Abstract | UNLABELLED: METHODS: RESULTS: Blood lurasidone concentration (plus major metabolite), but not dose, significantly correlated with D2 receptor occupancy. D2 receptor occupancy in several subcortical structures is associated with positive but not negative symptom improvement or the presence of movement symptoms. DISCUSSION: Blood concentrations greater than 70 ng/mL may be required to achieve a 65% occupancy level in subcortical areas. Intersubject blood concentrations at fixed dose were highly variable and may account for the lack of dose correlations. CONCLUSIONS: Positron emission tomography (PET) occupancy data suggest that greater than 65% occupancy can be achieved across the dose range of 80-160 mg/day and that some patients require higher doses to achieve antipsychotic efficacy; this finding supports prior randomized clinical trial results.
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Authors | Steven G Potkin, David B Keator, Marilyn L Kesler-West, Dana D Nguyen, Theo G M van Erp, Jogeshwar Mukherjee, Nikunj Shah, Adrian Preda |
Journal | CNS spectrums
(CNS Spectr)
Vol. 19
Issue 2
Pg. 176-81
(Apr 2014)
ISSN: 1092-8529 [Print] United States |
PMID | 24073841
(Publication Type: Journal Article, Randomized Controlled Trial, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antipsychotic Agents
- Benzamides
- Isoindoles
- N-((1-allyl-2-pyrrolidinyl)methyl)-5-(3-fluoropropyl)-2,3-dimethoxybenzamide
- Pyrrolidines
- Receptors, Dopamine D2
- Thiazoles
- Lurasidone Hydrochloride
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Topics |
- Adult
- Algorithms
- Antipsychotic Agents
(therapeutic use)
- Benzamides
(pharmacokinetics)
- Brain
(diagnostic imaging, drug effects)
- Dose-Response Relationship, Drug
- Female
- Humans
- Isoindoles
(therapeutic use)
- Lurasidone Hydrochloride
- Male
- Middle Aged
- Positron-Emission Tomography
- Psychiatric Status Rating Scales
- Psychotic Disorders
(diagnostic imaging, drug therapy)
- Pyrrolidines
(pharmacokinetics)
- Receptors, Dopamine D2
(metabolism)
- Schizophrenia
(diagnostic imaging, drug therapy)
- Statistics as Topic
- Thiazoles
(therapeutic use)
- Young Adult
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