May P R, Van Putten T, Jenden D J, Yale C, Dixon W J
Arch Gen Psychiatry. 1981 Feb;38(2):202-7. doi: 10.1001/archpsyc.1981.01780270088012.
Plasma and saliva levels of chlorpromazine hydrochloride were measured by gas chromatography-mass spectrometry, after a standard dosage had been administered to 48 newly admitted schizophrenic patients over 28 days. Other treatments were rigorously controlled. Saliva chlorpromazine concentrations were higher than plasma concentrations generally by about four to 50 times. Saliva and plasma chlorpromazine levels were significantly related. There was great variability in individuals between plasma and saliva peaks and values over time, in plasma/saliva ratios, and in change in plasma/saliva ratio over time. Chlorpromazine plasma and saliva levels at the end of fixed, sustained dosage treatment did not correlate with the amount of improvement as measured by ten criteria from the Brief Psychiatric Rating Scale and the Mobility, Affects Cooperation, and Communication Scale. Yet levels obtained in the 24 hours after the first dose did seen related to outcome, more strongly for saliva chlorpromazine than for plasma chlorpromazine levels. A reexamination is in order of our concepts of the relationships between levels of antipsychotic drugs in the body and treatment effect.
在28天内给48名新入院的精神分裂症患者服用标准剂量的盐酸氯丙嗪后，采用气相色谱 - 质谱法测定血浆和唾液中盐酸氯丙嗪的水平。其他治疗方法得到严格控制。唾液中氯丙嗪浓度通常比血浆浓度高约4至50倍。唾液和血浆中氯丙嗪水平显著相关。个体之间血浆和唾液峰值及随时间变化的值、血浆/唾液比值以及血浆/唾液比值随时间的变化存在很大差异。在固定的持续剂量治疗结束时，氯丙嗪的血浆和唾液水平与通过简明精神病评定量表和活动、情感、合作及沟通量表的十个标准所测量的改善程度无关。然而，首剂后24小时内测得的水平似乎与治疗结果相关，唾液中氯丙嗪水平比血浆中氯丙嗪水平的相关性更强。有必要重新审视我们关于体内抗精神病药物水平与治疗效果之间关系的概念。
