What is Picamilon?
Picamilon, also known as N-nicotinoyl-GABA and nicotinyl-y-aminobutyric acid, is a synthetic smart drug produced in the Soviet Union in 1969. (4) Presently it’s patented by a pharmaceutical company in Russia, where it is prescribed for depression, attention, chronic alcoholism, brain trauma, and other conditions.
Chemically, Picamilon is a combination of GABA (g-aminobutyric acid), our main inhibitory neurotransmitter, and niacin, which is vitamin B3. It is thanks to the niacin that the GABA in Picamilon is able to cross into the brain through the blood-brain barrier.
As a nootropic, it’s unique properties allow users to experience improved mental energy combined with a calming effect. Neurohackers use it to relieve stress, enhance mood, fight depression, improve sleep, and boost overall cognition. It helps to relax the user without producing a sedative effect.
In Russia, this drug has been studied in humans, however this literature is not fully available to the rest of the world. Without abundant literature, many neurohackers will ask, does Picamilon work?
While this compound itself is not extensively studied in the US, both GABA and niacin are. Studies show that this drug leads to increased GABA and niacin in the brain, making it possible to elucidate the benefits through those found with these two compounds.
Mechanisms of Action
Picamilon is able to easily cross over the blood-brain barrier, where it is hydrolyzed into the two compounds responsible for its nootropic benefits: GABA and niacin.
GABA (gamma-aminobutyric acid) is an inhibitory neurotransmitter. (2) When GABA comes in contact with the GABA receptors in the brain, it exhibits anxiolytic effects. (7)
GABA protects the brain from excessive glutamate activity. Glutamate is the main excitatory neurotransmitter - a balance between these two is critical for optimal brain health and mood.
High stress can lead to excess glutamate; GABA acts to reduce this effect. Insufficient GABA and excess glutamate are implicated in anxiety conditions, insomnia, mood problems, and general restlessness.
Drugs that increase the activity and quantity of GABA in the brain have been found to increase the production of alpha brain waves, which are associated with a calmer state of mind. (8)
Niacin, also known as vitamin B3 or nicotinic acid, increases cerebral blood flow and decreases blood pressure through vasodilation. (7) This compound is thought to increase blood flow to the brain better than Piracetam and some prescription drugs.
Through enhanced blood flow, Niacin improves oxygen and glucose supply to the brain. This helps to boost cell metabolism, contributing to improvements in cognitive function and memory.
In a rat study on Parkinson’s disease, it was found that Picamilon helped to normalize serotonin and dopamine levels in the brain. (9) Its action was particularly strong on improving dopamine uptake. Dopamine is involved in reward, concentration, and new memory formation.
Anxiety and Depression
Deficiencies in GABA and imbalances between GABA and glutamate have been implicated in anxiety, stress, and depression. (7,11) Picamilons efficacy is such that it is prescribed for those with depression in Russia.
Animal studies have shown promise when it comes to Picamilon treating anxiety and depression. In one study, injections of this drug were found to normalize depressed and anxious behavior. (12)
Many of the current anxiolytic drugs act to increase GABA in the brain. (7) Thanks to its ability to do just that, Picamilon is likely to reduce feelings of stress and anxiety.
GABA prevents the over-stimulation of neurons by glutamate, allowing users to feel calm and relaxed, rather than restless and anxious. With the additional boost in cerebral blood flow, improved cognitive health and cellular metabolism may also contribute to a positive mood.
Through its impact on depression and anxiety, it is thought that this drug may help improve focus in those with ADHD. Additionally, the niacin is able to boost mental energy, helping to promote focus and logical reasoning.
These effects act together to promote feelings of relaxed focus and concentration.
Excess glutamate can lead to insomnia and trouble sleeping. By reestablishing homeostasis through counteracting glutamate, the GABA found in Picamilon leads to a calmer, more peaceful state of mind. This balancing of neurotransmitters can help you to get a good night's sleep.
Headaches and Migraines
This nootropic may help those suffering from migraines and tension headaches. Niacin has been found to be effective at reducing the frequency of migraines and headaches in humans. (10) This ability is likely thanks to improved blood flow and cellular metabolism.
