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Baclofen: alternative for Phenibut ????

phenibut baclofen troll fake character manipulation ?

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#1 Sarif

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Posted 23 February 2016 - 03:35 PM


I read a lot about the mood enhancing affect of Phenibut, and since anything else hardly work for my depression, social anxiety and insomnia (more on: http://www.longecity...e-1#entry730339 ), I tried to give it a shot. But just after ordering it, I read some pretty horrifying story of phenibut withdrawal. Since I have very bad impulse control, I am sure that I’ll not be able to maintain the dosage properly so I cancelled the order.
 
Upon further research, I came across the name of Baclofen which is mentioned as the only safe alternative for phenibut. I bought it before 2 days. My main goal was to sleep improvement and if possible mood enhancement – 
 
1. First day I took 40 mg of baclofen 2 hours before bed. I slept pretty well. In the morning felt like drunk. Whole day felt sleepy.
2. Second day I took 20 mg of baclofen 2 hours before bed. Sleep was good, but the same sleepiness was there for the whole day.
 
Now, can you please help me with the below doubts –
 
1. Is it safe?
2. Is there anything I can do for the sleepiness? I want to continue taking this as this is one of the few things which helps me sleep properly. I don’t think modafinil is an option for me for wakefulness since I react pretty badly to it. 
3. Is pehnibut as bad as it is made out to be?
 
Thanks for your time,
 


#2 Oracle Laboratories

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Posted 24 February 2016 - 05:25 AM

Phenibut and Baclofen are essentially almost the exact same compound.  Both are the amino acid GABA (Gamma-Aminobutyric Acid) - the primary inhibitory neurotransmitter of the Central Nervous System - with the addition of a phenyl ring on the GABA chain to make the molecule lipophillic (fat soluble) enough to cross the Blood-Brain-Barrier, which GABA itself does not. The only difference, is that Baclofen has the addition of a single chloride atom on the 4 position of the phenyl ring.  

 

This additional chloride atom has one major advantage, in that is significantly protects the moecule from the extensive first-pass metabolism that Phenibut encounters in the stomach, which is why a typical dose of Baclofen might be 20mg, whereas an equal oral dose of Phenibut would be around 2000mg.  However, other that that, the are almost pharmacologically identical.  Both act as full agonists at the GABA -B Receptors and cause mild sedation, skeletal muscle relaxation, a slight sense of euphoria (due to a slight in-direct Ca+ mediated dopamine releasing effect based on our research), and both can cause mild physical dependence.

I hear all of these way over-exaggerated horror stories about Phenibut withdrawal.  Well, Baclofen works in an identical pharmacological mechanism-of-action, and it too will cause discomfort, dysphoria, insomnia, and rebound anxiety if it is taken regularly, or in large doses, and then is discontinued abruptly, just like Phenibut.  I will also state, that I think you would be much better off taking the Phenibut, as Baclofen does not provide nearly as noteworthy anxiolytic effects in most people, compared to Phenibut.  My institute has experimented with dozens of GABA-derivative amino acids and related esters.  

Even though both Phenibut and Baclofen bind as full agonists at the GABA -B Receptors, it seems that the same chloride atom that protects Baclofen from the extensive first-pass metabolism in the stomach that Phenibut is subject too, is the exact reason why Baclofen does not act as strong an agonist at GABA -B binding sites as Baclofen does.  Additionally, Phenibut also possesses one pharmacological action that Baclofen doesn't.  In addition to Phenibut's action at the GABA -B Receptors, it also acts as an antagonist at the TAAR1 Receptors (Trace Amine-Associated Receptor), which blocks the binding of the endogenous substance B-phenethylamine in the brain.  The phenethylamine backbone is the prototype carbon backbone for a class of synthetic drugs known as "the phenethylamines", which includes the amphetamines and some of the substituted amphetamines, as well as other stimulant drugs that cause anxiety, such as Cathinone, Mephedrone, etc.  This is because the TAAR1 Receptor is responsible for triggering the release of the neurotransmitters dopamine and norepinephrine (also known as nor-adrenaline), which can bring upon the "fight-or-flight response" and cause anxiety.  Because Phenibut both out-competes B-phenthylamine at TAAR1 Receptors, and actually functions as an antagonist at this site (rather than an agonist (activator) like B-phenethylamine), this is another way that Phenibut exerts it's anti-anxiety effects.  Again, because of the additional chloride atom on the phenyl ring of Baclofen, the TAAR1 receptor is not antagonized, and Baclofen in fact produces almost no measurable affinity for the TAAR1 Receptors at all, so this is an anti-anxiety effect unique to Phenibut. 

Now to the question of Phenibut being some big scary drug.  ANY GABA -A or GABA -B Receptor agonist that is used for an extended period of time, or in massive dosages, is going to cause some form of GABA-mediated withdrawal syndrome, simply because your GABA Receptors become down-regulated, and are used to having the presence of a strong agonist activating them.  When the GABA agonist drug is stopped, the endogenous GABA in your brain is not enough to adequately agonize it again, as it did before you started using the GABA agonist drug.  Eventually, the GABA Receptors do normalize, and everything returns to normal, but in some cases it can take a while.

