Markianos M, Hatzimanolis J, Lykouras L
Athens University Medical School, Psychiatric Clinic, Eginition Hospital, Greece.
Psychopharmacology (Berl). 1999 Apr;143(3):270-2. doi: 10.1007/s002130050946.
The atypical neuroleptic risperidone, in addition to its dopamine receptor blocking activity, has a high affinity for serotonergic receptors. Since both dopaminergic and serotonergic neuronal activities participate in regulation of the pituitary gonadal axis (PGA), it is expected that a switch from treatment with haloperidol to treatment with risperidone should influence plasma levels of PGA hormones.
To study the effects of a drug with dopamine and serotonin receptor blocking activity on PGA hormones in patients who were on treatment with a dopamine receptor blocker.
Plasma levels of testosterone, luteinizing hormone (LH) and follicle stimulating hormone (FSH), as well as prolactin and cortisol, were measured in 16 male schizophrenic patients during treatment with haloperidol (mean dose 23.3 mg daily, SD = 16.9) and 6 weeks later after switching to treatment with risperidone (mean dose 11.8 mg daily, SD = 2.9). Psychopathology was assessed by BPRS.
After switching to risperidone, total BPRS score and the scores in its subscales for positive, negative, and general symptoms were all significantly reduced in the order of 35-45%. Prolactin levels were significantly increased from 39.5+/-22.3 to 58.9+/-28.5 ng/ml (F= 4.61, P = 0.04), while cortisol, testosterone, LH, and FSH remained unchanged. No significant correlations between prolactin increases and reduction in BPRS or in its subscale scores were found.
The results show that blocking of both dopamine and serotonin receptors does not influence the pituitary gonadal axis but considerably increases prolactin release.
非典型抗精神病药物利培酮,除了具有多巴胺受体阻断活性外,对血清素能受体也有很高的亲和力。由于多巴胺能和血清素能神经元活动都参与垂体性腺轴(PGA)的调节,因此预期从使用氟哌啶醇治疗转换为使用利培酮治疗应会影响PGA激素的血浆水平。
研究一种具有多巴胺和血清素受体阻断活性的药物对正在接受多巴胺受体阻滞剂治疗的患者PGA激素的影响。
在16名男性精神分裂症患者使用氟哌啶醇治疗期间(平均剂量每日23.3毫克,标准差=16.9)以及转换为使用利培酮治疗6周后(平均剂量每日11.8毫克,标准差=2.9),测量其血浆睾酮、促黄体生成素(LH)、促卵泡生成素(FSH)以及催乳素和皮质醇水平。通过简明精神病评定量表(BPRS)评估精神病理学。
转换为利培酮治疗后,BPRS总分及其阳性、阴性和一般症状分量表得分均显著降低,降幅为35%-45%。催乳素水平从39.5±22.3显著升高至58.9±28.5纳克/毫升(F = 4.61,P = 0.04),而皮质醇、睾酮、LH和FSH保持不变。未发现催乳素升高与BPRS或其分量表得分降低之间存在显著相关性。
结果表明,多巴胺和血清素受体的阻断并不影响垂体性腺轴,但会显著增加催乳素的释放。