Phenibut Pregabalin Cross Tolerance
I made an account just for this question!From what I understand, cross tolerance is simply the accumulation of tolerance to a specific drug through the build up of tolerance to a different but related drug that acts on the same receptors. Cross dependence is the process whereby taking different but related drugs contributes the development of the same physical dependence.
Oct 29, 2016 Do Gabapentinoids increase benzo tolerance? (Pregabalin, Gabapentin, Phenibut) Specifically, lyrica, in this case. And I disagree with your statement on Gaba-a and -b are cross-tolerant - If my benzo tolerance is 300mg of etizolam w/o blacking out (normal dosage at this time was 40-50mg a day) (My tolerance is nowhere near this right now, I. Xanax gabapentin cross tolerance 14 September Individuals taking Xanax xanax gabapentin. Gabapentin Gabapentin enacarbil Phenibut Cross tolerance.
For instance, using a moderate dose of ambien one night to sleep, temazepam the next day and klonopin the day after that would lead to dependence. Even though using each individual drug once every three/four days in the same way, but without using the other drugs, would likely lead to no dependence. Those substances would be cross dependent. So really I have two questions:1) What confuses me is to what extent can substances be considered cross tolerant but not cross dependent? What I mean by that is substances seem to be able to share cross tolerances, yet do not perpetuate the dependence of the other. For instance, during my GBL withdrawal period I used baclofen and phenibut to completely eliminate withdrawal symptoms and emerge from the other side basically experiencing no withdrawal at all.
But if I had used GBL for the 2 weeks that I used its 'cross tolerant' substances (i.e. Baclofen and phenibut) and instead of them, obviously I would have have had to emerge from those two weeks looking forward to a week plus of shakes, no sleep and the whole schabang. So why do these substances get me through withdrawal scot-free when they directly ramp up tolerance to the drug that I'm withdrawing from? Shouldn't they just prolong withdrawal as would happen if I just took GBL instead, given that they act on identical receptors?2) More importantly, what are the implications of this when it comes to developing dependency? I was under the impression that alternating or rotating between two drugs that hit the same receptors would contribute to a 'GABA B' dependence if we were to use the example of rotating GBL, phenibut and baclofen on different days PRIOR to the development of dependency to any one of those drugs. Is this not the case?
If it is not the case, how is that reconciled with the fact that, for example, alternating between different benzos will definitely lead to a singular dependency on benzos? Is it because all benzos act on the same receptor in the same way, whilst GBL, phenibut and baclofen act on the same receptor in different ways?Or am I missing something more obvious here?TLDR: why does phenibut get me out of GBL withdrawal without having to go through more withdrawals even though it acts on the same receptors, and does this have implications when it comes to alternating drugs that act on the same receptor before getting dependent on any one of those particular drugs? But surely I would have experienced something after finishing baclofen? The GBL withdrawals started so I took phenibut for about 4 days and then i switched to baclofen for about 7 days on the advice of some research into the subject. After I came off the baclofen I felt practically nothing.
So basically those drugs eliminated the withdrawals that I should have had from GBL and didn't 'continue' the withdrawals which were due to GABA-B downregulation in the first place. It just strikes me as strange since I was under the impression that the GBL withdrawals are consequential on GABA-B downregulation. And I also thought phenibut and baclofen both cause further GABA-B downregulation by agonising GABA-B just like GBL. Unless I'm totally wrong about either of those things or being overly simplistic? I guess what I'm trying to get at is working out how dependence works between different drugs that act on the same receptor given my experience here.
Would you be able to expand a bit on this please? In terms of how exactly having different affinities for different isoforms results in 'masking' withdrawals without prolonging them, despite acting on the same receptor. Also do you know anything about how this interacts with cross dependence? What I mean by that is would the same mechanism you describe result in a much lower degree of cross dependence between drugs that act on the same receptor, versus taking a single drug in that category?
But surely I would have experienced something after finishing baclofen? The GBL withdrawals started so I took phenibut for about 4 days and then i switched to baclofen for about 7 days on the advice of some research into the subject.
