Kratom Metabolism: What You Need to Know

May 01, 2019 Articles, Kratom Alkaloids, Kratom Research

Online kratom vendors have made many bold and damaging claims about kratom use in recent years. Much of this information is not corroborated by experts and is not based on scientific data of any kind.

Here at Kratom Crazy, we strive to give visitors a reasonable and accurate account of kratom effects, kratom interactions and the science behind kratom. We believe that it is essential to the future of this amazing Ayurvedic herb that the public know the difference between the truth and the hype.

In the last week of research alone, I have come across a staggering number of false claims and dangerous recommendations by second-rate botanical blogs and e-commerce sites. One page I read even falsely suggested that users should consume large amounts of kratom over a long period of time for best results.

In reality, nothing could be farther from the truth. Most seasoned kratomites already know that chronic use of kratom can be hazardous to their health. Long-term use can result in tolerance, addiction, overdose or even death.

What they may not know is exactly how kratom’s alkaloids are metabolized and what that can mean for the integrity of their bodily functions. We endeavor to change that with today’s post.

MITRAGYNINE METABOLISM—THE MAIN KRATOM ALKALOID & THE THREAT IT POSES

Mitragynine is by far the most abundant indole alkaloid present in kratom. This opioid-receptor agonist occurs at only 1.2-2.1% in dry kratom leaf, but it can occur at concentrations of up to 66% in kratom powder.

In in vitro tests, kratom extracts inhibited CYP1A2, CYP3A4 and CYP 2D6 enzymes, the corollary of which is a substantial potential for drug interactions. This goes far towards explaining why several kratom-related deaths resulted from combining kratom with prescription medications.

Kratom metabolism as a whole is rather complex, but mitragynine metabolism, in particular, is fairly well-documented by the scientific community. For instance, we know that metabolite profiling and the enzymes responsible for the metabolism of mitragynine have been identified by the Department of Medicinal Chemistry at the University of Florida.

We also know that this metabolism occurs in the human liver microsomes (HLM) AND S9 fractions. This tells us that kratom consumption can be potentially problematic for those with preexisting liver disorders, such as alcoholic fatty liver or other forms of liver disease.

Mitragynine is primarily metabolized to O-demethylated and monooxidative metabolites in lab rats and in three metabolites to glucuronides and three metabolites to sulfates in humans. Further analysis has shown that mitragynine is metabolized in humans via hydrolysis of the side-chain ester.

This same study found that the metabolism of kratom concurrent with that of other drugs can provoke extreme side effects and observed interactions with carisoprodol, modafinil and prophylexedrine (Datura stramonium). This study also references a death in the US that involved caffeine, diphenhydramine, fentanyl, kratom and morphine.

The mitragynine metabolism pathway is largely the same as that of alcohol abuse. Those who drink heavily put themselves at serious health risk because alcohol metabolism can cause oxygen deficits in the liver. Alcohol is largely metabolized via the hepatic enzyme alcohol dehydrogenase IB (Class I). Kratom metabolism occurs via phase I and phase II mechanisms.

Although the kratom mechanism of action is something that continues to be explored, we know that mitragynine is largely responsible for the main mechanism of action as it exerts selective u-opioid receptor activity.

Most users agree that using kratom in moderation results in this mechanism of action and that micro-dosing can be safe and effective. However, there is inconclusive scientific evidence to support the notion that kratom is safe for everyday use by those suffering from preexisting health conditions.

THINGS TO CONSIDER BEFORE BURNING KRATOM

Those suffering from heart disease, such as high BP (blood pressure), peripheral artery disease, heart murmur (prolapsed valve), congenital heart disease, arrhythmia or a history of stroke should not use kratom.

Those with chronic liver problems, such as nonalcoholic fatty liver, hemochromatosis, hepatitis B or C, or cirrhosis should avoid kratom use altogether. Despite reports by many recovering alcoholics who have claimed that kratom helped them kick the habit, the science does not support its efficacy as a rehab or detox treatment, and kratom powder may cause irreparable harm to your liver.

Additionally, kratom should not be ingested if you are pregnant or feeding. If you or a loved one suffer from one of these medical conditions and have consumed kratom, you should discontinue use at once and consult with your physician.

While kratom deaths have often been caused by ingesting kratom in tandem with other substances, especially prescription medications, there is no way to know what effect this powerful natural stimulant may have on any given individual.

IS KRATOM ILLEGAL?

Kratom legality varies from state to state and country to country.

Here in the United States, it is currently legal in Alabama, Alaska, Arizona, California, Colorado, Connecticut, Delaware, Florida (except for Sarasota County), Georgia, Hawaii, Idaho, Illinois, Iowa, Kansas, Kentucky, Louisiana, Maine, Maryland, Massachusetts, Michigan, Minnesota, Mississippi, Missouri, Montana, Nebraska, Nevada, New Hampshire, New Jersey, New Mexico, New York, North Carolina, North Dakota, Ohio, Oklahoma, Oregon, Pennsylvania, Rhode Island, South Carolina, South Dakota, Texas, Utah, Virginia, Washington, West Virginia and Wyoming.

States that have banned kratom have done so at the expense of their residents, many of whom used kratom to treat chronic pain disorders, IBS (Irritable Bowel Syndrome), Crohn’s Disease, MS (Multiple Sclerosis), RA (Rheumatoid Arthritis), insomnia and a host of other ailments.

HOW LONG DOES KRATOM STAY IN YOUR SYSTEM?

Kratom metabolism occurs quite quickly and so, too, does its presence in your body. Recent research suggests that kratom may have a half-life of just seven hours, placing total elimination after approximately 1.6 days.

This is good news for those who may be subject to a kratom drug test since kratom could take only nine days or less to be completely eliminated from one’s system.

BOTTOM LINE

As you can see, there are many pros and cons to burning kratom and I think you’ll agree that there is plenty to think about when it comes to kratom use. Those who wish to purchase kratom should always take proper precautions. Be safe, be smart and be well.

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