What is Kratom?

An Introduction to Kratom

Mitragyna speciosa korth, or kratom, is a medicinal herb that belongs to Rubiaceae family, along with coffee (Koehbach & Gruber, 2015). This type of tree is native to tropical and sub-tropical regions of Southeast Asia and Africa. Those in  its native east Asian countries of Vietnam, Thailand, Indonesia and Malaysia have utilized the leaves of the kratom tree as alternative medicine for generations. Each type of kratom is comprised of its own distinct alkaloid profile, which is responsible for kratom’s many beneficial effects.

M.speciosa contains more than 40 compounds. The major portion is of these are indole alkaloids, which are bioactive compounds which elicit various pharmacological actions (Kukula-Koch & Widelski, 2017). More than 25 alkaloids have been extracted from M. speciosa with mitragynine being the most abundant at approximately 66% of total alkaloid weight. This alkaloid is primarily responsible for much of the anecdotal pain relieving effects of kratom as it is a partial mu-opioid receptor agonist. (Al-Hasani & Bruchas, 2011).

Traditionally, the leaves of the kratom tree have been used to treat muscle pain, intestinal infections, cough, and diarrhea. In addition, Asian laborers have long used kratom as a productivity aid when working long hours in hot and humid climates. On top of its reported analgesic effects, the compounds found in kratom have been studied for their antipyretic, antidepressant, anxiolytic, antiviral and antidiabetic effects – just to name a few. Kratom’s alkaloids are also being explored for strengthening the immune system and regulating blood pressure (Agrawal, Nandini, & Sharma, n.d.).

Kratom and it’s Alkaloids

Kratom contains up to about 66% mitragynine, which is responsible for a great deal of the plant’s analgesic, antitussive, antidiarrheal, adrenergic and antimalarial properties. It acts as weak opioid receptor agonist that has high affinity for the µ-opioid receptors. Although the FDA continues to spread fabricated stories about the dangers of kratom, studies following a dose-adjusted protocol have found mitragynine to be no more than one-tenth the strength of morphine (Kikura-Hanajiri et al., 2009). Its effects slightly vary from person to person and mostly depends upon one’s individual sensitivity and internal chemistry.

Is Kratom Safe?

As of the date of this writing, all available reports of fatal kratom overdoses have involved other, often multiple, drugs or subjects with histories of poor health. To date, there has been zero cases of death in which kratom was ascertained to be the sole cause. One would become violently sick long before reaching such a level of toxicity in the blood. The leaves of the kratom tree have generations upon generations worth of heavy usage within Southeast Asian culture, so real-world application in humans has certainly been evaluated.  That said, there have been kratom products that were found to contain adulterants, and even recreational drugs. When deciding to consume kratom, it is of vital importance to select only pure, organic kratom with no additives.

On the original question regarding kratom safety, we have some information from real academics, scientists, doctors, and others qualified to speak on the subject, though this short list is non-exhaustive:

  • Dr. JE Henningfield (Johns Hopkins University School of Medicine) and his associates performed an eight-factor analysis to assess the addition, abuse, and danger profiles of kratom. The team found the following (Henningfield, 2017):
    • Kratom, unlike opioid medications, is associated with benefits in terms of occupational performance and social outcomes (Swogger, 2015).
    • At the levels that today’s kratom user consumes the leaf, kratom is not usually associated with negative health consequences
    • Kratom is about as addictive as caffeine, with the worst-case scenario involving mild dependence at most
    • Kratom’s predominantly oral consumption route contributes to its relative safety as well as its low abuse potential
    • Despite the false and embellished claims by certain agencies in the media, there appears to be no significant abuse of kratom in the United States
    • A study using 10 years of data from 63 hospitals, which documented 23,005 emergency room visits related to dietary supplements, featured zero cases involving kratom or mitragynine (see alkaloid profiles below)
  • The DEA no longer features kratom on its list of drug threats
  • When the FDA released its own eight-factor analysis describing kratom as a harmful drug with significant abuse and dependence potential, it was quickly and fully discredited by a panel of 11 independent doctors, medical and otherwise, who actually have credibility in the field (Babin, et al., 2018)

Returning to the alkaloids present inside the kratom leaf, here is a short snippet about them and the individual effects that each has been studied for (“Kratom Alkaloids & Effects | Kratom Science,” 2018):

