Drug intelligence / Profile preview

bupropion

Development stage
Approved
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Bupropion is an antidepressant medication primarily indicated for the treatment of major depressive disorder (MDD), seasonal affective disorder (SAD), and as an aid to smoking cessation. It is also used off-label for attention deficit hyperactivity disorder (ADHD) and weight management when combined with naltrexone. Bupropion acts as a norepinephrine-dopamine reuptake inhibitor (NDRI), weakly inhibiting the reuptake of norepinephrine and dopamine by binding to their respective transporters—norepinephrine transporter (NET) and dopamine transporter (DAT)—thereby increasing their synaptic concentrations. Additionally, bupropion functions as a nicotinic acetylcholine receptor antagonist. Unlike many other antidepressants, it does not significantly affect serotonin receptors or other neurotransmitter systems[2][5][6][8]. The drug was originally developed by Burroughs Wellcome Company.

Brand names
WellbutrinWellbutrin SRWellbutrin XLZybanAplenzinBudeprion XLForfivo XL
Other names
bupropion SRbupropion hydrochloride sustained-releasebupropion HCl SR
02

Targets

DAT (Dopamine plasma membrane transport protein)NET (Norepinephrine Transporter)

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