A clinical review of bupropion and pain
P. Chue1, H. Shaltout1, E. Owusu1, J. Chue2, M. Tate2
1University of Alberta, Psychiatry, Edmonton, Canada, 2Amygdala Associates, Clinical Trials & Research Program, Edmonton, Canada
Background: Antidepressants have been demonstrated to have analgesic and anti-inflammatory activity in animal models and clinical settings. Analgesic effects appear to be independent of mood. While tricyclic antidepressants (TCAs) have been used historically off-label for neuropathic and fibromyalgia pain, the selective serotonin and norepinephrine reuptake inhibitors (SNRIs) duloxetine and milnacipran, and pregabalin have formal indications for the latter.
Bupropion is a norepinephrine and dopamine reuptake inhibitor (NDRI). The norepinephrine reuptake is mediated principally via its active metabolite, hydroxybupropion. It does not act on serotonin directly. It has been shown to have an anti-inflammatory effect and to decrease TNFα. It is also a noncompetitive nicotinic acetylcholine receptor antagonist. Bupropion is used in the treatment of depression including seasonal depression and smoking cessation. It is generally regarded as an activating antidpressant and is also used in combination with other antidepressants to mitigate side effects such as sedation, weight gain or sexual dysfunction.
Bupropion is a norepinephrine and dopamine reuptake inhibitor (NDRI). The norepinephrine reuptake is mediated principally via its active metabolite, hydroxybupropion. It does not act on serotonin directly. It has been shown to have an anti-inflammatory effect and to decrease TNFα. It is also a noncompetitive nicotinic acetylcholine receptor antagonist. Bupropion is used in the treatment of depression including seasonal depression and smoking cessation. It is generally regarded as an activating antidpressant and is also used in combination with other antidepressants to mitigate side effects such as sedation, weight gain or sexual dysfunction.
Aims & Objectives: To evaluate bupropion’s role in the treatment of pain and discuss in the context of our clinical experience.
Method: An initial literature search using the terms “bupropion”, “pain”, “neuropathic pain” and “fibromyalgia” was conducted.
Results: Anti-nociceptive and anti-inflammatory effects are demonstrated in animal models, postulated to be mediated via central and peripheral mechanisms. Clinical studies show benefit in neuropathic but not in non-neuropathic pain conditions. There are very limited data for fibromyalgia with a positive case report but no clinical trials.
Discussion & Conclusions: This review of the literature coupled with our clinical experience suggests that bupropion may be an agent to consider in the management of neuropathic and fibromyalgia-related pain symptoms, particularly when accompanied by low energy and depressed mood.
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