Review of the pharmacology and clinical profile of bupropion, an antidepressant and tobacco use cessation agent

Dwoskin, Linda P.; Rauhut, Anthony S.; King‐Pospisil, Kelley A.; Bardo, Michael T.

doi:10.1111/j.1527-3458.2006.00178.x

Cited by 259Smoking Behavior and CessationTreatment of Major DepressionNeurotransmitter Receptor Influence on Behavior

Review of the pharmacology and clinical profile of bupropion, an antidepressant and tobacco use cessation agent

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Dwoskin, Linda P., Rauhut, Anthony S., King‐Pospisil, Kelley A., Bardo, Michael T.·2006·CNS Drug Reviews

DOI 10.1111/j.1527-3458.2006.00178.xPMC PMC6506196

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Abstract

Bupropion hydrochloride ((+/-)-2-tert-butylamino)-3'-chloropropiophenone x HCl) is a nonselective inhibitor of the dopamine transporter (DAT) and the norepinephrine transporter (NET) and is also an antagonist at neuronal nicotinic acetylcholine receptors (nAChRs). In animal models used commonly to screen for antidepressant activity, bupropion shows a positive response. Also using animal models, bupropion has been shown to attenuate nicotine-induced unconditioned behaviors, to share or enhance discriminative stimulus properties of nicotine and to have a complex effect on nicotine self-administration, i.e., low doses augmenting nicotine self-administration and high doses attenuating self-administration. Current studies show that bupropion facilitates the acquisition of nicotine conditioned place preference in rats, further suggesting that bupropion enhances the rewarding properties of nicotine. Bupropion has been shown to attenuate the expression of nicotine withdrawal symptoms in both animal models and human subjects. With respect to relapse, current studies show that bupropion attenuates nicotine-induced reinstatement in rats, but large individual differences are apparent. Clinically, bupropion is used as a treatment for two indications, as an antidepressant, the indication for which it was developed, and as a tobacco use cessation agent. In clinical trials, bupropion is being tested as a candidate treatment for psychostimulant drug abuse, attention-deficit hyperactivity disorder (ADHD) and obesity. Bupropion is available in three bioequivalent oral formulations, immediate release (IR), sustained release (SR), and extended release (XL). Extensive hepatic metabolism of bupropion produces three pharmacologically active metabolites, which may contribute to its clinical profile.

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Bupropion is prescribed as both an antidepressant and as an aid to smoking cessation.
“The most striking connection between smoking and depression is the norepinephrine-dopamine reuptake inhibitor bupropion, which is prescribed as both an antidepressant and as an aid to smoking cessation (Dwoskin et al., 2006; Hayford et al., 1999).”
From It is not “either/or”: Activation and desensitization of nicotinic acetylcholine receptors both contribute to behaviors related to nicotine addiction and mood (2008) · cites this paper as Dwoskin et al., 2006
Bupropion is a non-competitive antagonist of nAChRs.
“bupropion, while having effects on monoamine transporters, has also been shown to be a non-competitive antagonist of nAChRs (Dwoskin et al., 2006).”
From It is not “either/or”: Activation and desensitization of nicotinic acetylcholine receptors both contribute to behaviors related to nicotine addiction and mood (2008) · cites this paper as Dwoskin et al., 2006
Both bupropion and nicotine increase catecholamine concentrations in midbrain limbic regions.
“both increase catecholamine concentrations in midbrain limbic regions [214, 227].”
From Mechanistic insights into nicotine withdrawal (2011) · cites this paper as [214]

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Authors: Dwoskin, L. P., Rauhut, A. S., King‐Pospisil, K. A., & Bardo, M. T.
Affiliations: University of Kentucky (US)
Dickinson College (US)
Corresponding author: Dwoskin, Linda P.
ORCID: Rauhut, Anthony S.
Bardo, Michael T.
Venue: CNS Drug Reviews
Publisher: Wiley
Published: 2006-09
Volume: 12
Issue: 3-4
Pages: 178-207
ISSN: 1080-563X (ISSN-L)
1527-3458
DOI: 10.1111/j.1527-3458.2006.00178.x
PMC: PMC6506196
OpenAlex: W2067382805
Cited by: 259
References: 207
Citations by year: 2026: 8 · 2025: 9 · 2024: 5 · 2023: 2 · 2022: 12 · 2021: 14 · 2020: 12 · 2019: 10 · 2018: 13 · 2017: 12 · 2016: 21 · 2015: 11 · 2014: 22 · 2013: 18 · 2012: 13
FWCI: 1.71
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: onlinelibrary.wiley.com/termsAndConditions#vor (vor, 132 d)
Locations: CNS Drug Reviews (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Funders: National Institutes of Health (DA07304, DA-05312)
National Institute on Drug Abuse (DA 017548, DA 07304, DA018372, U19DA017548, DA05312, R21DA018372)
National Institute of Environmental Health Sciences (T32ES007266, ES 07266)
Topics: Health Sciences › Medicine › Physiology › Smoking Behavior and Cessation
Health Sciences › Medicine › Pharmacology › Treatment of Major Depression
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
Keywords: bupropion, antidepressants, tobacco cessation, nicotine self-administration, nicotine withdrawal, dopamine transporter inhibition, norepinephrine reuptake inhibition, nicotinic acetylcholine receptor antagonism, attention deficit hyperactivity disorder, obesity, hepatic metabolism, pharmacokinetics, sustained-release formulation
MeSH terms: Animals, Humans, Tobacco Use Disorder, Bupropion, Antidepressive Agents, Second-Generation, Tobacco Use Cessation

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Review of the pharmacology and clinical profile of bupropion, an antidepressant and tobacco use cessation agent

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