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Bupropion plasma levels and CYP2D6
Pollock BG, Sweet RA, Kirshner M,
Reynolds CF 3rd.
Department of Psychiatry, University of
Pittsburgh School of Medicine, Pennsylvania, USA.
antidepressants with the exception of fluvoxamine and nefazodone either
are metabolized by cytochrome P450 2D6 (CYP2D6) and/or inhibit this
isozyme. To date, nothing in this regard has been published concerning
bupropion. We report that plasma level/dose ratios for bupropion, and
its metabolites erythrohydrobupropion and threohydrobupropion, were not
associated with debrisoquine metabolic status in 12 patients, three of
whom were poor 2D6 metabolizers. The plasma level/dose ratios for the
metabolite hydroxybupropion were, however, significantly higher in poor
2D6 metabolizers. In three patients, who received a second phenotyping
test during treatment with bupropion, debrisoquine metabolic ratios were
not increased. It is thus inferred that bupropion is neither metabolized
by nor inhibits CYP2D6. The potential accumulation of hydroxybupropion
after CYP2D6 inhibition may, however, contribute to toxicity and impair
bupropion's therapeutic effectiveness.
PMID: 8885123 [PubMed - indexed for