effect of testosterone treatment on liver.Testosterone therapy improves ins...BACKGROUND Non-alcoholic fatty liver disease(NAFLD)is highly prevalent in people with diabetes with no available treatment.AIM To explore the effect of testosterone treatment on liver.Testosterone therapy improves insulin resistance and reduces total body fat,but its impact on the liver remains poorly studied.METHODS This secondary analysis of a 40 wk,randomised,double-blinded,placebocontrolled trial of intramuscular testosterone undecanoate in men with type 2 diabetes and lowered serum testosterone concentrations evaluated the change in hepatic steatosis as measured by liver fat fraction on magnetic resonance imaging(MRI).RESULTS Of 88 patients enrolled in the index study,39 had liver MRIs of whom 20 received testosterone therapy and 19 received placebo.All patients had>5%hepatic steatosis at baseline and 38 of 39 patients met diagnostic criteria for NAFLD.Median liver fat at baseline was 15.0%(IQR 11.5%-21.1%)in the testosterone and 18.4%(15.0%-28.9%)in the placebo group.Median ALT was 34units/L(26-38)in the testosterone and 32units/L(25-52)in the placebo group.At week 40,patients receiving testosterone had a median reduction in absolute liver fat of 3.5%(IQR 2.9%-6.4%)compared with an increase of 1.2%in the placebo arm(between-group difference 4.7%P<0.001).After controlling for baseline liver fat,testosterone therapy was associated with a relative reduction in liver fat of 38.3%(95%confidence interval 25.4%-49.0%,P<0.001).CONCLUSION Testosterone therapy was associated with a reduction in hepatic steatosis in men with diabetes and low serum testosterone.Future randomised studies of testosterone therapy in men with NAFLD focusing on liver-related endpoints are therefore justified.展开更多
Importance:Children with 5-alpha-reductase deficiency(5α-RD)and hypospadias present with micropenis,which makes it difficult to obtain sufficient tissue for urethral reconstruction.Objective:We investigated the thera...Importance:Children with 5-alpha-reductase deficiency(5α-RD)and hypospadias present with micropenis,which makes it difficult to obtain sufficient tissue for urethral reconstruction.Objective:We investigated the therapeutic effects of oral testosterone undecanoate and established a standard androgen treatment protocol for patients with 5α-RD with micropenis.Methods:Patients with 5α-RD were treated with oral testosterone undecanoate for 3 months as a course.All patients were treated with no more than 3 courses.If the penile length(PL)reached 2.5 cm(the minimum criterion for surgery)or greater than or equal to−2.5 standard deviations(SDs)(lower limit of normal),testosterone undecanoate was considered to be effective.Results:The median age of 90 patients with 5α-RD was 1.7 years(0.9,3.1 years).The baseline PL was 1.9±0.6 cm before treatment.At the end of the first course,the PL of 63 patients(70%)reached 2.5 cm,and 49 patients(54%)reached greater than or equal to−2.5 SDs.After two treatment courses,the PL of 81 patients(90%)reached 2.5 cm,and 90 patients(100%)reached greater than or equal to−2.5 SDs.After three courses,the PL of all patients reached 2.5 cm,and all patients reached a PL greater than or equal to−2.5 SDs.No abnormal increase was observed in height-SD score,weight-SD score,or ratio of bone age to chronological age during the 1-3-year follow-up.Interpretation:After 3-9 months of treatment,PL increased to the target length.No severe adverse reactions were observed during follow-up.Testosterone undecanoate was safe and effective in children with 5α-RD with micropenis.展开更多
