Misc Fun with GABA agonists

[Jug]

Hi all.
I recently started taking Baclofen for Depression and it helps heaps. Only problem is I have a bad tolerance to it and I'm taking twice the amount of the official recommended dose.
I'm thinking of trying a similar agent like.
Tiagabine
Vigabatrin

Pregablin but I'm pretty sure it would have a complete cross tolerance from the Baclofen wouldn't I?

Also do you thing things like l- Glutamine, Valerian, L-theanine, KAVA, taurine would reduce tolerance or potentiate or anything?

Do any of you guys like these things or could you recommend anything else similar?

Regards

 

[R(x)AGE]

are you taking 160mg? (as in the 80mg recommended max?)

I am also taking baclofen, albeit not for depression. However, I do struggle very much with depressive symptoms. I am on a very minimal daily dose and I often find myself needing to take more than prescribed per day. I was glad to read that it is not just me! I am not sure about baclofen's efficacy for depression, have you tried more first line treatments including some other more conventional psychotropics. In my experience baclofen may help depression, however at the same time it seems risky to use it for that purpose, I would seriously try to add something that is better suited for depression, however if baclofen works why fuck with things. Your depression is none of my business.

I am concerned with your use of baclofen. In my case I use it intended to serve as a sedative somewhat (and the added gaba action); my prescription cannot sustain misuse lol, anyways, i often have to take days off of baclofen in which i rely on marijauna and sometimes benzos however i am weary about benzos, i am much more comfertable with baclofen. I have taken them together and it was good. not my cup of tea, because i might as well just take lots of benzos or only take baclofen, and because baclofen is not as rough I choose it. I am always deliberating this. I can say that it might help, however you might abandon the baclofen lol, so you should probably just take baclofen. LOL. Im not telling you what to do, this is my opinion, you can take this as advice or something else.

However, as Znegative points out below, benzos and baclofen might work on different receptors or in that case, gabba pentin, so the use of benzos shouldn't target the same site as baclofen however, taken together the effects are synergistic. and with gabbapentin and lyrica not targeting a or b, and both not having cross tolerance with the other is pretty good to know! here is a chart from wikipedia (GABA page) that really helped me see which drug targets which receptor and this way you maybe able to generally infer (watch out though, there are logical problems here) which would interact and cause cross tolerance. and while I notice many of the ones you mention below, I wonder if you already have made reference to this: (http://en.wikipedia.org/wiki/GABA)
(notice the a/b receptor ligands)

GABAa receptor ligands
Agonists/Positive allosteric modulators: ethanol, barbiturates, benzodiazepines, carisoprodol, chloral hydrate, etaqualone, etomidate, glutethimide, kava, methaqualone, muscimol, neuroactive steroids, z-drugs, propofol, scullcap, valerian, volatile/inhaled anaesthetics.
Antagonists/Negative allosteric modulators: bicuculline, cicutoxin, flumazenil, furosemide, gabazine, oenanthotoxin, picrotoxin, Ro15-4513, thujone.

GABAb receptor ligands
Agonists: baclofen, GBL, propofol, GHB, phenibut.
Antagonists: phaclofen, saclofen.
GABA reuptake inhibitors: deramciclane, hyperforin, tiagabine.
GABA-transaminase inhibitors: gabaculine, phenelzine, valproate, vigabatrin, Lemon balm (Melissa officinalis).
GABA analogues: pregabalin, gabapentin.
Others: GABA (itself), L-glutamine, picamilon, progabide, tetanospasmin.

 

[Psychedelic Jay]

You are toying with fire...

You can’t substain this without going into the void of no return.

You will need help getting off any of those long term.

 

[Znegative]

Baclofen effects GABA B if I'm correct, so I don't think Pregabalin would be effected by cross tolerance. Pregabalin and Gabapentin don't actually directly effect GABA A or B, it's through some indirect mechanism (strangely, I'm pretty sure gabapentin doesn't have a cross tolerance with Pregabalin and vice versa).

I honestly prefer Gabapentin, but I'm probably the odd man out with that opinion.

