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What is Phenibut HCL (hydrochloride) and is it safe to take?
Phenibut Hydrochloride (Phenigamma) is a nootropic agent with anxiolytic and mood-enhancing effects. It is prescribed in Russia for its psychologically calming effects that appear to enhance rather than inhibit cognitive function.
It is commonly taken as an off-label smart drug to enhance sleep quality, promote emotional balance, support focus and by bodybuilders to support workout recovery.
While it is reasonably well tolerated at low doses, it can cause serious adverse reactions if taken in high dosages. It is also dangerous to combine with other GABAergic substances like alcohol and benzodiazepine drugs.
Phenibut HCl refers to the hydrochloride salt form of this product. It is the most widely available version of this nootropic drug. However, some users are switching to Phenibut Free Amino Acid (FAA) because it is better-suited for sublingual administration.
This article reviews the uses, effects, possible benefits, recommended dosages, and safety profile of this popular nootropic agent.
Anxiety
Mood
Sleep & Insomnia- Powerful anxiolytic for stress reduction
- Stimulates GABA receptors & supports sleep
- Neuroprotective & supports cognitive function
What Is Phenibut Hydrochloride?
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- User Review
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- Dosage Recommendations
- Effects & Mechanisms of Action
- Experience Reports
- Anti-Anxiety Effects
- Using Phenibut for Sleep
- How to Take
- Negative Side Effects
- Withdrawal Dangers
- Risks with Alcohol Combination
- Comparison to Picamilon
- Buying Phenibut Guide
- Using Bulk Powder
- Primaforce Phenibut Review
- SNS Phenibut XT Review
Phenibut HCL is a neuropsychotropic drug that has anxiolytic (reduces anxiety), sedative and CNS (central nervous system) depressant effects.
It was first synthesized in 1963 in St. Petersburg by a Soviet Union scientist named Perekalin. It was discovered as a derivative of the original nootropic agent Piracetam.
3-phenyl-4-aminobutyric acid was found to exhibit a tranquilizing effect but did not interfere with cognitive faculties. In 1975, the Sovient Union began distributing this novel compound to cosmonauts in its space program.
Phenibut was said to help alleviate the stress of long space missions while supporting mental acuity and making it easier to focus on demanding work.
Its use spread widely in Russia and other parts of Europe as a medicinal drug for the treatment of anxiety, panic attacks, stuttering in children, vestibular (balance) disorders, Parkinson’s disease, neuroses, epilepsy, hyperactivity, insomnia and post-traumatic stress disorder.
It is available over-the-counter (without a prescription) as a prophylaxis for stress. People report taking it before stressful events such as speaking in public, travelling on an airplane or before medical procedure.
However, phenibut hydrochloride is not approved by the US FDA as a drug for the treatment of any medical conditions. In the USA and Canada, it is not a controlled substance which means it can be purchased as a bulk powder without a prescription.
Most vendors online sell bulk Phenibut HCL powder, but there are some suppliers who sell this nootropic in capsule form. [1] In Russia, it is sold as a pharmaceutical drug under various trade names including Noofen, Fenibut, and Anvifen. [2]
Phenibut HCL vs Phenibut FAA
The Natural Medicines Comprehensive Database (NMCD) states that there are currently 58 phenibut supplements registered on the US market. [4]
Most products that contain this nootropic ingredient will provide it in the HCL form, even if not specified on the label. Up until recently, this was the only form of phenibut available to buy through major retailers.
However, there is now a Free Amino Acid form that is growing in popularity due to its perceived higher potency level. What is the difference in effects and pharmacokinetics between these two formulations?
According to Wikipedia, “In chemistry, a hydrochloride is an acid salt resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base.” [2]
As the name suggests, the phenibut molecule (C10H13NO2) serves as the organic base for Phenibut Hydrochloride. It is a C10H13NO2 molecule bound to a hydrochloric acid (HCl) molecule.
You will sometimes see this written out full as beta-phenyl-gamma-aminobutyric acid HCl.
Hydrochloride acid is found in many supplement and pharmaceutical drug preparations. It is also present in stomach acid.