We have investigated the feasibility of administration of testosterone undecanoate (TU)-Ioaded injectable in situ-forming implant (ISFI) for contraception in adult male Sprague-Dawley rats. Male rats were treated ...We have investigated the feasibility of administration of testosterone undecanoate (TU)-Ioaded injectable in situ-forming implant (ISFI) for contraception in adult male Sprague-Dawley rats. Male rats were treated with vehicle, TU-Ioaded ISFIs (540, 270 and 135 mg TU kg-1) or TU injections (45 mg TU kg-1 every 30 days) for 120 days. Fertility tests served for determining infertility or restoration of fertility in treated rats. Serum testosterone concentration, epididymal sperm count, motility, morphology, and histology of the testis were monitored. The TU-Ioaded ISFIs increased serum testosterone levels in rats steadily without fluctuation over 3 months. One month after TU administration, the epididymal sperm count decreased significantly in all experimental groups. After 3 months, the animals treated with 270 and 135 mg kg-~ TU-Ioaded ISFIs were 100% infertile, and no implantation sites were produced in the mated females. However, some of males treated with 540 mg kg-~ ISFI or TU injections were still fertile but numbers of implantation sites were also significantly lower than control values. TU-Ioaded ISFI at an appropriate dose has potential as a long-acting male contraceptive drug that suppresses spermatogenesis consistently over a period of 3 months.展开更多
Gon adotropin therapy is comm only used to in duce virilizati on and spermatoge nesis in male isolated hypog on adotropic hypog on adism (IHH) patients. In clinical practice, 5.6%-15.0% of male IHH patients show poor ...Gon adotropin therapy is comm only used to in duce virilizati on and spermatoge nesis in male isolated hypog on adotropic hypog on adism (IHH) patients. In clinical practice, 5.6%-15.0% of male IHH patients show poor responses to gonadotropin treatment;therefore, testosterone (T) suppleme ntation can serve as an alter native therapy to no rmalize serum T levels and promote virilization. However, treatment with exogenous T impairs spermatogenesis and suppresses intratesticular T levels. This retrospective study aimed to determine whether oral testosterone undeca noate (TU) suppleme ntation together with human chorionic gonadotropin (hCG) would negatively affect spermatogenesis in IHH patients compared with hCG alone. One hundred and seven IHH patients were included in our study. Fifty-four patients received intramuscular hCG and oral TU, and 53 patients received intramuscular hCG alone. The median follow-up time was 29 (range: 12-72) mon ths in both groups. Compared with the hCG group, the hCG/TU group required a shorter median time to normalize serum T levels (P < 0.001) and achieve Tanner stage (III and V) of pubic hair and genital development (P < 0.05). However, there were no significant differences in the rate of seminal spermatozoa appearance, sperm concentration, or median time to achieve different sperm concentration thresholds between the groups. In addition, there were no significant differences in side effects, such as acne and gynecomastia, observed in both groups. This study indicates that oral TU supplementation together with hCG does not impair spermatogenesis in treated IHH patients compared with hCG alone, and it shortens the time to normalize serum T levels and promote virilization.展开更多
Objective To assess the effectiveness of testosterone undecanoate on sperm motility and pregnancy incidence in men with asthenospermia. Methods A clinical trial was performed. Fifty men with asthenospermia were includ...Objective To assess the effectiveness of testosterone undecanoate on sperm motility and pregnancy incidence in men with asthenospermia. Methods A clinical trial was performed. Fifty men with asthenospermia were included to receive placebo (control group, n=9) or T undecanoate 80 mg/d (study group, n=41). Pregnancy incidence and sperm characteristics after 1, 2 and 3 months of medication and 3 months after the end of the trial were measured. Results Compared with the placebo, T undecanoate treatment produced a satisfactory improvement of seminal motility (F=55.904, P=0.000). In study group, the incidence of pregnancy was 28.2% while the incidence of pregnancy in control group was 11.1%. In study group, 26patients took T undecanoate for more than 3 months. In the 3 months, semen volume showed no statistical difference (F=1.206, P=0.312) before and after treatment, sperm concentration (F=0.023, P=0.000) and motility a, b, a +b (P=0.000) showed statistical differences. Motility grade a showed significantly higher increment in 2 and 3 months after treatment than 1 month and there was no statistical difference between 2 and 3 months. So did grade b. Conclusion The results indicate that T undecanoate increases semjnal motility, leading to a higher incidence of pregnancy in couples with infertility related to asthenoaspermia.展开更多
