Transplacental transfer and metabolism of bupropion.
OBJECTIVE
In order to evaluate the potential use of bupropion as smoking cessation therapy during pregnancy, the aim of this investigation was to determine transplacental transfer and metabolism of bupropion and its distribution among placental tissue and maternal and fetal circuits of the dually perfused placental lobule.


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 microg/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.
Earhart
Angela D
AD
Department of Obstetrics & Gynecology, University of Texas Medical Branch, Galveston, Texas 77555-0587, USA.
Patrikeeva
Svetlana
S
Wang
Xiaoming
X
Abdelrahman
Doaa Reda
DR
Hankins
Gary D V
GD
Ahmed
Mahmoud S
MS
Nanovskaya
Tatiana
T
D016642:Bupropion / Q000378:metabolism* / Q000493:pharmacokinetics*; D002470:Cell Survival / Q000187:drug effects; D006063:Chorionic Gonadotropin / Q000032:analysis / Q000097:blood; D018765:Dopamine Uptake Inhibitors / Q000378:metabolism / Q000493:pharmacokinetics / Q000627:therapeutic use; D005260:Female; D006801:Humans; D008431:Maternal-Fetal Exchange / Q000187:drug effects; D008954:Models, Biological; D009924:Organ Culture Techniques; D010477:Perfusion; D010920:Placenta / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D011247:Pregnancy; D011485:Protein Binding; D012709:Serum Albumin / Q000378:metabolism; D016540:Smoking Cessation / Q000379:methods; D014470:Umbilical Cord / Q000378:metabolism
D006063:Chorionic Gonadotropin; D018765:Dopamine Uptake Inhibitors; D012709:Serum Albumin; D016642:Bupropion