As the population keeps on growing exponentially, so is the demand for various categories of drugs, compounds/peptides, supplements, etc.
Medical research has been going on for centuries now.
As soon as researchers sense a gap in the market, a new product is introduced to either meet the sense of urgency or just recreational demand.
Likewise, as the usage of nootropics became prevalent in the recent past, a lot of scientific research was diverted to developing new and effective nootropics.
One such synthetic ‘smart drug’ that we are talking about today is Picamilon.
With a unique set of constituents, Picamilon seems to be quite effective both on paper as well as in clinical trials.
Let’s try to understand what Picamilon really is and how it works along with the prospective benefits that it offers.
I will also make sure to discuss any limitations of the nootropic so that you make a cautious decision before really starting to use it!
What is Picamilon?
Picamilon, a synthetic smart drug developed in a lab of the Soviet Union in 1969, is known by multiple names, such as Pikatropin, Pikamilon, nicotinyl-gamma-aminobutyric acid, and nicotinyl-GAB, etc.
Biochemically, Picamilon is a combination of gamma-aminobutyric acid (GABA), an essential inhibitory neurotransmitter, and niacin, which is vitamin B3 (1).
At the moment, it is patented by a pharmaceutical company in Russia and is quite commonly used as a prescription medication in the country.
While one may argue that this compound itself is not extensively studied in the US and other countries, both GABA and niacin are well-studied. Studies show that this drug leads to increased levels of GABA and niacin in the brain, making it possible to elucidate the benefits that these two individual ingredients offer.
Mechanism of Action
If you are a fan of nootropics, you must have an idea of what GABA really does in the body. As an inhibitory neurotransmitter, it tries to create a calm and relaxing environment within the body (2).
So, the question is that if GABA can create the latter effects itself, why is there a need for Niacin?
The answer lies within the pharmacodynamical studies of GABA. This inhibitory neurotransmitter can’t cross the blood-brain barrier, so niacin or Vitamin B3 helps in crossing the blood-brain barrier and raising the GABA levels within the brain (3).
Now that we know the importance of both ingredients, let’s try to read how the two components create calming and relaxing effects.
Upregulating GABA effects
GABA (gamma-aminobutyric acid) is an inhibitory neurotransmitter. When GABA binds to the GABAergic receptors in the brain, it exhibits anxiolytic effects.
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 (4).
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.
Niacin, also known as vitamin B3 or nicotinic acid, increases cerebral blood flow and decreases blood pressure through vasodilation. This compound is thought to increase blood flow to the brain better than Piracetam, a racetam nootropic, and some other prescription drugs (5).
Through enhanced blood flow, Niacin improves oxygen and glucose supply to the brain. This helps to boost cellular metabolism, thus contributing to improvements in cognitive function and memory.
Regulates other Neurotransmitters
In a rat study on Parkinson’s disease, it was found that Picamilon helped regulate the serotonin and dopamine levels in the brain. Its actions were particularly strong on improving dopamine uptake. Dopamine is involved in reward, concentration, and new memory formation.
Benefits of Picamilon
Now that we know how Picamilon interacts within the body, it is time to understand each of the benefits that it offers and whether the benefits are strong enough to convince the users.
Anxiety and Depression
As stated earlier, deficiency of GABA and imbalance between GABA and glutamate have been involved in anxiety, stress, and depression. Research suggests that Picamilon is found to be effective in managing anxiety and depression, thus leading to widespread prescription for those with depression in Russia.
In one study, administering Picamilon was found to normalize depressed and anxious behavior in the subjects.
GABA also prevents the over-stimulation of neurons due to glutamate, therefore 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 and attention in those with ADHD. Additionally, the niacin is able to boost mental energy, helping to promote concentration and logical reasoning.
Lowers blood pressure
Recent studies have found that due to improvement in cerebral blood flow and its vasodilatory effects, Picamilon may lower the blood pressure by affecting the peripheral circulation (6).
While more studies are needed to confirm this, if proven true, it may open gateways to new pharmacological therapies.
Excess glutamate can lead to insomnia and trouble sleeping. By reestablishing homeostasis through counteracting excess glutamate, the GABA found in Picamilon leads to a calmer and more peaceful state of mind.
Relieves 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 owing to improved cerebral blood flow and cellular metabolism.
