Accumulation of fluoxetine and norfluoxetine in human brain during therapeutic administration



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Am J Psychiatry 1992; 149:1592-1594
Copyright © 1992 by American Psychiatric Association

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Accumulation of fluoxetine and norfluoxetine in human brain during therapeutic administration

PF Renshaw, AR Guimaraes, M Fava, JF Rosenbaum, JD Pearlman, JG Flood, PR Puopolo, K Clancy and RG Gonzalez
MGH-NMR Center, Massachusetts General Hospital-East, Charlestown.

In vivo 19fluorine nuclear magnetic resonance spectroscopy was used to measure the brain concentration of fluoxetine and norfluoxetine in five patients with obsessive-compulsive disorder and three with major depression. The mean brain:plasma ratio of the parent drug plus the metabolite was significantly elevated to 2.6 (SD = 1.0) (95% confidence interval = 1.9-3.3). This accumulation may have implications for understanding both the therapeutic and the toxic effects of fluoxetine.

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