Health Magazine

Kratom: Mitragynine For Beginners

By Dirkh @dirk57

An organic alternative to methadone? Kratom: Mitragynine For Beginners
A disclaimer: Everything I know about kratom, I learned on the Internet and in science journals. I have no real world experience with this opiate-like plant drug, haven’t used it, don’t know very many people who have. Although it comes from a tree indigenous to Thailand and Southeast Asia, and has presumably been around forever, a recent journal article referred to kratom as “an emerging botanical agent with stimulant, analgesic and opioid-like effects.” Which makes it sound like a combination of heroin, amphetamine, and strong weed. In reality, however, it is evidently a fairly mild stimulant with additional sedative effects when the leaf is chewed. If that sounds contradictory, it is, but the overall effect is reported to be more in league with coca leaves than injected morphine. Addictive? Erowid notes that the leaves can vary widely in potency, but yes, probably addictive at the level of coffee and coca leaves in its natural state.  So it’s not entirely surprising that kratom has been used in Asia, and increasingly in Europe and the U.S., as a self-managed treatment for pain and for opioid withdrawal. You can find kratom for sale all over the web. You will also find it in smoke shops and herbal outlets. But is any of it legal? And, as with methadone and buprenorphine: Is kratom part of the problem or part of the solution?
According to one web site maintained by kratom aficionados, the legality of kratom can be hard to determine. It is definitely illegal in Australia, Malaysia, Burma (Myanmar), and Thailand. However: “In the United States, access to county, state, and federal laws are often available online and it’s a simple matter of reading through the material (dense as it may be) to determine the actual legality of Mitragyna speciosa…. the only state where kratom is illegal in 2013 is Indiana. That’s not to say other state legislators haven’t tried to get kratom scheduled as an illicit substance. States to keep your eye on, especially if you’re a resident, are: Iowa, Hawaii, Vermont, Virginia, and Arizona. Louisiana hasn’t outright banned kratom, but they don’t allow it to be marketed as ‘for human consumption’ and thus we suggest, if you live in Louisiana, you exercise extra caution in your purchases.” In addition, you may rest assured that kratom is on the U.S. Drug Enforcement Administration (DEA) list of “Drugs and Chemicals of Concern.”
In other countries, kratom is controlled through licensing and prescription, similar in certain respects to the medical marijuana market in the United States. Nations in this category include Finland, Denmark, Romania, Germany, and New Zealand.
Kratom (Mitragyna speciosa) contains several psychoactive ingredients. The plant can be chewed, smoked, brewed into a tea—or made into an extract for sale as capsules or tablets (with accompanying arguments about “full-spectrum” extracts vs. “standardized” extracts).  According to Erowid, it is “unknown how long alkaloids retain their potency after being isolated from kratom leaves,” and furthermore, “many manufacturers are clearly exaggerating the potencies and quantities of whole leaf kratom used in their extracts.”
The leaves contain a plethora of psychoactive alkaloids, but the two primary stimulators of opioid receptors appear to be mitragynine and 7-hydroxymitragynine. These two compounds are considered to be stronger analgesics than euphorics, although users do sometimes report visual effects. Kratom is not considered toxic, but overdoses can be quite unpleasant, Erowid relates. Chronic heavy use reportedly leads to insomnia, dry mouth, constipation, and darkening of the skin.  Importantly, Erowid says they are “not aware of any cases of severe poisoning or death resulting from its use. Animal studies have found even very large doses of mitragynine (920 mg/kg) to be non-lethal.”
Last year, writer David DiSalvo, who blogs at Forbes, turned guinea pig, experimented with kratom, and blogged about the results. DiSalvo purchased an entirely legal supply of kratom—Lucky, Mayan, Nutmeg, and OnlineKratom by brand—and ran the self-experiment for a few weeks.
Here are excerpts from DiSalvo’s report: “My overall takeaway is that kratom has a two-tiered effect. Initially it provides a burst of energy very similar to a strong cup of coffee. Unlike coffee, however, the energy I derived from kratom was longer-lasting and level…. The second-tier effect was relaxing, but fell short of being sedating. I never felt sleepy while taking kratom, but I did experience a level relaxation that was pleasant, and balanced out the initial energy-boosting effects nicely.” Not surprisingly, DiSalvo’s major concern was that “it’s not easy to nail down the specific amount to take.” As for withdrawal, DiSalvo ranked it beneath caffeine withdrawal for severity.
“Having now experienced the product myself for a number of weeks,” he wrote “I can see no reason why it should be banned, or on what basis such a product would be banned if people can walk into a typical coffee shop and buy an enormous cup of an addictive substance that’s arguably more potent than any kratom available anywhere.”
In September, Larry Greenemeier examined the case for kratom legalization in an article for Scientific American that tracks the herb’s “strange journey from home-brewed stimulant to illegal painkiller to, possibly, a withdrawal-free treatment for opioid abuse.” Greenemeier interviewed Edward Boyer, director of medical toxicology at the University of Massachusetts Medical School, who first became familiar with kratom after a software engineer who had been using kratom tea for pain ended up at Massachusetts General Hospital after combining kratom with modafinil and suffering a seizure. (The case was reported in the June 2008 issue of Addiction).
According to Boyer, mitragynine “binds to the same mu-opioid receptor as morphine, which explains why it treats pain. It’s got kappa-opioid receptor activity as well, and it’s also got adrenergic activity so you stay alert throughout the day.” As if that weren’t enough, kratom also binds with serotonin receptors. “Some opioid medicinal chemists would suggest that kratom pharmacology might reduce cravings for opioids while at the same time providing pain relief. I don’t know how realistic that is in humans who take the drug, but that’s what some medicinal chemists would seem to suggest…. So if you want to treat depression, if you want to treat opioid pain, if you want to treat sleepiness, this compound really puts it all together.”
And again, unlike heroin and prescription painkillers, which can lead to respiratory difficulties and death, “in animal studies where rats were given mitragynine, those rats had no respiratory depression,” according to Boyer.
However, Boyer cautions that, like any other opioid, kratom has abuse liability. “Heroin was once marked as a therapeutic product and later was criminalized,” he reminds us. 
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