Striatal dopamine-2 receptor occupancy as measured with (123I)iodobenzamide and SPECT predicted the occurrence of EPS in patients treated with atypical antipsychotics and haloperidol.

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作   者：

Tauscher J;  Kufferle B;  Asenbaum S;  Tauscher Wisniewski S;  Kasper S; 

作者机构：

Wahringer Gurtel 18-20;  University of Vienna;  Department of General Psychiatry;  1090 Vienna;  Austria. johannes.tauscher@akh-wien.ac.at; 

关键词：

Dopamine D2;  多巴胺D2;  Iodobenzenes;  Haloperidol;  抗精神病剂;  单光子;  氟哌啶醇;  碘苯类;  Antipsychotic Agents;  Receptors;  体层摄影术;  发射型计算机;  受体;  Corpus Striatum;  纹状体; 

期刊名称：

Psychopharmacology

i s s n：

0033-3158

年卷期：

2002 年 162 卷 1 期

页   码：

42-49

页   码：

摘   要：

RATIONALE: Extrapyramidal symptoms (EPS) are common with conventional antipsychotics. Clozapine and other novel antipsychotic substances with lower in vitro affinity for dopamine-2 (D(2)) receptors have a lower propensity to induce EPS. OBJECTIVE: We investigated whether striatal D(2) receptor occupancy predicted the occurrence of EPS with atypical antipsychotics and the typical neuroleptic haloperidol. METHODS: [(123)I]Iodobenzamide (IBZM) and single photon emission tomography (SPECT) were used to quantify receptor occupancy in 71 patients treated with antipsychotics. EPS were rated according to the Simpson-Angus scale (SAS). EPS were deemed clinically relevant, if the SAS score was > or = 5 and/or anticholinergic medication was required. Patients received atypical antipsychotic monotherapy for at least 14 days with amisulpride ( n=2), clozapine ( n=6), haloperidol ( n=10), olanzapine ( n=6), quetiapine ( n=4), risperidone ( n=14), sertindole ( n=13), or zotepine ( n=16). RESULTS: The striatal D(2) receptor occupancy ranged from < 20% to almost saturation. The lowest occupancy was seen with quetiapine and clozapine, the highest with haloperidol. Twenty-two of 71 patients (29%) experienced clinically relevant EPS. These patients displayed significantly higher mean striatal D(2) receptor occupancy (77%) than those without EPS (61%; P=0.002). We found a positive correlation between the percentage of striatal D(2) receptor occupancy and the SAS score ( r=0.28; P=0.02), despite 18 of these patients receiving anticholinergics, thus lowering their SAS score. CONCLUSIONS: Striatal D(2) receptor occupancy as measured with [(123)I]IBZM and SPECT predicted the occurrence of EPS in patients treated with atypical antipsychotics and haloperidol. In vivo imaging of brain receptors with SPECT may provide a useful clinical tool to titrate doses individually and avoid motor side effects in patients treated with novel antipsychotics.