Baclofen and relationship to GHB

[krill]

Hey,

I've been reading this site for about a month. I ordered and started baclofen ("bac." from here on) about a month ago. I am now up to 60 mg a day taken as (approximately, 15 mg 2AM, 15 mg 7AM, 15 mg 12 noon, and 15 mg. around 8:00 PM). I used GHB back in the day as a recreational ( and, as it turned out, highly addictive drug) and loved/feared the intense buzz it gave me. I am a long-time runner and was trying to reduce my daily use, as it scared the hell out of me. I took it before work (teacher) and about four times per day. Fortunately (in retrospect), the U.S. Postal police invaded my home around 2001 0r 2002 and put an end to my GHB use (Scary, scary event, but God works in mysterious ways. Thankfully I didn't go to jail! I have a serious job and a handicapped partner who I dearly love and who depends upon my support).

So. Here's the essence of this tread. Am I the only one here who has been taking bac. and understands that it is clearly a GHB analog? Similar (but not quite as intense buzz), same "shivery" body feelings that peak about three hours after a 15-18 mg dose? Same over-powering somnolence throughout the dosage cycle? Am I the only one here who has done GHB and has seen the obvious relationship to baclofen? I know that both drugs are (reportedly) GABA-B agonists, but doesn't anyone else here feel that they promote an obvious dopamine rush too?

[Ne/Neva Eva]

Baclofen and relationship to GHB

Hi, Krill. Me again.

I don't know if you've seen the responses I've given on the other threads related to this? I ask only because sometimes new people post and then don't see responses...
I don't have direct experience with GHB, but I have experienced what you're describing with bac. (I abbreviate it mostly because I don't want it to come up with a google hit. That thought used to bother me a lot...Not so much anymore.)

Anyway, I think there were some people around here who have experienced both, and I'll leave it to them to answer. If you haven't seen the responses on the other threads, and/or if no one gets back to you, I'll try to link them here soon.

[rangiatea]

Baclofen and relationship to GHB

Bacs can induce dopamine and serotonin rushes.But they go away very quickly.I had the rushes many months ago.Shivery comeups,followed by closed and open eyed visuals,rushes and some sleepiness and mood swings.It was a bac OD.Many MWO members experienced similar effects when they OD or titrate too much too fast.You are not alone.

[MusiciansMallet]

Baclofen and relationship to GHB

krill;1342046 wrote: I've been reading this site for about a month. I ordered and started baclofen ("bac." from here on) about a month ago. I am now up to 60 mg a day taken as (approximately, 15 mg 2AM, 15 mg 7AM, 15 mg 12 noon, and 15 mg. around 8:00 PM). I used GHB back in the day as a recreational ( and, as it turned out, highly addictive drug) and loved/feared the intense buzz it gave me. I am a long-time runner and was trying to reduce my daily use, as it scared the hell out of me. I took it before work (teacher) and about four times per day. Fortunately (in retrospect), the U.S. Postal police invaded my home around 2001 0r 2002 and put an end to my GHB use (Scary, scary event, but God works in mysterious ways. Thankfully I didn't go to jail! I have a serious job and a handicapped partner who I dearly love and who depends upon my support).

So. Here's the essence of this tread. Am I the only one here who has been taking bac. and understands that it is clearly a GHB analog? Similar (but not quite as intense buzz), same "shivery" body feelings that peak about three hours after a 15-18 mg dose? Same over-powering somnolence throughout the dosage cycle? Am I the only one here who has done GHB and has seen the obvious relationship to baclofen? I know that both drugs are (reportedly) GABA-B agonists, but doesn't anyone else here feel that they promote an obvious dopamine rush too?There surely is an obvious similarity between these two substances, as they are agonists at the same receptor- GABA-b. Although, due to GHB's legal status & bac poorly studied nature (not-patentable, no big bucks to come out of major pharmacological studies)- we DON'T know the intricacies of any different binding affinity for different GABA-b subunits (this is why there is a difference between a benzodiazepine and a Z-drug like "Ambien"- b/c Ambien binds purely to the alpha-1 subunit at the GABA-a; where as benzodiazepines bind to many subunits).

As far as dopamine is concerned- stimulation of the "GHB receptor" by GHB does increase dopamine levels, although high doses will stimulate too much GABA & thus inhibit this effect via GABA-b modulation. Baclofen does NOT bind to the GHB-receptor. And baclofen does not increase dopamine levels (nor does it interact with dopaminergic receptors in anyway), at least to any clinically appreciable level. All the similar effects between GHB & baclofen you notice will be a result of agonism at the GABA complex, at the -b receptor subtype (i.e., GABA-b agonist in plain english)!

Sorry if i used too much Jargon! I tend to do that sometimes... but, the GABA complex is the most complicated receptor system in the human brain, hands down. So, sometimes it is needed. Feel free to ask my ANY questions if need be, about ANY of the jargon i've used!
Anyway, hope this helps!



raniatea wrote: Bacs can induce dopamine and serotonin rushes.

