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Kratom pharmacokinetics and Cayenne, black pepper and Turmeric

gingerbaker

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Dec 3, 2013
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I've read from a few sources that cayenne, black pepper and tumeric can potentiate the effects of Kratom. I can't find ANY pharmacokinetic information on Kratom and have no idea how it is metabolized. Also, I have no idea if it acts as a pro-drug wherein the 7OHM is actually an alkaloid that is absorbed directly or if it is a metabolite. That μ effect is what I'm after (for analgesia) and I'm curious how/why Kratom would be potentiated by the aforementioned substances.

I've also heard that NMDA antagonists are good potentiators, but it's my understanding that Kratom already contains an alkaloid with NMDA antagonist activity (although un-competitive if I remember correctly) so would something like Cat's Claw have a ligand with stronger affinity?

Why would a significant amount of people claim that tumeric, cayenne and black pepper potentiate the experience? Would it be due to enzymatic inhibition or something BA-wise because of pH or some other direct effect on the GI?

Thanks!
 
This is purely anecdotal but taking curcumin along with kratom seems to prolong the effects every time I've done it, not sure about making them any stronger though
 
So that sounds like there might be some enzymatic inhibition going on then. I just found this: "It appears that Curcumin from Turmeric and Piperine from Black Pepper (commonly taken together) both inhibit a number of Cytochrome P450 enzymes. P450's such as CYP3A4 and CYP2D6 are responsible for a large amount of drug metabolism and the use of Curcumin and Piperine might explain some of the reactions people are experiencing upon co-administration with drugs such as Benzodiazepines and Amphetamine type drugs... Interesting stuff and something people, especially those using this forum, should be aware of." posted by perfectphase.

I'm actually more curious about NMDA antagonists. I've heard that Mg+2 has some NMDA activity but does anyone know what the affinity is and what the best salt is for NMDA anatagonism?
 
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as gingerbaker said, they're enzyme inhibitors potentially potentiating (heehee) the alkaloids in kratom.

i had some that contained the same spices but i gave them away. i took 13 caps of kratom in one go and got a productive codeine-like high minus the sedation, but he took 10 of the spice blended kratom caps and began nodding and "dreaming with his eyes open".
 
Right, but I'm trying to find the pharmacokinetics for kratom.

What is primarily responsible for the metabolism of kratom's alkaloids (I would assume at least a couple, since there are so many distinct alkaloids)

Does kratom form any active metabolites that would be decreased if one were to use enzymatic inhibitors? If so, are the active metabolites more potent than the ones found naturally?

Also, regarding Mg as an NMDA antagonist, can anyone suggest the best salt/preparation to use? I am also suffering from constipation so it's okay if it's one that has a laxative effect. Also, how strongly does Mg act as an antagonist (Ki or EC50)?

Thanks.
 
Also, how strongly does Mg act as an antagonist (Ki or EC50)?

It's much stronger in cell culture than it is in vivo, seeing as nobody gets dissociative effects typical of NMDA antagonists when large doses are administered.
 
It's much stronger in cell culture than it is in vivo, seeing as nobody gets dissociative effects typical of NMDA antagonists when large doses are administered.
Right, so using it for tolerance-reduction efforts (with kratom) would be useless? I could never believe that it was a very potent NMDA antagonist because no one ever gets anywhere near the same dissociative effects from it than even tiny doses of Ketamine, PCP, etc
 
Although it may be only marginally useful for tolerance reduction, it certainly cannot hurt to have magnesium in your diet anyway. There is probably much more of a noticeable effect in cases of Mg deficiency.
 
I can't find any studies regarding Mg in regards to NMDA activity. Do you happen to know of any?

Are there any others with experiences regarding Magnesium as an NMDA/tolerance substance?
 
I am on Bali/Indo right now mixed with 1mg of xanax, and three beers. I find I get a decent opiate type buzz from this mixture.
 
That's great, but irrelevant to the question at hand... namely how krtaom's active principles are metabolised. Nobody disputes kratom is an opioid.
 
Also, I'd like to add NMDA antagonists to the topic.

For instance, I was wondering what alkaloid specifically possesses the NMDA antagonist activity that is supposedly inherent? Also, is it selective and what is its affinity?

Also, what is the safest NMDA antagonist to take regularly to keep tolerance at bay? I know that therapeutic doses of DXM should be safe (and legal) so I'd like to try that route but am curious about DXO and if there is any kitchen chemistry or enzymatic ways to increase the amount of DXO from common cough preparations. I'm not talking about synthesis, just ways to increase NMDA antagonist activity from what I have access to (which is DXM, I don't know of any other legal NMDA antagonists that are potent enough). Would taking 30mg twice a day be a good way to go about it or should it be before each time I dose Kratom? Would a sustained-release preparation like the DXM-Polisterex be a good way to do it?
 
I don't there if there exists conceptually anything more nauseating than being 'on' any form of kratom regimen lol

I agree. I just bought an ounce mixed with bali and indo. I never realized kratom was actually an opiate.
 
Correct, it is a plant containing an admixture of alkaloids, some of them opioids. Bah, semantics.

Rhynchophylline is the dominant NMDA antagonist alkaloid in M. speciosa. Same fella as in Cats Claw (Uncaria tomentosa). What its affinity is I have no idea.

It is my understanding that NMDA antagonists work more so at preventing tolerance rather than lowering it.

You will find an unbearable amount of gobshite on some of the Kratom forums. The power of suggestion is nauseating.
 
OP first of all the only smart information here is that Turmeric should be taken with Kratom, because we do not have enough evidence on what Mitragyna speciosa does to the Human liver. Turmeric is one of the best natural substances in liver defense.

pharmacokinetic's of Mitragyna speciosa don't just involve the time the effects are being felt, This is the entire life span of the drug in your system...

I am sure Wild dagga would potentiate Kratom better than anything

EB
 
kratom + MXE + weed will give you the dream state nod/mind movies/euphoria/intense bodily sedation effects of kratom ;)

one time I smoked a decent amount of black pepper and nutmeg and got pretty distinguishable non placebo effects from it, idk if that adds to discussion but putting it out there anyway.
 
returning to the original post, let's get all 'spiced up'. :p

ebola
 
Be sure to add black pepper when using turmeric because curcumin is poorly absorbed on it's own. I have noticed potentiation when taking kratom with turmeric and black pepper.
 
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