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DISCLAIMER: The following article addresses a plant which is a powerful drug. Just because it’s natural and legal (for now) do not write it off as herbal-ecstasy crap or take it lightly if you decide to take it at all. I do not condone the use of this or any drugs by anyone under 18 or anyone under 180lbs for that matter. In fact, drugs are bad, you shouldn’t do drugs, mmmmmmK?

In mankind’s never-ending quest to gain an edge over genetic limitations, feelings of discontent, and/or other members of the species, we often turn to doctors and their prescription pads to fill our medicine cabinets and ease our minds. Despite the massive pharmaceutical machine dominating modern medicine, Mother Nature is still a source and inspiration for modern medicines. Synthetic versions of human hormones are perhaps the best example for Mind & Muscle readers. Another excellent example is seen in the Opium Poppy and the dozens of natural and synthetic drugs that have been derived from it. However, unlike hormones and opiates, one very versatile source of pharmacologically active alkaloids, capable of producing three distinctly different effects, has flown under the radar (at least in our neck of the woods). Native to Thailand and Malaysia (and illegal in both countries as well as Australia), the leaves of the Kratom tree (Mitragyna speciosa) may be as close as modern medicine will get to the fabled panacea of patent-medicine days. The claims made on antique medicine bottles from the late nineteenth century, once laughable, may soon be laudable, and true.

Though heed this warning before reading on: Kratom is one plant that we do not want to see go the way of ephedra, GHB, and PH/PS supplements. Myself and other ethno-botanists envision fears of unethical chemists synthesizing 99% pure Mitragynine (Kratom’s major alkaloid) or other analogues; spawning a new generation of junkies free-basing and mainlining what could improve the quality of life for millions of people. Actually, we fear the pharmaceutical industry using their foot-soldier-senators along with the FDA will put the above scenario into the minds of millions of Americans. So please, for the love of mankind, for the love of what freedoms we have left, let’s not ruin this one too.

Pharmacology

Kratom contains over twenty different active alkaloids, the major one being the indole-alkaloid Mitragynine.1 Other alkaloids vary depending on the age and geographic origin of the plant. Specifically, studies of Kratom’s constituents has led to the isolation of several “9-methoxy-Corynanthe-type monoterpenoid indole alkaloids.”1 Although the analgesic effects of Mitragynine resemble that of morphine (Mitragynine is approximately ¼ the potency of morphine1), structurally the alkaloids are similar to those found in the yohimbe tree (Corynanthe yohimbe). In fact, over twenty Corynanthe-type Oxyindole alkaloids have been found in Kratom leaves, explaining its differing effects at different doses. Yet why would alkaloids with stimulant, appetite suppressant, and vasodilating properties completely change their in vivo effects with larger doses, and activate kappa, delta, and mu opiate receptors?

The answer is pretty involved. Anyone who has experimented with various opiates knows that some knock you out (morphine, codeine), while others get you wired (hydrocodone, Buprenex, oxycodone). Even these effects differ from person to person. The effects of Mitragynine and several of its derivatives were completely reversed by the opiate antagonist naloxone,1 proving Mitragynine to be a potent opiate receptor agonist, though it’s not technically even an opiate.

Bodybuilding Applications & Dosages

For legal reasons, this section will be limited. I am not a doctor, and even if I were, I cannot claim “if you take X amount of Kratom, Y will happen” without breaking any laws. That being said, as far as know (and I spent quite a bit of time looking) there are no laws against purchasing or selling Kratom for human consumption in the United States (there is conflicting information on this). However, like many other legal botanicals, it is not listed on the FDA’s GRAS list. There are currently five basic preparations of Kratom available on the Internet. The first, and cheapest, is crushed, dried leaf which contains ~2.5mg/g. of alkaloids. The second, resins, can vary drastically; not just in alkaloid concentration, but in alkaloid content as well. The reason being that some alkaloids are water soluble, while others are soluble in alcohol, and still others in acetic acid (yes, vinegar).

