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DC Field | Value | Language |
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dc.contributor.author | Suzuki, Takefumi | - |
dc.contributor.author | Graff-Guerrero, Ariel | - |
dc.contributor.author | Uchida, Hiroyuki | - |
dc.contributor.author | Remington, Gary | - |
dc.contributor.author | Caravaggio, Fernando | - |
dc.contributor.author | Borlido, Carol | - |
dc.contributor.author | Pollock, Bruce G. | - |
dc.contributor.author | Mulsant, Benoit H. | - |
dc.contributor.author | Deluca, Vincenzo | - |
dc.contributor.author | Ismail, Zahinoor | - |
dc.contributor.author | Mamo, David | - |
dc.date.accessioned | 2017-11-16T10:55:41Z | - |
dc.date.available | 2017-11-16T10:55:41Z | - |
dc.date.issued | 2013 | - |
dc.identifier.citation | Suzuki, T., Graff-Guerrero, A., Uchida, H., Remington, G., Caravaggio, F., Borlido, C., ... & Mamo, D. (2013). Dopamine D2/3 occupancy of ziprasidone across a day: a within-subject PET study. Psychopharmacology, 228(1), 43-51. | en_GB |
dc.identifier.uri | https://www.um.edu.mt/library/oar//handle/123456789/23921 | - |
dc.description.abstract | Rationale Ziprasidone is an atypical antipsychotic recommended to be administered twice daily. Objectives The purpose of this study was to investigate whether occupancy of the dopamine D2/3 receptors by ziprasidone is maintained across a day employing a within subject design. Methods Positron emission tomography (PET) scans with [11C]-raclopride were performed in 12 patients with schizophrenia while treated with ziprasidone 60 mg twice daily. Each patient completed [11C]-raclopride PET scans at 5, 13 and 23 h after the last dose of ziprasidone. Dopamine D2/3 receptor occupancy was estimated with reference to binding potential data of 44 age- and sex-matched control subjects in the caudate, putamen and ventral striatum. Results Eleven scans were available at each time point, and the mean occupancies at 5-, 13- and 23-h scans were 66, 39 and 2 % in the putamen; 62, 35 and −6 % in the caudate; and 68, 47 and 11 % in the ventral striatum, respectively. The time-course of receptor occupancy across the regions indicated an occupancy half-life of 8.3 h. The serum level of ziprasidone associated with 50 % D2/3 receptors occupancy was estimated to be 204 nmol/L (84 ng/ml). Prolactin levels were highest at 5-h post-dose and none showed hyperprolactinemia at 23-h scans. Conclusions The absence of ziprasidone striatal D2/3 receptor binding 23 h after taking 60 mg under steady-state conditions is consistent with its peripheral half-life. The results support our earlier report that ziprasidone 60 mg administered twice daily appears to be the minimal dose expected to achieve therapeutic central dopamine D2/3 receptor occupancy (i.e. 60 %). | en_GB |
dc.language.iso | en | en_GB |
dc.publisher | Springer | en_GB |
dc.rights | info:eu-repo/semantics/openAccess | en_GB |
dc.subject | Receptors, Dopamine | en_GB |
dc.subject | Pharmacokinetics | en_GB |
dc.subject | Tomography, Emission | en_GB |
dc.subject | Schizophrenia | en_GB |
dc.title | Dopamine D2/3 occupancy of ziprasidone across a day : a within-subject PET study | en_GB |
dc.type | article | en_GB |
dc.rights.holder | The copyright of this work belongs to the author(s)/publisher. The rights of this work are as defined by the appropriate Copyright Legislation or as modified by any successive legislation. Users may access this work and can make use of the information contained in accordance with the Copyright Legislation provided that the author must be properly acknowledged. Further distribution or reproduction in any format is prohibited without the prior permission of the copyright holder | en_GB |
dc.description.reviewed | peer-reviewed | en_GB |
dc.identifier.doi | 10.1007/s00213-013-3012-1 | - |
dc.publication.title | Psychopharmacology | en_GB |
Appears in Collections: | Scholarly Works - FacM&SPsy |
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nihms447050.pdf | 711.16 kB | Adobe PDF | View/Open |
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