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Research ArticleArticle

Pharmacokinetics of Bupropion and Its Pharmacologically Active Metabolites in Pregnancy

Valentina M. Fokina, Meixiang Xu, Erik Rytting, Sherif Z. Abdel-Rahman, Holly West, Cheryl Oncken, Shannon M. Clark, Mahmoud S. Ahmed, Gary D.V. Hankins and Tatiana N. Nanovskaya
Drug Metabolism and Disposition November 2016, 44 (11) 1832-1838; DOI: https://doi.org/10.1124/dmd.116.071530
Valentina M. Fokina
Department of Pharmacology and Toxicology (V.M.F.), Maternal-Fetal Pharmacology and Biodevelopment Laboratories, Department of Obstetrics and Gynecology (M.X., E.R., S.Z.A.-R., M.S.A., T.N.N.), and Department of Obstetrics and Gynecology (H.W., S.M.C., G.D.V.H.), University of Texas Medical Branch, Galveston, Texas; and University of Connecticut Health Center, Farmington, Connecticut (C.O.)
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Meixiang Xu
Department of Pharmacology and Toxicology (V.M.F.), Maternal-Fetal Pharmacology and Biodevelopment Laboratories, Department of Obstetrics and Gynecology (M.X., E.R., S.Z.A.-R., M.S.A., T.N.N.), and Department of Obstetrics and Gynecology (H.W., S.M.C., G.D.V.H.), University of Texas Medical Branch, Galveston, Texas; and University of Connecticut Health Center, Farmington, Connecticut (C.O.)
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Erik Rytting
Department of Pharmacology and Toxicology (V.M.F.), Maternal-Fetal Pharmacology and Biodevelopment Laboratories, Department of Obstetrics and Gynecology (M.X., E.R., S.Z.A.-R., M.S.A., T.N.N.), and Department of Obstetrics and Gynecology (H.W., S.M.C., G.D.V.H.), University of Texas Medical Branch, Galveston, Texas; and University of Connecticut Health Center, Farmington, Connecticut (C.O.)
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Sherif Z. Abdel-Rahman
Department of Pharmacology and Toxicology (V.M.F.), Maternal-Fetal Pharmacology and Biodevelopment Laboratories, Department of Obstetrics and Gynecology (M.X., E.R., S.Z.A.-R., M.S.A., T.N.N.), and Department of Obstetrics and Gynecology (H.W., S.M.C., G.D.V.H.), University of Texas Medical Branch, Galveston, Texas; and University of Connecticut Health Center, Farmington, Connecticut (C.O.)
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Holly West
Department of Pharmacology and Toxicology (V.M.F.), Maternal-Fetal Pharmacology and Biodevelopment Laboratories, Department of Obstetrics and Gynecology (M.X., E.R., S.Z.A.-R., M.S.A., T.N.N.), and Department of Obstetrics and Gynecology (H.W., S.M.C., G.D.V.H.), University of Texas Medical Branch, Galveston, Texas; and University of Connecticut Health Center, Farmington, Connecticut (C.O.)
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Cheryl Oncken
Department of Pharmacology and Toxicology (V.M.F.), Maternal-Fetal Pharmacology and Biodevelopment Laboratories, Department of Obstetrics and Gynecology (M.X., E.R., S.Z.A.-R., M.S.A., T.N.N.), and Department of Obstetrics and Gynecology (H.W., S.M.C., G.D.V.H.), University of Texas Medical Branch, Galveston, Texas; and University of Connecticut Health Center, Farmington, Connecticut (C.O.)
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Shannon M. Clark
Department of Pharmacology and Toxicology (V.M.F.), Maternal-Fetal Pharmacology and Biodevelopment Laboratories, Department of Obstetrics and Gynecology (M.X., E.R., S.Z.A.-R., M.S.A., T.N.N.), and Department of Obstetrics and Gynecology (H.W., S.M.C., G.D.V.H.), University of Texas Medical Branch, Galveston, Texas; and University of Connecticut Health Center, Farmington, Connecticut (C.O.)
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Mahmoud S. Ahmed
Department of Pharmacology and Toxicology (V.M.F.), Maternal-Fetal Pharmacology and Biodevelopment Laboratories, Department of Obstetrics and Gynecology (M.X., E.R., S.Z.A.-R., M.S.A., T.N.N.), and Department of Obstetrics and Gynecology (H.W., S.M.C., G.D.V.H.), University of Texas Medical Branch, Galveston, Texas; and University of Connecticut Health Center, Farmington, Connecticut (C.O.)
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Gary D.V. Hankins
Department of Pharmacology and Toxicology (V.M.F.), Maternal-Fetal Pharmacology and Biodevelopment Laboratories, Department of Obstetrics and Gynecology (M.X., E.R., S.Z.A.-R., M.S.A., T.N.N.), and Department of Obstetrics and Gynecology (H.W., S.M.C., G.D.V.H.), University of Texas Medical Branch, Galveston, Texas; and University of Connecticut Health Center, Farmington, Connecticut (C.O.)
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Tatiana N. Nanovskaya
Department of Pharmacology and Toxicology (V.M.F.), Maternal-Fetal Pharmacology and Biodevelopment Laboratories, Department of Obstetrics and Gynecology (M.X., E.R., S.Z.A.-R., M.S.A., T.N.N.), and Department of Obstetrics and Gynecology (H.W., S.M.C., G.D.V.H.), University of Texas Medical Branch, Galveston, Texas; and University of Connecticut Health Center, Farmington, Connecticut (C.O.)
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Abstract

