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Long-term perospirone treatment with a single dose at bedtime in schizophrenia : relevant to intermittent dopamine D2 receptor antagonism
| Title: | Long-term perospirone treatment with a single dose at bedtime in schizophrenia : relevant to intermittent dopamine D2 receptor antagonism |
| Authors: | Kusumi, Ichiro Browse this author →KAKEN DB | | Masui, Takuya Browse this author | | Koyama, Tsukasa Browse this author |
| Keywords: | Perospirone | | ID-15036 | | plasma concentration | | maintenance | | intermittent D2 blockade | | schizophrenia |
| Issue Date: | 15-Feb-2008 |
| Publisher: | Elsevier |
| Journal Title: | Progress in Neuro-Psychopharmacology and Biological Psychiatry |
| Volume: | 32 |
| Issue: | 2 |
| Start Page: | 520 |
| End Page: | 522 |
| Publisher DOI: | 10.1016/j.pnpbp.2007.10.008 |
| PMID: | 18006133 |
| Abstract: | Perospirone, a serotonin 5-HT2A and dopamine D2 receptor antagonist, is metabolized to ID-15036 by CYP3A4 and the elimination half-life (T1/2) for the latter is longer than the former. The active metabolite ID-15036 is an 8-times weaker D2 antagonist than perospirone, although it has a high affinity for 5-HT2A receptor. In this study, we measured the plasma concentrations of peospirone and ID-15036 in the long-term stable schizophrenic patients with a single dose of perospirone at bedtime. The mean level of perospirone at 11-15 hrs after a last dosing was much lower (0.49 ng/ml) than that of ID-15036 (2.89 ng/ml). These results show that a long-term perospirone monotherapy with a single dose at bedtime is effective for the maintenance treatment of chronic schizophrenia and also suggest the possibility that intermittent D2 receptor blockade may be sufficient for effective relapse prevention. |
| Relation: | http://www.sciencedirect.com/science/journal/02785846 |
| Type: | article (author version) |
| URI: | http://hdl.handle.net/2115/33033 |
| Appears in Collections: | 北海道大学病院 (Hokkaido University Hospital) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)
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Submitter: 久住 一郎
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