Psycho-Babble Medication Thread 448915

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Re: Are any of these new GABA meds effective?

Posted by Willyee on January 28, 2005, at 0:02:13

In reply to Are any of these new GABA meds effective?, posted by 3 Beer Effect on January 27, 2005, at 21:17:24

> It has been a few years since i've been a regular poster on here so I've lost track of all these new GABA meds.
>
> I am always looking for a 3 Beer Effect type medication & sadly, have never found anything better than the 1.5 Beer Effect of Prozac or Zoloft 100 mg.
>
> The Benzos were a big dissapointment to me. They seem to have severe disadvantages of tolerance, dumbness "they are supposed to impair thinking & memory by about 10%), mild depression, & the rebound anxiety when you stop taking them is ridiculous. I had never had a panic attack until I stopped taking Klonopin a few years ago. Not only that but they don't have any of the positive effects of alcohol, namely the extreme self confidence that alcohol gives you. The only meds that seem to replicate this confidence are Prozac, Zoloft, and Dextrostat/Dexedrine.
>
> No one prescribes the barbituates or Miltown anymore, but I have a feeling that they would be closer to a 3 beer effect because of their greater similarity to alcohol. Chloral Hydrate looks good on paper, but it supposedly knocks you out rather than curing anxiety.
>
> But there are all these new GABA meds out there. Gabitril intrigues me because isn't it almost like an MAOI of GABA?
>
> What about Pregabalin? Does it cross the blood brain barrier easier than neurontin? Neurontin is weird cause you have to take like 90 million mgs 10 x per day for it to do anything.
>
> What about this stuff on the internet called Picamilone? It says that it is GABA bonded to Niacin & that IT CROSSES THE BLOOD BRAIN BARRIER! Wouldn't that make it like GHB? (definitely a 3 Beer Effect drug!) Somehow that seems to good to be true (& with most herbals producing little to no results I imagine it is).
>
> What other GABAergic meds are in the pipeline? Because GABA is an inhibitory transmitter, does that mean all GABAergic drugs are "dumb drugs'?
>
> Cheers 3 Beer Effect

I can hopefully answer the above post on gabitril here also,kill two birds with one stone.

You are not missing much by avoiding most of the gaba meds,aside from benzos,rarly do u see people get any stable long term relief from them alone.Gaba increases quickly accumalte,so as dopamine accumalation from excess deprenyl causes anxiety agitation,an abundance of gaba cause horrable depression,general weakness,a real bad attitutde,a feeling of stupour like you cant imagine,oh and worsens anxiety.

Most gaba meds are best when used in very small doses as an add-on to a AD.Strong gaba agents taken alone may feel good once or twice,like a high,but will quickly have you feeling terrable.I rember gabitril taken alone had me having horrific nightmares,and falling asleep constanly,i also had this sick gut feeling.I rember reading a post from someone who said gabitril actualy CAUSED him convulsions,and it alone does seem to cause me to twitch.

Benzos do more than simply increase gaba,they play a role in a few things happening,i had a article stating klonopin played a role in a few nuerontransmitters,xanax i believe has a role on serontion,they are not simply increasing gaba,they are more complex,which is why they tend to make one feel somewhat normal at regualr dosages,than high,even when taken alone.

GHB,well thats in a class of its own,and that too is not just a gaba enhancer,and no med,and especialy no supplement can even be compared to it.

GHB at very small doses actualy raises dopamine,and at high doses raises ghb,a chemical of its own,i believe a metabolite of gaba or precursor,cant rember,but its a substance on its own,and ghb intake has shown does not neccassrly increase over all gaba,but increases ghb.

Also the sedative effects of it are STRONG,but quick,and you avoid a lot of straight gaba side effects because before you know it the stored dopamine is relaesed,so you dont have either or,you actualy still have the sedative relaxing attributes,as you beging to feel the stimulant effects of the dopamine rebound kicking in slowly.When its done,you have increased ghb levels and dopamine levels,so you feel relaxed and sharpened.This of course is with responsable strict use,it is easly abused,the pro social,pro sexual,pro mood,properties of it make abuse easy to even the most responsable person.This might be so because it has an extremly sharp dose curve,a mg or so can make a difference.

Having tried gaba meds,and still a user of uh well,i can tell you ghb is non comparable to any gaba med or supplement.The premises of ghb seems great,but it is just too complex too use,and there are real real horror stories of addiction,more than should be on a therputic substance,i use it now mostly for an occasional sexual benifit,once in a blue moon,i simply seen to many people fall victim,and the withdrawal is said to be for some unbearable,for many requiring being hospitlized.Here is a quick run down of my exper.....

Nuerontion - Very unnatural feel of gaba,feels like plastic in your head,can provide benifits at initial onstart,but unless used as a add-on quickly builds to the menitoned above,in fact localy there are ads running concerning the drug possably causing sucidal ideation.

Gabitril - A more natural feel,but accumalted is no different than nuerontion in its side effects,nightmares,depression,anxiety etc

Tegatrol - This is a wierd one,seemed very different,very mild compared to the above two,but also very blah,dident seem helpful at all.Defitnaly not in the class of the above two which are HEAVY HITTERS.

Picamilion - Plain sh*tty,subtle,and useless.

Phenibutt - As far as supplements go,this could be a med,this is a very unique supplment,has late onset,and will get you very very stoned,its late onset makes it easy to take to much,and it remains active for a while,but while it is makes you social and i guess depression is not there.This was hoped to be the ghb repleacment,however consensus agrees it as a defintive poop out,and results are said not to return.


Kava Kava - Another substance not to be compared to a gaba substance,valerian increases gaba,and the two are very different,reason being kava is one of the most complex substances,hitting approx 15 receptor sites depending on dosage,and can affect almost every nuerontransmitter.

It does however have a high affinity for gaba,but does not simply increase it,and in no way resembles any of the gaba meds.