After I came off the baclofen I felt practically nothing. So basically those drugs eliminated the withdrawals that I should have had from GBL and didn't 'continue' the withdrawals which were due to GABA-B downregulation in the first place. It just strikes me as strange since I was under the impression that the GBL withdrawals are consequential on GABA-B downregulation. And I also thought phenibut and baclofen both cause further GABA-B downregulation by agonising GABA-B just like GBL.
Unless I'm totally wrong about either of those things or being overly simplistic? I guess what I'm trying to get at is working out how dependence works between different drugs that act on the same receptor given my experience here. Phenibut isn't a selective GABA-B agonist. In fact, it has a few times stronger affinity for voltage-dependent calcium channcels (VDCC) than it has for GABA-B, effectively making its action more akin to classical selective VDCC blocker gabapentinoids such as gabapentin and pregabalin, with a hint of GABA-B agonism if you like. Baclofen, on the other hand, has negligible VDCC blockage at doses used due to its 100-fold higher GABA-B affinity than phenibut, so that one is more GABA-B in nature. Still, if you used only phenibut for first 7 days, it could have masked the withdrawals through VDCC as well, because VDCC blockers are used for many types of withdrawal with considerable success.7 days of low-level agonism compared to hardcore agonism of GHB is plenty time to upregulate GABA-B so that long half-life baclofen can act as a taper afterwards.Well, that's how I would explain it with my knowledge. Some more knowledgeable people may know better.
Phenibut isn't a selective GABA-B agonist. In fact, it has a few times stronger affinity for voltage-dependent calcium channcels (VDCC) than it has for GABA-B, effectively making its action more akin to classical selective VDCC blocker gabapentinoids such as gabapentin and pregabalin, with a hint of GABA-B agonism if you like. Baclofen, on the other hand, has negligible VDCC blockage at doses used due to its 100-fold higher GABA-B affinity than phenibut, so that one is more GABA-B in nature.
Gabapentin Phenibut Cross Tolerance
Still, if you used only phenibut for first 7 days, it could have masked the withdrawals through VDCC as well, because VDCC blockers are used for many types of withdrawal with considerable success.7 days of low-level agonism compared to hardcore agonism of GHB is plenty time to upregulate GABA-B so that long half-life baclofen can act as a taper afterwards.Well, that's how I would explain it with my knowledge. Some more knowledgeable people may know better. Phenibut isn't a selective GABA-B agonist. In fact, it has a few times stronger affinity for voltage-dependent calcium channcels (VDCC) than it has for GABA-B, effectively making its action more akin to classical selective VDCC blocker gabapentinoids such as gabapentin and pregabalin, with a hint of GABA-B agonism if you like. Baclofen, on the other hand, has negligible VDCC blockage at doses used due to its 100-fold higher GABA-B affinity than phenibut, so that one is more GABA-B in nature.
Still, if you used only phenibut for first 7 days, it could have masked the withdrawals through VDCC as well, because VDCC blockers are used for many types of withdrawal with considerable success.7 days of low-level agonism compared to hardcore agonism of GHB is plenty time to upregulate GABA-B so that long half-life baclofen can act as a taper afterwards.Well, that's how I would explain it with my knowledge. Some more knowledgeable people may know better.
Phenibut and GABA are two supplements that are often compared for their effects and benefits. Both of these chemicals are associated with a reduction of stress, anxiety inhibitions and insomnia. Phenibut and GABA will sometimes be used together by individuals who want to combat anxiety as well as bodybuilders and weight lifters. What you should know is that designed to be a lot more effective than its parent. This is because Phenibut can cross over the blood-brain barrier while GABA cannot unless it has a dedicated carrier. This makes the effects of Phenibut as an oral supplement far more pronounced than any GABA pills or powder you might take. Topics.What’s unique about phenibut as a supplement is that it falls into three classifications:.
A nootropic which improves cognitive functions. An anxiolytic which relieves anxiety. A sleep aid to promote a sounder deeper sleep.There really isn’t a standard dosage for phenibut. Different people require different doses due to several factors which are covered below. GABAPhenibut crystals are the solids synthesized, a neurotransmitter in the brain. You may find brands of phenibut in powder form which is really the result of grinding down the pure crystals so they can easily be dissolved in liquid.When GABA molecules stimulate the GABA receptors the ion channels open on the neurons.
