Picamilon – An Overview

Picamilon (also known as N-nicotinoyl-GABA, pycamilon, and pikamilon), is a synthetic nootropic that may be useful for the following:

• Lowering anxiety and stress
• Improving mood
• Increasing cerebral circulation
• Improving memory and learning
• Addiction recovery

It works primarily through increasing GABA levels in the brain. Typically, GABA cannot cross the blood-brain barrier, making direct supplementation ineffective.

However, picamilon gets around this by attaching a Vitamin B3 (niacin) molecule to a GABA molecule.

The B3 molecule allows the GABA molecule to cross into the brain and start taking action. ¹Dorofeev BF, Kholodov LE. Pikamilon pharmacokinetics in animals Farmakol Toksikol. 1991

It was originally developed in Russia during the ’60s and is still prescribed for anxiety, attention disorders, and addiction recovery.

Like Phenibut, it can promote feelings of relaxation and well-being without the drowsiness or impairment of traditional tranquilizers. ²R. P. Kruglikova-L’vova, et al. Pikamilon-a new vasoactive and nootropic preparation Pharmaceutical Chemistry Journal. 1989

Is Picamilon Banned?

Not quite, although this supplement has caused some controversy in the US with regulatory agencies.

In 2015, the FDA determined that “picamilon is a substance that does not meet the statutory definition of a dietary ingredient.”

It demanded that some companies pull products “adulterated” with this product, as it is not approved for sale in the US as a human supplement.

However, despite this recent controversy, picamilon is still technically legally available for purchase in the USA. Just not branded for human consumption.

Please consult your local regulations to see if picamilon is legal to purchase where you live.

What Does Picamilon Do?

Picamilon For Anxiety

Although the FDA has never approved picamilon for use in the USA, it is used in Russia as a treatment for anxiety, among other neurological conditions.

There is significant clinical evidence that this nootropic can decrease stress and increase cognitive function under pressure. ³Dorofeev BF, Kholodov LE. Pikamilon pharmacokinetics in animals Farmakol Toksikol. 1991

Drugs that can mimic or increase GABA activity in the brain, such as picamilon, have the potential to provide anti-anxiety and antidepressant effects.

Research shows that people with too little GABA may be at a higher risk for developing anxiety.⁴Shephard RA. Behavioral effects of GABA agonists in relation to anxiety and benzodiazepine action Life Sci. 1987 ⁵Matsuyama K, et al. Evaluation of isonicotinoyl-gamma-aminobutyric acid (GABA) and nicotinoyl-GABA as pro-drugs of GABA Chem Pharm Bull (Tokyo). 1984 ⁶Nemeroff CB. The role of GABA in the pathophysiology and treatment of anxiety disorders Psychopharmacol Bull. 2003

According to research, picamilon has a “depriming” effect on the system of negative emotions.

Anecdotally, many people say it helps them deal with stress and keep a clear head during difficult times.

Even better, it seems that picamilon can lower anxiety without impairing motor function or mental abilities like other anxiety medication. ⁷R. P. Kruglikova-L’vova, et al. Pikamilon-a new vasoactive and nootropic preparation Pharmaceutical Chemistry Journal. 1989

Picamilon For Depression & Mood

By balancing GABA/glutamate and increasing dopamine and serotonin, picamilon may have some antidepressant effects.

According to animal studies, this nootropic can prevent despair and encourage the “normalization of the behavioral parameters” in rats.⁸Akopian VP, Balian LS, Avetisian NA. The effect of hypokinesia on depression and on the central GABA-A receptor complexes in the rat brain Eksp Klin Farmakol. 2006

Many users report a mood boost when taking this nootropic. They say it gives them more energy and balances their emotions.

Although more human studies are needed, we think that there is some solid preliminary evidence picamilon may be useful for depression and raising mood.

Picamilon For ADHD & Motivation

Despite picamilon’s reputation as a calming agent, it also does have some stimulatory properties which may be useful for treating ADHD.

There is clinical evidence that it “has an activating effect on positive reinforcement structures,” i.e,. that it can increase motivation. ⁹R. P. Kruglikova-L’vova, et al. Pikamilon-a new vasoactive and nootropic preparation Pharmaceutical Chemistry Journal. 1989

This may be due to picamilon’s ability to balance GABA and glutamate, as well as its effects on dopamine, serotonin, and cerebral blood flow.

These are all critical aspects of attention, meaning picamilon can have an overall “balancing” effect.

Users often report a calm but energized focus while supplementing with this nootropic.

Picamilon For Drug and Alcohol Recovery

In Russia, picamilon has been used for decades to help addicts mitigate their withdrawal symptoms and reduce cravings.