Is Picamilon Legal?
Picamilon is a banned substance according to the FDA and any dietary supplements containing Picamilon are not allowed to be used.
However, in Russia, it is widely available as a prescription medicine and a lot of doctors prescribe it to treat anxiety, depression, and stress-related symptoms.
Recommended Dosage and Half-life
Daily dosage ranges from about 100 to 300 mg/day with food to enhance absorption. Most users report stimulatory effects only at 200 mg/day or more.
The half-life of Picamilon was found to be about 1-2 hours in humans. Because of this short half-life, it is best to divide your dosage out into 2-3 servings each day.
It is important to note that anxiety relief has been reported at both low and high doses.
However, do not exceed 300 mg/day to prevent niacin overdose. Too much niacin can lead to increased blood sugar (hyperglycemia), 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.
Side Effects and Interactions
While there have been no human studies confirming side effects and long-term safety profiles, it is likely that any side effects caused by GABA or niacin alone may also apply.
Niacin has been found to lead to the following:
- 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-term studies need to be done to confirm this.
Interactions may likely 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.
Now let’s read what the users have to say about their experiences with Picamilon and whether the scientific evidence has some anecdotal backing or not.
“For me, Picamilon is a blessing. I find that it is somewhere between Theanine and Phenibut in terms of anxiety relief.”
Another user said,
“Thank you for this comprehensive response, I just received some and was surprised at how subtly effective it was (200mg SUB actually induced a nap in a gentle, subtle way, not something that typically happens for me).”
Apra24 left a comment saying,
“I’ve been taking it for a week now, and have to say it’s amazing for someone with social anxiety. I work as a courier and about 1 hour after popping a 150mg pill, I feel extremely sociable and calm.”
Some people had mixed opinions on Picamilon as one of the users said,
“same. it has some really subtle effect, but it does nothing for anxiety”
Another one said,
“It was less relaxing than Phenibut but w/o the side effects.”
Where to Buy Picamilon
Because of FDA restrictions, buying Picamilon easily is quite a tough job and you wouldn’t find many stores selling the nootropic as it is banned to buy any supplements containing Picamilon till further research confirms its efficacy.
Nonetheless, I have picked one brand that you can genuinely put your trust in and make your purchase.
Picamilon by Pure Rawz
Pure Rawz offers a 5-gram variant of Picamilon Sodium NICOTINOYL-GABA Powder at a price range of $19.48.
With quality products offered, 100% satisfaction guaranteed, free shipping, and secure checkout options, I believe that Pure Rawz offers a lot in a considerable price range.
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Read full Pure Rawz Review
Picamilon vs Other compounds
Picamilon vs GABA
When you take Picamilon, it easily crosses over the blood-brain barrier to deliver GABA to the brain. In comparison, supplementary GABA is not able to easily cross through this protective barrier. 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. It is possible that these effects are due to GABA’s effects on the Enteric Nervous System (ENS). Our ENS is known as our second brain, or the brain in our gut.
In recent years, there has been a lot 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 the level of GABA found in the brain.
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 against anxiety.
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 because of the phenyl ring, and Picamilon able to do so due 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.
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.
Is Picamilon Legit?
Picamilon definitely seems to work against symptoms related to anxiety, depression and provides anti-stress effects and relief to the individuals.
I know that the FDA hasn’t approved the nootropic owing to a lack of sufficient clinical data but user experiences and limited research may provide you an insight on whether this nootropic should be used or not.
Perhaps in my opinion, if you really want to use nootropics that can enhance your GABAergic system, there are better options available on the market, so maybe try out those!
Is Picamilon Banned?
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 Picamilon is available.
Is Picamilon Addictive?
In comparison to other anti-anxiety drugs, Picamilon is considered to build less 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 below.
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 other drugs. It can lower blood pressure, so if you already have low blood pressure or are on medication to lower blood pressure, you may want to avoid taking it.
How long does Picamilon last?
Picamilon’s effects are generally felt quickly – within an hour for most people – and they normally last for four to six hours after each dose.
Does niacin cross the blood-brain barrier?
Niacin is metabolized in the liver to nicotinamide. Nicotinamide is widely distributed in the body. Nicotinic acid and nicotinamide can penetrate the blood-brain barrier.