Once the ion channels are opened chloride ions seep into the surface of the cells of the neuron. This has the effect of. Therefore the nerves are not as sensitive to outside or environmental stimuli and don’t react as readily.When neurons are in this state other areas in the brain are not as reactive either. This will result in a lessening of anxiety because you understand that your mind is reacting. Medications that Increase GABA ActivityThere are a number of medications designed to trigger a release of GABA and these include barbiturates, benzodiazepines, and alcohol.
The GABA that is released from consuming these substances affects the GABAa receptors.Drugs that increase GABA activity by stimulating GABAa receptors once the synapse is complete, have long been prescribed as sedatives, tranquilizers, hypnotics and anti-convulsants. As the most popular among doctors and patients. They even replaced barbiturates and in the 1970s became the most frequently prescribed medication in the Western hemisphere.Problems with these types of drugs emerged in the 1980s having to do with dependence and the subsequent reactions to withdrawal. Medical professionals needed to limit their use. As a result the focus of the medical community has recently shifted to a new classification of drugs.
These drugs promote GABA-ergic actions which involve a number of chemical mechanisms that do not directly involve the GABAa receptor.The drugs included in this group are gabapentin, tiagabine, vigabatrin, pregabalin, lamotrigine among others. These drugs were initially developed to treat epilepsy as anticonvulsant medications. However it’s been discovered that they are effective in treating a wider application, that of treating affective disorders, and various pain conditions.
It still has not been determined whether or not there would be problems associated with developing a tolerance, becoming dependent and having symptoms of withdrawal with long-term use. Phenibut is a Better OTC AlternativeThen phenibut enters the market as an over-the-counter alternative to stronger pharmaceutical medications. While phenibut can be as effective as these other medications and the potential for becoming dependent is relatively low when you compare it to pharmaceuticals.When phenibut is taken orally the answer is YES it can be more effective than GABA. Although this seems counterintuitive that something derived from GABA would be more effective than GABA, the real thing.Because phenibut is able to cross the blood-brain barrier it has more ability to affect brain chemistry when compared to orally-ingested GABA. Being capable of penetrating the blood-brain area is significant because as the brain’s biological shield from bacteria and toxins in the bloodstream, it’s almost impenetrable.Note: There are some structural similarities between phenibut and Baclofen and, both derived from GABA.
We discuss these here.Phenibut has positive secondary effects as a treatment to relieve stress for those suffering from PTSD and as a sleep-aid. Because of the similarity in molecular structure between phenibut and GABA, phenibut triggers many of the same physiological responses as GABA. There have been many reports of other benefits than just an anxiolytic. Phenibut is extremely good at inducing sleep even in people with extreme insomnia.Those who use phenibut feel a sense of well-being and happiness; they’re able to combat insomnia, stress and anxiety and are better able to cope with PTSD. Below is a deeper exploration of Phenibut’s benefits due to GABA stimulation.1.
To induce a deep sound sleep – Phenibut is often used as a sleep-aid and many who use this report that it is very potent. There are abundant reports that “nothing else comes close” when it comes to. There is evidence that a trend has emerged among drug users that, due to phenibut enabling them to sleep they are more comfortably able to withdraw from drugs.The primary paradigm seems to be that not only does phenibut enhance the quality of sleep it also brings about a distinct feeling of calm. As is true with other cognitive enhancers, phenibut provides benefits for strength trainers and bodybuilders because when someone is in a deep REM state of sleep growth hormones are secreted. This expedites muscle recovery when someone has been exercising intensely.2.
– Research done on mice who’ve been given higher and higher doses of phenibut showed significantly faster reaction times each time the concentration of phenibut increased. This was even more apparent when the mice were put in social situations with groups of other mice. This makes Phenibut more superior to other GABAergic drugs like Benzodiazepines.Trials are continuing and the results are promising. Similar effects are being shown on the brains of primates. The subculture community of Brain Hackers has mixed reviews, but for the most part they are positive.3. – Because phenibut also stimulates the neurotransmitter dopamine at low levels in addition to GABA, users often notice an increased sense of confidence, which is separate from a lowering in anxiety levels.
Dopamine is the brain chemical that regulates the pleasure/pain cycle as well as motivation. This means Phenibut’s effects cover a wider range than GABA on its own.
If you are deciding between Phenibut vs. GABA supplements, there is a clear winner.