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Does kava upregulate gaba receptors?

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Buddhacide

Kava Enthusiast
I believe a lot of stimulants upregulate as well, speed and what not.

Sure would be nice if these goddamn benzos Ive been on for a decade did.
 

yepimonfire

Kava Enthusiast
No they don't. I've been on pharmaceutical "speed" for ADHD and it down regulates the shit out of them, going off of them everything seems bleak and uninteresting and you can't focus. Stimulants do upregulate gaba as a compensatory measure, but this isn't exactly a good thing because part of amphetamine wd depression is caused by a giant gaba rebound.


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yepimonfire

Kava Enthusiast
A good rule of thumb is that if a drug has an effect on a particular neurotransmitter, the receptors or the brains production of that neurotransmitter is downregulated to compensate. Several drugs that agonize a particular system will cause opposing neurotransmitters to upregulate with repeat drug administration to try and reach homeostasis again. Take a benzo, and gaba receptors start "pruning" themselves and gaba production in the brain stops. Glutamate receptors and glutamate production increases to try and offset the memory problems. Drink coffee and adenosine receptors upregulate and the brain starts producing more adenosine and gaba to try and counter the coffees antagonistic effects on it, strangely, coffee also upregulates serotonin production as well.
 

Akava

Kava Enthusiast
But if its an enzyme inhibitor it would be different? Or would you then just stop producing the chemical to begin with?
(We're all such neurochemistry nerds)

And if kava did up-regulate Gaba does that mean the effects are permanent, because that would be awesome...
 

yepimonfire

Kava Enthusiast
The one enzyme kava inhibits is maob, it binds to it and renders it ineffective until the kavain is metabolized. I'm sort of confused what you're asking. Permanent yes, in the sense that if you have down regulated the receptors it apparently upregulates them until you down regulate them again. The body will always go for homeostasis, so having upregulated gaba receptors and more gaba than you're genetically coded for, will result in down regulation to normal levels. This also explains kavas shield effect. gaba remains upregulated for a time after kava has obviously worn off.
 

Akava

Kava Enthusiast
By permanent I mean if you drink a lot of kava and then stop you'll have higher gaba for the rest of your life? (Notice how kava and gaba sound similar)
 

Buddhacide

Kava Enthusiast
Just to play devils advocate, amphetamines, cocaine, and other stimulants do have documented upregulation effects - in addition to down regulation. Do a quick google search if your interested. I'm on my phone or I'd post some links.

Here's a quick one.

http://www.ncbi.nlm.nih.gov/m/pubmed/1816575/

Something else

http://onlinelibrary.wiley.com/doi/...sCustomisedMessage=&userIsAuthenticated=false

Seems to depend on what area of the DA system is involved and the amounts used. As an ex user myself, there is no doubt long term abuse causes the sort of sensitivity consistent with up-regulation. I am incredibly sensitive to stimulants these days. Even coffee I have to be careful with.
 
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R

Rusty Shackleford

Benzodiazepine withdrawal is far, far worse than phenibut withdrawal. I've experienced both and for me, phenibut withdrawal was a walk in the park in comparison.
 

Calpurrnia

Newbie
to keep this brief and to the point!

I've noticed Kava can highly potentiate opiates/opioids/phenibut/baclofen and some of the sedative qualities of many antihistamines (diaphenhydramine/bendryl)

source: to be immodest . . . my own anecdotal accounts and several graduate level chemistry classes with a fabulous professor who lives in many of the islands kava comes from during summer months

also to conclude . . .( i called this brief?! /scoff ) there are usually unpleasant side affects to this form of potentiation . . . aka dizziness, severe diarrhea and nervousness. . .
 