It increases GABA, the same receptor that alcohol effects, meaning it may be especially valuable for recovering alcoholics.

Patients taking this nootropic during recovery report less anxiety, less desire to relapse, and more motivation.¹⁰R. P. Kruglikova-L’vova, et al. Pikamilon-a new vasoactive and nootropic preparation Pharmaceutical Chemistry Journal. 1989

Memory

Picamilon can improve short and long term memory, as well as act as an anti amnesiac. This could be partially due to its niacin molecule, which is a proven memory aid.

Increasing cerebral blood flow and balancing neurotransmitters may also help improve memory. ¹¹Loriaux SM, Deijen JB, Orlebeke JF, De Swart JH. The effects of nicotinic acid and xanthinol nicotinate on human memory in different categories of age. A double blind study Psychopharmacology (Berl). 1985

On experimental models of animals with induced memory damage, picamilon showed antihypoxic and antiamnesic activity.

This means that picamilon may prevent and possibly reverse some aspects of amnesia and cognitive decline. ¹²Voronina TA, Garibova TL, Khromova IV, Tilekeeva UM. Dissociation of the anti-amnesic and antihypoxic effects of nootropic and antihypoxic preparations Farmakol Toksikol. 1987

How Picamilon Works In The Brain

Picamilon And GABA

GABA is the major inhibitory neurotransmitter in the brain, and it counteracts glutamate, the major excitatory transmitter.

Both of these neurotransmitters are critical to proper brain function and cognition, but it’s important that they stay in proper balance.

In particular, you need enough GABA to ensure glutamate levels do not get too high. Too much glutamate can lead to anxiety, dysfunction, and even be neurotoxic to brain cells.

Picamilon works by crossing the blood-brain barrier, where it is metabolized into GABA and nicotinic acid.

Increasing GABA can keep glutamate levels in check, and provide balance to your brain. This can ensure you stay calm, focused, and motivated. ¹³V. M. Kopelevich. V. I. Gunar. Some approaches to the directed search for new drugs based on nicotinic acid Pharmaceutical Chemistry Journal. 1999

Increased Blood Flow

Another major pathway picamilon works on is blood-flow.

Research proves it can significantly increase vascular flow to the brain.

As you can probably guess, more blood and oxygen in your brain cells leads to a healthier brain and better overall cognition. ¹⁴Bendikov EA, Shmuĭlovich LM, Kopelevich VM. Effect of gamma-aminobutyric acid, nicotinoyl-gamma-aminobutyric acid and its ethyl ester on central processes of formation of vasomotor reflexes Biull Eksp Biol Med. 1972

Picamilon also seems to have a secondary effect on dopamine and serotonin in the brain, which are crucial to overall mood and mental health.

Combined with its ability to balance GABA and glutamate, this makes picamilon a powerful and well-rounded nootropic for many users.¹⁵R. P. Kruglikova-L’vova, et al. Pikamilon-a new vasoactive and nootropic preparation Pharmaceutical Chemistry Journal. 1989 ¹⁶Kuchmerovs’ka TM, et al. Correction by nicotinamide and nicotinoyl-GABA of dopamine metabolism in rat brain in experimental Parkinson’s disease Ukr Biokhim Zh. 2001

How Much Picamilon Should I Take?

Most research has looked at therapeutic doses around 50-200mg/day, generally divided into 2-3 doses.

Some physicians recommend taking picamilon with a meal for better absorption.

It may take up to three weeks of daily use to see the full benefits of this nootropic.

We don’t recommend exceeding this dose, as it may actually decrease the effectiveness of the picamilon.

Picamilon Potential Side Effects

There are very few reported side effects from taking picamilon. Picamilon has extremely low toxicity and shows no allergenic or carcinogenic properties.

However, it may not mix well with substances like:

• Alcohol
• Tranquilizers
• Sedatives

Picamilon Reddit Reviews

[su_quote cite=”TrippinDannyTanner” url=”https://www.reddit.com/r/Nootropics/comments/acuf8z/any_experiences_with_picamilon_for_nootropic/”]My favorite uses of pica are before running- or any exercise, but running in particular.[/su_quote]
[su_quote cite=”Apra” url=”https://www.reddit.com/r/Nootropics/comments/20w7pn/experiences_with_picamilon/”]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. [/su_quote]
[su_quote cite=”u/RutgerB” url=”https://www.reddit.com/r/Nootropics/comments/1yiohv/picamilon_for_social_anxiety/”]It’s working for me, removes anxiety at 350mg to 700 mg. Also seems to help creative thinking. Use it sparse thought! [/su_quote]

Wrapping Up

Do you have questions about, supplementing with Picamilon? Do you have experience supplementing with Picamilon? Please share your thoughts in the comments below.

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