Picamilon: Nootropic Benefits, Dosage, & Side Effects


Article on the cognitive enhancement and calming effects of Picamilon, a nootropic compound.

Picamilon, a distinctive supplement often included in dietary supplements, has garnered attention for its unique properties that blend the benefits of GABA (gamma-aminobutyric acid) with niacin (vitamin B3).

Originally developed in Russia, this medical compound has found its place in the realm of cognitive enhancement and mood regulation in the U.S.

This comprehensive analysis aims to provide reliable information on Picamilon, exploring its role as a new nootropic agent and its therapeutic potential in improving blood circulation, particularly in the brain.

Read on as we shed light on the benefits of Picamilon in the world of dietary supplements and its place in cognitive wellness and mental health.

What is Picamilon?

Picamilon (also known as Pikamilon, Pikatropin, nicotinyl-gamma-aminobutyric acid, 4-(pyridine-3-carbonylamino) butanoic acid, or nicotinyl-GABA) is a synthetic nootropic compound that combines niacin (vitamin B3) with gamma-aminobutyric acid (GABA), a key neurotransmitter in the brain.(1)

Developed in Russia, this supplement is used for its various effects on brain function and mental health.

As a dietary supplement, Picamilon offers a novel approach to improving mental and physical health. However, Picamilon’s status as a dietary ingredient is not eligible to be approved by the FDA (Food and Drug Administration) due to it not being considered a clinical medication or substance.

Picamilon’s mechanism hinges on the combination of GABA, a primary inhibitory neurotransmitter in the brain, with niacin. When GABA combines with niacin, it enhances Picamilon’s ability to boost brain function and cross the blood-brain barrier, a limitation often faced by GABA alone in the body.

Once in the brain, Picamilon administration works to improve cerebral circulation by increasing blood supply to the brain. The increase in blood flow thereby boosts cognitive function and aids in the management of conditions like stress, anxiety, and various cerebrovascular disorders.

Overall, Picamilon is primarily used for its nootropic and neuroprotective effects. It’s touted for improving cognitive function, reducing symptoms of anxiety and depression, and enhancing overall brain health. It’s also used in the treatment of certain cerebrovascular conditions due to its ability to improve blood circulation in the brain.

The Picamilon product has been used as a prescription drug in Russia for its cognitive and cerebrovascular benefits. However, its availability and regulatory status as a dietary supplement or drug vary in different countries. 

Picamilon as a nootropic drug exhibits the properties of a tranquilizer with a stimulating component to balance its sedative effect. Unlike tranquilizer drugs, it does not leave you feeling side effects like drowsiness or lethargy even though it does induce muscle relaxation.

Pros:

  • Improved cognitive functions, such as a boost in concentration and memory
  • Improved mental alertness
  • Reduced stress and anxiety
  • Increased GABA levels

Cons:

  • Further human clinical trials are needed to define the long-term safety profile
  • Not approved as a prescription drug by the FDA

Mechanism of Action

Picamilon, a unique nootropic supplement, exerts its effects through its two key components: niacin (vitamin B3) and gamma-aminobutyric acid (GABA). Understanding its mechanism of action requires looking at how these components interact and function within the body, particularly in the brain.

  • Unique Structure: Picamilon is synthesized by the combination of niacin and GABA analogues. This chemical structure is crucial for its mechanism of action, as it allows Picamilon to effectively cross the blood-brain barrier, a challenge that GABA molecule cannot easily overcome alone.
  • Enhanced Absorption: Once ingested, Picamilon reaches the brain, where it is hydrolyzed into GABA and niacin. The presence of niacin enables this crossing, which is essential for the effects of GABA to be realized within the central nervous system.
  • Release in the Brain: After crossing the blood-brain barrier, Picamilon releases GABA and niacin (also known as nicotinamide) into the brain. These released components then individually exert their respective effects.
  • GABA’s Role: GABA, as an inhibitory neurotransmitter, helps to reduce neuronal excitability throughout the nervous system. This general action is associated with a decrease in anxiety and an increase in relaxation.
  • Improving Blood Flow: Niacin acts as a vasodilator, widening blood vessels. In the brain, clinical studies have shown that this leads to improved cerebral blood flow, which is beneficial for cognitive functions and overall brain health.(2)
  • Potential Neuroprotective Effects: Improved blood flow may also have neuroprotective effects, potentially aiding in conditions like brain trauma or cerebrovascular disorders.
  • Anxiolytic and Nootropic Effects: The combined effects of enhanced GABAergic activity and improved cerebral circulation contribute to Picamilon’s anxiolytic and cognitive-enhancing properties.
  • Impact on Mental Health: By modulating neurotransmitter activity and improving brain circulation, Picamilon in dietary supplements positively affects mood, stress levels, and cognitive functions like memory and concentration.