Last....L-Theanine- Some people love this stuff,increases both dopamine and gaba,sounds great dont it,well as many people who like it,prob triple hate it,myself being one.It seems to make me dumb,and very very angry.


All in all i tried using gaba agents alone once,and i was a walking iddiot,with anxiety,talking nonsense.

I have found great value however with low dose gabitril,kava,and ghb when added to my anti depressant,they gave it that little push that kept the AD one step behind of being pro social,and it allowed the AD to work,but also encouraged me to get out and interact,when they worked it was god send.

My AD doesent seem to help with getting me out and social,so i still use the above on low doses in combo,i switch around since they all seem to poop out.But again in small doses,add to a working AD,they do great.

Sorry for the long post,i just have had a lot of experiance in this field,until i finaly realized that gaba being the root cause of anxiety was just too simple,and stopped torturing myself with overloads of these.Anyone who read this whole thing,my hats off to you.


Note: Klonopin hands down is the most trust worthy still,just no fun at all to take.Also since there is a situation with Nuerontion causing possable sucidal ideation,id go with gabaitril if you are gonna take one,the lw suits are real and in action.

 

Re: Are any of these new GABA meds effective?

Posted by sabre on January 28, 2005, at 15:49:25

In reply to Re: Are any of these new GABA meds effective?, posted by Willyee on January 28, 2005, at 0:02:13

Hi Willyee
Thanks for your personal experiences with the GABA drugs. What problems were you taking the drugs for? Have you any experiences with other classes of drugs and if so, what were your reactions?

I am amazed at the variety and combinations of drugs many of the posters are able to obtain. I am unable to get scripts for benzos, anticonvulsants or MAOIs. As for GHB????????!
I am also amazed at the number of drugs posters are on at any one time.
My GP will give me scripts for one at a time only.
Is this only seen in the US? Are we behind in Australia? Or do you have to go to a psychiatrist for bulk orders?!

Your experiences, Willyee, are a worry because I was hoping a GABA drug or supplement might do the trick for social anxiety. Has it been the holy grail for anyone else? What are other poster's experiences with the drugs Willyee listed?
Thanks
sabre

 

Re: Are any of these new GABA meds effective?

Posted by mayajade on January 28, 2005, at 16:27:07

In reply to Re: Are any of these new GABA meds effective?, posted by Willyee on January 28, 2005, at 0:02:13

I have been taking Gabitril for just over a year. It quickly started working for me when I first started it, helped stabilize my moods and decrease anxiety. I started at 2 mg at night, gradually increasing to 12 mg. It worked well for a long time with minimal side effects (some dizziness at night after taking my dose). Now however, I fear it may not be working any longer - depression and anxiety have returned. My worst nightmare, as I've not found any other drugs that work for me.

 

Re: Are any of these new GABA meds effective?

Posted by sabre on January 28, 2005, at 16:39:16

In reply to Re: Are any of these new GABA meds effective?, posted by mayajade on January 28, 2005, at 16:27:07

Hi mayajade

Welcome to Babble.

What happens if you take a break from Gabitril and then come back on to it?

If you are not epileptic and you withdraw anticonvulsants is there an increased risk of having a seizure?

Could you try another anticonvulsant? What does your dr say?
sabre

 

Re: Are any of these new GABA meds effective?

Posted by TheOutsider on January 28, 2005, at 17:32:13

In reply to Re: Are any of these new GABA meds effective?, posted by sabre on January 28, 2005, at 15:49:25

Your experiences, Willyee, are a worry because I was hoping a GABA drug or supplement might do the trick for social anxiety. Has it been the holy grail for anyone else? What are other posters experiences with the drugs Willyee listed?
> Thanks
> sabre

For Sabre and anyone else who's interested!

I took GHB for years and found it very effective for social anxiety, far more effective than Klonopin.
I personally don't get on very well with the benzo's, I have tried Clonazepam and Diazepam.

Although I found Willyees post interesting I have to disagree with some of things he says about GHB.
I personally don't think the risks outweigh the benefits, as long as one is careful and doesn't take it to frequently.
Yes it can be addictive, but it is not inevitably addictive.

Also GHB withdrawal does not necessarily entail having to go to hospital.
I went through GHB withdrawal and although it was very unpleasant it ended after just three days.

I still think that GABA is probably key in social anxiety, although dopamine is also very important, just my opinion!

 

Re: Are any of these new GABA meds effective?

Posted by sabre on January 28, 2005, at 21:18:11

In reply to Re: Are any of these new GABA meds effective?, posted by TheOutsider on January 28, 2005, at 17:32:13

I've read a few references to GHB, Outsider, but where do you get it? Can you get a prescription for it or do have to hang around dark alleys at midnight?

sabre

 

Re: Are any of these new GABA meds effective?

Posted by Willyee on January 28, 2005, at 23:54:14

In reply to Re: Are any of these new GABA meds effective?, posted by sabre on January 28, 2005, at 21:18:11

> I've read a few references to GHB, Outsider, but where do you get it? Can you get a prescription for it or do have to hang around dark alleys at midnight?
>
> sabre


First i wanna say i did not intend to discourage the use of them,i see i inverntaly did.Remeber people here just post their own experieances,and if these meds taught us anything its that no one med works the same for everyone,i know when i feel something may be beneificial i usualy will try it regardless,ill just appreciate all info good and bad.

Second gaba agents are not useless,i personaly find used alone they are no good for my depression or anxiety,and just hieghten them all.But they are excellent in conjunction with my anti-depressant which is parnate.Parnate lifts depression but for me doesent give me a social kick,it kinda allows me to be isolated but be content with it,im able to spend my time alone and the depression stays at bay (when of course it works).I in fact use gaba agents,this goes well with my AD,it gives it the social effect im missing,which pushes me to want to interact more socialy.There might be some who find them alone to be benificial,i only specifiacly mentioned Nuerontion because that is under scrutiny for sucideal ideation,so it might make sense to simply ask for gabaitril if one is seeking,i thinks aside from benzos its prob the most effective gaba med.

