open access

https://hdl.handle.net/2115/33033

Long-term perospirone treatment with a single dose at bedtime in schizophrenia : relevant to intermittent dopamine D2 receptor antagonism

英語

schizophrenia

2008-02-15

Elsevier

Progress in Neuro-Psychopharmacology and Biological Psychiatry

32(2)

520-522

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.

学術雑誌論文

Accepted Manuscript

0278-5846

AA10532839