Abstract
Positron emission tomography (PET) allows the evaluation of target molecules of various psychotropic drugs in the living human brain. PET studies have demonstrated that conventional antipsychotics induce high (70-90%) dopamine D2 receptor occupancy in the striatum. The risk of extrapyramidal side effects increases when the striatal D2 receptor occupancy exceeds 80%. Thus, D2 receptor occupancy between 70 and 80% appears to represent the optimal therapeutic window, at which antipsychotic effect can be expected with a minimal risk of extrapyramidal side effects. The clinical dose of the second-generation antipsychotics nicely fit this range of D2 receptor occupancy. Serotonin transporter occupancy has been the main biomarker for the evaluation of antidepressants, and has been used in the assessment of selective serotonin reuptake inhibitors. Recently, we have successfully measured norepinephrine transporter occupancy of antidepressants. These occupancy markers are useful for setting optimal doses of antipsychotics or antidepressants.
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Schedule a callMore From: Rinsho yakuri/Japanese Journal of Clinical Pharmacology and Therapeutics
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