As for ghb,lol im a long term user,used to be very active on the group,and think its absurd to ban a med and label it as posion then turn around and script it with tight limits and sky rocket high profit margins.

I have never become addicted to it,but it was once touted as totaly safe because its "natural" and this for a fact isnt true,there are real horror stories on addiction.

I dident mean to imply the risks outweigh the benifits,i neglected to mention its pretty much obsolete,so i dont want to get stuck on a substance i cant get,you now have people who once saftly used it,and relied on it,in bad shape,even resorting to ingesting various cleaning agents from local stores just because it lists some unkown trace amount of ghbs precursor among a ton of toxins.This is not good.

GHB is available now in prescription form,for narcolepsy,and is one of the most tightly scheldued watched meds.A docter will be put through hell to prescribe,and i believe only a nuerologist can,for its intended use only,i dont believe off lableing is even a consideration.

The drug is dispendsed from a single local pharmacy,a video tape is reqquired to be viewed,etc etc,its not a med you could stroll down to walgreens and pick up with a script.

Oh i forgot to mention when it was totaly legal,the cost was approx a doller a gram,now in script form off the top of my head its around 300-400 for a small amount,i dont have the figures but its very expensive,and i know first hand the chemicals invovled to make it are dirt cheap,thats the FDA for ya!

When ghb first became illegal,it was still possable over the internet to obtain fairly quality supply for cheap,once however the med made its debut,their was a huge sweer labled "operation webslinger" unknowingly suppliers were all gathered up,as well as long term customers,and now the situation is a different story.The average person will more than likly find it impossable to obtain,i discourage ordering it from anyone who claims to have it,ghb users are being scammed out of money,sent who knows what,and infertrated by police,and all this makes it not worth it.

There are long term veterans who have a supplier or so,other than them the average joe will not obtain it,it is illegal in every country.

You can try to obtain it in script form,its under the name xyrem.When i used it frequently it did provide tremondous relief,now knowing i can not obtain any more,i use it sparingly in more of a recreational sense,such as it makes a sexual experieance mind blowing,tenseness,and insecurties are oblivated,its especialy great for woman who seem to have most trouble relaxing and being aggressive,i.e not wanting to have the lights on,or leaving partial clothing on,more than likly any woman using it will shed all garments lol.Oh and it intensifies erection for men,and orgasms for woman like ten fold.

The nieve public ate up the whole date rape drug without ever even asking what it is.Alcholol alone is the biggest date rape drug,any sedative added to that is basicaly a mickey,and the handful of ghb incididents were enough to demorlaize ghb simply by name.

GHB is gamma hydroxy butytric acid,it basicaly has a hydroxide,commonly sodium added to gaba to get it across the blood brain barrier.It was discovered it actualy already exists in the body,so albiet a drug,it is still a natural occuring substance.Of all drugs this one is the one i have researched most,their are tons of information out their,their is good and bad,any site that promotes pure negative or postive sides of the coin,and no other,is propaganda,its a unique,complex fantastic substance.

Kava kava was also attacked by the fda,and the nieve public bought the liver problems in a sec,95 percent of manufacuters pulled it,and by the time the claim was retracted,which it was (results came back stating no evidence at all suggests kava is linked to liver damage)the public scare was already in effect,and now there are only extremly crappy brands left on the market,i used to have tons of choices of brands,i loved it,they are all discontinued.

The fda required bright red warning labels go on the top of the bottles,great scare tactic.Well on the remaining brands those warnings are gone,unfortuantly so are all of the paying customers and all of the good brands hence of.

I dont wanna be re directed,but on alternative babble their should be info on Taurine,which is another great mild sedative that can saftly be added to almost any med.

 

GABA meds, For Sabre and Willyee

Posted by TheOutsider on January 29, 2005, at 8:45:15

In reply to Re: Are any of these new GABA meds effective?, posted by Willyee on January 28, 2005, at 23:54:14

High Sabre

Sorry I got your hopes up about GHB,
It is now all but impossible to get in the English speaking world, although I think its still available in Italy and France, if the legends are true!

It is also not a perfect drug, it deffinetly can be addictive.

Sorry if I cames across as being agressive Willyee,
I hear so much negative propaganda about GHB it makes me rather deffensive about it.

You certainly seem to know what your talking about, I see your point about combining GABA meds with Anti depressents is a good one.
On its own Klonopin just seems to make me depressed!
I have never heard of Phenibut, how effective was it for Social anxiety?
I'm a bit skeptical about supplements because picamilone was absolutely useless.

 

Re: Are any of these new GABA meds effective?

Posted by alienatari on January 29, 2005, at 14:58:24

In reply to Re: Are any of these new GABA meds effective?, posted by sabre on January 28, 2005, at 15:49:25

Hey maybe its just your GP. Im in Australia too and i am on an MAOI (Parnate), Largactil and Epilim. But i do see a psychatrist too. They kind of both perscribe for me (knowingly).

 

Re: Are any of these new GABA meds effective?

Posted by sabre on January 29, 2005, at 17:12:14

In reply to Re: Are any of these new GABA meds effective?, posted by alienatari on January 29, 2005, at 14:58:24

> Hey maybe its just your GP. Im in Australia too and i am on an MAOI (Parnate), Largactil and Epilim. But i do see a psychatrist too. They kind of both perscribe for me (knowingly).

Thanks, Alienatari
So it is possible to get these drugs. Did you find it difficult the to go and see a psychiatrist the first time? I get adrenaline surges just thinking about discussing my mental deficiencies with a complete stranger.
What are you taking these medications for?

sabre

 

Re: GABA meds, For Outsider and Willyee

Posted by sabre on January 29, 2005, at 17:24:49

In reply to GABA meds, For Sabre and Willyee, posted by TheOutsider on January 29, 2005, at 8:45:15

Thankyou both for the GHB information.

