Transplacental transfer and metabolism of bupropion

Methods. Placentas obtained from healthy term pregnancies were perfused with bupropion at two concentrations 150 ng/ml and 450 ng/ml, along with the marker compound antipyrine 20 mu g/ml. Radioactive isotopes of the two drugs were co-transfused to enhance their detection limits. Concentrations of bupropion and its metabolite were determined by liquid chromatography and liquid scintillation spectrometry. Results. The fetal/maternal concentration ratio of bupropion was 1.07 +/- 0.22. Following 4 h of its perfusion, 48 +/- 6% of bupropion was retained by placental tissue, 32 +/- 5% remained in the maternal circuit, and 20 +/- 6% was transferred to the fetal circuit. A metabolite of bupropion, threohydrobupropion, was identified. Conclusions. Bupropion was transferred from the maternal to fetal circuit and was biotransformed by placental tissue enzymes to its metabolite threohydrobupropion. Bupropion and its metabolite did not affect placental tissue viability or functional parameters. These data suggest that bupropion has the potential of being used for smoking cessation during pregnancy and should be further investigated for its safety and efficacy.