Whether you are using Baclofen or Phenibut for an extended period of time, you will develop some degree of withdrawal syndrome upon abrupt cessation of the drug.  For most people, Phenibut entails a week or two of restless nights, minor cold sweats, and rebound anxiety.  However, if used habitually, Baclofen will cause the same withdrawal syndrome. (So why not use the Phenibut and receive a better anti-anxiety effect from it?)  When we talk about GABA Receptor agonist drug withdrawal, we are usually talking about the GABA -A Receptors, to which drugs like the benzodiazepines, barbituates, and drugs like meprobamate, and methaqualone bind to.  The metabotropic GABA -A Receptors are indeed much different receptors, structurally, compared to the ionotropic GABA -B Receptors.  While abrupt cessation of a GABA -A Receptor agonist drug, like a benzodiazepine or barbituate can cause Tonic Clonic, Opoclonic, and Gran Mal Seizures, and can be a medical emergency, GABA -B Receptor agonist drug withdrawal is ultimately benign. - And, unless you are a pre-existing epileptic, will not cause convulsions like many GABA -A Receptor agonist drugs do upon discontinuation.

The most severe withdrawal symptoms from GABA -B agonists like Phenibut or Baclofen, is insomnia, cold sweats, moodiness, and rebound anxiety.  How do you eliminate this?  Simply by gradually weaning down your dose, so that your up-regulated GABA Receptors have time to re-balance their neuronal Ca+ transmission.  As long as you do not abruptly stop taking Phenibut, you should not experience any discomfort when you finally decide to discontinue it's use, as long as you wean down your dose gradually and do not stop it abruptly.  I assume that this is what you meant when you said that you heard of Phenibut being "dangerous".  Remember, Phenibut is just a Blood-Brain-Barrier permeable version of the neurotransmitter GABA that is already in your brain.  No GABA agonists really suppress respiration much, and GABA -B Receptor agonists have virtually no affect on respiratory suppression.  In addition to that, the LD50 (lethal dose 50%) value in rodents is very high, meaning that you would need to take a ton of Phenibut to actually cause significant Central-Nervous-System or Peripheral-Nervous-System damage.

 

Being a psychopharmacologist and a sufferer of horrendous Panic Attack Disorder myself, I am a huge proponent of Phenibut.  It really is not sedative to me at all, like it is in some people. However, I also take prescription clonazepam (a GABA -A agonist benzodiazepine), and I work with experimental benzodiazepine analogues, and other GABA -A agonist compounds, so my tolerance for GABAergic drugs is significantly higher than most people's.  In all honesty, I may not be able to live outside of an institution sometimes if it weren't for Phenibut.  This led to my development of over a dozen GABA-chain / Phenibut esters and derivatives, many of which we are in the in-vivo and in-vitro testing phases now, with promising results thus far.  According to conventional wisdom, I take a massive daily dose of Phenibut (I will weight it tomorrow), and have been at this does for years.  I used to experience minor discomfort such as cold sweats, insomnia, and rebound anxiety if I went without taking it, but anymore, even if I skip a day or so, I do not feel much discomfort.  As long as you sensibly wean down your dose before stopping Phenibut "cold turkey", you shouldn't experience much of any discomfort.  As far as it'a general use, Phenibut is a very benign and helpful substance, if used in the recommended dosage range.

Although Baclofen acts as a GABA -B Receptor agonist just like Phenibut, the addition of the chloride atom on the Baclofen molecule appears to pretty notably diminish it's anxiolytic effects.  Phenibut combats anxiety much better, and Baclofen will cause the exact same withdrawal syndrome upon abrupt discontinuation, so I would definitely choose Phenibut over Baclofen.  Even for it's intended purpose - as a skeletal muscle relaxant, Baclofen is a rather inefficient drug.

I hope this helps you some.

 

 

-John Gona
Psychopharmacologist
Psychotropic / Nootropic Treatment Specialist

Oracle Laboratories
NeuroPsych Institute 
 


Edited by Oracle Laboratories, 24 February 2016 - 05:58 AM.

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#3 stillwater

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Posted 24 February 2016 - 06:38 PM

Being a psychopharmacologist and a sufferer of horrendous Panic Attack Disorder myself, I am a huge proponent of Phenibut.  It really is not sedative to me at all, like it is in some people. However, I also take prescription clonazepam (a GABA -A agonist benzodiazepine), and I work with experimental benzodiazepine analogues, and other GABA -A agonist compounds, so my tolerance for GABAergic drugs is significantly higher than most people's.  In all honesty, I may not be able to live outside of an institution sometimes if it weren't for Phenibut.  This led to my development of over a dozen GABA-chain / Phenibut esters and derivatives, many of which we are in the in-vivo and in-vitro testing phases now, with promising results thus far.  According to conventional wisdom, I take a massive daily dose of Phenibut (I will weight it tomorrow), and have been at this does for years.  I used to experience minor discomfort such as cold sweats, insomnia, and rebound anxiety if I went without taking it, but anymore, even if I skip a day or so, I do not feel much discomfort.  As long as you sensibly wean down your dose before stopping Phenibut "cold turkey", you shouldn't experience much of any discomfort.  As far as it'a general use, Phenibut is a very benign and helpful substance, if used in the recommended dosage range.

 

Although Baclofen acts as a GABA -B Receptor agonist just like Phenibut, the addition of the chloride atom on the Baclofen molecule appears to pretty notably diminish it's anxiolytic effects.  Phenibut combats anxiety much better, and Baclofen will cause the exact same withdrawal syndrome upon abrupt discontinuation, so I would definitely choose Phenibut over Baclofen.  Even for it's intended purpose - as a skeletal muscle relaxant, Baclofen is a rather inefficient drug.

I hope this helps you some.


