Bupropion (Wellbutrin®, Forvivo®, Zyban®, Aplenzin®)

Overview

Bupropion is an aminoketone antidepressant medication indicated for the treatment of major depressive disorder and to reduce withdrawal symptoms during smoking cessation. It potentiates norepinephrine and dopamine signaling in the CNS by inhibiting the presynaptic norepinephrine and dopamine transporters (NET and DAT, respectively).  Inhibition of neurotransmitter reuptake can improve mood in depressive conditions and may also produce a therapeutic stimulant effect in hyperactivity disorders.  Bupropion is thought to derive some of its efficacy with in smoking cessation from its antagonistic properties at CNS nicotinic cholinergic receptors.

Bupropion is FDA-approved for the treatment of major depressive disorder, seasonal affective disorder, and in medication-assisted smoking cessation.  It is also occasionally prescribed off-label for attention-deficit/hyperactivity disorder (ADHD).  Unlike most other antidepressants, bupropion is not associated with weight gain and may result in weight loss over several months of treatment.  Bupropion/naltrexone combination therapy is often prescribed in medication-assisted weight loss programs.

Bupropion should be prescribed with caution in some populations.  It should be avoided in anyone at elevated risk of experiencing seizures, including individuals with previously diagnosed seizure disorders, eating disorders, or patients who are likely to abruptly discontinue alcohol, benzodiazepine, barbituate, sedative, or antiepileptic medication use.  Bupropion, like other antidepressants, can increase risk of suicide in young patients (<24y), and also carries a small risk of inducing other neuropsychiatric events including psychosis and homicidal ideation.  The most common side effects are headache, nausea, GI distress, upper respiratory infections, agitation and insomnia.

Bupropion Hydrochloride (HCl) vs. Bupropion Hydrobromide (HBr) 

  • The different salt forms of bupropion appear to be pharmacologically and clinically identical
  • Bupropion HBr is not available in generic form and is thus much more expensive
  • The HBr (Aplenzin®) form has not been approved for the treatment of ADHD

In Plain English

Your brain relies on neurotransmitters to communicate messages between different parts of your body.  Low levels these neurotransmitters can lead to dysfunctional signaling in your brain, and can give rise to psychiatric conditions like depression. Bupropion alters the flow of neurotransmitters in your synapses and can decrease depressive symptoms.

Clinical Considerations

bupropion_hclFigure 1. Bupropion HCl clinical considerations at a glance. (MDD = Major Depressive Disorder, SAD = Seasonal Affective Disorder)

bupropion_hbr

Figure 2.  Bupropion HBr clinical considerations at a glance. (MDD = Major Depressive Disorder, SAD = Seasonal Affective Disorder)

Evidence Basis

Recent Bupropion Research

 

Citations

  1. Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M. DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2017 Nov 8. doi: 10.1093/nar/gkx1037
  2. Epocrates Rx Online [Internet database]. San Mateo (CA): Epocrates, Inc. 2003. Retrieved at mobile.epocrates.com. Web-based; continuous content updates. Accessed 2018 May 21.
  3. “Prescription Prices, Coupons & Pharmacy Information – GoodRx.” Prescription Prices, Coupons & Pharmacy Information – GoodRxhttp://www.goodrx.com
  4. “DailyMed.” U.S. National Library of Medicine, National Institutes of Health, dailymed.nlm.nih.gov/dailymed/.
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