Misc Kratom questions

[gingerbaker]

First of all, yes, I've searched the forums and interwebs and done quite a bit of reading. That being said, I still have a few questions regarding kratom for treating chronic pain.

1. What is the best strain for chronic pain? I've seen Red Borneo and Bali and am curious if there is a difference between the two.

2. What is the longest lasting strain that can still reasonably used for analgesia? I'm thinking that there is a strain that might be long lasting but not necessarily the most analgesic-oriented.

3. How is Kratom metabolized? I know there are active metabolites, but is it a pro-drug situation like Tramadol, for instance (where the metabolites are more active/potent)?

4. What are some not-so-obvious [legal] potentiators (obviously GFJ, cimetidine, 1st gen anti-histamines would be good ones I'm assuming but I guess it sort of depends on the answer to #3)?

5. With kratom "powder" (finely ground leaves), why do people claim that the capsules slow down absorption?

6. What are good ways to increase bioavailability and what is the bioavailability of sublingual and oral ROAs?

7. Does consuming kratom on a stomach with some food in it just slow absorption or does it actually lessen the effects?

8. Regarding "boosting"; is it true that one must wait a few hours if the dose is not adequate? I've read that you can't really bump up the effects a notch or two by taking a little bit more say, half an hour after taking the 1st dose. That just doesn't seem logical but I can't find any info on the pharmscokinetics of kratom.

9. I've also read that tolerance doesn't really develop as rapidly or extensively as opioids. Obviously it develops to a certain extent and there is some risk of dependency but could someone quantify this? For example, if you start off with taking 5grams of X every 5hrs, what would the tolerance be in a month?

As always, thank you everyone for your help!

 

[Rybee]

Will keep an eye on his thread as I'm sceptical with regards to kratom. Would like to know some of the answers here!

 

[gingerbaker]

With the NMDA antagonist activity claimed I don't doubt some of the tolerance/dependence claims but I haven't really seen much actual research on Kratom (if that's what you're referring to).

 

[liftedgift]

I'll try to answer some of them

1.Bali is my go to strain, probably the most sedating although I've had maeng da that is sedating as well. I do not use kratom for pain so maybe someone else can chime in. I have never tried Borneo strains.

4. Phenibut definitely adds to the sedation but I wouldn't suggest using it often. I've heard good things about magnesium citrate before eating the kratom.

5. Maybe because your stomach has to get through the capsule? Not sure if I understand the question... It really needs to be powder to digest quickly not just ground up leaves.

7. I hardly feel kratom if I consume on a full stomach or eat right after I eat kratom. Eat it with an empty stomach, then 30-60 mins later eat a fatty meal. I have found this really increases the effects it and can often make it too powerful so know how much you need.

8.Never heard of this, as it will digest and increase effects.

9.With plain leaf, tolerance is very forgiving. I've been a daily kratom user for close to 2 years and my plain leaf use is always between 10-30gs a day. Even if I binge one day, I still need just 4-6gs in a dose to feel effects. Now with extracts it is a totally different story.

 

[gingerbaker]

Re: question 5, I've heard people say that capsules "don't work as well" although maybe all they're saying is that there is a delayed onset (but even that doesn't make sense as those capsules dissolve rapidly).

Just to clarify, what is considered plain leaf and an extract? Are there certain terms that are commonly used for those?

 

[cpuller]

Plain leaf is regular powder and crushed leaf, theres nothing added to it.
Extract can be a waxy, hash like thing or something "enhanced" meaning theres something on the leaf powder. (Maybe possibly added, they sometimes say its better plants and blabla but you never know whats really on the kratom)

 

[gingerbaker]

Alright thanks for clarifying that. What is UEI and why is it that extracts sound like they build tolerance much more rapidly? Are there any benefits to extracts? Do they usually contain certain alkaloids in a relatively higher proportion than in normal leaf?

Thanks again

 

[liftedgift]

Extracts are just that...extracted alkaloids from the kratom. So in short...they are way stronger that is why they build a tolerance quickly. Kratom has sooo many alkaloids, and I don't think they extract all the alkaloids from the plain leaf into the extracts. IMO, plain leaf has kind of a ceiling that when you take more than a certain amount all you get is negative effects.

With extracts, the ratio to euphoria:ill feelings(nausea,dizziness) is really high. Extracts are more like an actual opiate, they build tolerance fast and the withdrawal sucks more than just plain leaf withdrawal

 

[gingerbaker]

Thanks for clarifying that, sounds like I should stay away from them then. I think the "ceiling effect" is actually a good preventative property...

Anyways, I was throwing around the idea in my head of making an extended release preparation so that the effect would last longer and wouldn't need to re-dose 3-4 times a day. I plan on using capsules so does anyone know of a way to slow down the release to make it an extended-release type capsule?

 

[PANDAmonium]

I'll tackle a few that liftedgift didn't get to:

3. How is Kratom metabolized? I know there are active metabolites, but is it a pro-drug situation like Tramadol, for instance (where the metabolites are more active/potent

Unfortunately, we just don't know exactly how kratom is metabolized (other than by your liver enzymes, of course). The reason for this is that kratom contains dozens of alkaloids that contribute to it's effects. This is also why different strains have different effects. Some of the more well-known active components, like 7-hydroxymitragynine, have been studied, Some have been found to be mu opioid agonists, others kappa-agonists, and some opioid antagonists.

6. What are good ways to increase bioavailability and what is the bioavailability of sublingual and oral ROAs?
Most (including myself) will recommend eating kratom on an empty stomach. I, any many others, experience an enhanced high after eating 40-60 minutes after taking the kratom. You can't snort kratom. You can smoke it, but it wastes quite a lot of leaf, and doesn't get you as far. Kratom tinctures can be taken sublingually, but they're usually made with 99% ethanol, and that shit will probably burn your tongue. Other methods of increasing bioavailability are ones that you mentioned already, grapefruit juice, tumeric, basically anything that will inhibit the CYP3A4 enzyme, because many of the active metabolites are opiates.

 

[gingerbaker]

So 3A4 (and 2D6..?) seems to be the primary enzyme responsible for metabolizing Kratom?
Does Kratom seem to have any pro-drug effects where enzymatic inhibition would be counter-productive?

Also, what about the whole lemon juice thing I have seen where you consume kratom mixed in lemon juice? Is this just a pH thing (if so, it seems strange since the stomach should be more acidic than lemon juice)?