Thread: What's the deal with tiagabine and why don't we have more GAT1 inhibitors?

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    What's the deal with tiagabine and why don't we have more GAT1 inhibitors? 
    Bluelight Crew MagickalKat777's Avatar
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    Feb 2004
    Denver, CO
    So I know I'm probably going to get a lot of flack for posting this here but the members that post here are extraordinarily intelligent and I don't think this question can be answered in another forum... On top of that, we have multiple threads about using DXM to drop amphetamine and opiate tolerance and this was THE place to go when you wanted to know anything about MDPV or mephedrone... so yeah.

    I'm taking Gabitril as an adjunct therapy for benzodiazepines... Its crazy expensive (but Medicaid covers it) and it seems like a really complicated drug.

    My question - well I have a few...

    Many have compared it to GHB... I've never done GHB but I've abused Lyrica and I've been on benzos since 2004 (PD, GAD, Agoraphobia)... At 4mg this drug helps my anxiety a lot... But I'm curious about it for a number of reasons.

    First off, the pharmacological profile intrigues me. Secondly, the euphoria is nuts... its like a more sedating MDMA. Third, it hits faster than any pill I've ever taken - I'm ready to throw up within 5 minutes of taking it and it peaks within minutes. I'm not prone to getting sick from meds and other than that side effect, it seems relatively benign (although I would never drive on it, it makes me too tired, it doesn't really have any other side effects that I've noticed and those of you that know me, know that I get EVERY bad side effect from everything I take).

    My biggest curiosity... Chemically, its nothing like GHB yet it exerts GHB-like effects up to and including seizures, coma, and death in overdose. Its more sedating than the piperazine meds (trazodone and diphenhydramine being the biggest examples) and structurally... its confusing as hell how it even works. Maybe that's why there aren't more GAT1 inhibitors (although Saint John's Wort's adhyperformin is certainly an interesting case study)...

    So comparing it to benzos (which I can't do because I take the two together), I'm noticing that it GREATLY potentiates diazepam (never had euphoria from diaz before even when I was taking 60mg on a cross from 4mg of Klonopin)... but it lacks most of the side effects (except the blurry vision and somnolence)

    I have also noticed something that is really annoying - it makes you as dumb as topiramate although that effect goes away within an hour or two unlike topiramate which we call "Dope-A-Max" here because of just how stupid it makes you... But the structure doesn't lead me to believe its an AMP antagonist so that effect is curious...

    Its a really interesting drug... but why don't you hear about it more and why is vigabatrin, a much more toxic drug, preferred? I would think they would be handing this out like candy, especially considering that, besides Geodon before the 4 dollar offer came out, its by FAR the most expensive drug I've ever been put on... and its super effective for anxiety... And it doesn't potentiate alcohol or even have very many drug interactions period. Seems they would be doing a LOT of research into GAT1 inhibitors.

    Recreationally, I think I'd just fall asleep... but while it makes me dumb as fuck (note that I took 4mg about 30 minutes ago and I'm starting to ramble), its quite euphoric. I can tell you this, if its like GHB, I would totally love GHB...

    Anyway, back to my point. Are GAT1 inhibitors so rare or is it their abuse potential or is it something else that makes this such a rare drug? It seems highly effective...

    And I just officially got smacked off my rocker so I'll leave this at that. I'm just curious about this drug. Its certainly the most peculiar med I've ever had! And the rushes... Oh my god the rushes! Its like floating on your own personal cloud...

    A euphoric, non-addictive, GAT1 that costs a lot of money... why isn't it ever used?

    As for adhyperforin, I'm curious as well... What is it that makes these chemicals so special - and why aren't they being studied more?
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    Wow, Magicalkat, I'm right here with you, why don't we here more about this drug? I am a firm lover of pregabalin(lyrica) whichh works by speeding up the enzyme called glutamate decarboxylase that turns glutamic acid(Doule check that?maybe regular glutamate) into GABA, which in my belief besides opening ligand-gated ion channels as well so choride ions can flow, is purely what gives it's recreational effects. Anyways, me and many of my buddies consider this drug a longer lasting, dirtier but just as euphoric ghb(It's almost even more stimulating). So if this drug Tiagabine(sp?) is a GAT1 inhibitor, then the effects would be similar to preabalin in the sense that DNRI's(Coc, Dexmethylphenidate) feel similar to Amphetamines(specifically dex, and meth) which are potent monoamine releasers. Because the end result would be the build up of GABA due to the inhibition of re-uptake back into the cell. Pregabalin is a dirtier drug due to calcium channel actions, and ligand gated ion channel flooding I believe, but the end result is more GABA built up in the synapses, so same end result different mechanisms.