D

Deleted User01

I always go back to the simple adage, moderation in everything. I'm sure Kava does potentiate phenibut as it does an ice cold beer. I know Yepimonfire has been trying to find the right combo that makes him feel right (aren't we all). If a little Phenibut and a little Kava does it, then go for it. Whatever the side effects of Phenibut, they can't be as bad as heavy doses of Benzos and it is certainly not as bad as going thru life feeling miserable. Just take as much as you need and no more and watch out for that addiction thing. And as usual, keep us posted.
 

yepimonfire

Kava Enthusiast
Yeah, i hate benzos. Phenibut is like a stimulating version of a benzo, and instead of dulling your cognition, it actually enhances it. I can take phenibut and continue to work, lift weights at the gym, etc etc. Benzos make me feel anhedonic and i almost want to sleep, i feel dull and my memory is terrible, even on tiny 2 mg valium. I am currently tapering the phenibut, as i feel i don't need it on a daily basis anymore. down to 6.5g from 8g, i drop 500mg every 2-3 days. No ill effects.
 
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Deleted User01

Yepi old boy, when I first started using Kava, I would hold it under my tongue for a while so that it would absorb. I was also squeezing gelatin caps under my tongue for the same purpose. Have you ever done that with Phenibut? I guess I need to ask Chris if he has ever chewed a wad of fresh AWA and held it under his tongue for an instant effect. You know the old chewing tobacco commercial, "But a wad between your cheek and tongue and it sho is relaxin".
 

Nihilist

Kava Enthusiast
After drinking only a small amount of kava the night before, I had some phenibut at less then my normal dosage, and I noticed the effects were way more pronounced and needless to say I didn't even take the full amount I usually do and even felt like what I took was too much. Normally I don't even feel the phenibut but it still exerts it therapeutic anxiolytic actions. I was not under the influence of kava at this time. I also noticed even 2mg valium (a very low dose) made me totally unable to function after a night of kava.


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Had to post because of the dark fortress album cover.
 

yepimonfire

Kava Enthusiast
Yepi old boy, when I first started using Kava, I would hold it under my tongue for a while so that it would absorb. I was also squeezing gelatin caps under my tongue for the same purpose. Have you ever done that with Phenibut? I guess I need to ask Chris if he has ever chewed a wad of fresh AWA and held it under his tongue for an instant effect. You know the old chewing tobacco commercial, "But a wad between your cheek and tongue and it sho is relaxin".
Nope, it's extremely bitter. People claim phenibut takes hours to kick in but I don't really feel it does.


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Dustin

Kava Curious
After drinking only a small amount of kava the night before, I had some phenibut at less then my normal dosage, and I noticed the effects were way more pronounced and needless to say I didn't even take the full amount I usually do and even felt like what I took was too much. Normally I don't even feel the phenibut but it still exerts it therapeutic anxiolytic actions. I was not under the influence of kava at this time. I also noticed even 2mg valium (a very low dose) made me totally unable to function after a night of kava.


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Any Gabaergic is gonna hit you hard when combined with another. Doesn't matter if one's Gaba-a and one's Gaba-b or even sodium channel for that matter. I also don't wanna preach, but be reeeally careful with phenibut, the effects aren't worth the withdrawals. If it was more like kava and you could have it daily without problems then it would be a godsend to people, but unfortunately tolerance develops to that stuff faster than anything on the planet it seems. Twice a week is the max with phenibut. I'd just stick with kava quite frankly. I've been down the phenibut magical yellow brick road and it ended up as a wasteland with a road strewn with glass. Anyways, you probably already know this, but thought I'd say it anyways. Even every other day you'll eventually start having increased anxiety and sleep problems on the off day. It's just not worth it. The half life is only 5 hours but there's gotta be other active metabolites that keep your Gaba-b's active because there's no other explanation for the rapid tolerance. And 500mg a day reduction isn't noticeable at first if your at, say 3 grams, but when you get down to 1 gram and then 500 and then none, your gonna feel it man. Then what? Benzo's? Check out "another phenibut casualty" on mindandmuscle.net...it's just not that easy. The longer your on it, the worse it's gonna be. It's not just one week of withdrawals and then your okay, it lasts much longer. Not benzo long, but long enough. Also, at higher amounts it starts hitting Gaba-a as well. Now your having to get Gaba-a back to normal as well as Gaba-b. Higher than that and it affects dopamine. You'll start to have to dose multiple times a day (if you don't already) because otherwise you can't sleep and get anxious at night. When you have to take large amounts in the evening as well, the dopamine will keep you up. It's gonna turn into a trainwreck dude, trust me. Better try to find an alternative, a kava that's uplifting and not too sedating, and get off now. You can't take it forever, that just doesn't happen. Last but not least, it's not gonna be legal much longer.
 