 

[R(x)AGE]

Is Gabapentin a good sedative? I am constantly searching for the substance that will strike the perfect balance. I need a sedative type substance that can keep me calm and relaxed at all times. I find relief from Cannabis. Benzos work, but are unsuitable because I just end up taking too much. Baclofen works somewhat and I don't take that much, but still more than prescribed, and it still is not as sedating as I would like, I want to have to make a conscious effort to keep my eyes open and my head up lol. I have serious hyper vigilance, irritability, stress, agression, anger etc. I have tried opiates and maybe my dose or substance was too low or weak (20mg oxy) it did not have the sedative effect I was hoping for, but it was not bad, just could have been more sedating lol. In addition to the fact that I would be beyond lucky to have an opiate prescribed for this, I think that may be dangerous due to the fact I am not trying to ease pain but am trying to get reallllllllly lazzzzyyy bc if I used opiates Id have to use higer than necessary doses. Perhaps I should try heroin, however it maybe dangerous. I have been considering things like, Gabapentin for over a year. I have mainly been considering barbiturates (seconal) however I have been unsuccessful having this prescribed. I am thinking about Soma however, I am not sure, this may be harder to come by than benzos, baclofen, gabapentin etc. In the past I have found serious relief from Ketamine, however I am unable to have this prescribed (I want a constant supply), So for that reason I am considering gabapentin. So, is it sedating? If not what should I look into. Thanks

 

[Hiltoniano]

How does that account for the calming affects of l theanine?

 

[RobotRipping]

benzos are gaba-a agonists as well, they enhance action at the gaba receptor. If they were antagonists i don't think we'd be using them for anxiety or sleep.

if l-theanine is a mild gaba-a agonist it will calm you down by enhancing the action at the gaba receptor which calms people down.

 

[tricomb]

sorry to be "that guy" but there really is nothing but trouble barking up the GABAergic tree.

 

[Psychedelic Jay]

sorry to be "that guy" but there really is nothing but trouble barking up the GABAergic tree.

Exactly

 

[AlphaMethylPhenyl]

Honestly its not just the fact that you are taking ever increasing doses of GABAergic drugs which scares me, its that you're treating your depression with something that only helps with depression when you get high off it. See someone who can prescribe you an actually effective medication and taper down your self-medicating GABAergic use to nothing. I can just about guarantee you you'll be happier, and will definitely be better off in the long-term.

See just your thread title pertains to the fact that you're using this substance to get high so that you can ward off depression, which always either leads to the person wising up and getting help or an ever-escalating drug use until they crash/overdose.

What you're doing is a very temporary solution.

Think about it this way: GABA, which neurotransmitter you're increasing with your drug use, largely shuts down parts of the brain. There is no form of pure depression I'm aware of which is caused by an over-activity of the brain which would necessitate a decrease in neuro-transmission. Ok, maybe your depression is caused by anxiety; I don't know. Its also possible that you have psychotic depression, which is oftentimes treated with anti-psychotics. We just don't know with the information you told us and we couldn't know what's truly going on anyways since we're just talking over the internet and importantly (most of us) aren't doctors. Self-medication, however, is something we can urge you to stop.

Ad I really suggest seeing a psychiatrist if you really think you have a legitimate disorder. Even a therapist.

 

[RobotRipping]

^+1

most gabaergics cause depression over time. The only exception (with little evidence still) may be etizolam. I know when i was on benzos everyday i became depressed.

our understanding of depression is so limited, in some cases like PTSD, baclofen was shown to help depression. For many others (anecdotal and a few studies) show that baclofen causes depression. I don't know if seeing a psychiatrist would even help, they are heavily oriented to view depression and anxiety as a result of chemical imbalances and will just prescribe you medication after medication. Most psychs prescribe meds based on their own understanding of the brain, so a psych specializing in anxiety disorders may prescribe you benzos, while others will prescribe SNRIs or whatever and others will just throw you on stimulants or anti-psychotics.

Therapy is much more effective in helping you deal with depression, not a cure by any means but it will help you deal with it better if nothing else.

 

[Znegative]

Excuse my last post as it didn't really pertain to the main issue here. I was just trying to say that you need to be careful with Baclofen because it acts upon GABA B, just like GHB and I believe Phenibut and a few others. However, AFAIK there are few really long acting GABA B agonists around that could help one to detox-you'd probably have to use Baclofen to do it, or maybe Phenibut.

