The Scientist speaks with a clinical toxicologist to discuss how Kratom acts in the brain and what the FDA’s declaration of Kratom being an “Opioid” mean for research.

11 February 2018
The Scientist speaks with a clinical toxicologist to discuss how Kratom acts in the brain and what the FDA’s declaration of Kratom being an “Opioid” mean for research.

On Tuesday February 6, Ironically also the anniversary of the late great Bob Marley who was so well known and loved for his never ceasing battle against the international war on Marijuana, the FDA announced a new WAR on another medicinal herb announcing that it now considers Kratom to be an Opioid. In an attempt to convince people not to use Kratom the FDA and their war on Kratom are painting the picture of Kratom of just being another but un-researched Opioid similar to Morphine and such like.

 Kratom Mitragyna speciosa

 “We feel confident in calling compounds found in kratom, opioids,” FDA Commissioner Scott Gottlieb declared in the statement. “And it’s an opioid that’s associated with novel risks because of the variability in how it’s being formulated, sold and used recreationally and by those who are seeking to self-medicate for pain or who use kratom to treat opioid withdrawal symptoms.”

A recent study in 2017  by clinical toxicologist Oliver Grundmann of the University of Florida co-authored an a research paper about the neuropharmacology of kratom and its potential for abuse. He spoke with The Scientist about Kratom and the FDA’s announcement. 

The Scientist asked Grundmann to explain how Kratom works pharmacologically and if the FDA’s claims of Kratom being an Opioid not safe for medicinal use. “At low concentrations, if you take it you get more of a stimulant effect; in higher concentrations you get more of an analgesic, opioid-like effect. So, there’s a dose-dependent distinction in its effects.

The likely opioid-like compounds, or the compounds that act on the opioid receptors, are mitragynine and 7-hydroxy mitragynine. These are the two that have been currently identified and where extensive research is available.

On the molecular level, what we know in terms of interaction with the different opioid receptors is that yes, they bind to the opioid receptor. But how they interact with the opioid receptor is distinctly different from classical opioids. If you look at morphine or at something like fentanyl what we usually look at when we classically look at opioid receptors, these are G-protein-coupled receptors, where basically the morphine or another binding agent binds from the outside to the receptor and then you have a kind of second-messenger cascade that happens inside the cell.

Kratom, specifically Mitragynine and its derivatives interacts with the opioid receptors distinctly differently from classical opioids.

Grundmann goes on to explain “Now, what we know about the opioid receptors. It is opioid receptors that also recruit beta-arrestin. It has been shown to be responsible for a lot of the negative effects, especially in regards to respiratory depression and potentially even in regards to the addictive symptoms that are associated with opioid use, misuse, leading to abuse. That is something that Mitragynine is not doing. Mitragynine does not recruit beta-arrestin.”

When asked if he agreed with the FDA’s classification of Kratom as an Opioid, Grundmann explains that “The science is on the same page in regards to mitragynine and 7-hydroxy mitragynine and thereby certain compounds in kratom act on opioid receptors. My concern is we’ve got roughly 5 million kratom users—roughly, it’s a very rough estimate. In my survey that was published in 2017 I showed that this is a distinctly different user population from what you would expect to find in opioid users.

I fear that by banning kratom, we are creating a significant issue by hindering research. I am a proponent of regulating kratom as limiting the excess, as controlling products that are entering the United States to ensure they show quality, that there is actually kratom inside when kratom is mentioned on the label. I support that health care providers should be serving as intermediaries to provide patients and consumers with advice on what they actually take.

But phasing it into Schedule 1 makes it very hard to further conduct research. And this is a new class of endo-alkaloids that act very distinctly different on opioid receptors. And just because the FDA hasn’t received an NDA [New Drug Application] or IND [Investigational New Drug application] to actually conduct a study with Mitragynine to move it into a clinical trial, which we know costs, millions of dollars, doesn’t mean that it doesn’t have value for these 4 or 5 million kratom users, who I feel would have to go back to using prescription opioids or potentially going to street drugs.


Source The Scientist


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