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The relationship between the plasma concentration of blonanserin, and its plasma anti‐serotonin 5‐HT 2A activity/anti‐dopamine D 2 activity ratio and drug‐induced extrapyramidal symptoms
Author(s) -
Suzuki Hidenobu,
Gen Keishi
Publication year - 2012
Publication title -
psychiatry and clinical neurosciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.609
H-Index - 74
eISSN - 1440-1819
pISSN - 1323-1316
DOI - 10.1111/j.1440-1819.2011.02311.x
Subject(s) - chemistry , medicine , extrapyramidal symptoms , endocrinology , antipsychotic , schizophrenia (object oriented programming) , psychology , psychiatry
Aims: Blonanserin is a second‐generation antipsychotic that was developed in Japan. We investigated the relationships between plasma concentration, the plasma anti‐5‐HT 2A activity/anti‐D 2 activity (S/D) ratio and extrapyramidal symptoms (EPS) in blonanserin dosing. Methods: The subjects were 29 outpatients with schizophrenia. We assessed EPS using the Drug‐Induced Extrapyramidal Symptoms Scale (DIEPSS). The plasma concentrations were measured by high performance liquid chromatography, and the plasma anti‐D 2 and anti‐5‐HT 2A activities were measured by [ 3 H]‐spiperone and [ 3 H]‐ketanserin radioreceptor assays. Results: The results revealed that there were significant correlations between both the plasma concentration and the DIEPSS total score ( P < 0.05). A negative correlative tendency was found between the S/D ratio and the DIEPSS total score. Furthermore, the plasma concentrations were divided into a low plasma concentration group and a high plasma concentration group, and the S/D ratios were divided into a low S/D ratio group and a high S/D ratio group. We then compared each group based on the DIEPSS total scores. The score in the high plasma concentration‐low S/D ratio group was significantly higher than in the high plasma concentration‐high S/D ratio, low plasma concentration‐high S/D ratio and low plasma concentration‐low S/D ratio groups ( P < 0.05 for all). Conclusions: These findings indicate that the incidence of EPS during treatment with blonanserin is mainly determined by plasma concentration, but the incidence of EPS may be inhibited when anti‐5HT 2A activity is predominant over anti‐D 2 activity.