 

 

-John Gona
Psychopharmacologist
Psychotropic / Nootropic Treatment Specialist

Oracle Laboratories
NeuroPsych Institute 

 

 

 

 

Great post John, this has made me look at Phenibut in a different light, I periodically use Baclofen but was never all that happy with it.   As a fellow sufferer of panic disorder, I'm curious if you don't mind sharing if there's anything else you take for panic disorder ?

 

 

 

 


Edited by stillwater, 24 February 2016 - 06:42 PM.


#4 Sarif

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Posted 24 February 2016 - 07:03 PM

Hi John,

 

Thanks a lot for taking the time to reply. That was really informative.

 

I agree with you that phenibut gets it's bad name because some people can't keep it within limit - anything in excess will cause adverse effects. Keeping that mind, can you please suggest a safe routine that I can follow while taking phenibut? Is t ok to take this everyday? If yes how much? I don't mind the dependence as long as it works. But what about tolerance? It'll be a problem if the dosage that I took last week doesn't work this week and I have to keep increasing it every time.  

 

Also is there any particular brand that you would suggest? 

 

If I take baclofen before bedtime I feel sleepy the next day. Does that mean that I'll be sleepy while taking phenibut as well? Please note that I'm not looking to get high but rather function normally.

 

Thanks again,

 



#5 medievil

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Posted 24 February 2016 - 08:37 PM

Havent read the previous posts so i apoligise if its been posted before,

 

The main action of phenibut is that it acts on that same subunit as gabapentin and pregabalin with minimal gabab activity, it feels and acts completely differened to baclofen, which is a strong gabab agonist, not rewarding and shifts brainactivity to better decission making which explains for a part its effects in addiction.



#6 Oracle Laboratories

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Posted 24 February 2016 - 10:54 PM

stillwater,
 
As far as prescription GABA -A agonist medications, everything from the barbituates and drugs like meprobamate, to the modern day benzodiazepines are highly effective.  I butt heads with a lot of the psychiatrists that I work with and their prescribing habits on occassion, since they tend to like to prescribe SSRI's (Selective Serotonin Reuptake Inhibitors), or anti-psychotic dopamine antagonist drugs like thorazine to deal with Panic Attack Disorder.  First off, PAD is a VERY different condition than Generalized Anxiety Disorder or Agoraphobia (Social Anxiety Disorder), as these disorders tend be be modulated by serotonin, and go hand-in-hand with Serotonin-Mediated-Depression.  Whereas Generalized Anxiety Disorder is a mental condition, where individuals lay awake at night wondering how they are going to pay their car insurance bills, etc.,Panic Attack Disorder is not a typical mental disorder, and is more physical than anything - causing pain and/or tightness in the chest and/or head, causing severe sweats, and flooding the brain with the "flight or flight" panic sensation that leads people to believe that they are having heart attacks and/or dying.  Panic Attack Disorder is caused by an imbalance in two neurotransmitters - a deficiency in GABA, and an over-abundance in norepinephrine (or "nor-adrenalin").  
 
True Panic Attack Disorder has nothing directly to do with serotonin biosynthesis, release, reuptake, or metabolism.  Even more ridiculous than expecting an SSRI drug to effectively combat Panic Attack Disorder is using a dopamine antagonist anti-psychotic drug.  Panic Attack Disorder has literally nothing to do with synaptic or neuronal dopamine levels.  These drugs simply antagonize the dopamine receptors so much that a person is literally rendered a zombie, and just doesn't notice the panic attacks as pronounced.  (Think of the schizophrenic patients in mental wards who sit and look out of the window while drooling on themselves, unable to even think normally).  So, just because the dopamine antagonist drugs "zombify" you enough that you don't necessarily notice the panic attacks as much, does not mean that it's an appropriate treatment.  Using a good GABA -A Receptor agonist like a benzodiazepine tends to be the most effective prescription treatment.  Some Selective Serotonin Reuptake Inhibitors used alongside of a benzodiazepine can benefit panic attacks indirectly.  Ideally, a good norepinephrine (adrenergic) antagonist drug would be a great development to combat the "flight or flight" panic reflex that is the cause of the panic attacks in the first place.  Myself and my colleagues at our institution are working on several prototype drugs of this class currently.
 
As far as over-the-counter nootropic or herbal supplements, the kavalactone alkaloids found in the Kava Kava plant can be beneficial, and the brand Yogi now makes a kava stress-relief tea.  Some of the flavonoids in Chamomile can be helpful in taking the edge off of panic attacks as well, and I highly recommend name brand Celestial Seasonings Sleepytime Tea.  You can also look into the herb Withania somnifera (Ashwagandha), as it possesses some alkaloids that modulate neuronal GABA transmission.  However, in my experience, Phenibut is far more effective than any other supplemental or nootropic substance, and if it is combined the correct way with a prescription drug regimen, it can significantly improve one's quality of life.  Also, unlike many GABA -A Receptor agonists (like benzodizepines), tolerance to Phenibut does not occur nearly to the same degree.  The intial sedating effects will become less prevalent over time, but the anxiolytic properties remain intact at right around the same dose.  I have been at the same dosage for years, and have even been able to cut my dose down a bit more recently, and still maintain great control over anxiety.
 