Please be careful raniatea with *what* you post and the information you pass as fact.. Baclofen is a GABA-B agonist; & GABA is the most widespread neurotransmitter in the brain & it is inhibitory, and will cause general decreases in dopamine & serotonin, and NOT "rushes". Furthermore, there is no known (or observed) secondary action of bac that is dopaminergic or serotonergic.

[Ne/Neva Eva]

Baclofen and relationship to GHB

MusiciansMallet;1342338 wrote: Baclofen is a GABA-B agonist; & GABA is the most widespread neurotransmitter in the brain & it is inhibitory, and will cause general decreases in dopamine & serotonin, and NOT "rushes". Furthermore, there is no known (or observed) secondary action of bac that is dopaminergic or serotonergic.

Not to distract from the concerns of the OP...But I will ask here anyway.

There is something somewhere in my mind that remembers that there might be an increase in dopamine at the lower doses, and a decrease at higher doses. (This is largely irrelevant, but something that has long confused me.)

I'll see if I can figure out where and from whom I had this discussion previously.

Is it relevant, in general, with how/why bac works? If not, why not?

[ignominious]

Baclofen and relationship to GHB

Hi Krill
Absolutely yes to knowing that there are many similarities between Bac and GBH. They were both on my list, along with phenibut, GBL and a bunch of other things to buy when I first considered brain chemistry as an option!! After a couple of false starts I found I could get Bac over the counter and was on my way!

This is the 2nd time on HDB for me and one of the advantages is that I can recognize similarities from my 1st experience. !st time I was too confused and overloaded with new experiences to be able too analyse it.

Cut a long story short. I recognize the rushes you are talking about. Fairly infrequent but definitely there and enjoyable. I also have come to the conclusion that they are similar to amphetamines and therefore must be dopamine. However I know next to nothing about brain chemistry and love to be educated by the likes of Mallet, who clearly has a lot of knowledge in this area.

Yo Mallet. I also have some difficulty following you at times. So would appreciate it if you dumb it down a notch and if I want more I can ask.

Great topic

[MusiciansMallet]

Baclofen and relationship to GHB

ignominious;1347730 wrote: Yo Mallet. I also have some difficulty following you at times. So would appreciate it if you dumb it down a notch and if I want more I can ask.

Yea, i've been getting this a lot... I try my best; the thing is though, when you understand neurophysiology, by dumbing things down or oversimplifying it; you can convey inaccurate information. I am thinking of starting a thread, w/ pictures and all, explaining the basic terminology & concepts... which wouldn't be too long.

[MusiciansMallet]

Baclofen and relationship to GHB

ignominious;1347730 wrote: However I know next to nothing about brain chemistry and love to be educated by the likes of Mallet, who clearly has a lot of knowledge in this area.

The "rushes" you're speaking of is most likely one of the follow:

A) a result of agonism (agonism/agonist = just "plugging into a receptor") at the GHB receptor which is completely different than any other receptor;

B) a specific result of GABA-b stimulation, most likely through a sub-unit receptor (this just means a specific TYPE within the GABA-b family of receptors, which are being stimulated by any agonist like GHB or baclofen for example)... of which is currently not known; ~OR~

C) through interaction at a completely different receptor system (not GABA, not the GHB-receptor), which would obviously not yet be known to modern science/medicine. Which isn't a surprise with GHB (and related GHB drugs like GBL or GVL) and baclofen; since the former is illegal and the latter is an older drug & no pharmaceutical companies can make big bucks on it, therefore they wont pump any cash into studying its pharmacology, at least here in the US where health care is a f*cking business. One can only hope that the gov'ts of Europe, UK, Canada, Japan, or Australia decide to investigate the medical viability of at least baclofen (and its pharmacology) more thoroughly, especially once the effectiveness of baclofen as a moderator of addiction is more widely noticed & accepted!

If I had to bet on it; i'd go for option "B" though.

[StuckinLA]

Baclofen and relationship to GHB

What I've been curious about, and keep in mind I know nothing about the chemistry, is that if bac works because it hits what alcoholics are trying to hit with alcohol, wouldn't it make sense that there are similar effects?

By that I mean the calmness that O.A. describes. So when I (please Christ or whoever) hit my switch, won't it kind of be like walking around with 3-4 drinks in me, which is when I'm my calmest/happiest/most confident?

I don't know, and have no basis for this guess, but it's pretty much what I imagine...

[MusiciansMallet]

Baclofen and relationship to GHB

StuckinLA;1347952 wrote: What I've been curious about, and keep in mind I know nothing about the chemistry, is that if bac works because it hits what alcoholics are trying to hit with alcohol, wouldn't it make sense that there are similar effects?

By that I mean the calmness that O.A. describes. So when I (please Christ or whoever) hit my switch, won't it kind of be like walking around with 3-4 drinks in me, which is when I'm my calmest/happiest/most confident?

I don't know, and have no basis for this guess, but it's pretty much what I imagine...

No, alcohol "activates" or "plugs into" GABA-a receptors (which means it is a GABA-a agonist) where as baclofen "activates" or "plugs into GABA-b receptors (i.e., its a GABA-b agonist drug). There is no cross-tolerance between the two drugs (meaning, drugs that are GABA-a agonists don't plug into GABA-b agonists)... proof in this is that when you start baclofen, you don't start at HUGE doses to make up for your alcohol tolerance.... if you're following me?

