Transplacental transfer and metabolism of bupropion

Angela D. Earhart, Svetlana Patrikeeva, Xiao-Ming Wang, Doaa Reda Abdelrahman, Gary Hankins, Mahmoud Ahmed, Tatiana Nanovskaya

Research output: Contribution to journalArticle

25 Scopus citations

Abstract

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 150ng/ml and 450ng/ml, along with the marker compound antipyrine 20μg/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 4h 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.

Original languageEnglish (US)
Pages (from-to)409-416
Number of pages8
JournalJournal of Maternal-Fetal and Neonatal Medicine
Volume23
Issue number5
DOIs
StatePublished - May 2010

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Keywords

  • Bupropion
  • Metabolism
  • Pregnant smokers
  • Smoking cessation
  • Transplacental transfer

ASJC Scopus subject areas

  • Pediatrics, Perinatology, and Child Health
  • Obstetrics and Gynecology

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