Phenibut

Every now and then, a drug is becoming a “Hot topic”. In the first month of this year Andreas Cahling posts about the new YouTube clip from Jerry Brainum: "Why are bodybuilders suddenly talking about using this illegal Russian drug known as Phenibut?

You might find this drug name pop up in bodybuilding forums. So what's the deal? Does this have any benefits towards lifting? Or is it something else entirely?

Phenibut was first synthesized as an experimental medicine to aid the Russian cosmonauts and help them cope with stress levels without affecting their performance in space.

Astronauts who experienced stress as a result of living in space for extended periods of time were prescribed Phenibut. Studies in Russia have also shown that it may be effective for treating insomnia, post-traumatic stress disorder and stuttering.

It continues to be used widely in Russia to treat stress. However, its use grew beyond just reducing stress and anxiety, and today it is also used as a sleep aid and immune-boosting supplement.

As Phenibut is available for purchase legally in many countries without any prescription, its popularity is on an increase; this has started attracting the attention of Western medicine practitioners. In 2001, over 300 scientific publications have studied Phenibut’s nootropic and pharmacological properties.

Phenibut is a derivative of GABA (gamma-aminobutyric acid). GABA is the primary neurotransmitter in your body that regulates the neuronal excitability of the central nervous system. Basically, GABA makes sure that your brain does not become hyperactive.

Why not just supplement with GABA directly then? Phenibut crosses the blood-brain barrier more effectively than GABA itself in supplement form. GABA is naturally produced in the brain itself, therefore it normally does not need to cross the blood-brain barrier (BBB) to be effective. Taking GABA in supplementform does not alleviate anxiety because it is unable to cross the BBB. That's why phenibut works so well, because phenibut is simply GABA with a phenyl ring attached. The phenyl ring is what allows it to cross the BBB and exert its effects on the receptors.

In humans, Phenibut supplementation has a few effects. First it is a nootropic (smart drug), it primarily increases motivation, attention and concentration with a weaker effect on memory and little effect on overall intelligence.

It is a strong anxiolytic (anxiety killer). Phenibut is used to treat panic attacks, stuttering, Parkinson’s disease, neuroses, vestibular (balance) disorders, spasticity, epilepsy, hyperactivity, insomnia and post-traumatic stress disorder. Pick-up artists use Phenibut to shake the nerves of cold-approaching beautiful women. Both are the result of Phenibut’s effect on the activity of your nervous system.

In addition, Phenibut has mood enhancing effects. It has thymoleptic (anti-depressant) properties  and can reduce irritability and fatigue. It is clinically used to treat asthenic-depressive syndrome.

These psychoactive effects are similar in mechanism to alcohol but without the depressant effects. In the upper/downer classification of drugs, alcohol is a downer, but Phenibut is neither. Phenibut gives you focus and calmth without the jitters of caffeine or the cloudiness of alcohol.

Phenibut’s effects can easily last the rest of the day, even though Phenibut’s plasma half-life is only 5.3 hours. This is because Phenibut’s action on the GABA receptors can linger long after your kidneys have excreted all the Phenibut.

Phenibut has a few more effects that are particularly relevant for bodybuilders.

• Phenibut can increase resting and post-exercise growth hormone secretion. In a study of weight training men, GABA supplementation increased resting growth hormone concentrations by 375%. Post-exercise growth hormone concentration rose by 175%. Baclofen, which works almost exactly the same as Phenibut, also increases growth hormone synthesis.

• Phenibut is anti-hypoxic. When you train a muscle intensely, it can’t get enough oxygen anymore and become hypoxic. This metabolic stress mediates muscle hypertrophy. Phenibut may thus increase your tolerance to metabolic stress and allow you to train harder.

• Phenibut is neuroprotective and augments cell energy potential, again possibly allowing you to train harder.

One study also found that Phenibut increased muscle strength, but this finding is likely limited to neurotic and psychotic individuals, because the above study in resistance trained males did not find an increase in weight lifted. You shouldn’t think of Phenibut as a typical ergogenic or performance enhancer anyway.

The optimal Phenibut dosage

The vast majority of studies have only researched dosages up to 3 grams a day. At these dosages, no psychological side effects are found. However, many people take much higher dosages for longer periods of time. This is the same more is better fallacy that leads people to drastically overestimate how much protein they need per day and become addicted to caffeine. Like caffeine, Phenibut feels great and seems harmless, so people consume high amounts of it on a regular basis. The result is addiction: tolerance to the good effects and withdrawal when ceasing supplementation. And they pay the price. Phenibut withdrawal is hell. When coming off 20 grams a day, you can literally become psychotic for a while. Tapering off the dose will minimize withdrawal symptoms, but my recommendation is to avoid becoming addicted in the first place.