Gabapentin is a better choice (IME and IMO) as a GABAergic to be used for your purposes, simply because it takes a long time to become dependent, and you would have to not only be taking it for a long time, but also taking very high dosages. (I took dosages of 1200mg-4000mg/day for seven months and quit cold turkey with no problems. However, I've heard others have had some bad withdrawal experiences from the drug, so don't think I'm saying its 'non-habit forming') 300mg-600mg/day is the best dose for Gabapentin IMO because its low enough that tolerance never becomes such an issue that it renders the drugs effects useless, and also because if you do take super high dosages of Gabapentin, less and less will be absorbed (For Example, say you consume 900mg of Gabapentin-the BA is around 60%. If you take 1.2grams, the BA drops to 47%. If you take 4.8grams, the BA is only 27%, meaning that of the dose of 4.8g's, only 1,300mg was absorbed).

Anyway, I'll just join the choir and warn you not to get yourself over your head in GABAergic drugs. I was so arrogant for so long, thinking that I'd never get really bad withdrawals, or that I could allow myself to binge for a few weeks and then go back to my measly 1mg dose of Clonazepam and feel just fine. I'm not saying you're arrogant, I'm just warning you that if you have those types of rationalizations playing through your head, don't kid yourself. For me and most others who've been through it, Benzo withdrawal is not something one would wish on their enemy.

 

[DexyDevil]

I highly reccomend Lyrica (Pregabalin). Oddly enough it doesn't have any direct effect on GABA. It is a very strange substance because it can be used in place of other GABA agonists (benzos, baclofen) without experiencing withdrawal but only Pregabalin can prevent Pregabalin withdrawal.

It has many applications, lifting and stabilizing mood, relaxing yet increasing energy. Basically, it's the shit.

 

[benzoheadplus44]

Is Gabapentin a good sedative? I am constantly searching for the substance that will strike the perfect balance. I need a sedative type substance that can keep me calm and relaxed at all times. I find relief from Cannabis. Benzos work, but are unsuitable because I just end up taking too much. Baclofen works somewhat and I don't take that much, but still more than prescribed, and it still is not as sedating as I would like, I want to have to make a conscious effort to keep my eyes open and my head up lol. I have serious hyper vigilance, irritability, stress, agression, anger etc. I have tried opiates and maybe my dose or substance was too low or weak (20mg oxy) it did not have the sedative effect I was hoping for, but it was not bad, just could have been more sedating lol. In addition to the fact that I would be beyond lucky to have an opiate prescribed for this, I think that may be dangerous due to the fact I am not trying to ease pain but am trying to get reallllllllly lazzzzyyy bc if I used opiates Id have to use higer than necessary doses. Perhaps I should try heroin, however it maybe dangerous. I have been considering things like, Gabapentin for over a year. I have mainly been considering barbiturates (seconal) however I have been unsuccessful having this prescribed. I am thinking about Soma however, I am not sure, this may be harder to come by than benzos, baclofen, gabapentin etc. In the past I have found serious relief from Ketamine, however I am unable to have this prescribed (I want a constant supply), So for that reason I am considering gabapentin. So, is it sedating? If not what should I look into. Thanks

i use 32 or 24mg and an hr later eat my benzo army....

l am a speed freak rx dex tabs... use 100 to 190mg ish a day rxed 20 qid,, so it helps me take an edge off... and save my benzos... valium i cant help but take 50 tbhen 40 then 40... while i get only 20 bid... it helps but the valium is very euphoric.. i have a few now i got lorazepam maybe kpins soon to help... ii used xanax in my four locos yesterday smoked out of an apple and the speed just left me holdin on to reality but i was taking bars with val in booze all day... the best benzo combo for me 60mg val and two bars with 60mg dex.... couple kpins to last the entire time be nice... i am going for temazies soon here now... love them...

