In vivo 123I IBZM SPECT imaging of striatal dopamine-2 receptor occupancy in schizophrenic patients treated with olanzapine in comparison to clozapine and haloperidol.

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作   者：

Tauscher J;  Kufferle B;  Asenbaum S;  Fischer P;  Pezawas L;  Barnas C;  Tauscher Wisniewski-S;  Brucke T;  Kasper S; 

作者机构：

University of Vienna;  Department of General Psychiatry;  Austria. johannes.tauscher@akh-wien.ac.at; 

关键词：

Dopamine D2;  多巴胺D2;  Antipsychotic Agents;  Receptors;  精神分裂症;  受体;  Corpus Striatum;  Pirenzepine;  抗精神病剂;  哌仑西平;  纹状体; 

期刊名称：

Psychopharmacology

i s s n：

0033-3158

年卷期：

1999 年 141 卷 2 期

页   码：

175-181

页   码：

摘   要：

We investigated the degree of striatal dopamine-2 (D2) receptor occupancy in six schizophrenic patients receiving clinically effective antipsychotic treatment with olanzapine 10-25 mg/day in comparison to patients treated with clozapine 300-600 mg/day (n = 6) or haloperidol 5-20 mg/day (n = 10). 123I Iodobenzamide (IBZM) and single photon emission computerized tomography (SPECT) were used for the visualization of striatal D2 receptors. For the quantification of striatal D2 receptor occupancy, striatal IBZM binding in patients treated with antipsychotics was compared to that in untreated healthy controls (n = 8) reported earlier. Olanzapine led to a mean striatal D2 receptor occupancy rate of 75% (range 63-85). Haloperidol-treated patients showed dose-dependently (Pearson r = 0.64; P < 0.05) a significantly higher (P < 0.05) mean occupancy rate of 84% (range 67-94). During clozapine treatment, the mean D2 receptor occupancy of 33% (range < 20-49) was significantly lower than with olanzapine (P < 0.005). The higher striatal D2 receptor occupancy of haloperidol was correlated with the incidence and severity of extrapyramidal motor side-effects (EPS). No clinical relevant EPS occurred during treatment with olanzapine or clozapine. There was no correlation between the degree of striatal D2 receptor occupancy and clinical improvement.