Avoid Developing A Tolerance

Using 3 grams of Phenibut a day consistently results in a strong tolerance to Phenibut’s effects and withdrawal when no longer taking the drug. Addiction takes less than 10 days to develop . A 5’10” (1.78 m) adult weighing 176 lb (80 kg) will develop a tolerance to using 1.2 grams of Phenibut a day. It is unfortunately not known how low the Phenibut dose has to be not to result in addiction, so it’s best to err on the side of safety.

Phenibut is better taken after than before your workouts. Based on the above stats, just 0.4 gram of Phenibut decreases motor cortex activity, muscle tone, coordination and body temperature. I already explained how these factors contribute to the best time to work out, but the short version is simply that too much pre-workout phenibut is bad for your performance.

Phenibut can be a wonderful drug, but it is not to be trifled with. In short, don’t be an idiot. This may seem like common sense, but “if sense were common, everyone would have it”. In fact, it bears repeating. Don’t be an idiot. Use the above formulas to calculate the best Phenibut dosage for your goal. Limit your pre-workout dosage to a maximum of ~0.5 gram, your daily dosage to ~1 gram and never consume more than ~3 grams unless you know exactly what you’re doing.

Perhaps most importantly, Phenibut’s effects are highly mediated by stress and anxiety. So your personality type and the situation strongly determine how much benefit you will experience from Phenibut. If you are not in a stressful or social situation and you have a naturally calm personality, you may not feel anything from Phenibut unless you take several grams. So experimentation and timing is everything to find the dosage that works for you. It’s a drug, not some supplement you take daily just to take it.

Buying Phenibut

Phenibut is a legal dietary supplement in practically every country and is generally available over the counter. This is another reason why people underestimate it. There is almost no relation whatsoever between the legal status and the safety of drugs. Seriously, don’t be naive, learn to think for yourself and stop blindly internalizing what your government tells you. Phenibut is one of those drugs that fortunately seems to have slipped through the (many) cracks of legislation, but this won’t be for long if more idiots start mega-dosing the stuff and the media gets a hold of someone hallucinating in a McDonald’s pointing at fat people and hysterically shouting at the manager “It’s alive!”

Selfmedication

As I posted earlier, the pharmaceutical industry in Europe and the USA, earns-steals an incredible amount of money on overpriced patented drugs. With this money they corrupt the medical community and politicians. Through their lobbying, the pharmaceutical industry succeeds to block effective medicine. The doctors are forced to fight the symptoms rather than the actual disease or its cause. Very often it is possible, to prevent or cure a disease with a change of lifestyle and/or with preventive supplementation, but Big Pharma rather sells their drugs.

In Russia, there still are very good medicines freely available and very cheap. A very good drug like meldonium, which was, under pressure from the US, placed on the banned list by "doping fighters" from WADA etc (which are basically an extension of the pharmaceutical industry). Many anabolic steroids such as nandrolone, sustanon and dianabol were freely available in some countries, until those countries were allocated Olympic, winter or summer games, and after a visit from the DEA these drugs were then forbidden for free (OTC) sale. In Russia, however, you can still acquire a lot of good drugs, very cheap. They are of pharmaceutical grade and often cheap and payable with bitcoins.

Phenibut as an Immune Boosting Supplement.

Traditionally, Phenibut has been used strictly for anxiety and stress disorders — its use as an immune system booster is a relatively new development. Moreover, recent reports show that Phenibut has a mild stimulant effect (like drinking a strong cup of coffee or tea) by boosting the levels of dopamine in the brain.

When we experience excessive stress—whether from internal worry or external stimuli—a bodily reaction is triggered, called the “fight or flight” response. This response actually corresponds to an area of our brain called the hypothalamus, which—when stimulated—initiates a sequence of nerve cell firing and chemical release that prepares our body for running or fighting.

Tests also showed that those under stress had become less sensitive to cortisol  which is a stress hormone which reduces immune function. This causes the body’s inflammatory response to grow. Increased stress levels enhance the production of cortisol, a hormone that is associated with weakening the immune system. Various studies show that chronic stress affects the immune system and its ability to combat infections, making one more vulnerable to common infections such as cold, cough and flu.

Other elements of our modern lifestyle are also causing stress levels to rise. Smoking tobacco or drinking too much coffee because caffeine at any dose can also trigger cortisol release into your bloodstream. Cortisol is the stress chemical, and too much of it leads to anxiety, mental fog, and depression.

Drinking alcohol is another bad way to deal with stress. Like nicotine, alcohol is another depressant. It eases the anxiety that normally accompanies stress. Alcohol can become an addiction and it has negative impacts on both your psychological and physical health.

In addition, modern unhealthy diets have are high in fat and salt, exacerbating this problem.

Below you can find a summary of the findings of these studies and what they mean for reducing stress in humans.