 
Sarif, 
 
There are two major forms of Phenibut that can be purchased by supplement suppliers - Phenibut in it’s free-amino-acid form (“Phenibut FAA”), and the hydrochloride salt of Phenibut (Phenibut hydrochloride, or “Phenibut HCL”).  Both have their advantages. Generally water-soluble salts of different drugs are more easily absorbed by the gastrointestinal tract, however since Phenibut is a water-soluble amino acid in it’s pure form, Phenibut Free-Animo-Acid is still absorbed fairly well. (Phenibut is subject to extremely degradable first-pass metabolism in the stomach and GI tract, and so large doses of either form have to be used, as a large majority of the oral dose will be destroyed in the stomach). Phenibut Free-Amino-Acid has the advantage of not being so horribly sour in the mouth compared to Phenibut hydrochloride, and so it can be taken sublingually (dumped under the tongue to dissolve, and be absorbed by the veins under the tongue). 
 
Whether taking Phenibut in free-amino-acid form or as Phenibut hydrochloride, most people dose once to twice daily. Personally, I have always only ever needed to dose once in the morn ing, as I feel the anxiolytic effects last a good twenty-or-so hours. Since the Phenibut in free-amino acid form, is it’s pure form, and does not contain the hydrochloride portion of the molecule on it, like Phenibut hydrochloride does, it is about 18% more potent, milligram for milligram than Phenibut hydrochloride. Either way, typical starting doses are 500mg to 1000mg, and after you titrate up to your ideal dosage, doses of 4000mg are not all that uncommon. (I’ll have to weight my usualy daily dosage tomorrow morning, as I take what most people consider to be an enormous dose). Most Phenibut supplement suppliers recommend only taking Phenibut twice per week to avoid the development of the mild dependence that Phenibut can cause, but that really isn’t realistic if you are using Phenibut for a legitimate therapeutic purpose. I have dosed every day for years, and as long as you gradually wane your dose down before discontinuing use, you should avoid the withdrawal syndrome, and the rebound anxiety. - That is the difference between addiction and dependence. You certainly can become mildly dependent on Phenibut, but is anybody really “addicted” to Phenibut?  I’ve never heard of anybody gathering up their buddies to get together and get f#cked up on Phenibut.  There are many people who are dependent on blood-pressure medications like lisinopril or beta-blocker like metoprolol, but are they “addicted” to these drugs?  Of course not.
 
As I mentioned above, unlike GABA -A Receptor agonist drugs like benzodiazepines, tolerance to Phenibut does not occur to a very noteworthy degree. The initial sedating effects will become somewhat less apparent over time, but the anxiolytic properties are generally maintained by a steady, effective dose. I have taken the same dose for years, and I have even cut that dose down a bit recently, and I still retain very good anxiety control from my usual dose. If Baclofen sedates you, than yes, Phenibut is going to sedate you to some degree as well, as they function almost identically pharmacologically. (With Phenibut possessing a few unique properties, that I will touch on below).  As far as brand name manufacturers, I suggest Liftmode.com.  I have bought off them for years, and even ran analyses on some of their products, when they were still selling through Amazon, before the creation of their website. Their prices are great, and the quality is unsurpassed - the best that you will find.
 
 
medievil,
 
You are correct in some regards, and I touched briefly on the Ca+ neuro-transmission in my original post. Myself and my colleagues have both confirmed and measured the binding affinities of Phenibut, Baclofen, and over a dozen other GABA-chain esters and derivatives that I’ve developed, at the GABA -B Receptor, using in-vitro cloned GABA -B Receptors, and in-vitro Electrocondusive-Magnetic Resonance Imaging and Crystalline X-Ray Fluoroscopy. We have also confirmed the GABA -B binding and agonist activity on the overall effects of Phenibut on anxiety, by using the selective GABA -B Receptor antagonist Saclofen (and additionally using Phaclofen), which effectively cancelled out the majority of the anxiolytic effect of Phenibut in both in-vivo animal and human models. Both Phenibut and Baclofen have comparable binding affinity for the GABA -B Recetor, and both function as full agonists at this receptor, Baclofen’s agonist action is somewhat greater.
 
In addition, Phenibut antagonizes the TAAR1 (Trace Amine Associated Receptor), blocking the binding of endogenous B-phenethylamine in the brain. Also, you are correct that one of the pharmacological mechanisms-of-action that Phenibut possesses is as a gabapentinoid  (such as gabapentin and pregabalin), which acts of as a preferential blocker of a2o subunit-containing Voltage-Gated-Calcium channels of the GABA protein ligands, which is responsible for Phenibut’s in-direct modulation of synaptic dopamine release, and at which site Baclofen has no appreciable binding affinity for. (This effect of the Ca+ a2o-subunit likely additionally adds more sedating property, and anticonvulsant potential than pure GABA -B agonists typically do. Knowing this, in addition to classifying Phenibut as a GABA -B Receptor agonist, we can also classify it as a GABA -B Receptor Positive Allosteric Modulator.
 
It is incredible that the simple addition of a single chloride atom on the phenyl ring of Baclofen could cause such dramatic pharmacological actions. It is also amazing how much the simple addition of a cyclic phenyl ring on both of these compounds can change the simple action of GABA so much, and effect the compounds’ selectivity so much.
 