Nootropic Benefits of Picamilon

Picamilon is used for its unique ability to target GABA receptors in the brain, which play a critical role in neural processes. Here’s an overview of its potential nootropic benefits, as demonstrated in various studies. 

1. Targeting GABA Receptors

Picamilon’s primary action is on GABA receptors. GABA is an inhibitory neurotransmitter, and its engagement with these receptors has an inhibitory effect on neural activity, leading to a calming effect on the brain.

2. Normalization of Brain Function

Scientific research has shown that Picamilon helps in the normalization of brain functions, particularly in conditions where GABA’s natural balance is disrupted.(3)

3. Enhancement of Cognition

By improving neural communication and having a positive effect on neural networks, Picamilon has been shown to help improve cognition, including memory, focus, and mental clarity.(4)

4. Increased Blood Flow to the Brain

Niacin in Picamilon aids in dilating blood vessels in the brain, which enhances blood flow and, consequently, oxygen and nutrient delivery to brain cells.(5)

5. Neuroprotective Properties

Picamilon was shown to have neuroprotective effects, potentially safeguarding the brain against age-related decline and other neural disorders.

6. Amino Acid Uptake Improvement

Picamilon has been shown to improve the uptake of certain amino acids in the brain, which are crucial for various brain functions, including neurotransmitter synthesis.(6)

7. Stress Reduction and Mood Regulation

The interaction of Picamilon with GABA receptors can help in reducing stress and regulating mood, leveraging the natural inhibitory effect of GABA.

Uses of Picamilon

Pikamilon (nicotinyl-gamma-aminobutyric acid) has a range of uses, particularly in enhancing brain function and treating certain conditions.

Here are some of the notable uses of Picamilon:

  1. Cognitive Enhancement: Picamilon is often used to improve cognitive functions such as memory, focus, and mental clarity. By boosting brain activity, it helps in enhancing overall mental performance.
  2. Mood Regulation: Due to its impact on GABA receptors, Picamilon has a calming effect on the brain. This makes it useful in regulating mood and potentially alleviating symptoms of anxiety.
  3. Treatment for Alcoholism: One of the significant uses of Picamilon is in the treatment of alcoholism. It helps in reducing the symptoms of alcohol withdrawal and aids in the recovery process by stabilizing neural activity and reducing anxiety.
  4. Stress Reduction: The calming effect of Picamilon on the brain makes it beneficial in managing stress. Picamilon provides a sense of relaxation without sedation, helping individuals cope with high-stress situations more effectively.
  5. Improved Blood Flow: The nicotinate acid in Picamilon aids in dilating blood vessels, which can improve blood flow to the brain. This enhanced circulation is beneficial for brain health and function.
  6. Neuroprotective Effects: There is evidence to suggest that Picamilon may have neuroprotective properties, potentially safeguarding the brain against age-related decline and other neural disorders.
  7. Enhanced Sleep Quality: While primarily used for its cognitive and mood-regulating benefits, Picamilon also improves sleep quality, aiding in relaxation and ease of falling asleep for people with insomnia.

Where to Buy Picamilon

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Picamilon Dosage

Typically, the standard dosage of Picamilon falls between 50 mg to 300 mg per day. This range is often recommended for cognitive enhancement and mood regulation.

For certain conditions like the treatment of anxiety or alcohol withdrawal symptoms, the dosage may be on the higher end of the spectrum. In some cases, up to 300 mg per day, divided into two or three doses at a time throughout the day.

Note: Picamilon is available for both intravenous and oral administration. For those considering the injection, remember that IV administration of Picamilon is a medical procedure that should be performed only under the supervision of a healthcare professional. The dosage for IV administration is typically lower than oral dosages because of the direct delivery into the bloodstream, which makes it more potent.

Picamilon Side Effects & Safety

Although often well-tolerated, Picamilon can cause adverse effects in some individuals. The severity and type of these effects can vary based on dosage, individual sensitivity, and other factors.

Some potential side effects include: 

  • Dizziness
  • Nausea
  • Headaches
  • Irritability

Some safety considerations include:

  • Low Blood Pressure: Due to its vasodilating properties (stemming from the niacin component), Picamilon might cause a drop in blood pressure in some individuals.
  • Allergic Response: As with any substance, there is a potential for an allergic response to Picamilon. Symptoms of an allergic reaction can include itching, rash, swelling, and in severe cases, difficulty breathing.
  • Interaction with Other Medications: Picamilon can interact with other medications, especially those affecting the brain or blood pressure.
  • Dependence and Withdrawal: While not common, there’s a potential for dependence and withdrawal symptoms with long-term use, especially at high doses.

