Pharmacokinetics of Bupropion and Its Pharmacologically Active Metabolites in Pregnancy

Fokina, Valentina M.; Xu, Meixiang; Rytting, Erik; Abdel‐Rahman, Sherif Z.; West, Holly; Oncken, Cheryl; Clark, Shannon; Ahmed, Mahmoud S.; Hankins, Gary D.V.; Nanovskaya, Tatiana

doi:10.1124/dmd.116.071530

Cited by 18 publications

(27 citation statements)

References 37 publications

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“…17,18 Cotinine in urine was quantified using the validated liquid chromatography-mass spectrometry (LC/MS) method; 19,20 sample extraction was based on the procedure described by Peterson et al 21 Patients’ compliance to study medication was confirmed by concentrations of bupropion in urine and its metabolites (hydroxybupropion [OHBUP] and threohydrobupropion [TB]) using the method reported previously. 22,23 …”

Section: Methodsmentioning

confidence: 99%

Bupropion sustained release for pregnant smokers: a randomized, placebo-controlled trial

Nanovskaya

Oncken

Fokina

et al. 2017

American Journal of Obstetrics and Gynecology

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Background Bupropion is used to treat depression during pregnancy. However, its usefulness as a smoking cessation aid for pregnant women is not fully known. Objective To evaluate the preliminary efficacy of bupropion sustained-release for smoking cessation during pregnancy. Study design We conducted a randomized, prospective, double-blind, placebo-controlled, pilot trial. Pregnant women who smoked daily received individualized behavior counseling and were randomly assigned to a 12-week, twice-a-day treatment with 150 mg bupropion sustained-release or placebo. The primary study objectives were to 1) determine whether bupropion sustained-release reduces nicotine withdrawal symptoms on the quit date and during treatment period compared to placebo; and 2) whether it increases 7-day point prevalence abstinence at the end of treatment period and at the end of pregnancy. Results Subjects in the bupropion (n = 30) and placebo (n = 35) groups were comparable in age, smoking history, number of daily smoked cigarettes, and nicotine dependence. After controlling for maternal age and race, bupropion sustained-release reduced cigarette cravings (1.5 ± 1.1 vs 2.1 ± 1.2, P = 0.02) and total nicotine withdrawal symptoms (3.8 ± 4.3 vs 5.4 ± 5.1, P = 0.028) during the treatment period. Administration of bupropion sustained-release reduced tobacco exposure, as determined by levels of carbon monoxide in exhaled air (7.4 ± 6.4 vs 9.1 ± 5.8, P = 0.053) and concentrations of cotinine in urine (348 ± 384 ng/mL vs 831 ± 727 ng/mL, P = 0.007), and increased overall abstinence rates during treatment (19% vs 2%, P = 0.003). However, there was no significant difference in 7-day point prevalence abstinence rates between the two groups at the end of medication treatment (17% vs 3%, P = 0.087) and at the end of pregnancy (10% vs 3%, P = 0.328). Conclusion Individual smoking cessation counseling along with the twice-daily use of 150 mg bupropion sustained-release increased smoking cessation rates and reduced cravings and total nicotine withdrawal symptoms during the treatment period. However, there was no significant difference in abstinence rates between groups at the end of medication treatment and at end of pregnancy, likely due to the small sample size. A larger study is needed to confirm these findings and to examine the potential benefit/ risk ratio of bupropion sustained-release for smoking cessation during pregnancy.

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Section: Methodsmentioning

confidence: 99%

Bupropion sustained release for pregnant smokers: a randomized, placebo-controlled trial

Nanovskaya

Oncken

Fokina

et al. 2017

American Journal of Obstetrics and Gynecology

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“…While bupropion avoids fetal exposure to nicotine, there are limited data on effects to the fetus. Current research indicates that pregnant women metabolize bupropion similarly to nonpregnant women, with bupropion and its active metabolites found in umbilical venous plasma at concentrations lower than maternal plasma concentrations . Although overall data from available research on bupropion have not demonstrated any major teratogenic effects, a National Birth Defects Prevention study noted an association of a small absolute risk of left outflow tract heart defects (N = 10; adjusted OR, 2.6; 95% CI, 1.2‐5.7) .…”

Section: Tobacco Cessation Pharmacotherapy During Pregnancymentioning

confidence: 99%

Tobacco Harms, Nicotine Pharmacology, and Pharmacologic Tobacco Cessation Interventions for Women

