Misc Fun with GABA agonists

[R(x)AGE]

hey xxxyyy, i am taking baclofen and i am worried because it is supposed to be a sedative however i am having to take increasing doses to achieve that effect, how does it sound if i was to cut the baclofen down slowly over a few days and i could take some of the benzos i have. should i start the benzos asap, or should i wait it out and talk to the dr, and either, have a dose increase, take depakote or gabapentin. however the most practical seems to be the xanax. and currently i have taken about 50mg and am not asleep, i am considering taking 10 -20 mg more or taking some benzos. but this is why i ask, idk what to do. i need to be sedated

 

[xxxyyy]

baclofen all in all is a pretty weak sedative especially when compared to other gabaergics like benzos. like with all gabaergics, tolerance is a major factor. your best bet is to slowly, slowly reduce the dosage, i once did a 10-day taper down from 250mg to 0 by cutting 25mg a day. it didn't help at all, at the end i was still in pretty horrible withdrawal. benzos will help with some of the more obnoxious withdrawal symptoms, like insomnia and horrible anxiety, and while handy to have around, but it's very easily to slip into another dependence from there, happened to me more than once. i've been juggling gabaergics for quite a while like this, and nothing good comes from it. i know advice like this is not very helpful, but alas gabaergics really fuck over your brain chemistry massively after a while, to the point of almost no return. after 10 years of gabaergic abuse i find it very, very difficult to go a few days without any, nevermind a week.
it could be argued that baclofen's lack of intoxicating effects is a good thing, but when i get horribly dependent on some chemical i at least want to get a decent high out of it.
as far as tapering the baclofen down goes, i'd say drop 10mg every 3-4 days. that is about the quickest you'll able to manage without significant discomfort.
it really depends on how long you've been taking it. the longest i ever took it continually was maybe 2 weeks or so, and even after that time it was fucking awful, but i never had the feeling i was inching dangerously close to full blown psychosis like i did during GHB withdrawal, but then i had been taking insanely high dosages of that for months, and not weeks.

 

[Jug]

I don't find it sedating but I'm an insomniac.

 

[Jug]

Well it definatly helps my depression / Anxiety but my doses are through the roof so I'm taking a break from it and just taking Clonaz for now unfortunatly I require 4mg's of clonaz to though

 

[Jug]

Thanks for the in depth reply, I'm currently taking a break from the Baclofen and am feeling good on Clonaz, unfortunatly I require 4mg's of Clonaz but that would be much less toxic then all that Baclofen. I will have to save up some $ before I can try those other GABAnergics.

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.
Thanks for the in depth reply. My psych prescribed it for anxiety but it definatly helps with my depression. But yeah I'm defiantly taking way to high a dose so I'm going to stay off the GABAergics for a while. I'm doing good on clonaz but I require 4mg's of that as well :/ Still probably less toxic then all that Baclofen. I will have to save up some $ before I can try those other GABA agents.

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.

 

[Jug]

Cool thanks for that I will put it on my list.

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.

 

[Jug]

Cheers, might have to get some theanine. do you reckon L-Glutamine (Glutamate) could help my situation?

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.

 

[buckethed]

Sorry to repeat what others have said but....

GABA agonists are nothing but trouble in the long term... They have very, very helpful uses in the short term (days - 2 weeks max) if you are trying to treat a clinical depression, or a psychosis, and even then need to be used with caution. The Z-drugs are also basically benzos in disguise (they are only different in that they are better at causing cancer, and better at become addictive than most benzos!).

Coming off GABA agonists is hell-on-earth. I have heard of opiate users saying thehy would rather do 10 heroin cold-turkeys than a single benzo detox!

They are (along with Alcohol) classed as CNS Depressants - the opposite to antidepressants. When I was taking a lot of prescribed Benzos, I managed to maintain a stable mood (with antidepressants!), but, I found that after reducing the dose of Benzos, I could stop my antidepressant and remain reasonably stable in mood, and also found that acute benzo withdrawals were quite similiar to an amphetamine high (with the euphoria, but with more anxiety than you would get from amphetamines).

Withdrawal from Benzos / GABA agonists should always be done slowly, under medical supervision, due to the risk of status epilepticus etc. I would always recommend a Diazepam taper for any benzo detox (switch over to Diaz then slowly taper). The rule is one month worth of detox for each year you have taken Benzos - but that is a 'tough' detox... I took about 8 months after 2 years of benzos. This was comfortable with minimal withdrawals.