To be honest I didn't see it as an option but I'm interested to learn everything I can about drugs, neurotransmitters, people's experiences etc in the hope that it will help. I am continually amazed at the lengths some posters have had to go to in an attempt to ease their suffering.
Thanks
sabre

 

Re: GABA meds, For Sabre and Willyee

Posted by Willyee on January 30, 2005, at 0:58:29

In reply to GABA meds, For Sabre and Willyee, posted by TheOutsider on January 29, 2005, at 8:45:15

> High Sabre
>
> Sorry I got your hopes up about GHB,
> It is now all but impossible to get in the English speaking world, although I think its still available in Italy and France, if the legends are true!
>
> It is also not a perfect drug, it deffinetly can be addictive.
>
> Sorry if I cames across as being agressive Willyee,
> I hear so much negative propaganda about GHB it makes me rather deffensive about it.
>
> You certainly seem to know what your talking about, I see your point about combining GABA meds with Anti depressents is a good one.
> On its own Klonopin just seems to make me depressed!
> I have never heard of Phenibut, how effective was it for Social anxiety?
> I'm a bit skeptical about supplements because picamilone was absolutely useless.


Not at all,i just wanted to make sure people know everything i say can only apply to me,and otherwise be opinion.

As for GHB,it was once legal as a script med in i believe italy called Alcover,that is gone,and so is any supply of it whatsoever,totaly illegal to possess there as in the states.

In germany it was once a script med called Gamma-oh,that is no more,and neither is it period,as it is illegal there.

Aside from alleyway purchase,the last known popular product of it was its precursor gbl,which is basicaly ghb,it was a health supplement,called Renewtrient,and was long ago totaly banned,man companys try to sucker people by making Renewtrient 2 or Renewg keeping the name similiar,but all they are is a bunch of crap,herbs vitamins etc all bunched togther,the real Renewtrient that once was,was nothing more than gbl,nothing else in it.

GHB is legal in the form of xyrem a tightly watched scheldued script med for narcolpesy,it is illegal totaly and one hundred percent in every country.


Phenibutt is a gaba supplement,that also increas PEA,and is effective in crossing the brain.

Although nothing like ghb,as there does not exist anything like it,phenibut unlike other supplements will cross the brain and will have activity,and it will be notciable,it can very well have been made a script med.

By the way its not picamilion,i too was totaly P.O D with picamilion,and tossed it away qucikly,pure garbage for me.

 

Re: Are any of these new GABA meds effective?

Posted by todayisagiftxx on January 30, 2005, at 16:44:52

In reply to Re: Are any of these new GABA meds effective?, posted by mayajade on January 28, 2005, at 16:27:07

my sister is taking gabitril for anxiety and it doesn't seem to help her at all she is up to 4mg a day I think. i know she still experiences a fair amount of anxiety and she never has tried a benzo or anything either

 

Re: Are any of these new GABA meds effective?

Posted by medhed on January 31, 2005, at 3:00:00

In reply to Re: Are any of these new GABA meds effective?, posted by todayisagiftxx on January 30, 2005, at 16:44:52

GHB is great, U.S. made it scheduleI though. I don't like the addiction part so it really wasn't viable as a daily med. It is easily made from GBL but the legal question scares me.
Neurontin, you just have to take too much for it to be effective. (I have to take too much.)
Gabatril was OK for a short period of time but it pooped out. Some weird side effects were severe forgetfulness, dizziness, feeling drunk. Side effects went away quickly but that was the only thing to remind me I was taking it.
Then there's Klonipin, I like it but I don't like being dependant on benzos. (I tend to abuse them after a while.)
I really want to try Lyrica- I am in the progress with pdoc. I haven't heard to much on this drug except from the drug company and Wall St.

 

Re: Are any of these new GABA meds effective? » 3 Beer Effect

Posted by Michael Bell on January 31, 2005, at 4:59:05

In reply to Are any of these new GABA meds effective?, posted by 3 Beer Effect on January 27, 2005, at 21:17:24

>
None of the meds you mentioned are direct GABA agonists. Not Klonopin, not Gabitril, etc. The mechanism of action of Lyrica, like Neurontin, is still not 100% clear. Picamilon *theoretically* should raise GABA levels in the brain, but its effectiveness at crossing the blood-brain barrier is not proven (although it did provide me with some relief).

The only meds out there that truly and directly affect GABA are
1) the GABA transanimase inhibitors (such as Sabril, which is a dangerous drug b/c it causes permanent field of vision loss, and Nardil)

and

2) GABA receptor agonists - there is none yet on the market, but Ocinaplon is the closest. It is in phase III trials and is *supposedly* extremely effective for anxiety without the negative effect of benzos.

Sorry, the options are rather limited, but that's where we stand today. Good luck.


