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睾酮内酯相关的高雄激素水平,是药理效应还是实验室假象?

Testolactone-associated high androgen levels, a pharmacologic effect or a laboratory artifact?

作者信息

Cummings E A, Salisbury S R, Givner M L, Rittmaster R S

机构信息

Department of Pediatrics, IWK Grace Health Centre, Halifax, Nova Scotia, Canada.

出版信息

J Clin Endocrinol Metab. 1998 Mar;83(3):784-7. doi: 10.1210/jcem.83.3.4623.

DOI:10.1210/jcem.83.3.4623
PMID:9506727
Abstract

Testolactone, an aromatase inhibitor, blocks conversion of androgens to estrogens. In familial male precocious puberty, slowing of pubertal progression and growth velocity occurs with testolactone and spironolactone. Girls with McCune-Albright syndrome, given testolactone, respond similarly. A 2-yr-old female (case 1) on testolactone for non-McCune-Albright gonadotropin independent precocious puberty had marked elevations of androstenedione (18 ng/mL, normal: 0.2-3.1) and testosterone (3.6 ng/mL, normal < 0.2) but no virilization. Investigations were undertaken to determine whether elevations in testosterone and androstenedione were caused by interference in these RIAs. After a single oral dose of testolactone (5 mg/kg in case 1; 4 mg/kg in case 2, a 3-yr-old boy with familial male precocious puberty; 10 mg/kg in a healthy postmenopausal control), serum testosterone and androstenedione were measured serially by RIA for 24 h. Androstenedione went from normal to a mean peak of 45.4 ng/mL at 1-2 h and returned to baseline by 24 h. Testosterone, undetectable at baseline (case 1 and control) or 1.8 ng/mL (case 2) rose to a mean peak of 6.9 ng/mL and returned to baseline by 24 h. Testolactone, in serial dilutions, cross-reacted in the testosterone assay. Testolactone significantly interferes in these serum RIAs, making their use unreliable in follow-up of patients treated with testolactone.

摘要

睾酮内酯是一种芳香化酶抑制剂,可阻断雄激素向雌激素的转化。在家族性男性性早熟中,使用睾酮内酯和螺内酯可使青春期进程和生长速度减慢。患有McCune - Albright综合征的女孩使用睾酮内酯后也有类似反应。一名2岁女性(病例1)因非McCune - Albright综合征的促性腺激素非依赖性性早熟服用睾酮内酯,其雄烯二酮显著升高(18 ng/mL,正常范围:0.2 - 3.1),睾酮水平为3.6 ng/mL(正常<0.2),但无男性化表现。开展了相关研究以确定睾酮和雄烯二酮的升高是否是由于对这些放射免疫分析(RIA)的干扰所致。单次口服睾酮内酯后(病例1为5 mg/kg;病例2为一名3岁家族性男性性早熟男孩,剂量为4 mg/kg;一名健康绝经后对照者为10 mg/kg),通过RIA连续24小时测定血清睾酮和雄烯二酮。雄烯二酮从正常水平在1 - 2小时升至平均峰值45.4 ng/mL,并在24小时时恢复至基线水平。睾酮在基线时(病例1和对照)不可检测或为1.8 ng/mL(病例2),升至平均峰值6.9 ng/mL,并在24小时时恢复至基线水平。睾酮内酯在系列稀释时,在睾酮测定中出现交叉反应。睾酮内酯显著干扰这些血清RIA,使得在使用睾酮内酯治疗的患者随访中这些检测方法不可靠。

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