Olesen O V, Licht R W, Thomsen E, Bruun T, Viftrup J E, Linnet K
Institute for Basic Psychiatric Research, Department of Biological Psychiatry, Aarhus University Hospital, Risskov, Denmark.
Ther Drug Monit. 1998 Aug;20(4):380-4. doi: 10.1097/00007691-199808000-00004.
Steady state serum concentrations of risperidone and 9-hydroxyrisperidone (9-OH-risperidone), the active moiety, were measured in 42 patients. The concentration-to-dose ratios (C/D) varied by a factor of 20, from 1.8 to 36.8 (nmol/l)/(mg/24 hours), and 90% of the active moiety was constituted of 9-OH-risperidone. No correlation between the serum concentration of the active moiety and the side effects evaluated by the UKU Side Effect Scale was found. The absence of CYP2D6 (poor metabolizers) or the coadministration of drugs other than benzodiazepines increased the ratio between parent compound and metabolite but did not significantly influence the C/D of the total active moiety. A therapeutic range for serum risperidone has not been established, but 6 mg/day is considered the optimum dose for most patients. The authors found that in 90% of 22 patients administered 6 mg/day risperidone, the serum levels were within 50 to 150 nmol/l.
对42例患者测定了利培酮及其活性部分9-羟基利培酮的稳态血清浓度。浓度与剂量之比（C/D）变化范围为20倍，从1.8至36.8（纳摩尔/升）/（毫克/24小时），且90%的活性部分由9-羟基利培酮构成。未发现活性部分的血清浓度与通过UKU副作用量表评估的副作用之间存在相关性。缺乏CYP2D6（代谢不良者）或同时服用除苯二氮䓬类药物以外的其他药物会增加母体化合物与代谢物之间的比例，但对总活性部分的C/D没有显著影响。尚未确定血清利培酮的治疗范围，但6毫克/天被认为是大多数患者的最佳剂量。作者发现，在22例每天服用6毫克利培酮的患者中，90%的患者血清水平在50至150纳摩尔/升之间。
