Markianos M, Hatzimanolis J, Lykouras L
Athens University Medical School, Psychiatric Clinic, Eginition Hospital, Greece.
Psychiatry Res. 1999 Dec 20;89(2):115-22. doi: 10.1016/s0165-1781(99)00098-0.
The increases that occur in plasma prolactin (PRL) levels after i.m. administration of 5 mg of haloperidol (the HAL test) provide information about the responsivity of D2 dopamine receptors in the hypothalamus-hypophysis, and may be a measure of their occupancy during the neuroleptic treatment of schizophrenic patients. We studied these responses during treatment with haloperidol (doses 7.5-60 mg daily, mean = 20.6) in 12 male schizophrenic patients who did not have a satisfactory therapeutic response to the drug, and the test was repeated 6 weeks later, after the patients were switched to therapy with the atypical neuroleptic risperidone (8-16 mg daily, mean = 11.7). After the institution of risperidone treatment, the total score on the Brief Psychiatric Rating Scale (BPRS) fell by 38% (from a mean score of 47.2 to 29.3). BPRS subscale scores for positive, negative, and general symptoms were reduced by 38, 35, and 40%, respectively. Moderate PRL responses to the HAL test were found during haloperidol treatment and no responses at all during treatment with risperidone. Baseline PRL increased significantly from a mean of 35.0 (S.D. = 16.0) to a mean of 55.7 ng/ml plasma (S.D. = 19.6). This high potency of risperidone to increase PRL levels cannot be explained by the serotonergic blocking activity of the drug, and seems not to be restricted to its D2 receptor blocking capacity.
肌肉注射5毫克氟哌啶醇后(氟哌啶醇试验)血浆催乳素(PRL)水平的升高,可提供有关下丘脑 - 垂体中D2多巴胺受体反应性的信息,并且可能是精神分裂症患者接受抗精神病药物治疗期间受体占有率的一种衡量指标。我们对12名男性精神分裂症患者进行了研究,这些患者对氟哌啶醇治疗(剂量为每日7.5 - 60毫克,平均 = 20.6毫克)反应不佳,在治疗期间观察了这些反应。6周后,患者换用非典型抗精神病药物利培酮(每日8 - 16毫克,平均 = 11.7毫克)治疗,并重复该试验。开始利培酮治疗后,简明精神病评定量表(BPRS)总分下降了38%(从平均47.2分降至29.3分)。BPRS中阳性、阴性和一般症状的子量表得分分别降低了38%、35%和40%。在氟哌啶醇治疗期间发现对氟哌啶醇试验有中度PRL反应,而在利培酮治疗期间则完全没有反应。基线PRL从平均35.0(标准差 = 16.0)显著升高至血浆平均55.7纳克/毫升(标准差 = 19.6)。利培酮升高PRL水平的这种高效能不能用该药物的5-羟色胺能阻断活性来解释,而且似乎并不局限于其D2受体阻断能力。