Resins are by far the easiest way to consume the herb, as they can be heated, rolled into different size balls, and swallowed. However, caution must be used as resins vary drastically between suppliers and even batches. Different vendors use different techniques to extract the resin. Some unscrupulous vendors even combine other plants into their resins to bring the prices down. Ironically though, the resin I found to be the most potent is also the least expensive.

Different retailers refer to different strength preparations by various names, so to maintain objectivity rather than advocate one retailer, I will refer to the different grades of powdered Kratom as: premium (~7mg/g.), enhanced premium (~12mg/g.) and super-enhanced, which can range from ~15-20mg/g. of Mitragynine. The latter two simply infuse Kratom Resin over the leaf to jack-up the alkaloid content. For safety’s sake, your best bet is to find one retailer you like and stick to them. And, the biggest retailer is not necessarily the best when it comes to Kratom.

There are three distinct dosing levels for Kratom: a light dose acts as a stimulant, both mentally and physically and also suppresses the appetite. The light dose by far has the most potential bodybuilding applications, especially if some of the industry’s great minds start formulating their “proprietary blends.” This dosage ranges from 1-5 g. of dried leaf, depending on the grade and supplier. For more in-depth dosing guidelines, click here to read what Erowid.org has to say. Myself and others have found this dose to put one in a very focused state. It makes manual labor somewhat enjoyable and, combined with certain stimulant amino-acids such as L-tyrosine or ALCAR (NOT DLPA- we’ll discuss that later), is great for a workout.

The second dosing threshold is more suited for coming home after a hard day’s work and a grueling workout at the gym, and consists of approximately twice the “light” dose. At this higher dose, Kratom has some crossover to the mu-opiate receptors, possibly responsible for its addictive properties. With the second and third dosing threshold, the addition of 200-500 mg. D,L-Phenylalanine significantly increases the analgesia and euphoria; it can also cause nausea and a bit of a crash afterwards. A higher dose can ease the mind, numb the pain of DOMS without the drawbacks of anti-inflammatory medications, and provide a legal alternative to people who like to catch a buzz, but don’t enjoy alcohol. A word of advice for those of you who are “on”: there is really no information regarding hepatic or renal impairment from Kratom.

At the third and highest dosing threshold Kratom takes on disassociative effects, not unlike GHB or ketamine. Be warned though, there is no valid reason for using Kratom at such doses. No one knows how toxic it may or may not be. In addition, many people have reported severe tachycardia, paranoid delusions, and other effects that may bring about a trip to the emergency room. Never assume that just because you ate 5 grams of resin from supplier X, that you can eat five grams from supplier Y, or even the same dose from a different batch. If you’re going to go high dose with Kratom, resin is the obvious choice, along with some ginger for the nausea. And NEVER go at it alone.

Besides giving you an extra boost, or relieving the minor aches and pains of daily life, Kratom has stepped up to the plate and cleared the bases where even the strongest narcotics have struck out. Steven Abrahamson is a life-long fitness enthusiast who has been using dietary supplements since the industry first started expanding in the mid 90s. When his wife was diagnosed with Multiple Sclerosis in 2001, he redirected his efforts to find a natural way to help ease her pain and increase her quality of life. After much research and frustration with bogus and/or overpriced product as well as customs hassles Abrahamson added Kratom to his wife’s daily supplement regimen. He noted that it, “seems to have a much better effect on her overall pain and is less harsh on her system while also simultaneously boosting energy levels. This has been a godsend as M.S. brings on the most intense fatigue I have ever seen.” Abrahmson added that, “Kratom has allowed her to again live life with much less synthetic pain killers and a considerable amount more energy and overall quality [of life]. Kratom really has been a gift.” Abrahamson, like many others, emphasizes that although Kratom is a miracle plant for many people, retailers have a responsibility to keep government regulation out of the picture.

