Haloperidol Decanoate의 임상효과 및 항정상태 약동학

Clinical Efficacy and Steady-State Pharmacokinetics of Haloperidol Decanoate

The 12 chronic schizophrenic patients, previously treated with several low-dose antipsychotics, received oral Haloperidol(lOmg once a day) for 4 weeks in the first phase and then given intram uscular Haloperidol decanoate(15 tim es the previous oral dose given every 4weeks interval) for a total of 12weeks in the second phase. 1. Clinical Efficacy. Using Brief Psychiatric Rating Scale, there were no significant differences in efficacy between oral Haloperidol in day 0 or day 28 and Haloperidol decanoate on day 28，indicating that these patients were stabilized. But there was a significant improvement in both overall Brief psychiatric Rating Scale Score(p〈0.05) and individual item scores such as tension(p〈0.05), depression(p<0.01), and anxiety and thought disorder from Eighth week of Haloperidol decanoate treatm ent compared with the final ratings on oral Haloperidol treatm ent on day 28. 2. Extrapyramidal Side-effect. In the phase of oral Haloperidol, they tended to have more extrapyramidal symptoms such as rigidity and acute dystonia. These adverse effects were significantly diminished from 8weeks’ Haloperidol decanoate(p<C0.05). The incidence of extrapyramidal symptoms was similar, but these symptoms were less severe in the from of depot than oral Haloperidol. It seemed likely that there was a slight positive correlation between the plasma Haloperidol level and the severity of Extrapyramidal symptoms. 3. Pharmacokinetic analysis 1) Relative bioavailability of Haloperidol decanoate to oral Haloperidol was 1.59± 0.44 and it meant that a monthly dose of Haloperidol decanoate corresponded to 17.5times the previous daily oral haloperidol dose. 2) Mean plasma steady-state haloperidol concentration was 4.14土 1.25ng/ml on oral Haloperidol( 10mg once a day) and it was 3.33土 0.44ng/ml on Haloperidol decanoate(150mg at 4weeks/interval). 3) Mean tim e required to reach the peak of plasma haloperidol level on haloperidol decanoate was 92土 36hr and the haloperidol levels decreased gradually by about one fourth their initial value showing marked fluctuation in the blood levels compared with oral Haloperidol. 4) According to these results, the authors recommend the individualization of dosage and dosing interval for a constant haloperidol levels in the initial phase of Haloperidol decanoate treatm ent