  • Paynantheine (9%) & speciogynine (7%) –  smooth muscle relaxing effects.
  • 7-hydroxymitragynine (2%) – reported analgesic, antitussive and antidiarrheal properties. It is for these potential benefits that kratom is sometimes used to ease opiate withdrawal symptoms. It is believed that 7-hydroxymitragynine is 30 times stronger than mitragynine and 10 times stronger than morphine.
  • Speciogynine (1%) weak opioid agonist effects
  • Mitraphylline (<1%) vasodilation, antihypertension, smooth muscle relaxing, diuretic, antiamnesic, immunostimulant and anti-leukemic effects
  • Isomitraphylline (<1%) may act as an immunostimulant and anti-leukemic agent.
  • Speciophylline (<1%) studied for its benefits for those with leukemia
  • Rhynchophylline (<1%) may have a major role in blood pressure as it acts vasodilator, antihypertensive agent and calcium channel blocker. It is also reported to exhibit anti-inflammatory, antipyretic, anti-arrhythmic and antithelmintic properties.
  • Isorhynchophylline (<1%) possibly boosts the immune system.
  • Ajmalicine (<1%) researched as a cerebrocirculant, antiaggregant/anticoagulant, anti-adrenergic, sedative, anticonvulsant and smooth muscle relaxer.
  • Corynantheidine (<1%), corynoxine A (<1%), corynoxine B (<1%), mitrafoline (<1%), isomitrafoline (<1%), oxindale A (<1%) & oxindale B (<1%) are opioid receptor agonists, some of which act as calcium channel blockers and anti-locomotive agents.
  • Speciofoline (<1%), isospeciofoline (<1%), ciliaphylline (<1%), mitraciliatine (<1%), mitragynaline (<1%), mitragynalinic acid (<1%) and corynantheidalinic acid show antitussive and analgesic effects.

The content of each individual alkaloid inside the kratom leaf varies with the geographical location and age of the source tree. Older plants are richer in alkaloids, which is why our people are so picky during harvests. The curing process can also heavily influence the leaf’s constituents. One study found that roughly 8% of a leaf’s mitragnine can be converted to 7-hydroxymitragnine by the sun alone (Kruegel et al., 2016). Given the exponential relative strength of the latter alkaloid, this means that there is a major variance in psychoactive effects between a hastily-harvested leaf and one that is properly cured – even from the same tree.

Handling can indeed make or break raw materials in this business. Our suppliers have consistently stressed the importance of maintaining a constant soil pH level between 5.5 and 6.5. When we claim that we offer only the highest quality kratom one could find anywhere, it is because we take heed to the experience of many generations and we work iteratively on process optimization.

Potential Health Benefits of Kratom

Pain relief:

The analgesic, or pain relieving, effect is due to interaction of alkaloids with opioid receptors present in the brain. The result is an enhanced release of enkephalins and endorphins, which may numb the pain receptors of the body (“Leu-enkephalin,” n.d.). This action is sought after by those who choose to avoid prescription medications. Our customers have reported applications such as mild to moderate relief from cancer, rheumatoid arthritis, osteoarthritis, fractures, and post-operative procedures.

Stimulation:

The stimulation that is produced by M.speciosa occurs when it partially acts on mu-opioid receptors in the brain (Boyer, Babu, Adkins, McCurdy, & Halpern, 2008). This activates the body and mind in such a manner that one receives a subjective boost in mental energy and focus. Additionally, some claim that the kratom leaf, when used in the right amounts, enhances cognitive ability,

Uplifting of mood and reduced depression and anxiety:

The alkaloids present in the leaves of the kratom plant are commonly used for their euphoric, anti-depressant, and anxyolitic effects. Mitragynine and 7-OH-mitragynine are said to soothe the nerves and elevate the mood in such a way that users may forget all their worries and tensions and enjoy a feeling of contentment. This effect is again due to interactions with opiate receptors, which lead to a release of sympathetic neurotransmitters like dopamine and serotonin (“Mitragynine”, 2019.). Kratom’s alkaloids may also be useful for other symptoms of anxiety like insomnia, heart palpitations, sweating, and muscle cramps.