目的:探讨睾酮替代治疗对糖尿病合并迟发性性腺功能减退患者胰岛素抵抗的作用及其临床疗效。方法:82例糖尿病合并迟发性性腺功能减退患者随机分为睾酮治疗组(n=42)和对照组(n=40),两组患者均维持原有降糖、调脂治疗方案,治疗组在此基础...目的:探讨睾酮替代治疗对糖尿病合并迟发性性腺功能减退患者胰岛素抵抗的作用及其临床疗效。方法:82例糖尿病合并迟发性性腺功能减退患者随机分为睾酮治疗组(n=42)和对照组(n=40),两组患者均维持原有降糖、调脂治疗方案,治疗组在此基础上予十一酸睾酮胶丸口服,共治疗6个月,观察两组治疗前后体重指数、腰围、血糖、血脂谱、胰岛素敏感性、生殖激素以及中老年男性症状问卷(AMS)评估的相关症状评分及IIEF-5评分变化。结果:与治疗前相比,治疗组干预后体重指数(26.71±2.39 vs 25.15±2.28,P<0.05)、腰围(cm)(89.96±9.13 vs 85.03±9.58,P<0.05)、糖化血红蛋白(%)(7.73±1.31 vs 7.01±1.25,P<0.05)、甘油三酯(mmol/L)(1.97±0.83 vs 1.41±0.69,P<0.05)显著下降,总睾酮(μmol/L)(7.16±2.21 vs 14.22±2.63,P<0.05)显著升高,稳态模型评估的胰岛素抵抗指数(3.76±1.18 vs 2.55±1.03,P<0.05)和胰岛素敏感指数(96±51 vs 138±53,P<0.05)显著改善,AMS心理和躯体评分显著改善(P<0.05),但IIEF-5评分(13.28±6.38 vs14.95±6.08,P>0.05)改善不明显。结论:睾酮替代治疗可以改善糖尿病合并迟发性性腺功能减退患者胰岛素抵抗并具有确切临床疗效。展开更多
基金Financially supported by a"9th five-year" National Key Grant of Science and Technology (Grant number:969040401),and by Sichuan Committee of Education.
文摘Aim: To study the effect of testosterone undecanoate (TU) injection on spermatogenesis in rats. Methods:Twenty adult SD rats received vehicle or TU (8 mg/kg, 19 mg/kg or 625 mg/kg) injection, im, every 15 days for 60days, and another 38 animals received similar treatments for 130 days with half of them undergoing a recovery phase of120 days (5 rats for each treatment). At the end of the treatment, testes were removed and the diameter of the seminif-erous tubules and the number of late elongated spermatids (steps 15-19) per testis were estimated with stereologicalmethods as a measure of the spermatogenic efficiency. Results: Low dose (8 mg/kg) TU treatment virtually hadno effect on spermatogenesis. A dose of 19 mg/kg slightly suppressed spermatogenesis 60 days after treatment, and se-vere suppression occurred after another 70 days of dosing. Spermatogenesis was completely recovered at the end of therecovery phase. Large dose (625 mg/kg) TU treatment did not significantly affect spermatogenesis and was well toler-ated by animals. Conclusion: TU injection reversibly suppresses spermatogenesis in rats.
文摘Testosterone (T) as a compound for treatment of T deficiency has been available for almost 70 years, but the pharmaceutical formulations have been less than ideal. Traditionally, injectable T esters have been used for treatment, but they generate supranormal T levels shortly after the 2-3 weekly injection interval. T levels then decline very rapidly, becoming subnormal during the days preceding the next injection. The rapid fluctuations in plasma T are subjectively experienced as disagreeable. T undecanoate (TU) is a new injectable T preparation with a considerably better pharmacokinetic profile. After two initial injections separated by a 6-week interval, the following intervals between two injections are generally 12 weeks, eventually amounting to a total of four injections per year. Plasma T levels with this preparation are nearly always in the range of normal men, as are its metabolic products estradiol and dihydrotestosterone (DHT). It reverses the effects of hypogonadism on bone and muscle and metabolic parameters, and on sex functions. It is suitable for male contraception. Its safety profile is excellent because of the continuous normalcy of plasma T levels. No polycythemia has been observed and no adverse effects on lipid profiles. Prostate safety parameters are well within reference limits. TU is a valuable treatment option of androgen deficiency.