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yepimonfire

Kava Enthusiast
Any Gabaergic is gonna hit you hard when combined with another. Doesn't matter if one's Gaba-a and one's Gaba-b or even sodium channel for that matter. I also don't wanna preach, but be reeeally careful with phenibut, the effects aren't worth the withdrawals. If it was more like kava and you could have it daily without problems then it would be a godsend to people, but unfortunately tolerance develops to that stuff faster than anything on the planet it seems. Twice a week is the max with phenibut. I'd just stick with kava quite frankly. I've been down the phenibut magical yellow brick road and it ended up as a wasteland with a road strewn with glass. Anyways, you probably already know this, but thought I'd say it anyways. Even every other day you'll eventually start having increased anxiety and sleep problems on the off day. It's just not worth it. The half life is only 5 hours but there's gotta be other active metabolites that keep your Gaba-b's active because there's no other explanation for the rapid tolerance. And 500mg a day reduction isn't noticeable at first if your at, say 3 grams, but when you get down to 1 gram and then 500 and then none, your gonna feel it man. Then what? Benzo's? Check out "another phenibut casualty" on mindandmuscle.net...it's just not that easy. The longer your on it, the worse it's gonna be. It's not just one week of withdrawals and then your okay, it lasts much longer. Not benzo long, but long enough. Also, at higher amounts it starts hitting Gaba-a as well. Now your having to get Gaba-a back to normal as well as Gaba-b. Higher than that and it affects dopamine. You'll start to have to dose multiple times a day (if you don't already) because otherwise you can't sleep and get anxious at night. When you have to take large amounts in the evening as well, the dopamine will keep you up. It's gonna turn into a trainwreck dude, trust me. Better try to find an alternative, a kava that's uplifting and not too sedating, and get off now. You can't take it forever, that just doesn't happen. Last but not least, it's not gonna be legal much longer.
Your last sentence is one of the reasons I'm tapering off it. I'm down from 8g to 6 now. I'm tapering by 500mg every three days. Yeah I agree there has to be something more going on then just a 5hr half life because it takes almost 3 days to start to feel the drop in dose. Also why I only needed to dose it at night. How did you get off it? Dose? I have benzodiazepines on hand if needed. Takes several weeks to develop tolerance/dependence on them from what I hear.

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Dustin

Kava Curious
Your last sentence is one of the reasons I'm tapering off it. I'm down from 8g to 6 now. I'm tapering by 500mg every three days. Yeah I agree there has to be something more going on then just a 5hr half life because it takes almost 3 days to start to feel the drop in dose. Also why I only needed to dose it at night. How did you get off it? Dose? I have benzodiazepines on hand if needed. Takes several weeks to develop tolerance/dependence on them from what I hear.

