Lane H Y, Lin H N, Hwu H G, Jann M, Hu W H, Chang W H
Laboratory of Biological Psychiatry, Taipei City Psychiatric Center, Taiwan ROC.
J Formos Med Assoc. 1995 Nov;94(11):671-8.
Haloperidol and reduced haloperidol are interconverted. The plasma concentrations of these two butyrophenones have been suggested to be important factors in determining the clinical effect of haloperidol treatment. The steady-state plasma concentrations of haloperidol and reduced haloperidol were measured in 322 Taiwanese schizophrenic patients using high performance liquid chromatography. The daily doses of haloperidol varied from 5 to 200 mg (mean +/- SD, 35.3 +/- 34.6 mg). There was a positive correlation between plasma concentrations and doses, following the equation: haloperidol concentration (ng/mL) = 0.88 x dose (mg/day)-1.66. However, the interpatient variation in haloperidol concentrations was up to ten-fold even in patients receiving the same dose (20 mg/day, n = 88). The expected values were about 10% to 50% higher than those reported in Caucasian patients. The plasma reduced haloperidol concentrations were significantly lower than, and correlated with, those of haloperidol in patients with haloperidol levels lower than 25 ng/mL. However, once haloperidol exceeded 25 ng/mL, reduced haloperidol levels rapidly elevated and appeared significantly higher than haloperidol levels. While haloperidol could reach its steady state in about 1 week, reduced haloperidol needed at least 4 weeks to do so. Haloperidol doses of less than 30 mg/day and plasma concentrations lower than 25 ng/mL are recommended for most Chinese patients.
氟哌啶醇和还原氟哌啶醇可相互转化。这两种丁酰苯类药物的血浆浓度被认为是决定氟哌啶醇治疗临床效果的重要因素。采用高效液相色谱法测定了322例台湾精神分裂症患者氟哌啶醇和还原氟哌啶醇的稳态血浆浓度。氟哌啶醇的日剂量为5至200毫克(均值±标准差,35.3±34.6毫克)。血浆浓度与剂量呈正相关,符合以下方程:氟哌啶醇浓度(纳克/毫升)=0.88×剂量(毫克/天)-1.66。然而,即使在接受相同剂量(20毫克/天,n = 88)的患者中,氟哌啶醇浓度的个体间差异也高达10倍。预期值比白种人患者报告的数值高约10%至50%。在氟哌啶醇水平低于25纳克/毫升的患者中,血浆还原氟哌啶醇浓度显著低于氟哌啶醇浓度,且与之相关。然而,一旦氟哌啶醇超过25纳克/毫升,还原氟哌啶醇水平迅速升高,且明显高于氟哌啶醇水平。虽然氟哌啶醇约1周可达到稳态,但还原氟哌啶醇至少需要4周才能达到稳态。对于大多数中国患者,建议氟哌啶醇日剂量小于30毫克/天,血浆浓度低于25纳克/毫升。