Picamilon vs GABA
When you take Picamilon, it easily crosses over the blood-brain barrier to deliver GABA to the brain. (1) In comparison, supplementary GABA is not able to easily cross through this protective barrier. (2) Because of this bioavailability, Picamilon is superior in its anxiolytic and nootropic properties.
Although studies suggest low permeability of GABA supplements into the brain, benefits of supplementation have still been found. (2) It is possible that these effects are thanks to GABAs effects on the Enteric Nervous System (ENS). Our ENS is known as our second brain, or the brain in our gut. The ENS is so vast that it has as many neurons as our entire spinal cord.
In recent years, there has been lots of research regarding bidirectional communication between our ENS and brain. There is a connection between GABA food supplements, the vagus nerve that connects the brain and the ENS, and brain levels of GABA, although research regarding this effect is still in its infancy.
Because of these interactions, even though less GABA will reach the brain with a GABA supplement than with a Picamilon supplement, it may still benefit anxiety and cognition. (2)
Picamilon vs Phenibut
Both Phenibut and Picamilon are nootropics that exhibit their effects largely through mediating the GABAergic system. While they both appear to help relieve anxiety, Picamilon does so with a slightly stimulatory effect, reducing brain fog and promoting mental clarity.
This begs the question: Is it better than Phenibut?
While the primary use for both of these nootropics is to help with mood and anxiety, their chemical structure and other benefits differ.
Both are derivatives of GABA, with Phenibut able to cross the blood-brain barrier thanks to a phenyl ring, and Picamilon able to do so thanks to niacin.
The niacin supplied by Picamilon helps to increase mental clarity and energy through enhancing cellular metabolism and improving blood flow to the brain. This gives Picamilon a mentally stimulating calm, where users report feeling calm but focused.
Phenibut is considered more centered around only relieving anxiety, without having any stimulatory effects. Studies do suggest that both of these compounds positively influence the levels of dopamine in the brain, which can help to improve overall mood and concentration ability.
So which is better?
According to user reviews, Phenibut offers the strongest anxiety relief, but at the cost of tolerance. It may be best to cycle between these two to offset the tolerance, however, since both work on the GABAergic system, Picamilon too may lead to tolerance if high quantities are used for extended periods of time.
If you are looking for just anxiety relief, Phenibut may be the best option, but if you are looking for an anxiolytic with more apparent nootropic properties, Picamilon is a good choice.
Side Effects and Interactions
While there have been no human studies confirming side effects and safety, it is likely that any side effects caused by GABA or niacin alone may apply.
Niacin has been found to lead to the following (10):
- Lightheadedness and fainting
- Low blood pressure
Other users have reported headaches, although most users report fewer headaches when taking this drug. It does not appear to cause withdrawal or tolerance, however longer studies need to be done to confirm this.
Interactions may occur with other drugs that act upon GABA receptors or those that interfere with niacin. These include alcohol, Aspirin in high doses, barbiturates, nonbenzodiazepines, benzodiazepines, and uricosuric agents.
The half-life of Picamilon was found to be about 1-2 hours in humans. (3) Because of this short half-life, it is best to divide your dosage out into 2-3 servings each day.
Daily dosage ranges from about 100 to 300 mg/day with food to enhance absorption. You can use capsules or bulk powder forms. Most users report stimulatory effects only at 200 mg/day or more. Anxiety relief has been reported at both low and high doses.
Do not exceed 300 mg/day to protect against niacin overdose. Too much niacin can lead to increased blood sugar, which can be dangerous for those with diabetes. If you are concerned about blood sugar levels, start with a low dosage and monitor your response closely.
Users tend to agree that Picamilon is not as strong of an anxiolytic as Phenibut:
“I would say that Picamilon is about 25% as strong as good old original flavor Phenibut. I know it had some GABAergic action because at a time where I would take 800mg of Gabapentin I took 300mg of Picamilon and it quelled the urge.” -Reddit user review
Another user reported benefits when cycling these two nootropics:
“I use Picamilon when I’m cycling off Phenibut. Works great in higher doses like 300-500 mg.” -Longecity user review
When used on its own, most users report very subtle effects:
“Picamilon is very subtle..I think that's where pica really shines is when taking it before a run or when you’ve overshot the caffeine..Pica is highly underrated and can ease slight overstimulation.” -Reddit user review
Frequently Asked Questions
Is Picamilon Legal?