GABA alleviates emotional disorders

In one Russian scientific study conducted in 2010, rats and mice were administered GABA derivative compounds such as Phenibut and Baclofen to study their behavior and immune responses. The results were startling. The rats and mice had the functionality of their immune system enhanced drastically, and in some instances, disturbances in their behavioral responses were corrected to a significant extent.

What was even more startling was that the compounds also enhanced the intelligence of the rats and mice and increased their concentration levels. The animals were able to pass the “Suck” test (an activity to determine the directional investigative abilities or rodents) with flying colors.

The takeaway from this study was that we (humans) could potentially replicate the same effects at home by taking Phenibut at similar doses. Further, this shows is that Phenibut restores the immune system, even after it is been seriously compromised (great news for overeaters, big spenders, and over-indulgers of every kind). It also demonstrates that anxious behavior patterns can go away with Phenibut use.

Phenibut has immunocorrective properties

Another comparative study detailing the effects of Phenibut and its derivative compounds was published in Russia in 2009. The study was performed to find the immune-correcting effects of Phenibut and other derivative neurotransmitters, and their role in normalizing the cellular and humoral immunity in the body.

The study was performed on animals treated with cyclophosphamide, a drug used to induce autoimmune response from the body. Administering Phenibut was shown to have profound immune-correcting effects by normalizing the immune system functions to their original state.

What was surprising is that even other organic salts derived from Phenibut showed similar results. Hence, it can be concluded that improving immunity is an inherent property of such class of chemicals.

Thus, Phenibut was shown to have an enhancing effect on the immune system functions even in animals suffering from immunity disorders. If you are suffering from a weakened immune system, then trying Phenibut is not a bad idea, but only if taken in recommended dosages. Moreover, other research has shown that there are almost no negative effects of Phenibut, making it one of the safest immunity boosting drugs .

Immunomodulation with phenibut

An additional comparative study performed in Russia in 2010 was conducted on mice to study the immune-modulating effects of Phenibut and its derivatives. The mice were induced with immunodepression by administering them with cyclophosphamide, but low dosages of Phenibut (25 mg/kg) were shown to have vast improvement in their immune system reactivity and restoration of immune-affected organs.

This result clearly stands as an evidence for the profound immune system correcting properties of Phenibut. Moreover, it was also found that Phenibut mostly influences immune response pertaining to anxiety and stress levels, which is the common cause of lessened immune system functionality in most of the people.

Hence, small dosages of Phenibut taken regularly can alleviate stress and anxiety levels, and even play a great role in realizing the strengthening of the immune system. The immune system modulating properties of Phenibut were thus proven to be very effective.

Phenibut regulates the immune system

Yet another distinct study was conducted to study the immune-regulating effects of Phenibut on animals induced with immune stress due to lipopolysaccharides, which is found in the outer membrane of most bacteria and brings out a strong immune response in animals.

It was found that injecting Phenibut within a span of 5 days from the infection was enough to regulate the hyperactivity caused due to increased immune response, and it also restored the number of phagocytic cells, which are responsible for protecting the body against harmful foreign bodies by digesting them.

Hence, it can be derived that Phenibut shows high immune-regulating properties and restores the immune capacity of the body to its original levels. A strong defense against foreign particles such as bacteria, virus, and other dying cells means that one can better protect themselves against commonly occurring diseases by regular self-administration of Phenibut at home.

Phenibut vs Afobazol - which is better?

… translated Russian article:

Neurotic states can occur at any age, but they are especially characteristic for older people. The complex comorbidities, hormonal changes and sleep disturbances often come in a number of factors that lead to anxiogenic disorders. The prevalence of pathological anxiety states and phobias comes to 12%, and neurotic symptoms may experience up to 45% of people in this age category. Selective anxiolytics - a new generation of drugs that can cope with anxiety without the side sedation and cognitive effects. These include drugs such as Afobazol or Phenibut. The review presented below briefly discusses their basic properties.

Phenibut and Afobazol - what's the difference?

Afobazol and Phenibut both belong to a group of medicines, removing anxiety and have neuroprotective effects. The product form is the same – tablets, but the composition of the active substances varies. Both are developed and introduced into clinical practice in our country (Russia). In other countries, they are not approved.

Phenibut produced in Russia (OOO Ozon), Belarus (Belmedpreparaty RUE) and Latvia (Olainfarm).

The active ingredient of the same name was synthesized in Leningrad in the 60-ies. Phenibut can be called a product of "space technology", because it was included in the medicines needed in space flights. It was supposed to have a calming effect, but without the negative impact on attention and other psychosomatic functions.

Despite the fact that both drugs act on the same brain system, Phenibutum and Afobazol differ in how this effect is achieved. Phenibut is a chemical derivative of GABA, allowing it to "mimic" the natural neurotransmitter, showing tranquilizing effect. An interesting contrast from phenibut vs tranquilizers, benzodiazepines, is that it binds with other types of GABA receptors, so when it is used, it has no sedation inherent to diazepines.