文摘Aim: To study the anti-spermatogenic mechanism of supra-physiological doses of testosterone undecanoate (TU).Methods: Twenty fertile adult men received four intramuscular injections of TU at monthly intervals, 1000 mg uponadmission and 500 mg for the subsequent injections. The apoptotic germ cells in the semen were studied under light mi-croscope with tenninal deoxynucleotidyl tmnsferase-mediated dUTP-biotin nick end labeling (TUNEL) and Wright-Giem-sa staining methods. Results: After treatment, the sperm density and the number of spermatogenic cells in the semenwere significantly decreased ( P < 0.01), while the apoptotic ratios of spermatocytes and spermatids increased significantly( P <0.01) as compared with the pretreatment levels. Apoptosis was found to be augmented in the whole series of castoffspennatogenic cells. Conclusion: Besides its suppressive effect on spermatogenesis through a negative feed-backmechanism, TU enhances apoptosis of spermatogenic cells, which may be an additional mechanism of its anti-spermato-genic activity. ( Asian J Androl 1999 Sep; 1: 155 - 158)
文摘Objective To investigate possible causes resulting in the differences in the spermatogenesis suppression on individual treated with levonorgestrel (LNG) implants and testosterone undecanoate (TU) injectableMethods Totally 21 Chinese male volunteers were given treatment with LNG implants (four rods, 75 mg/rod) and intramuscular injection of TU (500 mg,bimonthly for 3 times). According to the effects of treatment, they were divided into two groups, namely, azoospermia group (group A) and oligozoospermia group (group O). Then seminal FSH, LH, T and estradiol (E2) were determined by immunoenzymetric assay, while seminal and serum dihydrotachysterol (DHT) and serum sex hormone binding globulin (SHBG) were by radioimmunoassay, and seminal transferrin (Tf) by scatter turbidimetry assay.Results Seminal FSH, LH and serum DHT, SHBG, FTI (T/SHBG ×100) levels were significantly lower in group A than in group O, while higher seminal concentrations ofE2 were observed in azoospermia group.Conclusion The differences in the spermatogenic suppression in Chinese men might be attributed to different rate of peripheral androgen metabolism, variations in serum SHBG levels, 5á-reductase activity and individual aromatase activity during LNG plus TU administration. In addition, seminal sex hormones might be more sensitive indexes to assess the extent of feedback inhibition on hypothalamus-pituitary-testis with exogenous testosterone plus progestogen in the efficacy hormone male contraceptive trials.
文摘The mechanism of antifertility effect of testosterone undecanoate on male rat was investigated. Eight 12-week old rats were injected with 20 mg/kg of testosterone undecanoate at bi--week intervals for 3 months. As compared to that in the 10 control rafs, the sperm density in testis rete fluid of the treatment rats declined by 7%, the motility of sperm from epididymis cauda reduced to 6%. While the testosterone level in serum increased to 255 %, the testosterone level in testis rete fluid decreased to 55%. All of these differences were significant. The androgen receptor gene expression in the testis and epididymis was suppressed in the treatment group. The decrease in output of the sperm and sperm motility of epididymis cauda may be due to the reduced testosterone production by Leydig cells and suppression of androgen receptor gene expression in testis and epididymis.
文摘BACKGROUND Non-alcoholic fatty liver disease(NAFLD)is highly prevalent in people with diabetes with no available treatment.AIM To explore the effect of testosterone treatment on liver.Testosterone therapy improves insulin resistance and reduces total body fat,but its impact on the liver remains poorly studied.METHODS This secondary analysis of a 40 wk,randomised,double-blinded,placebocontrolled trial of intramuscular testosterone undecanoate in men with type 2 diabetes and lowered serum testosterone concentrations evaluated the change in hepatic steatosis as measured by liver fat fraction on magnetic resonance imaging(MRI).RESULTS Of 88 patients enrolled in the index study,39 had liver MRIs of whom 20 received testosterone therapy and 19 received placebo.All patients had>5%hepatic steatosis at baseline and 38 of 39 patients met diagnostic criteria for NAFLD.Median liver fat at baseline was 15.0%(IQR 11.5%-21.1%)in the testosterone and 18.4%(15.0%-28.9%)in the placebo group.Median ALT was 34units/L(26-38)in the testosterone and 32units/L(25-52)in the placebo group.At week 40,patients receiving testosterone had a median reduction in absolute liver fat of 3.5%(IQR 2.9%-6.4%)compared with an increase of 1.2%in the placebo arm(between-group difference 4.7%P<0.001).After controlling for baseline liver fat,testosterone therapy was associated with a relative reduction in liver fat of 38.3%(95%confidence interval 25.4%-49.0%,P<0.001).CONCLUSION Testosterone therapy was associated with a reduction in hepatic steatosis in men with diabetes and low serum testosterone.Future randomised studies of testosterone therapy in men with NAFLD focusing on liver-related endpoints are therefore justified.
