Wiles D, Franklin M, Dencker S J, Johansson R, Lundin L, Malm U
Psychopharmacology (Berl). 1980;71(2):131-6. doi: 10.1007/BF00434400.
The relationship between plasma prolactin (PRL) and drug levels in patients receiving neuroleptic drugs is of special interest in view of evidence that the PRL elevation induced by these drugs reaches its maximum at sub-therapeutic doses. Plasma PRL and fluphenazine (FPZ) levels were measured by radioimmunoassay (RIA) in each of 11 chronic schizophrenics (nine men, two women) during two 4-week periods of treatment with FPZ enanthate at a "High Dose' (250 mg per week) and a "Low Dose' (12.5 mg per week) given in random order. Plasma PRL levels were above normal in 9 of 11 subjects during the last week of Low Dosage. High Dosage resulted in PRL levels significantly greater than found during Low Dose treatment in 9 of 11 patients. Thus the PRL response had not reached its "ceiling" during Low Dosage in most patients. A significant correlation between PRL and FPZ levels was found in seven subjects; evidence that immunoreactive FPZ levels relate to an effect caused by blockade of dopamine receptors. The plasma FPZ pattern between injections during week 1 of Low Dosage was remarkably stable; High Doses produced an initial drug peak at 1--2 h and a secondary peak occurring on days 2--3 followed by a return to preinjection levels by day 7.
鉴于有证据表明这些药物诱导的催乳素(PRL)升高在亚治疗剂量时达到最大值,接受抗精神病药物治疗的患者血浆PRL与药物水平之间的关系备受关注。采用放射免疫分析法(RIA)对11例慢性精神分裂症患者(9例男性,2例女性)在两个为期4周的治疗阶段进行血浆PRL和氟奋乃静(FPZ)水平测定,两个阶段分别随机给予“高剂量”(每周250mg)和“低剂量”(每周12.5mg)的庚酸氟奋乃静。在低剂量治疗的最后一周,11名受试者中有9名的血浆PRL水平高于正常。在11名患者中,有9名患者高剂量治疗后的PRL水平显著高于低剂量治疗时。因此,在大多数患者中,低剂量治疗期间PRL反应尚未达到“上限”。在7名受试者中发现PRL与FPZ水平之间存在显著相关性;有证据表明免疫反应性FPZ水平与多巴胺受体阻断所产生的效应有关。低剂量治疗第1周注射期间的血浆FPZ模式非常稳定;高剂量在1 - 2小时产生初始药物峰值,在第2 - 3天出现第二个峰值,到第7天恢复到注射前水平。