Accumulation of fluoxetine and norfluoxetine in human brain during therapeutic administration.
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.
Renshaw
P F
PF
MGH-NMR Center, Massachusetts General Hospital-East, Charlestown.
Guimaraes
A R
AR
Fava
M
M
Rosenbaum
J F
JF
Pearlman
J D
JD
Flood
J G
JG
Puopolo
P R
PR
Clancy
K
K
Gonzalez
R G
RG
D000328:Adult; D001921:Brain / Q000378:metabolism*; D016001:Confidence Intervals; D003866:Depressive Disorder / Q000097:blood / Q000188:drug therapy / Q000378:metabolism*; D005260:Female; D005461:Fluorine; D005473:Fluoxetine / Q000031:analogs & derivatives* / Q000097:blood / Q000378:metabolism* / Q000627:therapeutic use; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D009771:Obsessive-Compulsive Disorder / Q000097:blood / Q000188:drug therapy / Q000378:metabolism*
D005473:Fluoxetine; D005461:Fluorine; C036139:norfluoxetine