Gastric “juice” is needed to break down foods that we eat. Gastric “acid” is the HCL constituent of gastric juice. Gastric (hydrochloric) acid is the major constituent of gastric juice.
The FAA in Phenibut FAA denotes “free amino acid”. This refers to pure Phenibut that is free or unbound to any other molecules.
For instance, Liftmode Phenibut FAA, a popular brand of nootropic supplements, is reported to be 99.5% pure powder.
- Powerful anxiolytic for stress reduction
- Improves sleep and may reduce insomnia
- Neuroprotective and cardioprotective effects
Is FAA Better Than HCL?
The Free Amino Acid form tends to cost more than the Hydrochloride Acid form, but does it produce better results and is it worth the price difference?
The answer is yes and no: it depends on the method of administration used.
In the HCl salt form, phenibut is a stable crystalline powder that dissolves easily in water. This makes it shelf-stable and easy to handle and use as a bulk compound.
The purest phenibut HCL is about 87% phenibut and 13% hydrochloride. This means that a 1-gram dosage contains 870 mg of phenibut and 130 mg of hydrochloride.
Comparatively, 1 gram of the Free Amino Acid powder will yield approximately 995 mg of pure phenibut. Thus, a slightly lower dosage may be needed to achieve desired effects.
According to Liftmode, “When consumed in the usual way, Phenibut F.A.A. is about 15% more efficient than Phenibut HCl, but otherwise has few advantages.” [3]
However, Phenibut FAA becomes Phenibut HCL when it reacts with hydrochloric acid in the stomach. If taken orally there is minimal benefit to using the more expensive form.
The main advantages to the Free Amino Acid form is that it is better suited for sublingual (under the tongue) administration. With sublingual use, the compound is absorbed directly through the mucus membrane under the tongue into the bloodstream.
The FAA form is also said to be approximately 300% more bioavailable than the Hydrochloride form when taken under the tongue. This is because it is better absorbed via sublingual administration and avoids passage through the gastrointestinal tract.
Although Phenibut FAA is more expensive than the HCL form, many users feel the price difference is offset because so much less FAA is required sublingualy to induce the same effects.
Pure Phenibut FAA powder is very fine compared to crystalline Phenibut HCL powder or granules. The hydrochloric acid form can burn if placed under the tongue and has a bitter taste that many users find unpleasant.
Phenibut FAA has a milder and less-metallic taste that some users find easier to tolerate.
All things considered, there are no significant pharmacological differences between Phenibut HCL and Phenibut FAA. The primary different is personal preference regarding method of administration.
Phenibut vs. GABA
Phenibut was developed by Russian scientists as a synthetic GABAergic compound to use in calming down agitated children. [3]
Its scientific name, beta-phenyl-gamma-aminobutyric acid, denotes the fact that it is a phenylated derivative of the GABA molecule. Its chemical structure is GABA with a 6-carbon phenyl ring attached to it.
GABA (gamma-aminobutyric acid) is an inhibitory neurotransmitter that prevents over-activation of brain circuits and helps to calm anxiousness and hyperactivity.
Many drugs used to treat anxiety, insomnia and other mood disorders work by targeting GABA receptors in the brain. While GABA dietary supplements do exist, they are not believed to be very effective because of poor transportation across the blood-brain barrier.
Introduction to GABA
GABA(C4H9NO2) is an endogenous chemical, meaning it can be made inside the human body. It also serves as a non-essential nonproteinogenic amino acid.
GABA is produced when an enzyme called GAD (glutamic acid decarboxylase) and an active form of pyridoxine (vitamin B6) reacts with glutamate.
Glutamate is an anion (negatively-charged ion) of an alpha-amino acid. In vertebrates including humans, glutamate is by far the most abundant neurotransmitter.
Neurotransmitters are chemicals in the CNS that facilitate nerve-to-nerve communications. Neurotransmitters can be either excitatory or inhibitory. Glutamate is the primary excitatory neurotransmitter and GABA is the primary inhibitory type.
GABA is responsible for slowing down neuronal firing so that neurons do not become over-stimulated and burn out from excitotoxicity. It is responsible for balancing the excitatory effects of glutamate and is found in nearly all areas of the brain.
