Accumulation of fluoxetine and norfluoxetine in human brain during therapeutic administration

Autor: James G. Flood, R. G. Gonzalez, Perry F. Renshaw, Maurizio Fava, Jerrold F. Rosenbaum, P R Puopolo, Kathy Clancy, Pearlman Jd, Alexander R. Guimaraes
Rok vydání: 1992
Předmět:
Zdroj: American Journal of Psychiatry. 149:1592-1594
ISSN: 1535-7228
0002-953X
DOI: 10.1176/ajp.149.11.1592
Popis: In vivo l9fluorine nuclear magnetic resonance spectroscopy was used to measure the brain concentration offluoxetine 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.O) (95% confidence interval=1.9-3.3). This accumulation may have implications for understanding both the therapeutic and the toxic effects of fluoxetine. (Am J Psychiatry 1992; 149:1592-1594) T he potential that in vivo nuclear magnetic mesonance spectroscopy (MRS) holds for research in psychiatry has been the subject of recent reviews ( 1, 2). From a psychopharmacological perspective, MRS offers a means of noninvasively measuring the brain levels of those drugs which are MRS-visible. These agents include lithium and psychotropic medications that contain fluorine. To date, in vivo brain nesonances have been detected in human subjects taking lithium, tnifluopemazine, fluphenazine, and fluoxetine (3-5). The rationale for this work lies in the hypothesis that a knowledge of the brain levels of these drugs may contribute to an understanding of both their therapeutic and their toxic effects. Unfortunately, except for lithium, it has been difficult to quantitate brain drug levels on to correlate these values with comesponding plasma levels. Additionally, reports of spectra derived from subjects taking fluorinated psychotropic agents have generally consisted of data from a single subject taking unusually high doses of medica
Databáze: OpenAIRE