Bupropion sustained release is used to promote smoking cessation in males and nonpregnant females. However, its efficacy as a smoking cessation aid during pregnancy is not reported. The pregnancy-associated changes in maternal physiology may alter the pharmacokinetics and pharmacodynamics of bupropion and consequently its efficacy in pregnant smokers. Therefore, the aims of this study were to determine the steady-state pharmacokinetics of bupropion during pregnancy and the effect of functional genetic variants of CYP2B6 and CYP2C19 on bupropion pharmacokinetics in pregnant women. Plasma and urine concentrations of bupropion and its metabolites hydroxybupropion (OHBUP), threohydrobupropion, and erythrohydrobupropion were determined by liquid chromatography–mass spectrometry. Subjects were genotyped for five nonsynonymous single-nucleotide polymorphisms that result in seven CYP2B6 alleles, namely *2, *3, *4, *5, *6, *7, and *9, and for CYP2C19 variants *2, *3, and *17. The present study reports that the isoform-specific effect of pregnancy on bupropion-metabolizing enzymes along with the increase of renal elimination of the drug could collectively result in a slight decrease in exposure to bupropion in pregnancy. In contrast, pregnancy-induced increase in CYP2B6-catalyzed bupropion hydroxylation did not impact the plasma levels of OHBUP, probably due to a higher rate of OHBUP glucuronidation, and renal elimination associated with pregnancy. Therefore, exposure to OHBUP, a pharmacologically active metabolite of the bupropion, appears to be similar to that of the nonpregnant state. The predicted metabolic phenotypes of CYP2B6*6 and variant alleles of CYP2C19 in pregnancy are similar to those in the nonpregnant state.

Footnotes

    • Received May 12, 2016.
    • Accepted August 12, 2016.
  • ↵1 V.M.F. and M.X. contributed equally to the preparation of this manuscript.

  • This work was supported by National Institutes of Health National Institute on Drug Abuse [Grant RO1 DA030998] and Obstetric-Fetal Pharmacology Research Unit Network of National Institutes of Health National Institutes of Child Health and Human Development [Grant U10-HD47891].

  • The authors report no conflict of interest.

  • dx.doi.org/10.1124/dmd.116.071530.

  • ↵Embedded ImageThis article has supplemental material available at dmd.aspetjournals.org.

  • Copyright © 2016 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 44 (11)
Drug Metabolism and Disposition
Vol. 44, Issue 11
1 Nov 2016
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Research ArticleArticle

Pharmacokinetics of Bupropion in Pregnancy

Valentina M. Fokina, Meixiang Xu, Erik Rytting, Sherif Z. Abdel-Rahman, Holly West, Cheryl Oncken, Shannon M. Clark, Mahmoud S. Ahmed, Gary D.V. Hankins and Tatiana N. Nanovskaya
Drug Metabolism and Disposition November 1, 2016, 44 (11) 1832-1838; DOI: https://doi.org/10.1124/dmd.116.071530

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Research ArticleArticle

Pharmacokinetics of Bupropion in Pregnancy

Valentina M. Fokina, Meixiang Xu, Erik Rytting, Sherif Z. Abdel-Rahman, Holly West, Cheryl Oncken, Shannon M. Clark, Mahmoud S. Ahmed, Gary D.V. Hankins and Tatiana N. Nanovskaya
Drug Metabolism and Disposition November 1, 2016, 44 (11) 1832-1838; DOI: https://doi.org/10.1124/dmd.116.071530
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