Clonazepam / Klonopin / Rivotril apparently has GABA-A and GABA-B effects so a cautious cross-titration to Diazepam is recommended in case there are some withdrawals that aren't controlled by the Diazepam (no clinical papers supporting this but just be cautious).

Alcohol is very bad in combination with Benzos. If it doesn't kill you (which it can - as numerous Hollywood stars can attest to), then what it does do is develop RAPID tolerance to the benzos, making it much more difficult to come off in the long run. If you are addicted to benzos, the best thing to do is to stop alcohol completely, even if that means taking a bit more of the benzo, then once stabilised, start a slow taper.

It is worth coming off benzos - life will be better, happier, colours actually appear brighter, and so on (they are, after all, CNS depressants!).

 

[Jug]

My Psychiatrist has approved me taking up to 200mg's a day of Baclofen and without a GABA agent I can't get out of bed. But I guess I got to take the hard road and force myself out of bed or stay in bed and watch movies for a month or so.

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.

 

[Jug]

Thanks Mate

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.

 

[Jug]

Cheers all good info here. Fortunatly I don't get bad withdrawls but I might try and save the gaba's for social interactions and job interviews and just chill for a while.

No one mentioned if Glutamate or Glutamine could recover GABA cells though. I've done allot of research on it but know one really knows.

 

[xxxyyy]

Coming off GABA agonists is hell-on-earth. I have heard of opiate users saying thehy would rather do 10 heroin cold-turkeys than a single benzo detox!

i wholeheartedly agree with this

They are (along with Alcohol) classed as CNS Depressants - the opposite to antidepressants. When I was taking a lot of prescribed Benzos, I managed to maintain a stable mood (with antidepressants!), but, I found that after reducing the dose of Benzos, I could stop my antidepressant and remain reasonably stable in mood, and also found that acute benzo withdrawals were quite similiar to an amphetamine high (with the euphoria, but with more anxiety than you would get from amphetamines)

this is technically wrong. CNS depressant means the depressant (as in supressing) effect it has on the central nervous system wheras antidepressants are named for their efficacy in combating clinical depression, which are two very different things and not related to each other at all. in fact some antidepressants, like certain tricyclics, also have CNS depressant effects.

 

[buckethed]

I should have been more accurate; what I should say is that amongst CNS depressants, alcohol, benzos, z-drugs and most-GABAergic drugs
have depressogenic effects - increasing the risk of clinical depression; tricyclics on the other hand treat depression (that said, Amitripytline,
being the prototypical TCA, works well for depression is taken at night only, but, take it during the day and you do feel awful, almost
depressed due to the strange type of sedation it gives!)

 

[velmwend]

Have no probs with etiz and phenibut. Just have to be strict/responsible. if it stops, you stop.

 

[ShaunG]

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

Try Flexeril. Its a muscle relaxer, but holy shit. I sleep like a damn rock for 15 hours and I have a .5-1mg a day Xanax tolerance. I usually do not take my xanax if I take a Flexeril because I pass the fuck out before I can remember to take one. I do this when I drink too. I have enough Xanax in my system and do not take high enough doses to worry about missing one day, but if you are on higher doses of a benzo do not do this as Flexeril is supposed to lower seizure thresh hold so in combination with a little benzo WDs might not be good.

Out of all the pills I have taken for sleep, Flexeril probably made me sleep the best even over Ambien and what not. Maybe it has to do with the buildup on Xanax in my system mixing with it, but it knocks my friends and wife out too and they are not on benzos.

Let me add that Flexeril helped a lot with lowering my anxiety too. I was taking .25mg of Xanax a day at most when I was on Flexeril daily for back spasms. I was prescribed 10 mg 4x per day on the Flexeril, but usually only took one about 2 hours before bed. It takes about that long to kick in for me. The only negative was crazy lethargy the next day due to its long half life.

 

[RobotRipping]

Cheers, might have to get some theanine. do you reckon L-Glutamine (Glutamate) could help my situation?

i'm pretty sure that excess glutamate occurs during gaba withdrawal, so i definitely wouldn't add any more but maybe that's not the case with baclofen and not an issue if you're on clonazepam or baclofen. I don't really think any supplement will help once you've gone off into the deep end with gabaergics.

^flexeril is okay, it's a shitty muscle relaxer by all means but it's not bad when mixed with benzos, but that kind of defeats the purpose lol. Tolerance to it tho seems to rise rapidly, at least IME. First time with using it was good then couldn't get anything else out of it afterwards.