It has been a few years since i've been a regular poster on here so I've lost track of all these new GABA meds.
>
> I am always looking for a 3 Beer Effect type medication & sadly, have never found anything better than the 1.5 Beer Effect of Prozac or Zoloft 100 mg.
>
> The Benzos were a big dissapointment to me. They seem to have severe disadvantages of tolerance, dumbness "they are supposed to impair thinking & memory by about 10%), mild depression, & the rebound anxiety when you stop taking them is ridiculous. I had never had a panic attack until I stopped taking Klonopin a few years ago. Not only that but they don't have any of the positive effects of alcohol, namely the extreme self confidence that alcohol gives you. The only meds that seem to replicate this confidence are Prozac, Zoloft, and Dextrostat/Dexedrine.
>
> No one prescribes the barbituates or Miltown anymore, but I have a feeling that they would be closer to a 3 beer effect because of their greater similarity to alcohol. Chloral Hydrate looks good on paper, but it supposedly knocks you out rather than curing anxiety.
>
> But there are all these new GABA meds out there. Gabitril intrigues me because isn't it almost like an MAOI of GABA?
>
> What about Pregabalin? Does it cross the blood brain barrier easier than neurontin? Neurontin is weird cause you have to take like 90 million mgs 10 x per day for it to do anything.
>
> What about this stuff on the internet called Picamilone? It says that it is GABA bonded to Niacin & that IT CROSSES THE BLOOD BRAIN BARRIER! Wouldn't that make it like GHB? (definitely a 3 Beer Effect drug!) Somehow that seems to good to be true (& with most herbals producing little to no results I imagine it is).
>
> What other GABAergic meds are in the pipeline? Because GABA is an inhibitory transmitter, does that mean all GABAergic drugs are "dumb drugs'?
>
> Cheers 3 Beer Effect

 

Re: Are any of these new GABA ...Michael Bell

Posted by sabre on February 1, 2005, at 0:18:13

In reply to Re: Are any of these new GABA meds effective? » 3 Beer Effect, posted by Michael Bell on January 31, 2005, at 4:59:05

Michael, is Parnate also a GABA transanimase inhibitor?

How exactly do Parnate and Nardil differ?

Thanks
sabre

 

Re: Are any of these new GABA meds effective?

Posted by aazospiro on February 2, 2005, at 0:45:03

In reply to Re: Are any of these new GABA meds effective? » 3 Beer Effect, posted by Michael Bell on January 31, 2005, at 4:59:05

Ahmmm correction there mister,

Klonopin [Clonazepam] differs from the rest of the benzodiazepines in that in is a partial agonist at the BDZ receptors.

Interesting thing about thses neurotransmitters [from my many many readings] is that they display what I refer to as the "see-saw effect"

Specifically, GABAergic drugs loose their euphorigenic effects, calming properties which quickly turns to severe irritabilitywith chronic use, but add a dopaminergic agent like selegiline or Sinemet or even better a stim and its all back again like if you used it for the first time.

And while on the subject of stimulants, all the chit chat about glutamate antagonists like DXM being used for stim tolerance [which I cant dispute] hasn't anyone considered the effects that T-4 or T3 have on the responsiveness of adrenergic/ dopaminergic receptors. Apparently even though no receptor density changes are evident, the response is augmented and only very tiny doses are needed of the latter.

Certaintly food for thought

 

Re: Are any of these new GABA meds effective? » aazospiro

Posted by Michael Bell on February 9, 2005, at 21:37:41

In reply to Re: Are any of these new GABA meds effective?, posted by aazospiro on February 2, 2005, at 0:45:03

>
Uhh, no. You post actually proved my point. Klonopin is an agonist of the BDZ receptor. It does NOT act as an agonist of the GABA alpha subunits themselves. This is why it has anti-seizure, sedating, and anti-insomniac properties rather than acting as a pure anxiolytic. There is NO PURE GABA AGONIST on the market yet.

Ahmmm correction there mister,
>
> Klonopin [Clonazepam] differs from the rest of the benzodiazepines in that in is a partial agonist at the BDZ receptors.
>
> Interesting thing about thses neurotransmitters [from my many many readings] is that they display what I refer to as the "see-saw effect"
>
> Specifically, GABAergic drugs loose their euphorigenic effects, calming properties which quickly turns to severe irritabilitywith chronic use, but add a dopaminergic agent like selegiline or Sinemet or even better a stim and its all back again like if you used it for the first time.
>
> And while on the subject of stimulants, all the chit chat about glutamate antagonists like DXM being used for stim tolerance [which I cant dispute] hasn't anyone considered the effects that T-4 or T3 have on the responsiveness of adrenergic/ dopaminergic receptors. Apparently even though no receptor density changes are evident, the response is augmented and only very tiny doses are needed of the latter.
>
> Certaintly food for thought

 

Re: Are any of these new GABA meds effective? » sabre

Posted by HoldenYosarian on February 12, 2005, at 23:29:51

In reply to Re: Are any of these new GABA meds effective?, posted by sabre on January 28, 2005, at 15:49:25

I've had my share of experimening with better living through chemistry--tried almost every SSRI ever made--xanax, librium, Valium, Serax, Klonopin, Neurontin (briefly--might as well be placebo), in attempt to simply "normalize" and live a satisfying productive life...as well as an even more extensive foray into the "less sanctioned" versions of chemical recreation...I've also made an avocation out of studying the brain/mind and its workings, as well as biochemistry. I won't bore you with the details at this point.
The point is, if I understand it correctly, three beers, that you're looking more for the "illicit" goal than the societally-approved one (a pleasant buzz rather than simply the content stability promised--and of course rarely delivered---by the medical establishment). Far be it from me to judge. Frankly, I agree with you.
But I believe your entry focussed around manipulating GABA levels as a means of achieving this state. Of course, that's not surprising. That's all you hear about, practically, with respect to relaxation and contentment, these days..."GABA this, GABA that...".
The problem is, that it isn't as simple as focussing on GABA alone when trying to achieve that feeling of "pleasantly removed"...or should I say it..."Comfortably numb".
First of all, I agree totally with the guy who said that messing around with your GABA levels alone will, at best, leave you initially slow,
sluggish, and mentally foggy, but that the rebound anxiety involved with long periods of GABA increase--inevitable, of course--leaves you with the promise of overwhelming anxiety, which hardly made the stupor you were in during your GABA phase even worthwhile. And that's not to mention the Depression that's likely to accompany both the GABA boosting AND the detox.
Let me cut to the bottom line. People who find they need or even regularly want a "three beer effect" are usually those who need some sort of social lubricant or are otherwise uncomfortable with reality in a way that keeps them in a state of anxiety.
To put it simply, you're putting the cart before the horse. You've got to address that underlying cause before you can appreciate the quality or significance of the symptoms.
The answer is norepinepherine, not GABA. Call me paranoid, but getting caught up in the GABA merry go 'round is exactly what the Pharm. guys want. Addiction to the means of addressing symptoms, not an actual cure of the underlying imbalance/condition.
I don't have time at the moment to go into the relation btwn norep. and GABA, other neurotransmitters, etc--sorry. But if you want that "three beer effect", you're going to have to start with addressing your norepinepherine levels. Wellbutrin is a weak norepinepherine re-uptake inhibitor, as well as dopamine. Effexor is a stronger Nor. re-up inhib, and increases serotonin levels, as well. There's a new AD, called reboxetine, which is solely a Nor. re-up inhibitor, but I don't think you can get it in the states (guess why? As they say, just because I'm paranoid doesn't mean I'm wrong).
L-tyrosine, an amino acid, increases levels of Nor. (and Dopamine, but mostly Nor.) you should take at least 3g on an empty stomach for any results. There are other Nor. supplement precursors, as well, including D-phenylalanine, quite a few others, plus herbals.
For more info about importance of norepinepherine in the release and control of stress hormones and anxiety, do a search on "cortisol the hypothalamus and Nor.", "PTSD and Nor.,", "medication resistant depression and Nor."
Deal with the underlying reason, which almost certainly involves your Nor. levels, and then....drink three beers--or whatever.