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Glad to hear that your tapering off. It can start to get rough on your organs at higher amounts. Wow, 6-8 grams in the evening would keep me up from the dopamine. I was at 6 grams at the most and had been taking it over a year. I'm still tapering actually, I'm at 3 grams now. I have to go pretty slow because I have chronic myofascial pain (chronic muscle pain and trigger points [nasty knots]) in my back and legs. So being that phenibut is a Gaba-b agonist with muscle relaxing properties, tapering off gives my muscles hell. It's pretty damn painful. Robaxin is the only thing I've found that helps it some. Soma would help even more, but docs don't wanna prescribe it anymore. Ya, your right about the 3rd day, I start to feel it some at the end of the 2nd day. If your comfortable at 500mg every 3 days then keep with it, but it takes a week to get over the worst of a reduction. Also, as you get lower, I'd recommend reducing by smaller amounts because you start to feel it a lot more as you get lower. I've tapered off methadone twice because I took it before and after my back surgeries and it was definitely harder as I got lower. The last drop is always the worst. It really comes down to how you feel though, there's really no one single method. It affects everyone differently. There's a few supplements you can take to help also, with kava being the most effective aid (other than benzo's). The thing about kava and benzos though is that phenibut supposedly affects Gaba-a receptors also at higher amounts. So taking them a lot, IF that's true that it affects Gaba-a, wouldn't allow your Gaba-a's to recover. I use them anyways if needed, but try to keep it to a minimum. Also, different benzo's develop tolerance issues (and tolerance means withdrawals when you stop) at different rates, so it depends on which ones you use. Phenibut affects dopamine also at higher amounts, so as you get lower I'd start taking some L-tyrosine/phenylalanine to help with that. GABA (the supplement) with some vitamin b6 can help too some. L-theanine can help, at higher amounts, with anxiety/irritability also. Not a benzo, but I noticed it helps a little. Or IF you need a benzo, maybe do half the amount you need of it with a gram of L-theanine and keep the benzo use down lower. Taurine also helps, supposedly, get your Gaba receptors back to normal quicker. DXM, in cold medicines, is a NMDA antagonist and can help with sleep some (at normal dosages) because glutamate goes out of wack when you have GABA issues from tapering. This (glutamate) is what makes it hard to sleep and causes restlessness. Magnesium glycinate is also a weak NMDA antagonist and works good with the DXM. Not sure how good daily use of DXM is, so I try to take it only when needed. A good place to get tips is mindandmuscle.net (the "another phenibut casualty" forum). It's like 60-some odd pages long. If you have any questions or need any advice, there's always someone who can help.
 
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yepimonfire

Kava Enthusiast
I have found no cross tolerance between benzos and phenibut, 2mg diazepam knocks me on my ass, I tried to jump the phen down too fast and had a massive panic attack at the grocery, took a valium and it stopped it, also made me sleepy, and very spacey and all the other nasty benzo traits. It's only rumored phen hits gaba a, there isn't a lot of real info on it honestly. All we know for sure is it is indeed a gaba B agonist. I've also considered the DXM idea. What dose would I need? I know at high enough doses it can make you trip and I certainly want to avoid that. I think I'm gonna stay at 6g for about three more days as I really have been feeling it. I don't remember exactly how many days I've been at 6g but its atleast been 2. Today was bad before my phen dose. Took it at 1pm. I was taking it at night but have switched to early afternoon so I don't have to deal with wds all afternoon like usual. No difficulty sleeping at all. I could probably ride the wds out on kava but enough kava and I can't function. I lift weights and train almost daily and kava would wreak havoc on that due to the powerful sedative effects it has. What makes you think phen will not be legal for long?
Btw, read through the m&m thread long ago.

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Dustin

Kava Curious
Ya, etizolam works fine with me too. Just thought I'd mention it though. As far as DXM goes, just the recommended therapeutic dose (30 mg I believe). It won't knock you out, but should make it much more likely to sleep. Ya, I find a week to be a good time period to go with, otherwise your not over the last one and already starting another drop. I'd recommend dividing up your amounts, morning and evening, to avoid that withdrawal period. You'll have two weaker inter-dose withdrawal periods instead of one twice as worse one. I know I had to do that bc I took it mornings and that period before it finally kicked in reeeeally sucks and I was having trouble sleeping. Some guys divide it up into small amounts every six hours. With kava I think it's DHM that causes a lot of the muscle weakness, so maybe try out a really low DHM type. Much less sedating also that way. I just got some of BKH's Melo Melo to try out and a Hawaiian someone recommended, both with low DHM. The phenibut legality issue is partly just that it's already listed as a chemical of concern by the DEA. I mean ya, salvia has been on the list for years, but people aren't getting dependent and having withdrawals from salvia. I'm not saying its definitely gonna be banned this year or anything, but I just have a feeling it, and K@, are gonna go within the next 2 or 3 years at the most. There's no super rush to get off right now, so if your having trouble with it, then I'd slow down the taper. But knowing that it's not gonna be too long before it's gone motivates me to not quit tapering, although I'm going pretty slow.
 
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