Updated with June 2018 Research added to the end of this article.
Dangers of Synthetic Opioids
In 2015, the American Society of Addiction Medicine (ASAM) reported that individuals overdosing from prescription pain relievers like fentanyl, oxycodone, and hydrocodone accounted for 20,101 deaths during the year of 2015. This incredible statistic sheds light on how dangerous synthetic opioids truly are. In fact, in a 2014 survey released by JAMA Psychiatry, it was found that “94 percent of respondents… in treatment for opioid addiction said they chose to use heroin." As you can see, long-term synthetic opioid use can be very dangerous and even fatal. However, those that suffer from chronic pain, depression, anxiety, and fatigue could potentially benefit significantly from opioids. To get the benefits and prevent the risk from synthetic opioids, look to kratom, nature's alternative to synthetic opioids.
What is Addiction?
The dangers of synthetic opioids come from their very addictive nature. What is addiction? According to ASAM, "addiction is characterized by the inability to consistently abstain, impairment in behavioral control, craving, diminished recognition of significant problems with one’s behaviors and interpersonal relationships, and a dysfunctional emotional response. Addiction is caused by a chronic disease of brain reward, motivation, memory and related circuitry. Addiction affects neurotransmission and interactions within reward structures of the brain."
Synthetic opioids are addictive because of their destructive influence on the brain's reward system. A properly functioning reward system motivates a person to repeat behaviors needed to thrive, such as eating and spending time with loved ones. This happens through the release of dopamine. Dopamine is a neurotransmitter present in regions of the brain that regulate movement, emotion, cognition, motivation, and feelings of pleasure. Synthetic opioids overstimulate the reward system and floods the system with dopamine producing euphoric effects and desires for more opioids which can lead to addiction.
Dangers of Tolerance Build-Up
One of the ways our system tries to prevent our receptors from being overly activated by chemicals like synthetic opioids is by releasing arrestins. Arrestins are proteins that bind to receptors to help prevent other chemicals from attaching to the receptor and activating them. They are like plugs in a hole. Synthetic opiods recruit beta arrestins which reduces their ability to fire the receptor. The issue is individuals who previously used synthetic opioids desire the same euphoria and reward but cannot get it because of the build up of beta arrestins. They now have to increase their dosage to override the arrestins. This is what we call drug tolerance.
This is very dangerous because the higher use of synthetic opioids increases the effects of respiratory depression. In other words, the more synthetic opioids you use, the higher chance you can stop breathing. This is the leading cause of death from synthetic opioids.
All-Natural Bio-Active Alkaloids
Unlike synthetic opioids, kratom is a plant that receives its incredible benefits from several bio-active alkaloids. Bio-active alkaloids are nitrogenous organic compounds originating in plants that have pronounced physiological actions on humans. Laboratory research has been able to identify 28 different alkaloids within the kratom plant.
The most plentiful active alkaloid is mitragynine (up to 66% of the total alkaloid content). Mitragynine is a partial opioid-receptor agonist. An agonist is a chemical that binds to a receptor to activate it. In this case, mitragynine is a partial agonist to the µ-opioid (Mu) receptor which produces analgesic properties also known as pain relief. This is one of the main reasons people experience significant pain relief with kratom. There are many other active alkaloids within kratom such as 7-hydroxymitragynine, ajmalicine, and paynantheine. These alkaloids are being researched for their role in relieving pain, increasing blood flow, improving oxygen to the brain for cerebral health, inflammation reduction, muscle relaxation and relief for mood disorders like depression and anxiety.
Kratom v. Synthetic Opioids
If kratom is an opioid, how is it different from synthetic opioids? The answer can be found in the chemistry and science. There are three opioid receptors that manage pain: µ (Mu), δ (Delta), and κ (Kappa) opioid receptors. Synthetic opioids are agonist on all three receptors which means they activate them all. When all three are activated, dopamine is released creating euphoria reinforcing the need for more of the chemical that activated the receptors. This increase in dopamine and euphoria creates addiction.
Kratom is different in that it's main alkaloid, mitragynine, is only a partial agonist on the Mu receptor. This means that mitragynine activates the receptor to create analgesic effects or pain relief but does not aggressively bind to the receptor. Also, mitragynine is an antagonist to the Delta and Kappa receptors which means it blocks those receptors. The Kappa receptor manages dopamine and serotonin. Mitragynine's ability to block the Kappa receptor is limiting the chemical reward for using kratom thus preventing addiction. The Delta receptor rewards the use of the Mu receptor so, again, blocking it prevents dopamine and serotonin from flooding your system.
Another way kratom is different from synthetic opioids is the way they impact tolerance buildup. Synthetic opioids recruit beta arrestins to the opioid receptors making it harder and harder for them to be activated unless more of the drug is used. The two main analgesic alkaloids in kratom, mitragynine and 7-hydroxymitragynine do NOT recruit beta arrestins. This means the same amount of kratom can be used with similar effects over time. The issue of tolerance buildup you find with synthetic opioids is not an issue with kratom.
Is there an amount of kratom you can use where the reward system is activated and chemical reinforcement happens in the brain? Yes. According to Pinney Associates' Assessment of Kratom under the CSA Eight Factors and Scheduling Recommendation study, "a human would need to consume over 1,200 grams of kratom leaves (or extract) to obtain a reinforcing effect. Although kratom leaves also contain smaller quantities of other alkaloids including 7OH-MG, which is more potent at the Mu opioid receptor, very large quantities of kratom would have to be consumed to even see the levels of withdrawal seen in rats in this study." In other words, addiction and withdraw commonly associated with synthetic opioids are not issues found with kratom use.
What makes kratom so special is that its potential to be abused is relatively low, if not non-existent. Users that take too much kratom often experience diminishing returns after exceeding a certain dosage threshold. In fact, taking too much kratom can lead to temporary nausea, irritability, and sometimes dysphoria. For this reason, there is little reward for purposefully choosing to take more kratom than what is advisable.
Is Kratom Addictive?
So, is kratom addictive? From a scientific standpoint, the answer is 'no.' The way kratom's main bio-active alkaloids interact with opioid receptors without significantly releasing dopamine and serotonin, limit the recruitment of beta arrestins preventing tolerance buildup, and has diminishing returns with heavier use, makes the likelihood of kratom abuse next to non-existent. What can be reinforcing and result in more long-term use is the potential for improvements in health and general well-being. Those are good reason to continue to use kratom even when you are not chemically addicted to it.
As always, Etha™ encourages you to do your research, connect with other people with experience with natural medicines, and be informed about your health. Live Fully!
Update: June 2018 Research with Dr. Hemby
Kratom is different in its origin, chemistry, biological effects. Kratom does not show the toxicity, does not show the respiratory depression issues, and as commonly used in raw natural plant form, does not produce hyper pleasurable euphoric effects that lead to abuse and addiction. (Hemby June 2018)
“This is an important study that addresses the addictiveness of kratom,” says Jack E. Henningfield, Ph.D., at Pinney Associates, a health consulting firm. “It shows that the major naturally occurring constituent responsible for the health-related effects of kratom, mitragynine, is of very low abuse potential. A second substance, 7-HMG, which naturally occurs at such low levels in kratom that it might be of minimal health consequence, has higher abuse potential. This has at least two regulatory implications. First, the findings do not support the FDA’s claim that kratom is a narcotic-like opioid. Second, in regulating kratom products, the FDA could set standards to ensure that no kratom product contain levels of 7-HMG exceeding those that are commonly present in kratom leaves and products.”