 

Re: Are any of these new GABA meds effective?

Posted by sabre on February 13, 2005, at 23:13:36

In reply to Re: Are any of these new GABA meds effective? » sabre, posted by HoldenYosarian on February 12, 2005, at 23:29:51

Thankyou Thankyou Thankyou, Holden.

This is what I have been wanting to know.
Tyrosine is one of the only supplements that have yielded any results for me...at approx 2g/day. But the effect wears out after a few weeks and I have to go off it. I had been wondering about using Reboxetine as I can get in Australia and the gp said she was happy to prescribe it.

SSRIs are awful, including Tryptophan.

I started looking into GABA and have recently played around with GABA, Phenibut and Picamilon but didn't get the results I was after. I sidetracked to glutamine and have found it very stimulating esp at about 2g/day. I tried mixing 500mg with valium yesterday but the valium sedation won.

Propanalol and glutamine are a little better but not what I'm after.

I thought that perhaps if I found a regulator or enhancer of the glutamate to GABA conversion that I would find social ease. I've unearthed references to taurine and theanine having this function...in addition to GABA prescription drugs.

At the same time I also found a reference to
http://www.psychiatry.ufl.edu/Newsletters/Content/Krystal.pdf
It mentioned that NA and DA are modulators of glutamate to GABA conversion.
So is this what you are talking about?

I'll go and look up your suggestions.

Thanks again, Holden and welcome to Babble.

sabre

 

Re: Are any of these new GABA meds effective?

Posted by HoldenYosarian on February 15, 2005, at 2:46:38

In reply to Re: Are any of these new GABA meds effective?, posted by sabre on February 13, 2005, at 23:13:36

> Thankyou Thankyou Thankyou, Holden.
>
> This is what I have been wanting to know.
> Tyrosine is one of the only supplements that have yielded any results for me...at approx 2g/day. But the effect wears out after a few weeks and I have to go off it. I had been wondering about using Reboxetine as I can get in Australia and the gp said she was happy to prescribe it.
>
> SSRIs are awful, including Tryptophan.
>
> I started looking into GABA and have recently played around with GABA, Phenibut and Picamilon but didn't get the results I was after. I sidetracked to glutamine and have found it very stimulating esp at about 2g/day. I tried mixing 500mg with valium yesterday but the valium sedation won.
>
> Propanalol and glutamine are a little better but not what I'm after.
>
> I thought that perhaps if I found a regulator or enhancer of the glutamate to GABA conversion that I would find social ease. I've unearthed references to taurine and theanine having this function...in addition to GABA prescription drugs.
>
> At the same time I also found a reference to
> http://www.psychiatry.ufl.edu/Newsletters/Content/Krystal.pdf
> It mentioned that NA and DA are modulators of glutamate to GABA conversion.
> So is this what you are talking about?
>
> I'll go and look up your suggestions.
>
> Thanks again, Holden and welcome to Babble.
>
> sabre
>


O.K. sabre, a bit more advice--glad to help anyway possible, by the way.
1. You haven't been taking enough tyronsine. You need at least 3 g/ day to realize any potential antidepressant benefits. Problem is, it's metabolized not only into dopamine and noradrenaline (norepinepherine), but epinepherine, as well (i.e. adrenaline) in the medulla--which means if you have problems with anxiety to begin with, the epinepherine's going to aggravate it. However, you can forestall this with a beta-blocker--so my recommendation would be to try tyrosine again, increase to at least 3 g/day, progressing up to 5 before giving up, and adding a beta-blocker at the same time.

2. As far as the glutamine is concerned, don't take over 3 g/day. You'll risk burning out neurons with an "excitatory" effect at a higher dosage. This is serious sh*t. We're talking significant brain damage--if used at that strength for any length of time.

