摘要
目的 探讨奎硫平及其代谢产物血药浓度与疗效、副作用的相关性。方法 对15例精神分裂症患者给予富马酸奎硫平治疗,剂量为400mg·d-1,疗程为3周。采用阳性症状量表(SAPS)、阴性症状量表(SANS)、简明精神病量表(BPRS)和不良反应量表(TESS)于治疗前和治疗1、2、3周末分别评定疗效和副作用。治疗第8 d晨服药前和服药后1.5 h分别采静脉血2 mL,高效液相色谱-质谱联用测定奎硫平及其代谢产物血药浓度。结果治疗结束时,SAPS、SANS和BPRS评分较治疗前均显著降低;BPRS减分率及SAPS减分率仅与奎硫平的稳态谷浓度均呈正相关;SANS减分率与峰、谷浓度均不相关。不良反应主要为一过性头昏和心动过速;TESS中的抗α1肾上腺素因子分值与奎硫平稳态峰浓度正相关,TESS总分值及其他因子分值与奎硫平及其代谢产物血药浓度不相关。结论 奎硫平治疗精神分裂症疗效好、起效快、耐受性好;监测奎硫平血药浓度对优化奎硫平临床疗效和预防药物不良反应具有重要意义。
OBJECTIVE To explore the correlation between plasma concentration, treatment efficacy and side effects of quetiapine and its metabolites. METHODS Fifteen patients were recruited in the study. The dose of quetia-pine was 400 mg·d-1 and was used for 3 weeks. The SAPS, SANS, BPRS and TESS were used to assess the treatment efficacy and side effects before and at 1, 2, 3 weeks after the treatment. Blood samples (2 mL) were collected before and at 1. 5 h after the morning dose (200 mg) on day 8. The plasma concentrations of quetiapine and its metabolites were measured by High-performance Liquid Chromatography-electrospray Ionization Mass Spectrometry. RESULTS After the treatment, the scores of SAPS, SANS and BPRS decreased significantly compared with the baseline (P<0. 05). The decreasing ratios of SAPS and BPRS were correlated only to the trough plasma concentration of quetiapine steady state in the steady state, but not to the concentrations of its metabolites. The main side effects were dizziness and tachycardia. The score of α1 antiadrenocepter factor in TESS was correlated to the peak plasma concentration of quetiapine in the steady state, but the scores of other factors and the total score of TESS did not correlate with the concentrations of quetiapine and its metabolites. CONCLUSIONS Quetiapine is effective, rapid and has few side effects in treating patients of schizophrenia. Plasma concentration monitor for quetiapine is necessary to optimize the treatment protocol in the clinical use of quetiapine.
出处
《中南药学》
CAS
2003年第4期204-206,共3页
Central South Pharmacy
