Why kratom is NOT an opioid.

05 November 2018
Why kratom is NOT an opioid.

Kratom (mitragyna speciosa) is part of the coffee family, but has a very different chemistry than coffee beans. It’s been used in traditional medicine in Thailand and Malaysia for centuries, both as an energy booster and opium substitute. The plant contains a number of alkaloids, a primary one being mitragynine, which has opioid activity.

It and many other alkaloids in the kratom plant were recently called out as opioids by the Food and Drug Administration (FDA) commissioner. “A lot of people were upset about that at first, but I think they need to understand that an opioid is any molecule that can interact with opioid receptors or those proteins in the body,” McCurdy says.

In other words, an opioid is not identical to an opiate, derived from opium poppy, such as morphine, oxycodone or oxymorphone. Opioid is a generic term that includes even endogenous endorphins that bind to opioid receptors in your body. And, while mitragynine has opioid activity, it’s very different from other opioid molecules.

McCurdy’s research shows that compared to methadone and buprenorphine (two drugs used to treat opioid addiction and opioid withdrawal), kratom had a much cleaner profile and was milder in its action. Whereas buprenorphine and methadone are full agonists or activators of opioid receptors, mitragynine appears to be only a partial agonist. McCurdy explains:

“We initially sent out purified alkaloid of mitragynine for a screen across a whole panel of central nervous system drug targets … What we found was a really remarkable profile of this molecule. Mitragynine binds with opioid receptors … but it also interacts with adrenergic receptors, serotonin receptors, dopamine receptors and adenosine receptors.Adenosine receptors are the target for caffeine. It kind of explains why some of these alkaloids in the plant might cause this stimulant-like effect. It also interacts with alpha-2 adrenergic receptors, [which] are … used in opioid withdrawal. Agents that activate alpha-2 receptors, like clonidine, are used in opioid withdrawal treatment to stop withdrawal symptoms such as shaking, sweating and heart racing …In all honesty, when I got the report back from the company that screened the molecule, I thought, ‘Wow. We just found nature’s answer to opiate addiction’ because here it was interacting with many of the same targets that we would target pharmacologically on an individual basis.”

How Kratom Curbs Opiate Addiction

As explained by McCurdy, there are three traditional opioid receptors: mu, delta, and kappa, all three of which are associated with numbing or dulling pain. In other words, they’re analgesic receptors. They block or slow pain signal transmissions at the spinal cord level, so your brain doesn’t process the pain signals as much.The Mu receptor was named for its ability to interact with morphine. The mu receptor is responsible for the euphoric effects associated with opiates. It’s also primarily responsible for respiratory depression.The delta receptor is also a target for selective analgesics and does not appear to have as strongly addictive capabilities as the mu receptor. Unfortunately, the delta receptor is linked to convulsions, and many drug trials aimed at the delta-selective opioid receptor had to be halted due to seizures that could not be resolved. Kratom does not appear to significantly interact with delta receptors.The kappa receptor, while good for killing pain, causes dysphoria or aversion, meaning when you take a compound that activates kappa, it makes you feel so awful you don’t want to take it again. For this reason, kappa-activating pain drugs have repeatedly failed in clinical trials and people don’t want to continue the drug.Kratom appears to be a partial agonist for all of these receptors, only weakly affecting delta and kappa. And, while the mu receptor is the primary target of kratom, animal trials suggest the abuse potential of kratom is quite low. To learn more, see “Kratom as an Alternative for Opium Withdrawal” or listen to McCurdy’s interview.

 

Article written by Kelly Devine Veterans Care Alliance Botanicals KratomUnited.

 



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