 

[benzoheadplus44]

I highly reccomend Lyrica (Pregabalin). Oddly enough it doesn't have any direct effect on GABA. It is a very strange substance because it can be used in place of other GABA agonists (benzos, baclofen) without experiencing withdrawal but only Pregabalin can prevent Pregabalin withdrawal.

It has many applications, lifting and stabilizing mood, relaxing yet increasing energy. Basically, it's the shit.

im getting lyrica too they think i have fibromayalgia whiich i may.... ill abuse it is it generic yet...

 

[xxxyyy]

no, pregabalin is available only as pfizer-manufactured lyrica.
also i have to add that baclofen is one of the nastiest fucking substances to develop a dependence to. it's not addictive per se, not moreso than say, venlafaxine, and it's even more unpleasant to withdraw from. i'd be very careful with it, GABAb agonists seem even worse in withdrawal than the GABAa ones. if you discontinue it, slowly titrate down.

 

[xxxyyy]

Baclofen effects GABA B if I'm correct, so I don't think Pregabalin would be effected by cross tolerance. Pregabalin and Gabapentin don't actually directly effect GABA A or B, it's through some indirect mechanism (strangely, I'm pretty sure gabapentin doesn't have a cross tolerance with Pregabalin and vice versa).

I honestly prefer Gabapentin, but I'm probably the odd man out with that opinion.

well, i can't cite anything definitive on the subject, but in my experience they share significant cross-tolerance. their effects are notably different for me.

i should mention that baclofen is one of the nastiest substances to ever get dependent on. it's very similar to GHB, except that GHB is actually fun. for some reason GABAb agonists work exceptionally well for GABAa WD, however vice versa the same thing isn't true. baclofen even taken short term (say, 10 days) will produce a pronounced and highly unpleasant withdrawal syndrome. no matter the dosage you're taking, if you take it daily for any extended period physical dependence will follow. i'd recommend sticking to GHB instead, it is a lot more fun and having experienced withdrawal from both drugs i can safely say that both are just about equally nightmarish to withdraw from.

 

[RobotRipping]

^from what i hear phenibut is just as nasty and even the GHB horror stories i've read are just as concerning. Alcohol withdrawal is terrible as well, so i think there's some merit to what you're saying. I can't imagine something worse than a GABA-A agonist withdrawal and if GABA-B agonists are worse, then i wish those dependent on them the absolute best. I'd rather kill myself than go through a benzo withdrawal again.

 

[Mercc96]

im getting lyrica too they think i have fibromayalgia whiich i may.... ill abuse it is it generic yet...

I have fibromyalgia and was on lyrica for a good couple years (at the same time as abusing other Gabagernics/opiods/stimulants and so on) but I really really suggest that you do not try to abuse your lyrica script if you are actually prescribed it for fibromyalgia. It shoots your tolerance up almost every time you try to get a buzz of it due to already having a tolerance having to use it everyday. So for me being on max dose , if i wanted to get a buzz of it i would have to use several grams of it. Even then it was hardly a good buzz, but the problems came after. The next day my prescribed dose was basically useless and stayed that way for quite a while. Lyrica is also terrible for the cognitive defects and weight gain that those with fibromyalgia already experience. Both my rheaumatologist , my doctor and many other people I have spoken to agree that Lyrica and Gabapentin are actually not that desireable to be on for fibromyalgia.

 

[xxxyyy]

^from what i hear phenibut is just as nasty and even the GHB horror stories i've read are just as concerning. Alcohol withdrawal is terrible as well, so i think there's some merit to what you're saying. I can't imagine something worse than a GABA-A agonist withdrawal and if GABA-B agonists are worse, then i wish those dependent on them the absolute best. I'd rather kill myself than go through a benzo withdrawal again.

yes. alcohol and benzo withdrawal are without a doubt really horrible, however i'd take either one any day over either baclofen or GHB WD. i don't have any experience with phenibut WD, but based on my experiences with the aforementioned drugs i plan on never, ever finding out. what makes GABAb agonist withdrawal more horrible than any other drug i had the misfortune/stupidity to get dependent on is that nothing truly helps except more GABAb agonists. i know that no one plans on getting addicted, but believe me, a raging smack habit is preferable, and unless nothing else truly helps i recommend staying far the fuck away from taking baclofen daily.