Help in overcoming opioid addiction:

Kratom has been successfully used by our customers enduring opioid withdrawal as it eases the period of withdrawal symptoms, allowing one to taper off these drugs. It reportedly mitigates the typical symptoms of opioid withdrawal like cramps, vomiting, pain, anxiety etc. Its alkaloids are not traditional opioids, but they can partially bind with opioid receptors in place of opiate drugs and thus help in easing the effects of addiction (Greene, 2013).

Immune system modulation:

The kratom leaf may help to improve the immune system by helping to rid the body of free radicals and harmful microbes. Many of the alkaloids of kratom may work as immunostimulants (Rojas-Duran et al., 2012), which improve the immune system and combat against infections.

Improved focus:

The alkaloids 7-hydroxymitragynine and mitragynine tend to allow users to work harder for longer periods and with a focused intensity. Essentially, one becomes more satisfied with the task at hand. This happens with the release of neurochemicals like serotonin and dopamine which help to improve focus, attention span, and motivation. Also, the neurotransmitter acetylcholine relaxes the ruminating mind (Janowsky, El-Yousef, & Davis, 1974) and is thus also helpful in improving focus.

Increased motivation:

The activation of opioid receptors helps one to stay motivated and energetic to get the things done. We have one customer in particular who swears by taking kratom an hour before a study session or exam for a bit of an extra drive. These effects are elevated with the drastic increase in dopamine and serotonin that may occur once kratom’s alkaloids are metabolized in the body. Average duration of effects is said to be approximately four hours for most strains.

Improved heart health:

The alkaloids present in kratom leaves may be beneficial to the body’s hormonal balance and blood vessels and may thus be advisable for those with high blood pressure. These compounds are investigated as vasodilators, calcium channel blockers, antihypertensive agents, and diuretics. All of these properties collectively help to improve heart health and reduce blood pressure.

Anti-inflammation:

The major and primary alkaloid of kratom is mitragynine, which is often reffered to as a powerful anti-inflammatory agent. (Mossadeq et al., 2009). This property is similar to over the counter non-steroidal anti-inflammatories (NSAIDs) in that it reduces pain, inflammation, swelling and redness at the site of inflammation. Because of these properties, it is sometimes used in patients suffering with rheumatoid arthritis, osteoporosis, and osteoarthritis.

Antioxidant properties of kratom:

Some researchers claim that kratom leaves contain certain antioxidants that are helpful in protecting users against cancer. These antioxidants have an effect similar to your body’s natural antioxidants, like superoxide dismutase and glutathione, which aid in preventing the formation of free radicals. A reduction in free radicals may be strongly correlated with better odds in staving off cancer and adding to one’s lifespan.

Also being currently researched are several other health benefits of kratom leaves. Much remains to be learned about this special leaf.  In December of 2018, the University of Florida received a $3.5m grant to study the potential benefits of kratom’s alkaloids (UF College of Pharmacy, 2018). We are awaiting UF’s findings with great anticipation . Despite its oft-negative reputation in the media resulting from the US government’s fabricated stories, poor methodologies, and false science, pure, unadulterated kratom remains a generally safe compound with a plethora of potential benefits and generations upon generations of usage history.

These statements have not been evaluated by the FDA, and kratom is not approved by any government agency for medicinal use in the USA. It is not intended to diagnose, treat, or cure any disease. If you decide to being experimenting with kratom, we advise you to talk to your healthcare professional  regarding your current health condition and the possible implications of consuming such a substance. We do not recommend opioid-dependent patients abruptly stop taking their medication. The above claims are based on reports provided to us by our customers, friends, or other members of the community as well as academic, peer-reviewed journal articles on the subject.

