Pergolide mesylate: its effects on circulating anterior pituitary hormones in man.
Pergolide mesylate: its effects on circulating anterior pituitary hormones in man.
复制标题
甲磺酸培高利特：其对人体循环垂体前叶激素的影响。
DOI：
10.1210/jcem-53-4-772
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发表时间：
1981
期刊：
影响因子：
--
通讯作者：
M. Thorner
中科院分区：
文献类型：
--
作者：
R. L. Perryman;A. Rogol;D. Kaiser;R. Macleod;M. Thorner
甲磺酸培高利特是一种具有多巴胺激动剂特性的合成麦角林。采用双盲交叉设计，对6名正常男性的内分泌特征进行了研究。在基础状态和TRH（500 μ g iv）给药后4.5、11.5和23.5 h，在安慰剂或培高利特（100 μ g口服）给药后，测量循环PRL、TSH、GH、LH、FSH和皮质醇。培高利特在给药后60分钟开始将基础PRL从2-8 ng/ml抑制至低于2 ng/ml，并在整个23.5小时研究期间持续存在。对于三项TRH试验，观察到安慰剂和培高利特对TRH的峰值PRL（平均值+/- SEM）反应抑制分别为54.6 +/- 5.1 vs. 1.9 +/- 0.5、45.2 +/- 4.1 vs. 4.5 + 2 - 0.6和34.4 +/- 2.9 vs. 6.9 +/- 1.4 ng/ml。基础TSH水平不受培高利特的影响，但在培高利特后，对前两次TRH激发的峰值TSH反应减弱（安慰剂vs培高利特：分别为12.3 +/- 1.2 vs 6.8 +/- 1.0和14.8 +/- 2.0 vs 9.6 +/- 1.0）;然而，服用培高利特后，第三次TSH反应（9.8 +/- 1.1 vs.9.3 +/- 1.2）并未减弱。培高利特刺激GH分泌，在培高利特给药后60分钟内观察到一致的脉冲，在整个24小时内，后续GH脉冲的数量和幅度增加。培高利特给药后皮质醇水平升高，并在16.5 h时恢复至对照日水平。FSH水平不受影响，但LH水平降低培高利特。所有受试者均观察到恶心、呕吐和低血压等副作用。培高利特是一种强效多巴胺激动剂，具有预期的内分泌特征和临床效应;其长期作用为高泌乳素血症的每日单次给药治疗提供了希望。
Pergolide mesylate is a synthetic ergoline with dopamine agonist properties. The endocrine profile was studied in a double blind crossover design in six normal males. Circulating PRL, TSH, GH, LH, FSH, and cortisol were measured in the basal state and after TRH (500 micrograms iv) administration at 4.5, 11.5, and 23.5 h after placebo or pergolide (100 micrograms orally). Pergolide caused suppression of basal PRL from 2-8 ng/ml to less than 2 ng/ml commencing 60 min after administration and persisting throughout the 23.5-h study period. For the three TRH tests, a suppression of peak PRL (mean +/- SEM) response to TRH of 54.6 +/- 5.1 vs. 1.9 +/- 0.5, 45.2 +/- 4.1 vs. 4.5 +2- 0.6, and 34.4 +/- 2.9 vs. 6.9 +/- 1.4 ng/ml, respectively, for placebo and pergolide was noted. Basal TSH levels were unaffected by pergolide, but after pergolide the peak TSH response to the first two TRH challenges was blunted (placebo vs. pergolide: 12.3 +/- 1.2 vs. 6.8 +/- 1.0 and 14.8 +/- 2.0 vs. 9.6 +/- 1.0, respectively); however, the third TSH response (9.8 +/- 1.1 vs. 9.3 +/- 1.2) was not blunted after pergolide. GH secretion was stimulated by pergolide with a consistent pulse observed within 60 min of pergolide administration and an enhancement in the number and amplitude of subsequent GH pulses throughout the 24-h period. Cortisol levels rose after pergolide and returned to levels seen on the control day at 16.5 h. FSH levels were unaffected but LH levels were lowered pergolide. Side effects including nausea, vomiting, and hypotension were observed in all subjects. Pergolide is a potent dopamine agonist with the anticipated endocrine profile and clinical effects; its long duration of actions offers promise of single daily dose therapy for hyperprolactinemia.