Phenibut also shows nootropic effect, improving memory and mental performance indicators. It potentiates the action of other drugs, such as neuroleptics and hypnotics, and also has anti-hypoxic and neuroprotective properties.

Price difference

The price difference from Afobazol vs Phenibut significant. At 20 days of need 1 package (60 tablets) Afobazol cost from 316 to 380 rubles. Price package Phenibut. Russian production of about 220 rbl., That is 60 tablets will cost 660 rubles. And if you want to take Phenibut Latvian production, the amount should be multiplied by 2 times more.

In an attempt to decide for themselves the question, or Phenibut Afobazol - it is better to buy, be sure to consult with a specialist. After all, despite the fact that the purchase of these drugs do not require a prescription, you can harm yourselve in their uncontrolled use.

AFOBAZOL (aka Afobazole) - is a selective anxiolytic drug. It provides antianxiety and activating effects and is used to treat generalized anxiety disorder, neurasthenia, adjustment disorder, sleep disturbances, premenstrual syndrome, alcohol withdrawal.

Afobazol has no inhibitory effect on the central nervous system and helps to restore the natural mechanism which allows the nervous system to cope with stressful conditions. The drug doesn't provide muscle relaxant effect, drowsiness, negative effects on memory retention and consolidation. Long-term treatment of Afobazol doesn’t produce drug dependence. 17 EUR

Does Phenubut increases GH?

Growth hormone isoform responses to GABA ingestion at rest and after exercise. Powers et al 2008

Oral administration of the amino acid/inhibitory neurotransmitter gamma aminobutyric acid (GABA) reportedly elevates resting serum growth hormone (GH) concentrations.

To test the hypothesis that GABA ingestion stimulates immunoreactive GH (irGH) and immunofunctional GH (ifGH) release at rest and that GABA augments the resistance exercise-induced irGH/ifGH responses.

METHODS:

Eleven resistance-trained men (18-30 yr) participated in this randomized, double-blind, placebo-controlled, crossover study. During each experimental bout, participants ingested either 3 g of GABA or sucrose placebo (P), followed either by resting or resistance exercise sessions.

RESULTS: At rest, GABA ingestion elevated both irGH and ifGH compared with placebo. Specifically, peak concentrations of both hormones were elevated by about 400%, and the area under the curve (AUC) was elevated by about 375%. Resistance exercise (EX-P) elevated time-point (15-60 min) irGH and ifGH concentrations compared with rest. The combination of GABA and resistance exercise (EX-GABA) also elevated the peak, AUC, and the 15- to 60-min time-point irGH and ifGH responses compared with resting conditions. Additionally, 200% greater irGH and 175% greater ifGH concentrations were observed in the EX-GABA than in the EX-P condition, 30 min after ingestion. GABA ingestion did not alter the irGH to ifGH ratio, and, under all conditions, ifGH represented approximately 50% of irGH.

CONCLUSIONS:

Our data indicate that ingested GABA elevates resting and postexercise irGH and ifGH concentrations. The extent to which irGH/ifGH secretion contributes to skeletal muscle hypertrophy is unknown, although augmenting the postexercise irGH/ifGH response may improve resistance training-induced muscular adaptations.

On older one on GABA, but i.m.h.o. a relevant one:

Effect of acute and repeated administration of gamma aminobutyric acid (GABA) on growth hormone and prolactin secretion in man. Cavagni et al 1980

A single oral dose of 5 g gamma aminobutyric acid (GABA) was given to 19 subjects and serial venous blood samples were obtained before and 3 h after drug administration. A placebo was administered to 18 subjects who served as controls. GABA caused a significant elevation of plasma growth hormone levels, but did not consistently alter plasma prolactin concentration since only 5 out of 15 subjects showed an increase of the hormone.

Eight additional subjects were submitted to an insulin tolerance test before and after per os administration of 18 g GABA daily for 4 days. Protracted GABA treatment significantly blunted the response of growth hormone and enhanced that of prolactin to insulin hypoglycaemia. These results indicate that pharmacological doses of GABA affect growth hormone and prolactin secretion in man. The precise nature of GABA's effects as well as its mechanism of action remains to be clarified.

GABA ingestion acutely increased resting irGH concentrations and augmented the irGH response to resistance exercise. Additionally, GABA ingestion resulted in the release of ifGH at rest and after resistance exercise, indicating that GABA ingestion stimulates secretion of ifGH isoforms that are capable of dimerizing receptors and inducing signal transduction. In conclusion, GABA-induced irGH/ifGH secretion may alter substrate metabolism and/or enhance the skeletal muscle responses to resistance training, although this remains to be determined.