The legality of Picamilon varies from one country to another. In Russia it is legal only as a prescription drug. In the US it is considered an adulterating agent in supplements and was banned by the FDA in 2015, with certain companies at this time ordered to stop selling Picamilon. (5) While it is banned from being sold as a supplement or included in a supplements, the compound itself is not illegal.
In the UK it may be considered an illegal substance in certain countries. As of February 1, 2018, Phenibut is banned in Australia as a Schedule 9 prohibited substance, however it appears that users can find and purchase Picamilon online.
Is it Banned Anywhere?
Picamilon appears to be a grey area in many countries, leading to difficulty obtaining this nootropic. In some countries it is easy to find Phenibut but not Picamilon, and in other countries the reverse is true. As these laws continue to change, it is best to research reputable online vendors in your country to see if Picamilton is available.
Is Picamilon Addictive?
In comparison to other anti-anxiety drugs, Picamilon is considered to build less of a tolerance and produce fewer withdrawal symptoms when users stop taking it. There is no definitive answer as to the level of tolerance or addiction potential there is, but it appears to be low.
As it works on your GABAergic system, there is likely to be some level of tolerance after using it for extended periods of time.
Is Picamilon Safe?
Overall, this drug is considered to be safe at recommended dosages, however it may interact with some drugs. It can lower blood pressure, so if you already have low blood pressure or are on a medication to lower blood pressure, you may want to avoid taking it.
Where to Buy Picamilon
In the USA, Picamilon was previously carried in physical stores, including Vitamin Shoppe and GNC. It was also widely available through online supplement retailers, including Absorb Your Health and iHerb. Since the 2015 FDA ban, the availability of this nootropic has dramatically decreased, making it nearly impossible to find.
There is a theory that this nootropic is so hard to find thanks to its rights being owned by a Russian pharmaceutical company. Even if you do find this nootropic online, it is very likely that it will not be high quality.
Thanks to the difficulty in obtaining this nootropic, you may want look for an alternative. Good options for nootropics that both enhance cognitive function and decrease anxiety include:
- Mind Lab Pro
- Pikamilon pharmacokinetics in animals https://www.ncbi.nlm.nih.gov/pubmed/1884802
- Neurotransmitters as food supplements: the effects of GABA on brain and behavior https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4594160/
- Determination of picamilon concentration in human plasma by liquid chromatography-tandem mass spectrometry https://www.sciencedirect.com/science/article/pii/S1570023210001479?via%3Dihub
- Some approaches to the directed search for new drugs based on nicotinic acid https://link.springer.com/article/10.1007%2FBF02509934
- DBM Nutrition 11/30/15 https://www.fda.gov/ICECI/EnforcementActions/WarningLetters/2015/ucm474808.htm
- The new cerebrovascular preparation pikamilon https://www.ncbi.nlm.nih.gov/pubmed/2707413
- Effect of picamilon on the cerebral cortical blood supply and microcirculation in the pial arteriolar system https://link.springer.com/article/10.1007%2FBF00841781#page-1
- The role of GABA in the pathophysiology and treatment of anxiety disorders https://www.ncbi.nlm.nih.gov/pubmed/15131523
- Correction by nicotinamide and nicotinoyl-GABA of dopamine metabolism in rat brain in experimental Parkinson’s disease https://www.ncbi.nlm.nih.gov/pubmed/12199067
- The treatment of migraines and tension-type headaches with intravenous and oral niacin (nicotinic acid) https://nutritionj.biomedcentral.com/articles/10.1186/1475-2891-4-3
- Towards a glutamate hypothesis of depression https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3205453/
- The effect of hypokinesia on depression and on the central GABA-A receptor complexes in the rat brain https://www.ncbi.nlm.nih.gov/pubmed/16845932
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