Melis G B, Cagnacci A, Gambacciani M, Paoletti A M, Moggi L, Fioretti P
Department of Obstetrics and Gynecology, University of Pisa School of Medicine, Italy.
J Clin Endocrinol Metab. 1988 May;66(5):964-7. doi: 10.1210/jcem-66-5-964.
To determine whether antidopaminergic drug administration may modify endogenous opioid activity at the hypothalamic-pituitary level, the effects of naloxone infusion (1.6 mg/h for 4 h) on LH secretion were studied in six postmenopausal women before and after administration of the potent antidopaminergic drug veralipride for 20 days. Before veralipride administration, the naloxone infusion did not alter LH secretion. Chronic administration of veralipride resulted in a significant (P less than 0.01) decline in plasma LH levels. In addition, the naloxone infusion induced a significant (P less than 0.05) increase in plasma LH levels, which reached values similar to those before veralipride administration. These results demonstrate that in postmenopausal women the antidopaminergic drug veralipride can restore, at least in part, the activity of the endogenous opioid system. These findings suggest that endogenous opioid peptides may mediate the inhibitory effect exerted by chronic antidopaminergic drug administration on LH secretion in humans.
为了确定给予抗多巴胺能药物是否会在下丘脑 - 垂体水平改变内源性阿片样物质的活性，在6名绝经后妇女中，研究了纳洛酮输注（1.6毫克/小时，共4小时）对促黄体生成素（LH）分泌的影响，该研究在给予强效抗多巴胺能药物维拉唑酮20天之前和之后进行。在给予维拉唑酮之前，纳洛酮输注未改变LH分泌。维拉唑酮的长期给药导致血浆LH水平显著（P<0.01）下降。此外，纳洛酮输注导致血浆LH水平显著（P<0.05）升高，达到与维拉唑酮给药前相似的值。这些结果表明，在绝经后妇女中，抗多巴胺能药物维拉唑酮至少可以部分恢复内源性阿片样物质系统的活性。这些发现表明，内源性阿片样肽可能介导了长期给予抗多巴胺能药物对人类LH分泌的抑制作用。
