L'Hermite M, Denayer P, Golstein J, Virasoro E, Vanhaelst L, Copinschi G, Robyn C
Clin Endocrinol (Oxf). 1978 Sep;9(3):195-204. doi: 10.1111/j.1365-2265.1978.tb02200.x.
Normal men and normally menstruating women received i.m. injections of 0.1 to 4.0 mg/kg sulpiride. This psychotropic drug induced a very rapid (already significant after 5 minutes) and sustained (still significant after 7 hours) elevation of prolactin (PRL) concentrations in all subjects with no consistent modification of LH and FSH. After injection of 4.0 mg/kg, there was similarly no modification of mean TSH concentrations in the women tested in the luteal phase, as well as of mean GH levels in men. Sulpiride prevented the inhibitory effect on PRL levels of 500 mg levodopa, administered orally simultaneously; levodopa administered 2 hours prior to sulpiride failed to counteract the PRL-stimulatory effect of sulpiride. Under chronic sulpiride-induced hyperprolactinaemia, levodopa exhibited however a very slight inhibitory effect on PRL concentrations. These data are in agreement with the hypothesis that sulpiride acts mainly at the pituitary level by blocking dopamine receptors of the lactotropes and support the concept that the menstrual cycle perturbations observed under chronic sulpiride administration result from hyperprolactinaemia itself or from a mechanism quite similar to that by which sulpiride induces hyperprolactinaemia.
正常男性和月经周期正常的女性接受了0.1至4.0毫克/千克舒必利的肌肉注射。这种精神药物在所有受试者中都引起了催乳素（PRL）浓度非常迅速（5分钟后就已显著）且持续（7小时后仍显著）的升高，而促黄体生成素（LH）和促卵泡生成素（FSH）没有一致的变化。注射4.0毫克/千克后，处于黄体期的受试女性的平均促甲状腺激素（TSH）浓度以及男性的平均生长激素（GH）水平同样没有变化。舒必利可防止同时口服500毫克左旋多巴对PRL水平的抑制作用；在舒必利注射前2小时给予左旋多巴无法抵消舒必利对PRL的刺激作用。然而，在慢性舒必利诱导的高催乳素血症情况下，左旋多巴对PRL浓度表现出非常轻微的抑制作用。这些数据与舒必利主要通过阻断催乳细胞的多巴胺受体在垂体水平起作用的假设一致，并支持这样的观点，即长期服用舒必利时观察到的月经周期紊乱是由高催乳素血症本身或与舒必利诱导高催乳素血症的机制非常相似的机制引起的。