 
 
 
 
-John Gona
Psychopharmacologist,
Psychotropic / Nootropic Treatment Specialist
 
Oracle Laboratories
NeuroPsych Institute

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#7 medievil

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Posted 25 February 2016 - 05:43 PM

 

stillwater,
 
As far as prescription GABA -A agonist medications, everything from the barbituates and drugs like meprobamate, to the modern day benzodiazepines are highly effective.  I butt heads with a lot of the psychiatrists that I work with and their prescribing habits on occassion, since they tend to like to prescribe SSRI's (Selective Serotonin Reuptake Inhibitors), or anti-psychotic dopamine antagonist drugs like thorazine to deal with Panic Attack Disorder.  First off, PAD is a VERY different condition than Generalized Anxiety Disorder or Agoraphobia (Social Anxiety Disorder), as these disorders tend be be modulated by serotonin, and go hand-in-hand with Serotonin-Mediated-Depression.  Whereas Generalized Anxiety Disorder is a mental condition, where individuals lay awake at night wondering how they are going to pay their car insurance bills, etc.,Panic Attack Disorder is not a typical mental disorder, and is more physical than anything - causing pain and/or tightness in the chest and/or head, causing severe sweats, and flooding the brain with the "flight or flight" panic sensation that leads people to believe that they are having heart attacks and/or dying.  Panic Attack Disorder is caused by an imbalance in two neurotransmitters - a deficiency in GABA, and an over-abundance in norepinephrine (or "nor-adrenalin").  
 
True Panic Attack Disorder has nothing directly to do with serotonin biosynthesis, release, reuptake, or metabolism.  Even more ridiculous than expecting an SSRI drug to effectively combat Panic Attack Disorder is using a dopamine antagonist anti-psychotic drug.  Panic Attack Disorder has literally nothing to do with synaptic or neuronal dopamine levels.  These drugs simply antagonize the dopamine receptors so much that a person is literally rendered a zombie, and just doesn't notice the panic attacks as pronounced.  (Think of the schizophrenic patients in mental wards who sit and look out of the window while drooling on themselves, unable to even think normally).  So, just because the dopamine antagonist drugs "zombify" you enough that you don't necessarily notice the panic attacks as much, does not mean that it's an appropriate treatment.  Using a good GABA -A Receptor agonist like a benzodiazepine tends to be the most effective prescription treatment.  Some Selective Serotonin Reuptake Inhibitors used alongside of a benzodiazepine can benefit panic attacks indirectly.  Ideally, a good norepinephrine (adrenergic) antagonist drug would be a great development to combat the "flight or flight" panic reflex that is the cause of the panic attacks in the first place.  Myself and my colleagues at our institution are working on several prototype drugs of this class currently.
 
As far as over-the-counter nootropic or herbal supplements, the kavalactone alkaloids found in the Kava Kava plant can be beneficial, and the brand Yogi now makes a kava stress-relief tea.  Some of the flavonoids in Chamomile can be helpful in taking the edge off of panic attacks as well, and I highly recommend name brand Celestial Seasonings Sleepytime Tea.  You can also look into the herb Withania somnifera (Ashwagandha), as it possesses some alkaloids that modulate neuronal GABA transmission.  However, in my experience, Phenibut is far more effective than any other supplemental or nootropic substance, and if it is combined the correct way with a prescription drug regimen, it can significantly improve one's quality of life.  Also, unlike many GABA -A Receptor agonists (like benzodizepines), tolerance to Phenibut does not occur nearly to the same degree.  The intial sedating effects will become less prevalent over time, but the anxiolytic properties remain intact at right around the same dose.  I have been at the same dosage for years, and have even been able to cut my dose down a bit more recently, and still maintain great control over anxiety.
 
 
Sarif, 
 
There are two major forms of Phenibut that can be purchased by supplement suppliers - Phenibut in it’s free-amino-acid form (“Phenibut FAA”), and the hydrochloride salt of Phenibut (Phenibut hydrochloride, or “Phenibut HCL”).  Both have their advantages. Generally water-soluble salts of different drugs are more easily absorbed by the gastrointestinal tract, however since Phenibut is a water-soluble amino acid in it’s pure form, Phenibut Free-Animo-Acid is still absorbed fairly well. (Phenibut is subject to extremely degradable first-pass metabolism in the stomach and GI tract, and so large doses of either form have to be used, as a large majority of the oral dose will be destroyed in the stomach). Phenibut Free-Amino-Acid has the advantage of not being so horribly sour in the mouth compared to Phenibut hydrochloride, and so it can be taken sublingually (dumped under the tongue to dissolve, and be absorbed by the veins under the tongue). 
 
Whether taking Phenibut in free-amino-acid form or as Phenibut hydrochloride, most people dose once to twice daily. Personally, I have always only ever needed to dose once in the morn ing, as I feel the anxiolytic effects last a good twenty-or-so hours. Since the Phenibut in free-amino acid form, is it’s pure form, and does not contain the hydrochloride portion of the molecule on it, like Phenibut hydrochloride does, it is about 18% more potent, milligram for milligram than Phenibut hydrochloride. Either way, typical starting doses are 500mg to 1000mg, and after you titrate up to your ideal dosage, doses of 4000mg are not all that uncommon. (I’ll have to weight my usualy daily dosage tomorrow morning, as I take what most people consider to be an enormous dose). Most Phenibut supplement suppliers recommend only taking Phenibut twice per week to avoid the development of the mild dependence that Phenibut can cause, but that really isn’t realistic if you are using Phenibut for a legitimate therapeutic purpose. I have dosed every day for years, and as long as you gradually wane your dose down before discontinuing use, you should avoid the withdrawal syndrome, and the rebound anxiety. - That is the difference between addiction and dependence. You certainly can become mildly dependent on Phenibut, but is anybody really “addicted” to Phenibut?  I’ve never heard of anybody gathering up their buddies to get together and get f#cked up on Phenibut.  There are many people who are dependent on blood-pressure medications like lisinopril or beta-blocker like metoprolol, but are they “addicted” to these drugs?  Of course not.
 
