4.2 Article

Striatal D2/D3 receptor occupancy, clinical response and side effects with amisulpride:: An iodine-123-iodobenzamide SPET study

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PHARMACOPSYCHIATRY
卷 41, 期 5, 页码 169-175

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GEORG THIEME VERLAG KG
DOI: 10.1055/s-2008-1076727

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  1. Sanofi-Aventis, Berlin

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Introduction: Amisulpride appears to be an effective atypical agent for treating schizophrenia in a dose-dependent manner. Methods: 29 patients Suffering from schizophrenia or schizoaffective disorder were treated with a broad dose range of amisulpride (50-1200 mg/clay, mean: 455.2 +/- 278.8 mg/day). After 2 weeks, brain single photon emission tomography (SPET) scans were performed two hours after intravenous injection of 185 MBq [I-123]IBZM. Clinical evaluations and ratings of extrapyramidal symptoms were performed at baseline and after steady state treatment of two weeks with amisulpride. Results: In patients treated with amisulpride, specific binding of [I-123]IBZM to D2 receptors was significantly decreased (p < 0.001) compared to healthy controls. D2 receptor blockade correlated well with administered doses and plasma concentrations of amisulpride. Extrapyramidalside effects, which had to be treated with biperiden, were observed in 31 % of the patients. Clinical response was very good, without correlation between the response and striatal D2 occupancy. Discussion: Within the first two weeks of treatment with the atypical antipsychotic amisulpride a significant occupancy of striatal postsynaptic dopamine D2 receptors was achieved. At the same time amisulpride shows an excellent tolerability with good efficacy.

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