 

 

References

Agrawal, M., Nandini, D., & Sharma, S. C. (n.d.). (18) (PDF) Herbal remedies for treatment of hypertension. Retrieved April 1, 2019, from Research Gate website: https://www.researchgate.net/publication/266372360_Herbal_remedies_for_treatment_of_hypertension

Al-Hasani, R., & Bruchas, M. R. (2011). Molecular Mechanisms of Opioid Receptor-dependent Signaling and Behavior: Anesthesiology, 1. https://doi.org/10.1097/ALN.0b013e318238bba6

Babin, Boyer, Brown, Garcia-Romeu, Griffiths, Grundmann, Hemby, Henningfield, McCurdy, Raffa, Swogger, & Walsh (2018). Comment on FDA Kratom CSA 8-Factor Analysis. Retrieved from https://www.americankratom.org/images/file/Scientists-Response-to-FDA-Kratom-8FA–28-Nov-2018-FINAL.pdf

Boyer, E. W., Babu, K. M., Adkins, J. E., McCurdy, C. R., & Halpern, J. H. (2008). Self-treatment of opioid withdrawal using kratom (Mitragynia speciosa korth). Addiction (Abingdon, England), 103(6), 1048–1050. https://doi.org/10.1111/j.1360-0443.2008.02209.x

Greene, S. L. (2013). Chapter 15 – Tryptamines. In P. I. Dargan & D. M. Wood (Eds.), Novel Psychoactive Substances (pp. 363–381). https://doi.org/10.1016/B978-0-12-415816-0.00015-8

Henningfield, J.E., Fant, R.V. & Wang, D.W. Psychopharmacology (2018) 235: 573. https://doi.org/10.1007/s00213-017-4813-4

Janowsky, D. S., El-Yousef, M. K., & Davis, J. M. (1974). Acetylcholine and depression. Psychosomatic Medicine, 36(3), 248–257. https://doi.org/10.1097/00006842-197405000-00008

Kikura-Hanajiri, R., Kawamura, M., Maruyama, T., Kitajima, M., Takayama, H., & Goda, Y. (2009). Simultaneous analysis of mitragynine, 7-hydroxymitragynine, and other alkaloids in the psychotropic plant “kratom” (Mitragyna speciosa) by LC-ESI-MS. Forensic Toxicology, 27(2), 67–74. https://doi.org/10.1007/s11419-009-0070-5

Koehbach, J., & Gruber, C. (2015). Rubiaceae – an overview. Retrieved April 1, 2019, from Science Direct website: https://www.sciencedirect.com/topics/agricultural-and-biological-sciences/rubiaceae

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Kruegel, A. C., Gassaway, M. M., Kapoor, A., Váradi, A., Majumdar, S., Filizola, M., … Sames, D. (2016). Synthetic and Receptor Signaling Explorations of the Mitragyna Alkaloids: Mitragynine as an Atypical Molecular Framework for Opioid Receptor Modulators. Journal of the American Chemical Society, 138(21), 6754–6764. https://doi.org/10.1021/jacs.6b00360

Kukula-Koch, W. A., & Widelski, J. (2017). Alkaloids – an overview | ScienceDirect Topics. Retrieved April 1, 2019, from Science Direct website: https://www.sciencedirect.com/topics/neuroscience/alkaloids

Mossadeq, W. M. S., Sulaiman, M. R., Mohamad, T. A. T., Chiong, H. S., Zakaria, Z. A., Jabit, M. L., … Israf, D. A. (2009). Anti-Inflammatory and Antinociceptive Effects of Mitragyna speciosa Korth Methanolic Extract. Medical Principles and Practice, 18(5), 378–384. https://doi.org/10.1159/000226292

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Rojas-Duran, R., Gonzelz-Aspajo, G., Ruiz-Martel, C., Bourdy, G., Doroteo, V., Adelaida Albàn Castillo, J., … Deharo, E. (2012, July). Anti-inflammatory activity of Mitraphylline isolated from Uncaria tomentosa bark. Retrieved April 1, 2019, from Research Gate website: https://www.researchgate.net/publication/230588166_Anti-inflammatory_activity_of_Mitraphylline_isolated_from_Uncaria_tomentosa_bark

Swogger MT, Hart E, Erowid F, Erowid E, Trabold N, Yee K, Parkhurst KA, Priddy BM, Walsh Z (2015) Experiences of kratom users: a qualitative analysis. J Psychoactive Drugs 47(5):360–367.  https://doi.org/10.1080/02791072.2015.1096434
UF College of Pharmacy. (2018). UF College of Pharmacy receives $3.5 million NIDA grant to bolster kratom research. Retrieved April 12, 2019, from https://pharmacy.ufl.edu/2018/12/10/uf-college-of-pharmacy-receives-3-5-million-nida-grant-to-bolster-kratom-research/
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