Huang H F, Jann M W, Wei F C, Chang T P, Chen J S, Juang D J, Lin S K, Lam Y W, Chien C P, Chang W H
Taipei City Psychiatric Center, Taiwan, ROC.
J Clin Pharmacol. 1996 Oct;36(10):963-9. doi: 10.1002/j.1552-4604.1996.tb04764.x.
The pharmacokinetic interaction between buspirone and haloperidol was evaluated in schizophrenic patients in two different groups. In both groups, haloperidol doses (10-40 mg/day) remained constant for 6 weeks before the addition of buspirone 10 mg three times daily. Serial blood samples were obtained from the 11 patients in group I at baseline (before addition of buspirone) and after administration for 24 hours. The pharmacokinetic parameters of haloperidol were determined alone and with coadministration of buspirone. In group II, buspirone 10 mg three times daily was added to treatment with haloperidol in 27 patients. Blood samples were obtained before addition of buspirone and at weeks 2 and 6 of treatment with buspirone. Samples were obtained 10 to 12 hours after administration of the evening dose and before the morning dose. Haloperidol and its metabolite, reduced haloperidol (RH), were assayed by means of high-performance liquid chromatography with electrochemical detection. Significant changes in the pharmacokinetic parameters of haloperidol were not found in group I; a mean increase in the half-life (t1/2) of haloperidol from 21.5 to 28.1 hours was observed, but this finding was not statistically significant. Under steady-state conditions, plasma levels of haloperidol in the patients in group II did not change significantly from baseline to week 6. Plasma concentrations of RH remained unaltered in both groups. The results indicate that coadministration of buspirone does not markedly affect the pharmacokinetics or plasma concentrations of haloperidol.
在两组精神分裂症患者中评估了丁螺环酮与氟哌啶醇之间的药代动力学相互作用。在两组中，氟哌啶醇剂量（10 - 40毫克/天）在每日三次添加10毫克丁螺环酮之前持续6周保持恒定。从第一组的11名患者在基线（添加丁螺环酮之前）和给药24小时后采集系列血样。单独测定氟哌啶醇的药代动力学参数，并在与丁螺环酮合用的情况下进行测定。在第二组中，27名患者在使用氟哌啶醇治疗的基础上每日三次添加10毫克丁螺环酮。在添加丁螺环酮之前以及使用丁螺环酮治疗的第2周和第6周采集血样。在晚间剂量给药后10至12小时且在早晨剂量给药之前采集样本。采用高效液相色谱 - 电化学检测法测定氟哌啶醇及其代谢产物还原氟哌啶醇（RH）。在第一组中未发现氟哌啶醇药代动力学参数有显著变化；观察到氟哌啶醇的半衰期（t1/2）平均从21.5小时增加到28.1小时，但这一发现无统计学意义。在稳态条件下，第二组患者中氟哌啶醇的血浆水平从基线到第6周未发生显著变化。两组中RH的血浆浓度均保持不变。结果表明，丁螺环酮与氟哌啶醇合用不会显著影响氟哌啶醇的药代动力学或血浆浓度。
