A Review of the Neuropharmacology of Bupropion, a Dual Norepinephrine and Dopamine Reuptake Inhibitor
Prim Care Companion J Clin Psychiatry 2004;6(4):159-166
© Copyright 2015 Physicians Postgraduate Press, Inc.
Background: The neurochemical and biological
effects of antidepressant medications have become better defined
over the last decade. When the antidepressant bupropion was
introduced in the United States in 1989, the specific
pharmacologic basis of its clinical effects was uncertain.
Research conducted over the past decade has significantly
advanced the understanding of the neuropharmacology of bupropion
and has demonstrated a novel mechanism of antidepressant
activity. This article discusses the mechanism of action of
bupropion and relates the drug's neuropharmacologic effects to
its clinical efficacy and tolerability profiles.
Data Sources: Data were obtained via the MEDLINE
database in an English-language search spanning the period 1965
to May 2002 and using the search terms bupropion, bupropion
SR, and antidepressants, as well as from the
manufacturer's bupropion databases.
Conclusions: The preclinical and clinical data
show that bupropion acts via dual inhibition of norepinephrine
and dopamine reuptake and is devoid of clinically significant
serotonergic effects or direct effects on postsynaptic receptors.
Dual norepinephrine and dopamine reuptake inhibition is
associated with a unique clinical profile. Bupropion has
demonstrated efficacy comparable to that of other
antidepressants. However, because bupropion is a selective
norepinephrine and dopamine reuptake inhibitor with no
serotonergic activity, common antidepressant-associated side
effects, such as sexual dysfunction, weight gain, and sedation,
are not associated with bupropion therapy.