Buprenorphine, the Main Ingredient in Suboxone, Is a Great Pain Medication and a Powerful Antidepressant that Often Works Within One Week
It happened again. A patient’s account of how her medication made her feel made sense to me because of what I know about its pharmacology and a quick literature search confirmed that studies have proven exactly that.
“This patch works so much better than my oxys” , she said after her first week on the Butrans patch. And she added, “I feel better all over, my mood, my energy, my anxiety…I feel normal”.
I’ve heard these kinds of comments before, and I have sometimes been skeptical, thinking to myself doesn’t everybody feel better if they are slightly under the influence of something?
But this woman was on medication for depression, and one week after switching from oxycodone to the Butrans patch, she felt better than she had in a long time.
Oxycodone stimulates the opioid mu and kappa receptors, but buprenorphine stimulates the mu receptor and blocks the kappa receptor. It’s a little more nuanced than that, but that’s close enough for my day to day thinking. And if you stimulate the kappa receptor, you get tired and depressed.
Hearing her enthusiasm, I asked my young colleague, Dr. Google, to find me some articles on buprenorphine’s effect on depression. I found more support for its use than I had expected: It often reverses treatment resistant depression within a week, also in elderly patients, it often eliminates suicidal ideation just as quickly and it has been found to modulate emotional responses to emotional responses to angry facial expressions in humans and stressful laboratory conditions in rodents.
Sounds just as promising as ketamine, Spravato and mushrooms, doesn’t it? Here are some quotes:
(TRD = Treatment Resistant Depression, OUD = Opioid Use Disorder, MDD = Major Depressive Disorder)
Taken together, the studies discussed in this review tell a cohesive story: buprenorphine is an effective and safe antidepressant. Buprenorphine provides a unique antidepressant mechanism—opioid system modulation—which is a novel treatment option when used at low doses for many opioid-naïve individuals with TRD. At higher doses, buprenorphine can fulfill the dual role of staving off OUD symptoms and addressing MDD and pain which, given the high rate of comorbid MDD and OUD, are appealing properties for a therapeutic. Furthermore, buprenorphine has had success in diminishing suicidal ideation in both opioid-naïve and opioid-experienced groups.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9518754/
Buprenorphine (BPN) is an opioid drug with mixed pharmacology, approved by the US Food and Drug Administration for treatment of heroin dependence and chronic pain. Its most potent pharmacological actions are as a high-affinity partial agonist at the mu opioid receptor (MOR) and antagonist at the KOR. In addition, at higher concentrations, BPN is an antagonist at the delta opioid receptor (DOR) and a partial agonist at the opioid receptor-like 1 (ORL-1) receptor (Cowan, 2007; Lutfy and Cowan, 2004). In a handful of clinical studies, low doses of BPN produced impressive alleviation of depressive symptoms in patients that were considered treatment-resistant within 1 week of initiating administration (Bodkin et al, 1995; Nyhuis et al, 2008). Subsequently, a study with geriatric treatment-resistant MDD patients showed a significant mood-elevating effect of BPN after 1 week of treatment (Karp et al, 2014). Moreover, a recent study demonstrated significant antidepressant effects of ALKS5461, a combination of BPN and samidorphan, a MOR antagonist, following just 1 week of treatment in subjects with MDD (Ehrich et al, 2015). In addition, studies in healthy controls have shown that low doses of BPN can reduce the sensitivity to fearful facial expressions (Ipser et al, 2013) and enhanced the attention for more positive emotional cues (Syal et al, 2015), suggesting that BPN can modulate emotional valence in the absence of hedonic experiences.
https://www.nature.com/articles/npp201638