People who are over-anxious or psychologically stressed sometimes benefits from taking drugs that increase activation of GABA receptors in the brain. These drugs like benzodiazepines have anxiolytic effects and sedative effects.
Blood-Brain Barrier
GABA itself is not believed to be very effective for anxiety because it cannot cross the blood-brain barrier (BBB). This is the filtration mechanism that separates circulating blood from brain cells.
The phenylation of GABA makes it better able to cross the blood-brain barrier into the brain where it can bind to GABAergic receptors. Research shows that Phenibut does have good transportation across the BBB and that it can stimulates the same receptors as GABA does.
There are two primary subsets of neuroreceptors that respond to this neurotransmitter: GABA-A and GABA-B receptors. Phenibut HCL seems to act on GABA-B receptors much more so than it does the GABA-A type.
How Does Phenibut Work?
Researchers have not yet fully identified the mechanism of action involved in mediating the effects of beta-phenyl-gamma-aminobutyric acid hydrochloride in humans.
According to one source, over 300 research papers have been published on this substance. However, most of the previous research completed on this molecule was conducted in the Soviet Union during the Cold war era.
Much of this research is only available in Russian. There have not been many recent clinical studies conducted on phenibut use and it is not widely used anywhere else in the world outside of former Soviet Union contries.
Phenibut is believed to work primarily by activating GABA-B receptors, and to a lesser degree, GABA-A receptors. It appears to have a similar mechanism of action compared to baclofen (beta-(4-chlorophenyl)-gamma-aminobutyric acid, beta-(4-chlorophenyl)-GABA).
Baclofen is a CNS depressant and skeletal muscle relaxant that is used to treat spasticity and muscle pain.
Research also suggests that phenibut HCL works similarly to pregabalin, gabapentin, and other gabapentinoid compounds.
The NMCD reports that, in animal studies, phenibut has been shown to: [4]
- Decreased alcohol-induced behavioral disorders;
- Decrease the desire to consume alcohol;
- Decreased respiratory rate;
- Increased heart rate;
- Decreased anxiety;
- Caused sedation;
In animals, phenibut also seems to decrease respiratory arrest induced by the serotonin neurotransmitter.
Phenibut HCL is has also been studied for its potential to prevent cardiovascular toxicity. It is thought to help maintain cerebral blood flow after a traumatic brain injury.
There has been limited human research into the effects of this nootropic. More research is needed to determine its therapeutic efficacy and safety in humans.
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What Is Phenibut Hydrochloride Used For?
In the USA, Canada, and Europe, Phenibut HCL is used primarily as anxiolytic agent. This means it helps to reduce anxiety and alleviates mental stress.
It is also purported to increase prosocial behavior and promote a positive mental state. In anecdotal user reviews, it is reported to reduce fear of engaging in social situations like giving a speech or approaching someone of the opposite sex for a date.
Some people use it as an alternative to alcohol. It has been studied in animal trials for treating alcoholism and reducing the desire to drink.
Phenibut is described as having mild nootropic effects. Unlike other nootropic substances, it does not significantly influence memory or cognitive ability. Instead, it appears to help quiet the mind and make it easier to focus in people susceptible to anxious thoughts.
In Russia, Latvia, Ukraine and parts of eastern Europe, phenibut HCL is used medicinally to prevent or treat: [1]
- Insomnia and some other sleep disorders in neurotic or psychosomatic patients;
- Asthenia (abnormal physical weakness);
- Chronic anxiety, stress, fear, or tension;
- Pre or post-operative anxiety and fear;
- PTSD (post-traumatic stress disorder);
- Vestibular (balance) disorders;
- Ménière’s disease;
- Stuttering and tics;
- Motion sickness;
- Depression;
However, it has not been approved by the FDA as a drug for the prevention or treatment of any medical condition. Discuss use of phenibut HCL with your doctor before beginning to take this product.
Phenibut Hydrochloride Dosage
It is important to take the right dosage of this nootropic compound for your needs. Excessive dosages can cause serious health consequences, especially when combined with alcohol or other psychoactive substances.
