BIO AND IMMUNO‐ACTIVITY OF FSH IN SERUM AFTER INTRAMUSCULAR INJECTION OF HIGHLY PURIFIED URINARY HUMAN FSH IN NORMAL MEN

BIO AND IMMUNO‐ACTIVITY OF FSH IN SERUM AFTER INTRAMUSCULAR INJECTION OF HIGHLY PURIFIED URINARY HUMAN FSH IN NORMAL MEN
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正常男性肌内注射高度纯化的人尿 FSH 后血清中 FSH 的生物和免疫活性

DOI:
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发表时间:
1990
影响因子:
3.2
通讯作者:
E. Nieschlag
E. Nieschlag
中科院分区:
医学3区
文献类型:
--
作者:
F. Jockenhövel;U. Fingscheidt;S. A. Khan;H. Behre;E. Nieschlag

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在内源性FSH受到19-去甲睾酮注射抑制的健康男性志愿者中评价了临床实践中广泛使用的人FSH制剂的药代动力学。肌内注射150 IU FSH后9 - 7 h,平均免疫反应性峰浓度超过基线3-8 IU/1。注射450 IU FSH导致9 - 8 h时的平均免疫反应性峰值水平为10 - 4 IU/1。平均半衰期为24 - 6 h(150 IU FSH)和36 - 2 h(450 IU FSH)。注射19-去甲睾酮后,血清bioFSH浓度被抑制至检测限以下,并在FSH给药后升至注射前水平。450 IU FSH的平均生物活性峰值水平在7 - 4 h时为7 - 3 IU/1 FSH。bioFSH的半衰期计算为13 - 4 h,远短于免疫FSH的半衰期。19-去甲睾酮可抑制血清中FSH水平,且在注射FSH制剂后无显著变化,表明FSH剂量不足以引起这种生物学反应。可以得出结论,目前用于治疗男性性腺功能减退症的剂量方案不足以将血清bioFSH水平维持在正常范围内。
The pharmacokinetics of a human FSH preparation widely used in clinical practice was evaluated in healthy male volunteers whose endogenous FSH was suppressed by 19‐nortestosterone injections. 9‐7 h following intramuscular injection of 150 IU FSH the mean immunoreactive peak concentration over baseline was 3–8 IU/1. Injection of 450 IU FSH led to a mean immunoreactive peak level of 10‐4 IU/1 at 9‐8 h. Mean half‐life was 24‐6 h (150 IU FSH) and 36‐2 h (450 IU FSH). Serum bioFSH concentrations were suppressed below the detection limit after injection of the 19‐nortestosterone and rose to preinjection levels after administration of FSH. Mean bioactive peak level for the 450 IU FSH was 7‐3 IU/1 FSH at 7‐4 h. The half‐life of bioFSH was calculated to be 13‐4 h and is considerably shorter than the half‐life of immunoFSH. Serum inhibin levels were suppressed by 19‐nortestosterone and did not change significantly after injection of the FSH preparation, suggesting that the FSH dose was insufficient to elicit this biological response. It is concluded that the currently used dose regimen for the treatment of male hypogonadism is inadequate for maintenace of serum bioFSH levels in the normal range.
卵泡刺激素和黄体生成素在正常男性抑制素分泌控制中的相对作用。
DOI: 10.1172/jci113693
发表时间: 1988
期刊: The Journal of clinical investigation
影响因子: --
作者:
McLachlan,RI;Matsumoto,AM;Burger,HG;deKretser,DM;Bremner,WJ
通讯作者: Bremner,WJ