Sounds like your main issue is Noradrenaline, if Tyrosine was so helpful--dopamine is a byproduct of Tyrosine, of course, so I'd recommend you ask your pdoc for some wellbutrin, as well.
When referring to social ease, you'll find you're main concern is cortisol. L-theanine is a fairly good tool to head-off cortisol production (they haven't figured out exactly why or how) and is also metabolized into dopamine and norepinepherine. Epimedium (an herb) is one of the all around best cortisol fighters, and is considered an "adaptogen", as it contributes to increases in and stabilization of neurotransmitter function. L-Methionine should also be on your list. Tuanrine's a great calmative, and there's no L or D form, so don't bother looking---it's just called Taurine. Many swear by it.
One caveat...be wary of the psyches (you mentioned a site). They're not scientists--less so that the average physician--and only rarely do their homework, as a rule, I've found.
I can't say say I completely disagree with what you've said regarding the site's advice, expecially considering I haven't seen it---but if it is as you say, the context is off. You see, Glutamine is used as a fuel in the production of both Da, Na, and many other factors and co-factors. DA and NA are "modulators" of Glutamine translation to GABA because they are formed first, and it's only what's left over that's translated to GABA. It's main affect is on ATP production and cellular metabolism--thus the energy. Little is actually translated into GABA.
I understand your pain, and the everpresent desire for just a moment of relief. Unfortunately, GABA is not the answer. It's yet another corporate scheme to keep us on the roller coaster of consumption--Neurontin,gabatril, etc, etc. Have you ever known, or seen a post by someone who's reached a satisfied,stable state through the use of GABA influencing drugs? You won't find one. Again, give the reboxetine/effexor/wellbutrin a chance before you going any further chasing GABA. I think you'll be pleasantly surprised. I also get the feeling that you have ADD. Get tested. ADD is responsible for more misery and dysfunction than anyone unfamiliar with it has any idea of (I hope this isn't presumptuous, I have it too--I've just gotten good at reading the signs after lots of study). Also, when you feel your supps are wearing out, combine them with licorice root and bioperine complex (indian black pepper rhysomes).

Thanks for the welcome, hope to hear from you soon.

 

Re: Are any of these new GABA meds effective?

Posted by HoldenYosarian on February 15, 2005, at 3:35:41

In reply to Re: Are any of these new GABA meds effective?, posted by sabre on February 13, 2005, at 23:13:36

> Thankyou Thankyou Thankyou, Holden.
>
> This is what I have been wanting to know.
> Tyrosine is one of the only supplements that have yielded any results for me...at approx 2g/day. But the effect wears out after a few weeks and I have to go off it. I had been wondering about using Reboxetine as I can get in Australia and the gp said she was happy to prescribe it.
>
> SSRIs are awful, including Tryptophan.
>
> I started looking into GABA and have recently played around with GABA, Phenibut and Picamilon but didn't get the results I was after. I sidetracked to glutamine and have found it very stimulating esp at about 2g/day. I tried mixing 500mg with valium yesterday but the valium sedation won.
>
> Propanalol and glutamine are a little better but not what I'm after.
>
> I thought that perhaps if I found a regulator or enhancer of the glutamate to GABA conversion that I would find social ease. I've unearthed references to taurine and theanine having this function...in addition to GABA prescription drugs.
>
> At the same time I also found a reference to
> http://www.psychiatry.ufl.edu/Newsletters/Content/Krystal.pdf
> It mentioned that NA and DA are modulators of glutamate to GABA conversion.
> So is this what you are talking about?
>
> I'll go and look up your suggestions.
>
> Thanks again, Holden and welcome to Babble.
>
> sabre
>

Sabre--I've included the rather abstruse study to illustrate a point...while glutamine and glutamate is technically responsible for the creation of GABA, GABA is for the most part a transitional stage through which glutamate passes
on its way to become glutamine, and is exists during only brief stages during which this process takes place, for the most part.
The study follows:
"http://www.nutrition.org/cgi/content/full/131/9/2498S
The glutamate-glutamine cycle: biochemical and molecular considerations
The metabolism of neurotransmitter glutamate and GABA is linked to a substrate cycle between neurons and astrocytes involving glutamate, GABA and glutamine (Martin 1995 , Schousboe et al. 1993 , Van den Berg 1972 ). The efficient functioning of the glutamate-glutamine cycle is made possible by the physical segregation of specific enzymes between neurons and glia and the presence of specialized amino acid transporter proteins. Glutamate and GABA released into the synapse in response to nerve terminal depolarization, bind to their respective receptors and are cleared from the interstitum by uptake into astroglia. Within astroglia, glutamate (and GABA through an indirect process) is converted to glutamine by the astroglia-specific enzyme, glutamine synthetase (GS) (Martinez-Hernandez et al. 1977 ). Glutamine is transported from astroglia into neurons and is hydrolyzed to glutamate by the mitochondrial enzyme, phosphate-activated glutaminase (PAG) (Kanamori and Ross 1995 , Kvamme and Lenda 1982 ). Thus, this pathway results in a cyclic flow of carbon between nerve terminals and glia, i.e., a glutamate-GABA-glutamine cycle. Some of the key molecular components required for the operation of this cycle are described below.

Two other neuronal transporters, EAAT4 and EAAT5, are expressed on cerebellar GABAergic Purkinje cells and in the retina, respectively, and appear to differ from their cortical counterparts in gating Cl- ions. Although the functions of the neuronal transporters are not yet clear, one of them (EAAC1) is expressed on some GABAergic nerve terminals (Kanai and Hediger 1992 , Rothstein et al. 1994 and 1996 ) where it may have a role in the supply of precursor glutamate for GABA synthesis (Sepkuty et al. 2000).
Evidence from molecular (Rothstein et al. 1996 and 1994 ) and electrophysiologic studies (Bergles and Jahr 1997 and 1998 ) indicates that the astroglial transporters clear the majority of glutamate from the synaptic cleft. As discussed subsequently, the molecular findings are consistent with in vivo NMR study results showing that glutamate uptake into astroglia and its conversion to glutamine is the predominant path for recycling of neuronal glutamate in vivo (Rothman et al. 1999 ).
GABA transport.
Astroglia and neurons possess a high capacity for the transport of GABA (Henn and Hamberger 1971 , Hertz et al. 1978 , Ryan and Roskoski 1977 ). Molecular cloning studies have identified four high affinity, Na+ and Cl--dependent, GABA transporters (GAT) in the brain (GAT1, GAT2, GAT3, GAT4/BGT-1). With the exception of GAT-3, which is expressed on astrocytes, the other GAT subtypes are expressed on both neurons and astrocytes (Minelli et al. 1995 and 1996 , Ribak et al. 1996 ). The functional roles of the different GABA transporter subtypes in the clearance of GABA from synaptic, and possibly extrasynaptic sites remain to be elucidated. Rapid metabolism of GABA in astrocytes via an active GABA-transaminase (Chan-Palay et al. 1979 , Larsson and Schousboe 1990 ) maintains GABA at a low level in these cells, resulting in a large concentration gradient between GABAergic neurons and the surrounding transporter-rich astroglia
GABA synthesis depends on glutamine for its supply of glutamate precursors in vitro and in vivo (Balazs et al. 1973 , Patel et al. 2000 , Sonnewald et al. 1993 , Van den Berg 1972 ), indicating that some fraction of GABA released from GABAergic neurons is not recycled directly back into the terminal. ('Some Fraction--meaning not much)