As I mentioned above, unlike GABA -A Receptor agonist drugs like benzodiazepines, tolerance to Phenibut does not occur to a very noteworthy degree. The initial sedating effects will become somewhat less apparent over time, but the anxiolytic properties are generally maintained by a steady, effective dose. I have taken the same dose for years, and I have even cut that dose down a bit recently, and I still retain very good anxiety control from my usual dose. If Baclofen sedates you, than yes, Phenibut is going to sedate you to some degree as well, as they function almost identically pharmacologically. (With Phenibut possessing a few unique properties, that I will touch on below).  As far as brand name manufacturers, I suggest Liftmode.com.  I have bought off them for years, and even ran analyses on some of their products, when they were still selling through Amazon, before the creation of their website. Their prices are great, and the quality is unsurpassed - the best that you will find.
 
 
medievil,
 
You are correct in some regards, and I touched briefly on the Ca+ neuro-transmission in my original post. Myself and my colleagues have both confirmed and measured the binding affinities of Phenibut, Baclofen, and over a dozen other GABA-chain esters and derivatives that I’ve developed, at the GABA -B Receptor, using in-vitro cloned GABA -B Receptors, and in-vitro Electrocondusive-Magnetic Resonance Imaging and Crystalline X-Ray Fluoroscopy. We have also confirmed the GABA -B binding and agonist activity on the overall effects of Phenibut on anxiety, by using the selective GABA -B Receptor antagonist Saclofen (and additionally using Phaclofen), which effectively cancelled out the majority of the anxiolytic effect of Phenibut in both in-vivo animal and human models. Both Phenibut and Baclofen have comparable binding affinity for the GABA -B Recetor, and both function as full agonists at this receptor, Baclofen’s agonist action is somewhat greater.
 
In addition, Phenibut antagonizes the TAAR1 (Trace Amine Associated Receptor), blocking the binding of endogenous B-phenethylamine in the brain. Also, you are correct that one of the pharmacological mechanisms-of-action that Phenibut possesses is as a gabapentinoid  (such as gabapentin and pregabalin), which acts of as a preferential blocker of a2o subunit-containing Voltage-Gated-Calcium channels of the GABA protein ligands, which is responsible for Phenibut’s in-direct modulation of synaptic dopamine release, and at which site Baclofen has no appreciable binding affinity for. (This effect of the Ca+ a2o-subunit likely additionally adds more sedating property, and anticonvulsant potential than pure GABA -B agonists typically do. Knowing this, in addition to classifying Phenibut as a GABA -B Receptor agonist, we can also classify it as a GABA -B Receptor Positive Allosteric Modulator.
 
It is incredible that the simple addition of a single chloride atom on the phenyl ring of Baclofen could cause such dramatic pharmacological actions. It is also amazing how much the simple addition of a cyclic phenyl ring on both of these compounds can change the simple action of GABA so much, and effect the compounds’ selectivity so much.
 
 
 
 
 
-John Gona
Psychopharmacologist,
Psychotropic / Nootropic Treatment Specialist
 
Oracle Laboratories
NeuroPsych Institute

 

Since the GABAB agonism should be comparable, why is phenibut addictive and baclofen anti addictive? baclofen supresses da, so the drug is not associated with increased dopamine which makes a drug addictive, yet it looks like phenibut does increase da, is it possible the 

 

oh wait

 

 

 

which acts of as a preferential blocker of a2o subunit-containing Voltage-Gated-Calcium channels of the GABA protein ligands, which is responsible for Phenibut’s in-direct modulation of synaptic dopamine release

Do you have any source that this releases dopamine, id also like to read more in debt about the rewarding effects.

 

Also, do you happen to have studied ghb, and the effects of the GHB receptor on reward? i gues this is what makes amisulpiride effective anhedonia altough it has been shown to modulate the opiate like receptors.



#8 medievil

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Posted 25 February 2016 - 05:47 PM

 

 

 tolerance to Phenibut does not occur to a very noteworthy degree. The initial sedating effects will become somewhat less apparent over time, but the anxiolytic properties are generally maintained by a steady, effective dose. I have taken the same dose for years, and I have even cut that dose down a bit recently, and I still retain very good anxiety control from my usual dose. 

I share the same experience, but lets not ignore the countless anecdotes reporting immediate tolerance, so imo our experience does not proof much.



#9 sativa

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Posted 25 February 2016 - 06:39 PM

Regarding tolerance, wouldn't a combination of NMDA antagonists and general upregulators of neurotransmitter systems be a feasible method of resetting tolerences to a substance?

For example, memantine has been very useful for me in this context.

Lobelia inflata also, but perhaps this is more ideal for nicotine addiction/cessation.

Iboga is undoubtedly the most effective means of achieving this. Some argue its safety profile is cause for concern. I personally take micro doses of a liquid full spectrum extract.

And of course, combinations of other things that possess NMDA antagonist activity such as agmatine, magnesium etc

#10 medievil

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Posted 25 February 2016 - 06:43 PM

From the numerous threads ive made on the subject on tolerance prevention and NMDA antagonism, it seemed to appear that the results with GABAB acting substances was inconclusive, i do remember a anecdote of ibogaine resetting tolerance to GHB, and a anecdote of a girl i know saying she kept on getting really high on GHB when combined with DXM.


Tell me more about the micro doses you are taking, as ive been planning to take daily low ibogaine doses for a while now.



