Thursday, January 7, 2021

Debunking Kratom Myths: Potentiates

Most Potentiates that people use for Kratom are cyp3a4 inhibitors. The rationale behind this is that since this enzyme metabolizes 65% of known drugs, a lack of it would cause the alkaloids to build in the bloodstream causing a pronounced effect that lasts longer. This dangerous drug interaction with an inhibitor like grapefruit juice is what you are warned about on many prescription drug bottles. 

Recent research has been groundbreaking. We've discovered that the opioid (7ohm) on par with Morphine found in kratom is a metabolite and only found in trace amounts in the leaf. This alkaloid is converted primarily by the same enzyme mentioned above. So, while we were trying to get a greater opioid effect by inhibiting said enzyme, we may have actually been reducing the opioid effect. This would theoretically mean that the effects would be primarily from the alkaloid Mitragynine. Mitragynine is the reason we have stimulation through adenosine receptor antagonism, much like Caffeine. 

So, theroretically, you would get more stim from an inhibitor, and more opioid from an inducer. Try this experiment: take the same amount of the same strain of kratom for a week (or a day) while taking an inhibitor, then try it for a week (or whatever) with an inducer. See if you get different effects. Also theoretical: wobbles should be cured by taking an inducer assuming you believe that wobbles are caused by the "great neuromuscular blockade" effect of Mitagrynine (as cited by one study. 


[b]Inducers (increase cyp3a4)

[/b

]St. John’s wort [14, 15, 16]

Capsaicin [17, 18]

Common valerian [19]

Echinacea purpurea [20]

Vitamin D and UV exposure [6]

Being female [21]

Diabetes [22]

Fatty acids [22]

Polycyclic aromatic hydrocarbons (PAH) found in cigarettes [23]

Aflatoxin B1 [24]

Some drugs such as carbamazepine [10] and dexamethasone [25]


[b]Inhibitors (decrease cyp): 

[/b]

Grapefruit juice (and its compounds bergamottin, naringenin, and paradicin-A) [26, 4, 27]

Starfruit juice [28]

Aloe vera juice [29]

Mixed vegetable juices [30]

Kale [31]

Garden cress [32, 33]

Fennel [34]

Green tea [4, 35]

Black pepper [36, 37]

Herbs

Goldenseal [38]

Raspberry leaf [34]

Milk thistle (compounds silybin and isosilybin) [39]

Good link explaining the enzyme and citing studies: ]https://www.medsafe.govt.nz/profs/PUArticles/March2014DrugMetabolismCytochromeP4503A4.htm#:~:text=The%20liver%20and%20small%20intestine%20have%20the%20highest%20CYP3A4%20activity.&text=Potent%20inhibitors%20of%20CYP3A4%20include,John's%20Wort%20and%20glucocorticoids

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