Over the years as the use of Kratom has increased there was then multiple research done upon the benefits and information regarding the alkaloids for treating pain, management of the substance use disorder, dealing with the emotional and mental health conditions.
The two major alkaloids found in the strongest Kratom tend to be mitragynine and 7-hydroxymitragynine. These two are majorly discussed, however there are 43 other types of alkaloids found in Kratom.
The mitragynine and 7-hydroxymitragynine gets binded with the human µ-opioid and ƙ-opioid receptors that too with the nanomolar affinity. Based on this they function as partially strong agonists at the µ-opioid receptor and on the other hand as weak antagonists at ƙ-opioid and δ-opioid receptors.
For the 7-Hydroxymitragynine it has almost five times greater affinity at the μ-opioid receptor in comparison to the mitragynine. When it is activated the mitragynine and 7-hydroxymitragynine performs functional selectivity to signal the G-protein when no recruitment is performed for the β-arrestin.
Whereas in antinociception assays, the 7-hydroxymitragynine has 40 times more potency than the mitragynine and likewise, 10 times more potency than the usual morphine. In comparison to this mitragynine is less potent than morphine. The combination of mitragynine and morphine increases the effect of antinociception that morphine alone could produce.
The combination of mitragynine and morphine further eliminates the development of the tolerance of morphine. The mitragynine on the other hand, repeats the 7- hydroxymitragynine which also produces the dependency of antinociceptive plus the development of cross tolerance of morphine antinociceptive is created which creates the physical dependency.
Additionally, the studies have shown that mitragynine does not claim abuse liability and is further witnessed in reducing the effects of morphine. However, 7-hydroxymitragynine causes the liability for abuse and is witnessed for an increment in morphine that develops self-administration which was found in rats.
Kratom is seen to produce different variations in more than 40 alkaloids which is entirely based on the variations that are dependent on their genes and differences being created during the processing period.
Kratom leaves can either be chewed upon taking up 10 to 30 leaves per day, or it can even be dried and then crushed by consuming it in a powder form, mixing it in a tea or some people even smoke the extracts of the leaves using it as a way of consumption.
Mitragynine is the most popular form of alkaloid in it that accounts for 66% of the extract. It is one of the compounds which is responsible for the activity related to analgesic because of the property of potent opioid agonists present in it.
Mitragynine also acts upon mu (μ) and kappa (κ)-opioid receptors that are different from morphine and other pain killers that are regarded as opioid narcotic. Mitragynine and its analogues that are found in Kratom are the alkaloids of indole of the Corynanthe-type which possesses a monoterpene (iridoid) moiety.
Based on the concentration of mitragynine being present in Kratom tends to be 12% if the leaves are from Malaysia. However, the level of concentration found in Kratom if the leaves are from Thailand accounts to be 66% which is much higher than the one in Malaysia.
With monoterpene (iridoid) moiety there are other alkaloids also present that include speciogynine with a 7% of concentration level, paynantheine with 9% of concentration level, and speciociliatine with 1% of concentration level.
Mitragynine is also a major component for the properties related to anti-inflammatory of Kratom being found in it that suppresses the prostaglandin E2 (PGE-2) production.
The other alkaloid that has gained popularity is the 7-hydroxymitragynine which was once a minor constituent that accounted for 2% level. This alkaloid is usually isolated and shown as a potent antinociceptive activity which was discovered while the alkaloid was identified in mice.
7-hydroxymitragynine with time is now considered as a major element that has contributed towards the analgesic properties of Kratom that too because of the μ- and κ-opioid receptors selection.
Moreover, the presence of an hydroxyl group at C-7 is identified as increasing the level of potency of 7-hydroxymitragynine which is over 13 to 46 times higher that is even found in morphine or mitragynine alone.
Overall this shows and clearly indicates that 7-hydroxymitragynine comes under one of the major pharmacological alkaloid makers used in the different types of Kratom products quality and potency as well.
The Positive Effects Alkaloids
The positive effects of using Kratom with the concentration levels of different alkaloids combined in it brings is that for those who live in South East Asia use it as a antidiarrheal, cough medicine, anti-diabetic, intestinal deworming agent, and to clear off the intoxicants of heroin.
Whereas the people residing outside Asia generally tend to use it for chronic pain and to withdraw the opioid they are dealing with, instead of using the opioid analgesics.
Moreover, they are majorly known for exerting the analgesic, anti-anxiety, anti-drug addiction, and other antipsychotic effects that could be catered once the opioidergic, adrenergic, serotonergic, and dopaminergic are activated in the neurotransmission systems.
The Negative Effects Alkaloids
With the positive effects comes the negative effects. Sometimes these alkaloids cannot suit the people and create the reported side effects. These include constipation, loss of appetite, weight loss, insomnia, and discoloration that mainly occurs or is visible on the cheeks.
Regular use of it has caused people to become addicted to it. Many calls have been made in the CDC poison centers related to the Kratom overdose taken up by people. Even people who take up the substance in lower doses but still can witness the side effects that include mainly hallucinations.
People do believe that Kratom is a safe choice in comparison with the other medicines however, not enough studies have been conducted which prove this point. While it is witnessed that Kratom is seen to pose a deadly interaction if it is used with other drugs or medicines.