Actually, replacing alcohol with a barbiturate or a high-dose benzodiazepine is more similar to walking around with a couple of drinks in you. Unfortunately the exact mechanism as to how alcohol agonizes GABA-a isn't known- compared to how the medical community knows in what way benzodiazepines (like valium or xanax) bind to their own "type" of GABA-a receptor & how barbiturates (like phenobarbital or butalbital) modulate GABA-a, albeit in a more complex way. So, as i said, how alcohol acts as a GABA-a agonist is poorly understood. However, the end result of alcohol, benzodiazepine, & barbiturate effects are cross tolerant & produce similar effects (although alcohol is less selective & hits other receptors other than GABA-a, like glutamate for example).

To not be so confusing: quite simply the mechanism as to how baclofen relates to addiction just isn't known, unfortunately. Although, it is no surprise since (as I said) way before these benefits of baclofen were recognized, it was no longer under patent and therefore extensive studies by pharmaceutical industries were never done, since they couldn't make a buck or two (pretty sick when we have our own HEALTH and LIVE monetized, merely a product... but that's my own opinion; thus I digress....)

My personal view is there is either some unknown mechanism of GABA-b agonists (like baclofen or GHB) that interact favorably with dependency/addiction ~OR~ there is a yet-to-be-discovered mechanism of baclofen outside of being a GABA-b agonist which assists with treating dependency. But, i'd wager on the former w/ baclofen's effectiveness w/ addiction, at least w/ dependency upon GABAergic substances (like alcohol, benzos, barbiturates, etc). While they act on totally different receptors, the physiological action of these drugs are somewhat similar (i.e., meaning, you notice similar effects; but the effects in your brain are in different areas).


I'd go into more detail.. but, it would probably be even more confusing; feel free to ask me to rephrase or explain some concepts if they're hard to understand!

[Ne/Neva Eva]

Baclofen and relationship to GHB

StuckinLA;1347952 wrote:
By that I mean the calmness that O.A. describes. So when I (please Christ or whoever) hit my switch, won't it kind of be like walking around with 3-4 drinks in me, which is when I'm my calmest/happiest/most confident?


MusiciansMallet;1347975 wrote: No, alcohol "activates" or "plugs into" GABA-a receptors ...followed by lots of super scientific stuff...

Here, lemme try, MM.

No. It's not like that at all.

and :H for good measure.

[MusiciansMallet]

Baclofen and relationship to GHB

Ne/Neva Eva;1347991 wrote: Here, lemme try, MM.

No. It's not like that at all.

LOL :H ..OR you could say it that way. Must be in my genes... i'm just long winded ...I have this need to always explain "WHY".... IN FACT, i think this is my shortest post ever haha

[StuckinLA]

Baclofen and relationship to GHB

Rats! :H

[ignominious]

Baclofen and relationship to GHB

Got to say Ne's synopsis made me chuckle.

MusiciansMallet;1347940 wrote: The "rushes" you're speaking of is most likely one of the follow:

A) a result of agonism (agonism/agonist = just "plugging into a receptor") at the GHB receptor which is completely different than any other receptor;

B) a specific result of GABA-b stimulation, most likely through a sub-unit receptor (this just means a specific TYPE within the GABA-b family of receptors, which are being stimulated by any agonist like GHB or baclofen for example)... of which is currently not known; ~OR~

C) through interaction at a completely different receptor system (not GABA, not the GHB-receptor), which would obviously not yet be known to modern science/medicine. Which isn't a surprise with GHB (and related GHB drugs like GBL or GVL) and baclofen; since the former is illegal and the latter is an older drug & no pharmaceutical companies can make big bucks on it, therefore they wont pump any cash into studying its pharmacology, at least here in the US where health care is a f*cking business. One can only hope that the gov'ts of Europe, UK, Canada, Japan, or Australia decide to investigate the medical viability of at least baclofen (and its pharmacology) more thoroughly, especially once the effectiveness of baclofen as a moderator of addiction is more widely noticed & accepted!

OK, my version of dumbing it down:

A) Similar action on GHB receptor - Could conceivably cause dopamine.

B) Result of GABA b stimulation. We don't know. - Could result in dopamine.

C) Unknown reactions, You, I and we don't know. - Could result in dopamine.

[ignominious]

Baclofen and relationship to GHB

StuckinLA;1347952 wrote: What I've been curious about, and keep in mind I know nothing about the chemistry, is that if bac works because it hits what alcoholics are trying to hit with alcohol, wouldn't it make sense that there are similar effects?

By that I mean the calmness that O.A. describes. So when I (please Christ or whoever) hit my switch, won't it kind of be like walking around with 3-4 drinks in me, which is when I'm my calmest/happiest/most confident?

I don't know, and have no basis for this guess, but it's pretty much what I imagine...

Hi LA
IMO I don't think OA had a SE free journey.
I expect that he just viewed the effects positively. Maybe it will be like having some of the good effects of having 3-4 drinks without some of the cumbersome baggage that alcoholics have to endure