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Phenibut onset time and metabolism

I might be wrong, but as I understand it, Baclofen (and phenibut) doesn't cause a "dopamine rebound effect" as GHB does.

With GHB, dopamine release is caused by stimulation of the GHB receptor. Baclofen (and phenibut) doesn't have any affinity for that site, only for GABA-b.

About GHB:
"Activation of both the GHB receptor and GABA(B) is responsible for the addictive profile of GHB. GHB's effect on dopamine release is biphasic.[68] Low concentrations stimulate dopamine release via the GHB receptor.[69] Higher concentrations inhibit dopamine release via GABA(B) receptors as do other GABA(B) agonists such as baclofen and phenibut.[70] After an initial phase of inhibition, dopamine release is then increased via the GHB receptor."
from wiki

And about baclofen:
"Baclofen produces its effects by activating the GABAB receptor, similar to the drug GHB which also activates this receptor and shares some of its effects. However, baclofen does not have significant affinity for the GHB receptor, and has no known abuse potential.[12] The modulation of the GABAB receptor is what produces baclofen's range of therapeutic properties."
 
In terms of subjective effects, phenibut had a very odd and biphasic modus operandi when it comes to sedation. Around 45 minutes after taking it, drowsiness, anxiolysis and mild ataxia begin to set in. This tapers after around 3 hours giving a couple of hours of apparent baseline. However, the effects reemerge, and generally seem to be the emotional plasticity we're all familiar with from EtOH, as well as some decline in motor skills. Also, nausea and vomiting usually took place around 15 hours of dosing

Based on my experience, I can conjecture that Phenibut has some form of active metabolite that forms after first pass metabolism. Of course, my experience is only my experience, and I only took it about 6 times
 
I completely forgot about this thread and conducting the above experiment. Have any of yall heard of phenibut free amino acid? It's supposed to have a neutral pH and supposedly suitable for sublingual use, which is supposedly three times as strong.

Could this version make the onset time less than two hours? I think I may try snorting some, but I don't think I can get over the stigma of plugging the solution.

I can't find any information online about this and no chemical formula. I emailed the supplier and asked for a chemical name along with a NMR report.
 
From Experience
Sublingual: 2-3h quite effective but only recommended if you can get phenibut free amino acid(I didn't)
Ingestion: 3-6h depending on stomach contents

@Brutus it's not unreasonable to suspect(considering various compounds similar to phenibut) that inhibiting phenibut absorption by increasing it's pH could extend the trip and make it stronger. This comes with the assumption that the onset will also be extended.
 
Sorry - but what is the urgency with the onset? It usually only takes ~30 mins when I'm fresh on tolerance & have the plain ole goodness.

And Baclofen is dwarfed by Phenibut. Don't let the prescription status fool you.
 
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From my experience taking the drug phenibut can metabolize quicker depending on your batch(probably to do with pH). Typically onset is at least 2h but I've also come up in about 30 minutes a few times though having dosed phenibut hundreds of times I've found this to be a fairly rare with no conclusive evidence of causation. Baclofen is not dwarfed by phenibut unless you enjoy body load.
 
Isn't the issue that the phenylring of phenibut makes it relatively lipophilic so that it gets 'stuck' in places before enough arrives in the brain? Or that the acid function slows down BBB transport?
I doubt that what is available is the freebase, if that were true why does it dissolve well in water? Err that is inconsistent with what I just said, but it is inconsistent to me anyway.
A reason why it could sometimes be absorbed quicker may be due to administration together with food? Of course it may matter whether the food is fatty or not.

I'm not really saying these things, I am asking. :)
 
As far as baclofen goes, IMO it has absolutely ZERO abuse or recreational potential.

The only possible use for it other than as a myorelaxant, that I can imagine, is to treat GHB withdrawal.
 
If it´s fat soluble could a mix with Lecithin or maybe Propylene Glycol make it´s absorption better/faster?
 
Rather than make my own thread I searched and found the latest on phenibut..

Can anyone tell me if Phenibut makes its way into the G.I tract at all, or is it all metabolized in the stomach and such?

I ask because I've recently developed some gastrointestinal issues and aside from being afflicted by some kind of pathogen that I'll need to go and get antibiotics for, I thought maybe perhaps due to Phenibuts acidic nature it has somehow damaged my intestines, is that even possible? I am aware common side effects listed include things like diarrhea etc, but this is more of an ongoing issue that persists even when not taking it.

I use about 4-6 grams per week, 2g-2g-2g days in a row of a morning, and then a break until the next week. My threshold dose is about 1.5g hence the 2g dosages.
Might be worth noting (or not) that I don't seem to be addicted to it or get withdrawal symptoms upon cessation of usage.

I abstained from using it for a couple of weeks but the GI issues persist, so I'll probably be going the doctor's about it soon, but if it is due to Phenibut I would like to know, as I know there's a FAA (Free-amino-acid) version available which apparently isn't acidic and hopefully wouldn't exacerbate the issue or cause it again in the future.


Thanks if anyone has any info.
 
phenibut does make its way through the gi tract but it is not really that acidic. withdrawal from it would quite reasonably cause gastric issues associated with rebound anxiety though.

taking it as a sodium salt (phenibut is already a free amino acid, sodium phenibut is the "less acid" version) won't really make much of a difference - aside from increasing your daily sodium loading which is not something most people need, the acid in your stomach is going to do a really good job at putting protons back on all the carboxylate groups (read: phenibut is regenerated as a free acid. strong acid liberates the weak acid from the salt).
 
sekio said:
phenibut does make its way through the gi tract but it is not really that acidic. withdrawal from it would quite reasonably cause gastric issues associated with rebound anxiety though.

taking it as a sodium salt (phenibut is already a free amino acid, sodium phenibut is the "less acid" version) won't really make much of a difference - aside from increasing your daily sodium loading which is not something most people need, the acid in your stomach is going to do a really good job at putting protons back on all the carboxylate groups (read: phenibut is regenerated as a free acid. strong acid liberates the weak acid from the salt).
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I see, so you don't think it could be the cause of GI issues?

I'll go into detail if anyone cares to read, too much information ahead:

Constipation, when I do pass, the stools are normal brown-coloured, but in hard separate 'chunks', there is a *lot* of mucous, however it does not cause any irritation of my anus like regular diarrhea does. At times I will pass only a chunk of mucous. It's clear/brown, however last week there was a fair amount of blood mixed in. This week there has been no blood, so I am hoping the issue is resolving itself, I was prescriped some stool-softener meds from my doctor, but the stools are still relatively hard chunks. The blood that was mixed in with the mucous wasn't particularly dark (from my own research indicating an issue further up the digestive system), but it wasn't bright red, perhaps due to being mixed in with the poopy-brown-mucuous.

I haven't had a fever or vomiting, and my stomach/abdomen hasn't been in pain, however when I am 'going', I can massage my abdomen which seems to help work things through and out. If it goes on any longer I'm going to have to make a trip to the doctor's office. Here's hoping it's not colon cancer or something.

Thanks again.
 
ebola? said:
How much water are you drinking? How much fiber are you eating?

ebola
Click to expand...

I figured out the cause to be just 500mg of bacopa monniera. Stopped it for a few weeks and started again, symptoms returned. Binned the bottle. Guess the stuff doesn't agree with me.

As for phenibut, it's addictive potential is so erratic and unpredictable that I was getting withdrawal symptoms after taking it only once or twice with a couple of weeks breaks in-between, causing very intense 'primal fear' feelings. Took almost 2 weeks of hell to get past that. I think i'm done with phenibut for a while.
 
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