#11 sativa

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Posted 25 February 2016 - 07:07 PM

From the numerous threads ive made on the subject on tolerance prevention and NMDA antagonism, it seemed to appear that the results with GABAB acting substances was inconclusive, i do remember a anecdote of ibogaine resetting tolerance to GHB, and a anecdote of a girl i know saying she kept on getting really high on GHB when combined with DXM.

Tell me more about the micro doses you are taking, as ive been planning to take daily low ibogaine doses for a while now.

Well, from personal experience, I've used memantine to significantly lower my brain tolerances to all drugs. Iboga is a step up and will, via multiple mechanisms (as you are probably already familiar with) significantly lower tolerances across the board, ie for all neurotransmitters, which, of course, implies that all drugs will therefore be more effective.

I microdose iboga fairly sporadically nowadays, but also use it in a shamanistic context, if you see what I mean? Micro doses provide the benefits of neurotransmitter upregulation without a psychedelic journey "into the self" so to speak. I usually take it before bed.

I recently acquired 1g memantine HCL, which I will be using in an "ultimate" cognitive boosting combination, along with other alpha 7 nicotinic antagonists, and a general muscarinic antagonist (scopolamine). This will be followed by an acetylcholinesterase inhibitor and possibly a dopamine TAAR agonist (Celastrus Paniculatus fits the bill). I intend to fit a BDNF/NGF/GDNF promoting substance too (Theanine, kirkii, gotu kola are ideal)

Edited by sativa, 25 February 2016 - 07:08 PM.

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#12 medievil

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Posted 25 February 2016 - 07:12 PM

?

I recently acquired 1g memantine HCL, which I will be using in an "ultimate" cognitive boosting combination, along with other alpha 7 nicotinic antagonists, and a general muscarinic antagonist (scopolamine).

 

All those substances will be impairing, mem is individual and enhancing for some, but alpha7 antagonism is the great for tolerance and addiction but not for cognitive enhancement, also scopolamine, besides being interesting as its a extremely effective antidepressant after just one administration is cognitively impairing, while enhancing some negatives in shizo perhaps.



#13 sativa

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Posted 25 February 2016 - 08:41 PM

?
I recently acquired 1g memantine HCL, which I will be using in an "ultimate" cognitive boosting combination, along with other alpha 7 nicotinic antagonists, and a general muscarinic antagonist (scopolamine).

All those substances will be impairing, mem is individual and enhancing for some, but alpha7 antagonism is the great for tolerance and addiction but not for cognitive enhancement, also scopolamine, besides being interesting as its a extremely effective antidepressant after just one administration is cognitively impairing, while enhancing some negatives in shizo perhaps.


I understand where you are coming from, but the magic happens once the antagonsism wears of: aka upregulation of all those neurotransmitter systems! In the past this has significantly increased my overall cognition, reduced tolerances and of course provides a great mood uplifting effect ;)

Have you had personal experience with memantine?

Perhaps some context: I do not have any condition that I am intending to treat. I do not smoke or drink alcohol anymore. I use an array of adaptogens and botanicals, for all around improvement/enhancement.

Edited by sativa, 25 February 2016 - 08:46 PM.


#14 medievil

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Posted 25 February 2016 - 08:48 PM

lol is that a serieus question? im most famous online for my promotion of memantine and other nmda antagonists for tolerance.



#15 sativa

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Posted 25 February 2016 - 08:53 PM

lol is that a serieus question? im most famous online for my promotion of memantine and other nmda antagonists for tolerance.


Oh haha, I honestly didn't know!

Of course, during antagonsism cognition temporarily declines but afterwards it is boosted, is this not what you know to be?

#16 medievil

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Posted 25 February 2016 - 09:07 PM

Cognition temporary declines because of alpha7 antagonism, after those receptors upregulate this normalises, memantine does not interfere with normal glutaminergic transmission, only blocking excessive glutamate activity, in theory, well its kinda right, for most ppl it will be cognitively neutral, for those that have excessive glutamate it would improve cognition but its also individual, that said it increases tau wich is a measure of intelligence.

 

Dude im the sole reason memantine is talked about on fora like this, maybe not the sole reason but i could say that im pretty much the guy behind its popular use, even with professionals, many may not agree with me but ive done a shitload to make memantine popular for tolerance and the treatment of mental illness.



#17 sativa

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Posted 25 February 2016 - 09:11 PM

Cognition temporary declines because of alpha7 antagonism, after those receptors upregulate this normalises, ...


Isn't the new baseline level of a7 higher than before dosing memantine?

#18 medievil

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Posted 25 February 2016 - 09:31 PM

I didnt think so but thats an assumption, which what you are saying is too on your part i think ;)



#19 Sarif

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Posted 26 February 2016 - 05:38 AM

Guys......aren't we moving away from our original topic - 'phenibut safety' ?  ;)



#20 medievil

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Posted 26 February 2016 - 06:11 AM

Phenibut withdrawals are nothing to worry about if you got a weeksupply of diazepam, or even more so its never a worry, taking phenibut without having benzos around is just stupid, whenever you want to stop you take diazepam or clonazepam for a few days and you wont notice any issue.



#21 Galaxyshock

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Posted 26 February 2016 - 11:29 AM

Phenibut withdrawals are nothing to worry about if you got a weeksupply of diazepam, or even more so its never a worry, taking phenibut without having benzos around is just stupid, whenever you want to stop you take diazepam or clonazepam for a few days and you wont notice any issue.

