Perez-Lopez F R, Legido A, Sisskin M, Abos M D
Fertil Steril. 1980 Nov;34(5):452-5.
Serum levels of prolactin (PRL), luteinizing hormone (LH), and follicle-stimulating hormone (FSH) were measured in normally cycling women and normal men before and after oral admiministration of 1 mg of clebopride, a derivative of procainamide used in the treatment of gastrointestinal diseases. Clebopride produced a significant increase (P < 0.001) in serum PRL to a 6-fold peak as compared with basal levels. After 240 minutes the levels remained significantly higher (P < 0.05) than the mean basal level at -30 and 0 minutes. No significant effects of clebopride were noted upon the circulating levels of LH and FSH. The peak PRL response to clebopride was unaffected by pretreatment with 100 mg of nomifensine, although the secretory area from 120 to 210 minutes after clebopride was greater (P < 0.05) in the nomifensine-treated group than in the control experiment. When 5 mg of bromocriptine were given before clebopride, the PRL response was completely abolished as compared with the control experiment (P < 0.001). Our data provide new evidence that dopaminergic receptors of the adeylate cyclase system are involved in the regulation of PRL secretion, acting at the pituitary level rather than acting on the hypothalamus. The PRL-releasing activity of clebopride could be the explanation for the occasional menstrual disorders and galactorrhea registered in some cases of long-term treatment.
在正常月经周期的女性和正常男性口服1毫克氯波必利（一种用于治疗胃肠道疾病的普鲁卡因酰胺衍生物）前后，测定其血清催乳素（PRL）、黄体生成素（LH）和促卵泡激素（FSH）水平。与基础水平相比，氯波必利使血清PRL显著升高（P < 0.001），达到峰值时为基础水平的6倍。240分钟后，其水平仍显著高于-30分钟和0分钟时的平均基础水平（P < 0.05）。未观察到氯波必利对LH和FSH的循环水平有显著影响。氯波必利引起的PRL峰值反应不受100毫克诺米芬辛预处理的影响，尽管在诺米芬辛治疗组中，氯波必利给药后120至210分钟的分泌面积比对照实验中的更大（P < 0.05）。在氯波必利给药前给予5毫克溴隐亭时，与对照实验相比，PRL反应完全被消除（P < 0.001）。我们的数据提供了新的证据，表明腺苷酸环化酶系统的多巴胺能受体参与PRL分泌的调节，作用于垂体水平而非下丘脑。氯波必利的催乳素释放活性可能是长期治疗某些病例中偶尔出现月经紊乱和溢乳现象的原因。
