Brintellix and Rexulti
Posted by Dr. Vollmer on September 18, 2013
“In vitro studies indicate that vortioxetine is a 5-HT3, 5-HT7, and 5-HT1D receptor antagonist, 5-HT1B receptor partial agonist, 5-HT1A receptor agonist and inhibitor of the serotonin (5-HT) transporter (SERT). In vivo non-clinical studies have demonstrated that vortioxetine enhances levels of the neurotransmitters serotonin, noradrenaline, dopamine, acetylcholine and histamine in specific areas of the brain.”
We need new modalities of treatment. We have SSRIs, SNRIs, which changed our game in 1988 dramatically, but since then, the rate of progress has slowed considerably. Now, we have deepened our field by understanding two new important aspects of serotonin functions. There are SEVEN serotonin (5-HT) receptors subtypes. http://en.wikipedia.org/wiki/5-HT_receptor. Second, as I posted about in 2010, there is a sertonin transporter, which can be altered leading to a change in the amount of serotonin floating around the receptors. This understanding opens the field to more targeted drugs. In October, 2013, the FDA will decide whether to approve Vortioxetine, likely to be called Brintellix or Rexulti, for the treatment of Major Depression. New drugs give hope to the many folks who feel despair with their symptoms, especially if they have tried multiple modalities, with little success. We, psychiatrists, call these folks “refractory,” but in fact, their persistent symptoms point to our limited tool box. Expanding our tools, of course, can also come with risk, but in the world of depression treatment, our pharmacological interventions have been exciting because the risk/benefit ratio is so favorable. In essence, the upside far outweighs the downside. This change in the risk/benefit ratio is how Prozac changed our world. Prozac did not bring about greater efficacy than our old tools of tricyclic antidepressants, but it did change this ratio to expand the number of people we could try to help. Further, Prozac also taught us that personality characteristics, such as impatience, could significantly improve with pharmacological intervention. So, we could treat more people, and we could treat folks who did not have a psychiatric illness, but who did suffer from irritability and then subsequent relationship issues. This Prozac story gives us hope with each new drug that our world can change again, in ways we do not even understand yet. Drugs come out on the market, and then we learn more about them through the individual tales of experience. Listening to how people experience their medication, to reference my last post, is a fun part of my job. I listen not only to how they experience the medication, but how they choose to tell me how they experience their medication. Having a new medication to use, creates the wonderful combination of excitement and fear, which with trust in the FDA, makes the fear tolerable, and the excitement grand. Sure, there is a lot of post-marketing learning, but the FDA gives us a safety net to explore the uses of new medication or new devices. It is interesting that each country has their own oversight organization, so one country might approve a medication, while another country waits for more data. I do not know what the FDA will do, but the data look promising that Brintellix (the likely name) will see the light of day, giving me a new tool. Once again, I feel appreciative for my medical background which gives me the privilege of using these tools. Once again, stay tuned.