摘要
目的 :本文对长效雄激素注射剂十一酸睾酮 (TU) ,治疗原发性性腺功能低下 (Klinefelter综合征 )的药代动力学以及临床药效学进行观察 ,了解使用该药的最佳间隔时间和最佳剂量。同时为男子性腺功能低下的雄激素替代治疗和男性激素避孕研究与临床实践提供理论依据。 方法 :8例Klinefelter综合征病人接受初次 5 0 0mg或 10 0 0mgTU肌肉注射 ,间隔 3月后交叉剂量 ,5 0 0mg或 10 0 0mgTU注射。观察治疗前后性腺、第二性征变化。同时在不同时相取血 ,以放射免疫法 (RIA)测定有关激素的水平。了解一次注射该药后在体内维持有效浓度的时间 ,并用专用软件分析睾酮 (T)药代动力学。 结果 :注射两种剂量TU后 ,所有病人的性功能和第二性征都有改善。垂体激素FSH和LH均显著抑制 ,对LH作用较FSH更大。血清睾酮 (T)水平在注射后一周迅速升高达到峰值 ,在 5 0 0mg和 10 0 0mg两种剂量分别为 (4 7 8± 10 1)nmol/L和 (5 4 2± 4 8)nmol/L ,维持有效治疗T水平达 5 0～ 6 0d。两种剂量TU的半寿期分别为 (18 3± 2 3)d和 (2 3 7± 2 7)d ,平均滞留时间为 (2 1 7± 1 1)d和 (2 3 0± 0 8)d。第 2次注射5 0 0mgTU较第 1次注射产生更佳的药代动力学。 结论 :对性腺功能低下男子的雄激素替代治疗 ,单一剂量TU可维持 6～
Objectives: To investigate the effects of a newly available testosterone undecanoate(TU) preparation on hypogonadal men, to explore the best interval period between injections and the optimal doses, and meanwhile to explore the possibility of using injectable TU as testosterone (T) replacement for hypogonadal men and as a male hormonal contraceptive Methods: Eight patients with Klinefelter′s syndrome were first given either 500mg or 1 000mg of TU by intramuscular injections, and then received the crossover injections with alternate doses after three months Serum levels of reproductive hormones at regular intervals before and after the injections were measured with RIA to understand how long TU can maintain its effective concentration in body Pharmacokinetic parameters were analysed with software designed specially for pharmacokinetics Results: Both sexual function and the secondary sex characters were improved in all patients The elevated serum LH and FSH levels in patients with primary hypogonadism were decreased significantly by the injections of TU with either 500mg or 1 000mg doses, and LH levels were suppressed more pronouncedly than FSH levels Serum T levels increased significantly to the peak levels of (47 8±10 1)nmol/L and (54 2±4 8)nmol/L at the end of the first week after injections of TU 500mg and 1 000mg respectively Serum T levels maintained within the normal level of ≥ 10 nmol/L for 50 to 60 days Pharmacokinetic analysis showed a terminal elimination half life of (18 3±2 3)days and (23 7±2 7)days, and a mean retaining time of (21 7±1 1)days and (23 0±0 8)days, for the lower and higher doses respectively 500mg TU given as the second injection yielded more optimal pharmacokinetics Conclusions: Injecta
出处
《中华男科学杂志》
CAS
CSCD
2000年第4期225-229,共5页
National Journal of Andrology
基金
九五攻关项目!资助 (项目编号 96 90 40 40 1)
部分受AndrewW MellonFoundation支持
关键词
十一酸睾酮
原发性性腺功能低下
治疗
Testosterone undecanoate
Klinefelter's syndrome
Pharmacokinetics