    So Magical, thankyou so much for this post I'm going to try to get my father(a physician) to call some in for me, as an alternative for pregabalin which I am dependent on 400mg a day, and maybe that will alleviate the withdrawals long enough to help me get off preg. Also preg's take almost 2 hours to fully kick in, this only takes 5 mins? That's all i need to hear, I will report back with experience.
    This thread was extremly interesting, and the effects you describe except sedation seem similar to GHB and high dose lyrica.

    Another similarity I notice is you say it makes you dumb?? This is a complaint I've heard from many using the gabapentin, pregabalin drug class, because someone smarter may chip in but i've read long term use of both drugs prevent new synapses from being formed in certain parts of the brain(does anyone no my memory sucks lol) so thats another shocking similarity.

    I think your reallly onto something here magic, b/c if this drug is what we think, it could be my miracle to help alleviate lyrica w/d and taper off, as well as many others. If anyone has anymore contributions to make me and magical wwould appreciate it greatly, once again thankyou magical!!! this is an awesome contribution to BL.

    PS> Is this drug scheduled in the United States?
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    Bluelighter Psychedelic Jay's Avatar
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    Jun 2009
    Houston, Texas
    No, it is not scheduled.

    You can be physically dependent on this drug. It creates indirect GABA agonism.
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    Bluelighter dopamimetic's Avatar
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    Mar 2013
    locked in emotions
    Ok, have been stumbling about this one before, but wasn't available in switzerland (but well showed that here in France they do sell it, ... .... would have thought it had more of an effect, as I have not much GABA tolerance, to benzo like drugs at least... pregabaline starts at 200mg and above... and so is that gabitril thingy. Two 5 mg tablets don't feel like much ... less than 10 mg's of valium, I'd say. Have been careful after reading these precautions, but well have to see...
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    Bluelighter atara's Avatar
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    Apr 2010
    not intended to diagnose, treat, cure, or prevent any disease
    Because every preceding GABAergic has had disastrous kindling convulsant withdrawal syndromes that shackle people to the drug for decades, causing long-term neurodegeneration and come with a list of long-term side-effects that looks like it was torn out of some homeless guy's anti-pharmaceutical-conglomerate manifesto? Because we don't need yet another addition to what is unquestionably the most damaging class of psychiatric drugs?

    Or perhaps because the goal of an anticonvulsant is not to produce a sublime sedative MDMA-tenored euphoria, but to prevent seizures?

    Or both?

    You'd have to be willfully ignorant or insane to abuse this stuff, is what I'm saying.
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    Bluelighter dopamimetic's Avatar
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    Mar 2013
    locked in emotions
    Very promising substance so far, from the medical side of view. An anxiolyte that is 150-200% as effective as Lorazepam ever has been (while staying conscious), widely unknown but the same time literally free of [short time] side effects ... I feel totally no influence on cognitive function, also no real tiredness, albeit it -is- easier to fall and stay asleep and think there is also some level of psychical lethargy that leads to let time pass by without feeling really bored..

    In conclusion, some similarities but also some very huge differencies (also the way how the anxiolysis feels - if this is possible, it has more of a much, much cleaner version of the pregabaline high- without the euphoria at that dosage, of course- than any GABAergic benzodiazepine, picamilon etc. I know).

    So, we'll see ... as an antiepileptic, this stuff is made to take for long time. I know chances are bad, but after Pregabalin and it's tolerance (day two requiring 1.5x dose) it can't get worse.

    (Edit: Interestingly, found this chem to be said to -not- increase the over-all gaba concentration in the brain. Also that it is probably only selectively active in some areas of the brain. Giving hope that it could really be superior to BZDs. The fact that patients convulsing on over-dosages of this response to low dose BZD treatment supports that too, indicating that there is no cross tolerance buildup.)

    Currently at 20-25mg/d, definitely active, anxiolytic, but "odd" / "trippy" in it's own, very emotionally neutral way. No sedation or effects on sleep, maybe intensified dreaming (well, probably quite a bit- getting these lucid moments again where I begin to know that I'm asleep and dreaming). Definitely some kind of not-bzd-benzo ...


    But yes... while I do always find it interesting (and to some point helpful - especially when it comes to what they don't write into the leaflets) to read "trip" reports, be it the successful or disaster kind ... regarding this drug, the one posted in this thread is the ONLY one where someone got euphoria off (over)dosing Tiagabine. Seems the dosage range between that and convulsions is VERY small, if it even exists in many. Don't try it.
    Last edited by dopamimetic; 15-08-2013 at 19:17.
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