J Clin Psychopharmacol 2011 Dec;31 (6): 758-62. [IF:4.857]
Aripiprazole and dehydroaripiprazole plasma concentrations and clinical responses in patients with schizophrenia.
Lin SK , Chen CK , Liu YL .
From the *Taipei City Hospital and Psychiatric Center; Department of Psychiatry, Taipei Medical University, Taipei; Department of Psychiatry, Chang Gung Memorial Hospital at Keelung, Keelung; §Chang Gung University School of Medicine, Taoyuan; and ∥Division of Mental Health and Addiction Medicine, Institute of Population Health Sciences, National Health Research Institutes, Zhunan, Miaoli County, Taiwan, Republic of China.
台北医学大学，台湾长庚大学医学院，基隆长庚医院精神科，台北市立疗养院
Abstract
Aripiprazole is widely used to treat schizophrenia. Plasma levels of aripiprazole and its active metabolite dehydroaripiprazole and their clinical responses in patients were explored. Forty-five (male/female: 19/26) patients with schizophrenia were treated with aripiprazole after a washout period of at least 3 days. There was no concomitant psychotropic except benzodiazepines for insomnia. The Positive and Negative Syndrome Scale (PANSS) was used to measure the clinical response at baseline and at weeks 2, 4, and 6. Blood was drawn at week 6 to measure the plasma concentrations of aripiprazole and dehydroaripiprazole. Patients with a PANSS score that decreased by more than 20% were defined as responders after 6 weeks of treatment. There was no difference in baseline PANSS scores or the daily dosage used between responders (n = 28) and nonresponders (n = 17) (15.0 ± 5.9 vs 12.9 ± 6.9 mg, respectively; P = 0.203). The responders showed a trend toward a higher plasma concentration of aripiprazole than nonresponders (234.4 ± 156.7 vs 163.5 ± 77.2 ng/mL, respectively; P = 0.117) and a significantly higher plasma concentration of dehydroaripiprazole (101.6 ± 58.0 vs 66.0 ± 48.4, respectively; P = 0.023). Higher plasma concentrations of aripiprazole and its active metabolite dehydroaripiprazole were noted in responders than nonresponders. Compared with Western patients, Oriental patients had higher plasma concentrations of aripiprazole and dehydroaripiprazole at the same dose. We suggest that therapeutic drug monitoring of aripiprazole will help improve the response in clinical practice.
摘要:
阿立哌唑一直被广泛用于治疗精神分裂症。阿立哌唑和其活性代谢产物脱氢阿立哌唑的血浆浓度以及患者的临床治疗效果已经被进行了广泛地探讨。45名（男/女：19/26名）精神分裂症患者在治疗失败至少三天后予以阿立哌唑治疗。治疗后除了苯二氮卓类药物引起失眠外并没有伴随其它精神症状。阳性和阴性症状量表（PANSS）是用来衡量患者在最初治疗时和第2，4和6周的临床治疗反应。在第6周时采血测定阿立哌唑与脱氢阿立哌唑的血浆浓度。在治疗6周后患者的阳性和阴性症状量表分数减少了20%以上的被定义为有反应者。基线PANSS分数或者每日剂量介于有反应者(n = 28)和无反应者(n = 17)之间者（有反应者与无反应者剂量分别为15.0 ± 5.9mg，12.9 ± 6.9 mg；P = 0.203）并没有什么区别。这些有反应者显示了一种趋势：有反应者的阿立哌唑血浆浓度比无反应者要高（分别为234.4 ± 156.7ng/mL和163.5 ± 77.2 ng/mL；P = 0.117），且脱氢阿立哌唑的血浆浓度也明显增高（分别为101.6 ± 58.0 ng/mL和66.0 ± 48.4 ng/mL；P = 0.023）。有反应者相对无反应者的阿立哌唑及其活性代谢产物脱氢阿立哌唑血药浓度均较高。相比西方，在相同剂量的情况下东方患者具有有较高的阿立哌唑与脱氢阿立哌唑血药浓度。我们认为，通过监测阿立哌唑的血浆浓度可以帮助我们在临床实践中提高治疗效果。