 

What dosage of diazepam? My normal dosage 10mg didn't cover rebound anxiety from Phenibut, was pretty bad it suddenly hit me and it was only from 2 days usage if I remember correctly. Maybe because I'm tolerant to the benzo. I've been using Phenibut now for a week 2-4 g a day, gonna pick up 100x5mg diazepam should probably up the dosage for a few days then.



#22 jaiho

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Posted 26 February 2016 - 11:38 AM

John, its rare to get someone as knowledgeable with the academic background to support it here.

What do you think is the best treatment for Anhedonia?

For me, Phenibut is largely effective for the pleasure part, but not so much the emotional numbness. i have heeded the warnings of the Internet to abstain from daily dosing.



#23 medievil

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Posted 26 February 2016 - 01:26 PM

 

Phenibut withdrawals are nothing to worry about if you got a weeksupply of diazepam, or even more so its never a worry, taking phenibut without having benzos around is just stupid, whenever you want to stop you take diazepam or clonazepam for a few days and you wont notice any issue.

 

What dosage of diazepam? My normal dosage 10mg didn't cover rebound anxiety from Phenibut, was pretty bad it suddenly hit me and it was only from 2 days usage if I remember correctly. Maybe because I'm tolerant to the benzo. I've been using Phenibut now for a week 2-4 g a day, gonna pick up 100x5mg diazepam should probably up the dosage for a few days then.

 

As much diazepam as it takes, if you need high doses then you take high doses, just stop after a week and you are symption free after a painless week with perhaps some cognitive impairment from the benzos but nothing else.

 

Ive been using 4-6 gram of phenibut a day for years, but run out every 2 weeks or so which i notice nothing from as i take clonazepam.

 

Take in mind that only diazepam and clonazepam fully supress the withdrawals.



#24 Galaxyshock

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Posted 26 February 2016 - 03:54 PM

 

 

Phenibut withdrawals are nothing to worry about if you got a weeksupply of diazepam, or even more so its never a worry, taking phenibut without having benzos around is just stupid, whenever you want to stop you take diazepam or clonazepam for a few days and you wont notice any issue.

 

What dosage of diazepam? My normal dosage 10mg didn't cover rebound anxiety from Phenibut, was pretty bad it suddenly hit me and it was only from 2 days usage if I remember correctly. Maybe because I'm tolerant to the benzo. I've been using Phenibut now for a week 2-4 g a day, gonna pick up 100x5mg diazepam should probably up the dosage for a few days then.

 

As much diazepam as it takes, if you need high doses then you take high doses, just stop after a week and you are symption free after a painless week with perhaps some cognitive impairment from the benzos but nothing else.

 

Ive been using 4-6 gram of phenibut a day for years, but run out every 2 weeks or so which i notice nothing from as i take clonazepam.

 

Take in mind that only diazepam and clonazepam fully supress the withdrawals.

 

 

Alright, took 25mg diazepam feeling better now. Wierd how Phenibut worked very well for couple days this week, got the anxiolytic and mild euphoriant qualities, then suddenly the effect disappeared and was left with anxiety despiting taking doses. Perhaps I should try Fasoracetam as it's supposed to bring back the best effects of Phenibut.



#25 medievil

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Posted 26 February 2016 - 03:59 PM

Yes that could keep phenibut working, otherwise look into nmda antagonists or treshold ibogaine doses.


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#26 Sarif

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Posted 26 February 2016 - 04:35 PM

I'm sorry but can anyone please tell me what is rebound anxiety (I'm a total newbie) ? It sounds like something that happen even if you are not in withdrawal. If that's right, is there any way to prevent it? I mean continue taking phenibut regularly at a decent dosage without rebound?



#27 medievil

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Posted 26 February 2016 - 04:37 PM

Some people report rebound anxiety when phenibut wears off, this is simular to for example a amphetamine combine, temporary getting the opposite unpleasant effects due to receptor down or upregulation depending on the compound,

I personally never noticed this



#28 Sarif

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Posted 26 February 2016 - 05:25 PM

Thanks everyone for your insight. After reading everything I've decided that I'll start taking 250 mg of phenibut everyday. After someday I'll increase it to 500 mg. I may increase it to 1 gm but that'll be the maximum limit. If I continue taking like this and never go 'cold turkey' , will that be ok??????

 

Also, I'm from India so it'll be tough for me to get phenibut. The only source that supplies reliably is iherb.com.....but I checked thay have only primaforce brand. Moreover, the price becomes more than twice due to customs. Has anybody had experience buying from http://www.alibaba.com/ ? They are Chinese site, so they'll easily ship to India, but are the manufacturers trustworthy? 



#29 medievil

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Posted 26 February 2016 - 05:41 PM

The dose you take wont have much difference with regards to the tolerance or withdrawals, for example i can just go to 2 gram from 6 gram to avoid withdrawals, that said i beleive the withdrawals are as severe as with a low dose compared to a high dose, so if you take it just take as much as you need,

 

Please make sure you have a cheap diazepam supply nearby to never face the withdrawals which are horrific, that said i also beleive that keeping the dose low hasnt got any benefits in the tolerance department, so if you use it, use it in a way it really helps.

 

Order from a uk site, they pretty much all sell 100 gram for 20 pound or so in powder form, not sure my girlfriend orders it lol.



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#30 Sarif

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Posted 27 February 2016 - 01:37 PM

Thanks for all of your advice. I've ordered a 200 gm phenibut HCL tub from LiftMode.com. Will update you all once it arrives. 







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