A Complete Guide to Phenibut

Complete Guide to Phenibut

Phenibut is becoming an increasingly popular nootropic of choice for business professionals, college students, and laypeople alike. What’s particularly intriguing about phenibut is that it somewhat mimics the effects of having an alcohol buzz without the negative ramifications (like impaired cognition). As such, phenibut presents a great alternative to alcohol for people who want to go out and socialize without getting inebriated (and dealing with a hangover the next day). It also has strong anxiety-reducing properties, making it a worthwhile consideration for those with stressful lifestyles and/or high anxiety.

Read on as this article dives deep into how phenibut may benefit you, how it works, the research behind it, and how to properly use it.

What is phenibut and how does it work?

Chemically speaking, phenibut is a derivative of the chief inhibitory neurotransmitter gamma-aminobutyric acid (GABA). GABA is known to play an important role in producing feelings of calmness and relaxation since it readily inhibits the actions of glutamate (an excitatory neurotransmitter).

Naturally, GABA supplements have increased in popularity as people figure it will help reduce anxiety and improve mood. However, taking pure GABA (orally) is an inefficient means of increasing GABA levels in the brain since it doesn’t readily cross through the blood-brain barrier (BBB).

This is precisely why phenibut has gained ground as a more potent GABA-targeting nootropic, since its slightly modified chemical structure allows it to cross the BBB.

Once phenibut crosses into the brain, it actively binds to a subclass of GABA receptor called GABA-B. After binding to these receptors, G-proteins provide a liaison to open and close potassium-chloride ion channels in the plasma membrane of neurons. In turn, a membrane potential is created, which can inhibit the actions of glutamate.

Research behind Phenibut (and Other GABA-B Agonists)

While there are some useful studies looking directly at supplementation with phenibut, much of the research on GABA-B receptor agonism (activation) comes from the pharmaceutical compound baclofen (a chlorinated analogue of phenibut). It is safe to extrapolate such findings to the use of phenibut, since they act identically physiologically.

To give an example of just how effectively GABA-B agonists can make you feel calmer, a study in 2007 by Lhullier et. al treated hyperactive rodents (induced by cocaine administration) with baclofen and looked for changes in locomotion (movement) thereafter. [1] Yes, this study actually examined the activity of coked out rodents, pretty amazing what scientists come up with these days.

The findings of the study note that baclofen administration exhibits a significant dose-dependent decrease in locomotor activity in these rodents (despite being high on cocaine). In other words, a nootropic like phenibut can strongly calm you down from the high you get from stimulants. Let’s just hope you’re not using cocaine like these rodents were.

Furthermore, for people who have sleep issues (like insomnia), phenibut might be just the remedy. A study completed in 2009 by Cui et. al noted significant reductions in both time spent awake and the time it took to fall asleep in physically-stressed rats who were given baclofen. [2] As such, using phenibut prior to bed would be prudent to help you fall asleep and stay asleep.

Article: The 4 Best Adaptogens to Reduce Stress & Improve Mood 

A final noteworthy study completed in 2010 by Thomas et. al monitored the effects of baclofen on human thenar motor unit behavior (thenar refers to a group of muscles in the palm of your hand). [3] The results demonstrate that baclofen significantly increases the amount of motor units necessary to produce one Newton of force; in non-nerd lingo, these findings suggest that phenibut can decrease your muscle tone (i.e. make your muscles less tense), which is conducive to relaxation.

Phenibut Benefits

Phenibut is most commonly used for increasing relaxation and as a sleep aid, due mainly to its strong calming effects.Given the importance of proper rest and recovery on health/well-being, many people stand to benefit from phenibut.

In short, the most pertinent benefits derived from phenibut use:

  • Increases relaxation
  • Helps reduce anxiety and tension
  • Can replace alcohol in social situations
  • Improves sleep quality and duration
  • Enhances mood
  • Prevents neurodegeneration

Phenibut Dosing

Phenibut must not be used every day, but rather intermittently/on special occasions (i.e.going out for happy hour, the night before an exam, etc.). This is to reduce your dependency on it and the dreaded “phenibut hangover” side effect.

It’s also important to note that baclofen is much more potent than phenibut, so the two are not interchangeable dose-wise. Anecdotal evidence suggests that a proper starting dose of phenibut is 10 mg per kilogram of body mass.

If you’re anti-metric system, like the American government, here’s a sample calculation:

  • 180 lb male/2.2 lb per kg = ~82 kg of body mass –> 82 kg x 10 mg/kg = 820 mg phenibut

This dose can be increased to 20-30 mg/kg of body mass if you don’t feel the effects at lower doses, but it is suggested that side effects and withdrawal symptoms are more severe as dose increases (which we will discuss below).

As far as timing of phenibut ingestion goes, it is wise to consume it a few hours before intended periods of inactivity or down-time. Phenibut has a half-life between 5-6 hours, but it is slowly metabolized and may take 3-4 hours to exhibit its peak effects. Also, taking phenibut with food will slow the absorption rate, so that must be taken into consideration if you ingest it with a meal.

Avoiding Phenibut Withdrawal and Side Effects

As aforementioned, there have been case reports of individuals that ingest rather large daily doses of phenibut going through withdrawal upon cessation of its use.[4] However, these individuals were using upwards of 10 g per day of phenibut, and not cycling their use.

Some side effects commonly associated with increased GABA levels are:

  • Nausea
  • Euphoria
  • Gastrointestinal distress
  • Reduced cognitive awareness
  • Lack of energy
  • Tiredness (*might be a benefit for some)

It is unlikely that a nominal dose of phenibut taken up to four times per week will incur withdrawal symptoms, let alone any other side effects. However, do not use phenibut more than two consecutive days at a time, and do not exceed a dose of 50 mg/kg of body mass per day.

With that in mind, give phenibut a shot next time you want to go out and be social but don’t want to drink. Chances are you’ll be pleasantly surprised at how much it emulates the buzz of alcohol. Even if you are just looking for a relaxing night at home watching Netflix, phenibut is a great nootropic to free your mind from worry. Just remember not to take it every day, as it can work against you when misused.

References:

[1]Lhuillier, L., Mombereau, C., Cryan, J. F., & Kaupmann, K. (2006). GABAB receptor-positive modulation decreases selective molecular and behavioral effects of cocaine. Neuropsychopharmacology, 32(2), 388-398.

[2]Cui, R., Li, B., Suemaru, K., & Araki, H. (2009). The effect of baclofen on alterations in the sleep patterns induced by different stressors in rats. Journal of pharmacological sciences, (0), 0904060228.

[3]Thomas, C. K., Häger-Ross, C. K., & Klein, C. S. (2010). Effects of baclofen on motor units paralysed by chronic cervical spinal cord injury. Brain, 133(1), 117-125.

[4]Högberg, L., Szabó, I., & Ruusa, J. (2013). Psychotic symptoms during phenibut (beta-phenyl-gamma-aminobutyric acid) withdrawal. Journal of Substance Use, (00), 1-4.

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