Summary

In conclusion, Picamilon is a combination of niacin (vitamin B3) and GABA (gamma-aminobutyric acid).

This nootropic drug presents itself as a noteworthy nootropic with potential benefits ranging from cognitive enhancement and mood regulation to specific applications in treating conditions like alcoholism and anxiety.

Picamilon’s unique formulation, combining niacin and GABA, targets neural pathways and blood flow to the brain, offering a multifaceted approach to improving mental function and overall brain health.

However, the importance of adhering to appropriate dosages, whether taken orally or administered intravenously, cannot be overstated.

As with any nootropic supplement, the key lies in informed, cautious, and supervised use, ensuring that its benefits are harnessed effectively and safely.

FAQs

How long does Picamilon take to work?

Approximately 30 minutes to 1 hour after ingestion. Some users might experience effects sooner, especially at higher doses.

What is the elimination half-life of Picamilon?

About 1 to 2 hours. This short half-life means that Picamilon is metabolized and excreted relatively quickly, which influences how long its effects last.

Should you cycle Picamilon?

To reduce the risk of developing tolerance or dependence, it’s often recommended to cycle nootropics like Picamilon. A common approach might be using Picamilon for several weeks followed by a week or two off, but this can vary based on individual response and preferences.

Can I stack Picamilon with other nootropics?

Picamilon can be combined with other nootropics that have different mechanisms of action for a synergistic effect.

How should I store Picamilon?

Store it in a cool, dry place away from direct sunlight. Keep it away from moisture and excessive heat, as these can affect its stability. Additionally, it’s often best to keep it in its original packaging to protect it from environmental factors.


Sources, Studies, and Scientific Research
  1. Mirzoian, R S, and T S Gan’shina. “Novyĭ tserebrovaskuliarnyĭ preparat pikamilon” [The new cerebrovascular preparation pikamilon]. Farmakologiia i toksikologiia vol. 52,1 (1989): 23-6.
  2. Mirzoian, R S et al. “Vliianie pikamilona na krovosnabzhenie kory i mikrotsirkuliatsiiu v sisteme pial’nykh arteriol” [Effect of pikamilon on the cortical blood supply and microcirculation in the pial arteriole system]. Biulleten’ eksperimental’noi biologii i meditsiny vol. 107,5 (1989): 581-2.
  3. Zakharov, V V et al. “Lechenie bol’nykh s khronicheskoi ishemiei golovnogo mozga: opyt primeneniya kombinirovannogo neiroprotektivnogo preparata Pikamilon Ginkgo” [Treatment of patients with chronic cerebral ischemia: experience of using the combined neuroprotective drug Picamilon Ginkgo]. Zhurnal nevrologii i psikhiatrii imeni S.S. Korsakova vol. 122,9 (2022): 95-103. doi:10.17116/jnevro202212209195
  4. Voznesenskiĭ, A G et al. “Sravnitel’noe izuchenie vliianiia pikamilona i piratsetama na obuchenie krys v radial’nom labirinte” [Comparative study of the effect of picamilone and piracetam on learning in rats in a radial maze]. Farmakologiia i toksikologiia vol. 52,4 (1989): 14-7.
  5. Sapegin, I D, and A I Beketov. “Vliianie pikamilona i fenibuta na krovosnabzhenie golovnogo mozga v usloviiakh pokoia i pri gravitatsionnykh vozdeĭstviiakh” [The effect of pikamilon and fenibut on the blood supply of the brain at rest and under gravitational exposures]. Eksperimental’naia i klinicheskaia farmakologiia vol. 56,1 (1993): 28-31.
  6. Davydova, G A, and A I Mukha. “Rezul’taty primeneniia vazoaktivnogo preparata pikamilona pri pigmentnoĭ abiotrofii setchatki” [Results of the use of vasoactive preparation pikamilon in pigmented retinal abiotrophy]. Vestnik oftalmologii vol. 111,3 (1995): 20-2.

Jacob Kovacs is a cognitive neuroscientist and author at WholisticResearch, specializing in nootropics and neuroactive peptides. His expertise in neuroscience and psychopharmacology bridges cognitive science with drug development. Kovacs’ work focuses on enhancing cognitive functions and brain health through innovative, efficient neuroactive compounds that overcome traditional pharmacokinetic challenges. His contributions are pivotal in advancing the understanding and treatment of neurological diseases.

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