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Dose-finding study of paliperidone ER based on striatal and extrastriatal dopamine D2 receptor occupancy in patients with schizophrenia
https://repo.qst.go.jp/records/45147
https://repo.qst.go.jp/records/4514743152dd0-6035-4d8e-b28e-a830b5de20b6
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2008-05-07 | |||||
| タイトル | ||||||
| タイトル | Dose-finding study of paliperidone ER based on striatal and extrastriatal dopamine D2 receptor occupancy in patients with schizophrenia | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Arakawa, Ryosuke
× Arakawa, Ryosuke× Ito, Hiroshi× Takano, Akihiro× Takahashi, Hidehiko× Morimoto, Takuya× Sassa, Takeshi× Ohta, Katsuya× Kato, Motoichiro× Okubo, Yoshiro× Suhara, Tetsuya× 荒川 亮介× 伊藤 浩× 高野 晶寛× 高橋 英彦× 森本 卓哉× 佐々 毅× 加藤 元一郎× 大久保 善朗× 須原 哲也 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Rationale Paliperidone ER is a novel antipsychotic drug in an extended-release (ER) formulation.As with all antipsychotics, careful dose setting is necessary to avoid side effects. Objectives In this study, we measured striatal and extrastriatal dopamine D2 receptor occupancy during paliperidone ER treatment in patients with schizophrenia using positron emission tomography (PET) to compare regional occupancy and to estimate the optimal dose. Materials and methods Thirteen male patients with schizophrenia participated in this 6-week multiple-dose study. Six of them took 3 mg of paliperidone ER per day, four took 9 mg, and three took 15 mg. Two to 6 weeks after first drug intake, two PET scans, one with [11C]raclopride and one with [11C]FLB 457, were performed in each patient on the same day. The relationship between the dose or plasma concentration of paliperidone and dopamine D2 receptor occupancy was calculated. Results The dopamine D2 receptor occupancies in the striatum measured with [11C]raclopride and the temporal cortex measured with [11C]FLB 457 were 54.2–85.5% and 34.5–87.3%, respectively. ED50 values of the striatum and temporal cortex were 2.38 and 2.84 mg/day, respectively. There was no significant difference in dopamine D2 receptor occupancy between the striatum and the temporal cortex. Conclusions The data from this study suggest that paliperidone ER at 6–9 mg provides an estimated level of dopamine D2 receptor occupancy between 70–80% and that the magnitude of dopamine D2 receptor occupancy is similar between the striatum and temporal cortex. |
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| 書誌情報 |
Psychopharmacology 巻 197, 号 2, p. 229-235, 発行日 2008-04 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0033-3158 | |||||