基金Beijing Municipal Science&Technology Commission(No.Z201100005520061)Jinlei Pediatric Endocrinology Growth Research Fund for Young Physicians(PEGRF)(No.PEGRF201809006)。
文摘Importance:Children with 5-alpha-reductase deficiency(5α-RD)and hypospadias present with micropenis,which makes it difficult to obtain sufficient tissue for urethral reconstruction.Objective:We investigated the therapeutic effects of oral testosterone undecanoate and established a standard androgen treatment protocol for patients with 5α-RD with micropenis.Methods:Patients with 5α-RD were treated with oral testosterone undecanoate for 3 months as a course.All patients were treated with no more than 3 courses.If the penile length(PL)reached 2.5 cm(the minimum criterion for surgery)or greater than or equal to−2.5 standard deviations(SDs)(lower limit of normal),testosterone undecanoate was considered to be effective.Results:The median age of 90 patients with 5α-RD was 1.7 years(0.9,3.1 years).The baseline PL was 1.9±0.6 cm before treatment.At the end of the first course,the PL of 63 patients(70%)reached 2.5 cm,and 49 patients(54%)reached greater than or equal to−2.5 SDs.After two treatment courses,the PL of 81 patients(90%)reached 2.5 cm,and 90 patients(100%)reached greater than or equal to−2.5 SDs.After three courses,the PL of all patients reached 2.5 cm,and all patients reached a PL greater than or equal to−2.5 SDs.No abnormal increase was observed in height-SD score,weight-SD score,or ratio of bone age to chronological age during the 1-3-year follow-up.Interpretation:After 3-9 months of treatment,PL increased to the target length.No severe adverse reactions were observed during follow-up.Testosterone undecanoate was safe and effective in children with 5α-RD with micropenis.
文摘We have investigated the feasibility of administration of testosterone undecanoate (TU)-Ioaded injectable in situ-forming implant (ISFI) for contraception in adult male Sprague-Dawley rats. Male rats were treated with vehicle, TU-Ioaded ISFIs (540, 270 and 135 mg TU kg-1) or TU injections (45 mg TU kg-1 every 30 days) for 120 days. Fertility tests served for determining infertility or restoration of fertility in treated rats. Serum testosterone concentration, epididymal sperm count, motility, morphology, and histology of the testis were monitored. The TU-Ioaded ISFIs increased serum testosterone levels in rats steadily without fluctuation over 3 months. One month after TU administration, the epididymal sperm count decreased significantly in all experimental groups. After 3 months, the animals treated with 270 and 135 mg kg-~ TU-Ioaded ISFIs were 100% infertile, and no implantation sites were produced in the mated females. However, some of males treated with 540 mg kg-~ ISFI or TU injections were still fertile but numbers of implantation sites were also significantly lower than control values. TU-Ioaded ISFI at an appropriate dose has potential as a long-acting male contraceptive drug that suppresses spermatogenesis consistently over a period of 3 months.
基金the grant from the National Natural Science Foundation of China (Project No. 81671443, 81601270).