Astroglial metabolism of extracellular glutamate and GABA stimulates glutamine synthesis.
Glutamine synthesis in astroglia is generally considered the major net metabolic pathway for the metabolism of extracellular glutamate (Wanienski and Martin 1986 ). GABA metabolism in astroglia can also lead to glutamine synthesis. Unlike glutamate, however, GABA must be further processed in the astroglial tricarboxylic acid (TCA) cycle, a two-step reaction involving -ketoglutarate and NAD+ that converts GABA to succinic acid via GABA-transaminase (GABA-T) and succinic semialdehyde dehydrogenase. The initial transamination between GABA and -ketoglutarate catalyzed by GABA-T produces glutamate, which may then proceed to formation of glutamine."

May your path be straight, or as winding as the wisdom to which you are fated...

HoldenYosarian

 

How about a mushroom effect instead of a 3 beer

Posted by aphexonset on February 15, 2005, at 4:35:54

In reply to Are any of these new GABA meds effective?, posted by 3 Beer Effect on January 27, 2005, at 21:17:24

I went to my school psychiatrist, and was diagnosed with GAD. He was against benzos, even though a previous script from my physician helped alot, so he put me on Gabatril, since Its supposed to work similarly. After a week or so, I felt some relief in anxiety. I tapered up to what he felt is a normal dose for anxiety.

Then the anxiety pretty much came back. Then, mostly in situations where I'd become extra panicked, all space in my field of vision would become 2dimentional. I couldnt judge how deep a room went, the wall floor and ceiling just seemed pressed up against my eyes, except for a tunnel of regular 3d space in the center of my vision. Very weird. Like a street drug. Reminded me of the couple of times years ago I tried 'shrooms.

 

Re: How about a mushroom effect instead of a 3 beer

Posted by HoldenYosarian on February 15, 2005, at 12:33:16

In reply to How about a mushroom effect instead of a 3 beer, posted by aphexonset on February 15, 2005, at 4:35:54

> I went to my school psychiatrist, and was diagnosed with GAD. He was against benzos, even though a previous script from my physician helped alot, so he put me on Gabatril, since Its supposed to work similarly. After a week or so, I felt some relief in anxiety. I tapered up to what he felt is a normal dose for anxiety.
>
> Then the anxiety pretty much came back. Then, mostly in situations where I'd become extra panicked, all space in my field of vision would become 2dimentional. I couldnt judge how deep a room went, the wall floor and ceiling just seemed pressed up against my eyes, except for a tunnel of regular 3d space in the center of my vision. Very weird. Like a street drug. Reminded me of the couple of times years ago I tried 'shrooms.

aphexonet

Sorry about your predicament. GAD (although that's a catch all-term meaning little by itself--another thing the pdocs are good at) is hell, I know. ONe prob is the "consultation" kickbacks that most pdocs receive for prescribing the newest meds--whether they're indicated, efficacious, or not. My recomendation is Effexor. It's a GAD agent, too--but without the GABA thrown in that makes you loopy. DOn't quit on it until you've reached 300 mg. The Noradrenaline uptake inhibition will regulate your GABA, as it's supposed to. Try D,L phenylalanine to top it off--it'll booost your available NOR., Dopamine--but I'd also add Taurine to counteract the increase in epinepherine that comes along with it--as well as l-theanine--and L-Methionine.
By the way, if you're school pdoc thinks that Gabatril and benzos are comparable, he needs to go back to school himself.

Keep me posted

Holden

 

Re: Are any of these new GABA meds effective? » HoldenYosarian

Posted by franco neuro on February 15, 2005, at 13:51:51

In reply to Re: Are any of these new GABA meds effective? » sabre, posted by HoldenYosarian on February 12, 2005, at 23:29:51

You're dispensing some good advice my friend. Glad to see there are people out there doing their homework. I too have been helped more by that $10 bottle of tyrosine than bucketloads of SSRI's, GABAergics and dreaded TCA's. Unfortunately, i only got wise this past year. But the "tyrosine effect" as i like to call it has finally helped to point me in what i hope is the right direction. I'll be starting Wellbutrin soon and hopefully it'll work. There aren't too many "clean" norepinephrine and/or dopamine agonists out there. I think in my case that Wellbutrin is the best choice. Definitely reboxetine for norepinephrine. I have read about a medication that is hard to come by called survector which is supposed to be really dopamine selective. It's funny how when you mention anxiety or panic meds. the first ones that jump into peoples' heads are the SSRI or GABA meds. When in fact the most powerful anti-panic/anxiety drugs are actually the MAOI's. Which have fallen out of favor (supposedly) due to their side effects. I've never taken one so I have no first hand experience as to their efficacy. By the way i wash my tyrosine down with grape juice. I've heard that the carbs help to facilitate it's transport. Any thoughts on this?


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