Baraona¹,

Lovelace²,

Daniels³

et al. 2017

J Midwife Womens Health

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Firsthand and secondhand tobacco use is linked to a multitude of harmful illnesses, adverse perinatal outcomes, and death. Cessation attempts among women may be hampered by their unique biologic response to nicotine. Current research has revealed epigenetic changes from intrauterine nicotine exposure that have intergenerational consequences. Multiple studies have demonstrated the efficacy of various pharmacologic tobacco cessation interventions in conjunction with behavioral counseling. Based on this evidence, the US Preventative Services Task Force (USPSTF) 2015 guideline recommends pharmacologic therapy for all nonpregnant persons who smoke in addition to behavioral counseling. The effectiveness of pharmacologic treatments among pregnant women is less clear, with far fewer studies evaluating potential benefits and harms. While exposure to pharmacologic therapies raises concerns for fetal safety, these potential risks must be weighed against those of continued tobacco use, which guarantees fetal exposure to nicotine. First-line tobacco cessation medications include nicotine replacement therapy (NRT), bupropion, and varenicline. Second-line medications include nortriptyline and clonidine. Pharmacokinetics, effectiveness, regimens, and safety profiles for nonpregnant, pregnant, and lactating women are reviewed. Alternative tobacco cessation options and potential new pharmacologic tobacco cessation agents are discussed. Initiating brief interventions, using the 5A's and 5R's model is described.

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“…Os níveis de bupropiona e de vareniclina não são alterados durante a gravidez 2,17 . Em um artigo publicado por Bérard et al …”

Section: Intervenções Comportamentaisunclassified

Tabagismo e gravidez

Cavalsan¹,

Rennó²,

Rocha³

et al. 2017

Debates em Psiquiatria

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-revista debates em psiquiatria ResumoOs dados da literatura são unânimes em confirmar os malefícios do fumo na população geral e, sobretudo, em gestantes. Fumo na gestação é preditor para resultados adversos no nascimento, como nascimento prematuro e baixo peso ao nascer, bem como para maior mortalidade fetal e infantil. A abstinência do cigarro sempre deve ser estimulada em gestantes. Para maior sucesso do tratamento, devem-se considerar as vulnerabilidades sociais, as doenças associadas (principalmente depressão e ansiedade), o nível de maturidade emocional, o desejo pela gestação e as incertezas sobre o futuro. O objetivo deste artigo é identificar as gestantes que estão mais propensas a permanecer fumando durante a gestação, orientar sobre a abordagem médica, avaliando se há tratamentos seguros durante a gravidez e qual a melhor modalidade terapêutica a ser oferecida. Atualmente, a terapia comportamental, em especial a terapia cognitiva comportamental, é o melhor tratamento para a abstinência do cigarro, para pacientes gestantes ou não. Em caso de dependência grave de nicotina, é necessária a introdução de medicações. A medicação mais usada é a bupropiona, apesar de os estudos ainda não garantirem a sua segurança em relação ao feto. Na prática, não se observam complicações nas gestantes e nos fetos.Palavras-chave: Gestação, fumo, tratamento. AbstractThe literature is consistent in confirming the harmful effects of smoking in the general population and especially in pregnant women. Smoking during pregnancy is a predictor of adverse birth outcomes, such as preterm birth and low birth weight, as well as of increased fetal and infant mortality. Smoking cessation should always be stimulated in pregnant women. To increase treatment success, it is important to consider social vulnerabilities, associated diseases (especially depression and anxiety), emotional maturity, whether or not the pregnancy was desired, and uncertainties about the future. The objectives of this article were to identify the pregnant women who are more vulnerable to continue smoking during pregnancy, to provide guidance on the management of these cases, evaluating the availability of treatments that can be used safely during pregnancy, and to identify the best treatment to offer to these women. Currently, behavioral therapy, especially cognitive behavioral therapy, is the best treatment available for smoking cessation, both for pregnant women and in general. Severe nicotine dependence may require pharmacotherapy. In these cases, the medication most commonly used is bupropion, despite the lack of evidence regarding its safety for the fetus. In clinical practice, no complications for the fetus or for the pregnant women have been reported.

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Pharmacokinetics of Bupropion and Its Pharmacologically Active Metabolites in Pregnancy

Cited by 18 publications

References 37 publications

Bupropion sustained release for pregnant smokers: a randomized, placebo-controlled trial

Bupropion sustained release for pregnant smokers: a randomized, placebo-controlled trial

Tobacco Harms, Nicotine Pharmacology, and Pharmacologic Tobacco Cessation Interventions for Women

Tabagismo e gravidez

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