文摘Gon adotropin therapy is comm only used to in duce virilizati on and spermatoge nesis in male isolated hypog on adotropic hypog on adism (IHH) patients. In clinical practice, 5.6%-15.0% of male IHH patients show poor responses to gonadotropin treatment;therefore, testosterone (T) suppleme ntation can serve as an alter native therapy to no rmalize serum T levels and promote virilization. However, treatment with exogenous T impairs spermatogenesis and suppresses intratesticular T levels. This retrospective study aimed to determine whether oral testosterone undeca noate (TU) suppleme ntation together with human chorionic gonadotropin (hCG) would negatively affect spermatogenesis in IHH patients compared with hCG alone. One hundred and seven IHH patients were included in our study. Fifty-four patients received intramuscular hCG and oral TU, and 53 patients received intramuscular hCG alone. The median follow-up time was 29 (range: 12-72) mon ths in both groups. Compared with the hCG group, the hCG/TU group required a shorter median time to normalize serum T levels (P < 0.001) and achieve Tanner stage (III and V) of pubic hair and genital development (P < 0.05). However, there were no significant differences in the rate of seminal spermatozoa appearance, sperm concentration, or median time to achieve different sperm concentration thresholds between the groups. In addition, there were no significant differences in side effects, such as acne and gynecomastia, observed in both groups. This study indicates that oral TU supplementation together with hCG does not impair spermatogenesis in treated IHH patients compared with hCG alone, and it shortens the time to normalize serum T levels and promote virilization.
基金supported by Planned Science and Technology Project of Shenzhen (No.200902069)
文摘Objective To assess the effectiveness of testosterone undecanoate on sperm motility and pregnancy incidence in men with asthenospermia. Methods A clinical trial was performed. Fifty men with asthenospermia were included to receive placebo (control group, n=9) or T undecanoate 80 mg/d (study group, n=41). Pregnancy incidence and sperm characteristics after 1, 2 and 3 months of medication and 3 months after the end of the trial were measured. Results Compared with the placebo, T undecanoate treatment produced a satisfactory improvement of seminal motility (F=55.904, P=0.000). In study group, the incidence of pregnancy was 28.2% while the incidence of pregnancy in control group was 11.1%. In study group, 26patients took T undecanoate for more than 3 months. In the 3 months, semen volume showed no statistical difference (F=1.206, P=0.312) before and after treatment, sperm concentration (F=0.023, P=0.000) and motility a, b, a +b (P=0.000) showed statistical differences. Motility grade a showed significantly higher increment in 2 and 3 months after treatment than 1 month and there was no statistical difference between 2 and 3 months. So did grade b. Conclusion The results indicate that T undecanoate increases semjnal motility, leading to a higher incidence of pregnancy in couples with infertility related to asthenoaspermia.
文摘目的:探讨睾酮替代治疗对糖尿病合并迟发性性腺功能减退患者胰岛素抵抗的作用及其临床疗效。方法:82例糖尿病合并迟发性性腺功能减退患者随机分为睾酮治疗组(n=42)和对照组(n=40),两组患者均维持原有降糖、调脂治疗方案,治疗组在此基础上予十一酸睾酮胶丸口服,共治疗6个月,观察两组治疗前后体重指数、腰围、血糖、血脂谱、胰岛素敏感性、生殖激素以及中老年男性症状问卷(AMS)评估的相关症状评分及IIEF-5评分变化。结果:与治疗前相比,治疗组干预后体重指数(26.71±2.39 vs 25.15±2.28,P<0.05)、腰围(cm)(89.96±9.13 vs 85.03±9.58,P<0.05)、糖化血红蛋白(%)(7.73±1.31 vs 7.01±1.25,P<0.05)、甘油三酯(mmol/L)(1.97±0.83 vs 1.41±0.69,P<0.05)显著下降,总睾酮(μmol/L)(7.16±2.21 vs 14.22±2.63,P<0.05)显著升高,稳态模型评估的胰岛素抵抗指数(3.76±1.18 vs 2.55±1.03,P<0.05)和胰岛素敏感指数(96±51 vs 138±53,P<0.05)显著改善,AMS心理和躯体评分显著改善(P<0.05),但IIEF-5评分(13.28±6.38 vs14.95±6.08,P>0.05)改善不明显。结论:睾酮替代治疗可以改善糖尿病合并迟发性性腺功能减退患者胰岛素抵抗并具有确切临床疗效。