As a prescription drug, phenibut is available in 250 milligrams (mg) oral tablets. It can also be used in the form of a 10 mg/mL liquid solution for intravenous infusions. IV administration should be conducted in a hospital setting only.
Phenibut HCL is available in both bulk powder form and oral capsules. Manufacturers typically recommend serving sizes of between 250-1000 mg per day. [5]
LiftMode recommends taking it in a dosage of “500 – 2000mg per day, in up to two to three separate servings, depending on the desired effect.”
Phenibut has a long half-life and most users find they need no more than a single dose in a 24-hour period.
In moderate doses, this nootropic is said to induce calmness and tranquility in most users. A higher dosage will likely cause sedation.
It is always best to begin using any nootropic agent like phenibut at the lower end of its common dosage recommendations. Start with the lowest effective dosage to gauge tolerance and slowly increase the dose as needed to experience desired effects.
Do not exceed 2000 mg per day and do not take this nootropic in high amount on consecutive days due to the risk of a tolerance developing. Liftmode recommends not taking more than 4 grams per week and other sources suggest regularly cycling on and off to prevent tolerance.
According to LiftMode, “Phenibut requires careful, disciplined and responsible cycling and limited consumption in order to maximize benefits and minimize potential drawbacks.”
Safety Warnings
Phenibut HCL is commonly reported to have a strong potential for tolerance development, addiction, hangover symptoms, withdrawal symptoms, and overdose.
Severe side effects are possible when this nootropic is misused or used in excess.
Dr. Ray Sahelian reports that some possible phenibut side effects include: [1]
- Grogginess and eventual sedation;
- Decreased libido (sex drive);
- Low motivation levels;
- Constipation;
Other possible negative effects can include nausea, irritability, headache, skin rash, allergic reactions, loss of balance, and increased anxiety.
More severe side effects are possible if phenibut HCL is used recreationally in excess. Some possible symptoms of overdose include hallucinations, acute psychosis, and severe rebound anxiety.
When used appropriately and short-term, phenibut seems to be well-tolerated in most users. Low dosages have been used by thousands of individuals in Russia where it is available as a non-prescription drug.
Tolerance can occur when your GABA receptors downregulate to become less sensitive to the effects of GABAergic compounds. Signs of tolerance can include anxiety, insomnia, depression, headaches and irritable moods.
To avoid tolerance and withdrawal symptoms, use phenibut supplements sparingly and regularly cycle on and off. Never increase your dosage if you feel that you are becoming less sensitive to lower dosages.
People who use phenibut regularly should have their liver enzymes checked periodically. Routine use can increase the risks of developing FLD (fatty liver disease) and a disorder marked by high white blood cell counts called eosinophilia.
Overdoses have been reported with doses over 7 grams. Some users take large doses as a party drug to get the “Phenibut High”. This can cause severe vomiting, heavy sedation, hypotension (low blood pressure), fatty liver degeneration, seizures, and unconsciousness.
Taking phenibut HCL along with other CNS depressants can cause potentiation and increased duration of effects. Tolerance to other GABAergic drugs can also influence tolerance to this nootropic.
Be very careful using phenibut hydrochloride with sedatives, anxiolytics, anticonvulsants, barbiturates, benzodiazepines, opioids, tetracyclic antidepressants, antipsychotics, and alcohol.
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- Sahelian, R. Phenibut supplement side effects, tolerance and withdrawal symptoms, dose and dosage, caution, danger, adverse reactions, addiction, capsules, powder. Nov 20, 2017. Accessed April 6, 2018
- Wikipedia contributors. "Phenibut." Wikipedia, The Free Encyclopedia. Wikipedia, The Free Encyclopedia, 13 Mar. 2018. Web. 6 Apr. 2018
- LIFTMODE Staff. SO WHAT IS PHENIBUT? - 5 SIMPLE FACTS FOR NEWBIES. Accessed April 6, 2018
- Natural Medicines Comprehensive Database. Phenibut Professional Monograph. Accessed April 6, 2018
- Nootriment Staff. Phenibut Nootropic Effects, Side Effects and Dosage Guide. Accessed April 6, 2018
Article last updated on: July 4th, 2018 by Nootriment