Abrahamson, and his partner Stan Leavy, frown on retail sites that make wide generalizations about Kratom. In effect, as Abrahamson puts it some sites are, “slapping the FDA in the face by making wide medical claims on a retail site which may or may not be true about Kratom’s use as a pharmaceutical replacement.” He adds that despite what many retailers are claiming about Kratom’s safety, he himself almost overdosed, and urges people to use the herb responsibly.

Is It Addicting?

Chronic use of Kratom, at any dose, is without a doubt habit forming. Whether Kratom is actually physically addicting is still up for debate, however Kratom chewers in Thailand tend to start in their mid to late thirties and stay addicted for an average of twenty years.3 With daily use comes tolerance and increased dosages, which correlate to more binding with the mu opiate receptors and a higher chance of addiction. Going back to pharmacology briefly, kappa and delta opiate receptors remain unchanged by chronic administration of opiate agonists, while mu receptors become drastically down-regulated causing tolerance and addiction4. This may explain why Kratom is believed to be addicting after years of use and constantly increasing dosages. The take-home lesson here, as with everything in life, is moderation; not just in consumption of Kratom but in how we discuss it, who we share it with, and exactly what we use it for. Another proprietor of Kratom, Mike Mills, is a daily Kratom user by his own admission, and has the following to say regarding its addictive potential “I am not recommending that others should take it every day – it is a personal choice. My own experience has been that Kratom is not highly physically addictive, but it can certainly be habit forming, and can cause mild discomfort if you stop taking it after continuous use for a while.”

Future Applications

Over the past thirty years, several derivatives of Mitragynine have been developed for various applications. 7-hydroxymitragynine, was found to act as an opioid agonist with higher potency than that of morphine.2,5 Another derivative, Mitragynine Pseudoindoxyl, first synthesized in 1974, has a higher affinity to bind to opiate receptors than morphine, and a ten-fold greater binding affinity than Mitragynine.2 Only time will tell whether or not these interesting compounds find their way into our medicine cabinets, become demonized street drugs, or merely remain in the annals of medical literature. One thing is certain though: with commercially available Kratom becoming increasingly potent, Kratom will inevitably gain unwanted attention.

While some retailers will no doubt play a large role in the downfall of Mitragyna speciosa, it will be the individual who is truly responsible for this marvelous plant’s future. That’s right, it’s up to the American (or any country where it’s still legal) public to show some responsibility. If you look at our track record, it would appear that Kratom is doomed. But do not loose all hope—remember prohibition? We did it once and we can do it again if need be.

For now though, get it while the getting’s good. Finally, I’d like to thank Stan Leavey, Steven Abrahamson, Mike & Beth Mills, and Bodhi for all your useful information. As you’ve probably noticed, I did not plug any retail sites that sell Kratom as I have a journalistic responsibility to remain objective. However, we do have a forum for such discussion and I will be glad to answer any questions on said forum in an honest and subjective manner.

References

1. Takayama, Hiromitsu. “Chemistry and Pharmacology of Analgesic Indole

Alkaloids from the Rubiaceous Plant, Mitragyna speciosa.” Chemical & Pharmaceutical Bulletin. 52(8) 916—928 (2004).

2. Leonardo T. Yamamoto, et. al. “Opioid receptor agonistic

characteristics of mitragynine pseudoindoxyl in comparison with mitragynine derived from Thai medicinal plant Mitragyna speciosa.” General Pharmacology 33 (1999) 73–81

3. Suwanlert, Sangun. “A Study of Kratom Eaters in Thailand.” Bulletin

on Narcotics. 1975 v.27(3): 21-27. Online: 24 September 2005. Available: www.erowid.org/plants/kratom/kratom_journal3.shtml

4. Bhargava, H.N. “Multiple opiate receptors of brain and spinal cord

in opiate addiction.” General Pharmacology. 1991;22(5):767-72.

5. Hiromitsu Takayma, et. al. “Formation of an Unusual Dimeric Compound

by Lead Tetraacetate Oxidation of a Corynanthe-Type Indole Alkaloid, Mitragynine.” Chemical & Pharmaceutical Bulletin. 50(7) 960—963 (2002).

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