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Picamilon is a synthetic compound made of GABA and vitamin B3 (niacin). It crosses the blood-brain barrier much more easily than GABA alone. It is reported to improve cognitive function and reduce anxiety. Read on to learn about the potential uses and side effects of picamilon.

Introduction

Picamilon (N-nicotinoyl-GABA) is a synthetic combination of GABA and niacin (vitamin B3) used in the treatment of anxiety disorders [R].

GABA is a neurotransmitter with relaxing and anti-anxiety effects.

Niacin is a vitamin involved in DNA repair, fat and cholesterol synthesis, and widening of blood vessels.

When taken as an oral supplement by itself GABA is not able to cross the blood-brain barrier (only a small amount does). However, picamilon (GABA bound to niacin) is able to cross the blood-brain barrier [R, R, R].

Picamilon was first developed in the Soviet Union in the late 1960s and has been sold as a prescription drug for anxiety in Russia since the 1980s [R, R].

It is not approved as a prescription drug in the United States. In 2015, the FDA ruled that picamilon can’t be sold as a dietary supplement because it does not fit the definition of one and subsequently ordered five companies to remove it from their products. However, there are still some companies based in the United States that sell it [R].

Mechanisms of Action

Picamilon’s ability to cross the blood-brain barrier is mostly due to the ability of niacin to widen blood vessels. Once picamilon enters the brain, the molecule is broken down by water into GABA and niacin [R].

Once in the brain, GABA activates GABA (both GABAA and GABAB) receptors, while niacin increases blood flow to the brain by dilating blood vessels. This additional blood flow to the brain provides many of the neuroprotective and nootropic benefits of picamilon. New blood coming into the brain brings fresh oxygen and other essential nutrients that nourish brain cells [R].

Uses of Picamilon

1) Picamilon May Decrease Anxiety and Depression

GABA is the brain’s primary inhibitory neurotransmitters, and greater levels of this molecule are associated with decreased levels of anxiety [R].

When released, GABA slows the firing rate of neurons. Too much glutamate can contribute to feelings of anxiety, muscular tension, and even increased the risk of seizures. GABA slows neuronal firing rates by blocking the activity of glutamate, the brain’s primary excitatory neurotransmitter [R].

GABA’s main role in the brain is to slow down excitatory communication between neurons.Too little GABA can cause restless thinking, anxiety, and insomnia. Increasing GABA in the brain alleviates all of these symptoms [R, R].

People with excessively low levels of GABA tend to develop anxiety disorders, suggesting that increasing GABA could provide an effective treatment for anxiety [R].

Picamilon reversed both anxiety and depression and activated GABA receptors in rats [R].

In animal studies, picamilon blunts aggressive responses to startling stimuli and slows orientation to such stimuli. This indicates a diminished anxiety response [R].

2) Picamilon Improves Vision

The macula is the center of the retina of the eye, where vision is sharpest. In a study of 60 patients with macular degeneration, three months of picamilon supplementation improved visual acuity [R].

Central chorioretinal dystrophy is a hereditary retinal disorder that results in progressive visual loss. In a study of 48 patients with central chorioretinal dystrophy, picamilon improved the ability to distinguish shapes and colors (contrast sensitivity), increased peripheral vision, and reduced glaucoma severity [R].

3) Picamilon May Improve Memory

Picamilon improved both short- and long-term memory as well as navigation ability in rats. It also prevented electroshock-induced memory impairment [R].

4) Picamilon May Protect the Brain

Picamilon protects neurons from being overactivated to the point of death (excitotoxicity). It has also been shown to increase mitochondrial function in the brain cells of rats who have sustained brain trauma [R].

Picamilon protected the brain and immune cells of sleep-deprived rats by preventing cell membrane damage and oxidative stress [R].

5) Picamilon Increases Blood Flow to the Brain

In one study, picamilon increased blood flow in the brain more than both piracetam and vinpocetine, two nootropics that are known for their ability to increase blood flow to the brain [R].

Picamilon is often prescribed in Russia to treat migraine headaches and is thought to be effective for this condition due to its ability to open constricted blood vessels in the brain [R].

6) Picamilon May Help with Parkinson’s Disease

Picamilon brought serotonin and dopamine up to near normal levels and increased the uptake of dopamine in the brain in a rat model of Parkinson’s disease [R].

7) Picamilon Protects Against Nerve Inflammation (Neuropathy)

Picamilon reduced inflammation of the nerves (neuropathy) in diabetic rats [R].

Side Effects of Picamilon

Picamilon is safe and has relatively low toxicity. Side effects include [R, R]:

At high doses, picamilon can lower blood pressure, which may be unsafe for those with already low blood pressure [R].

Limitations and Caveats

Many of picamilon’s benefits have yet to be investigated outside of animal studies and human trials are lacking.

Though the current research shows positive results, caution is still advised when using picamilon.

Drug Interactions

Any drug that modulates the GABA receptors has the potential to alter the effects of picamilon. These include:

  • Alcohol
  • Barbiturates
  • Benzodiazepines
  • Nonbenzodiazepines (or Z-drugs) like Ambien

Drug interactions for niacin include [R]:

  • High-dose aspirin
  • Uricosuric agents
  • Alcohol

Dosage

The dosage used in clinical trials ranges from 10 to 300 mg once daily. Users report greater efficacy when taken away from food to maximize absorption.

User Reviews

One user reported increased “mental clarity” and “energy without the need for stimulants like nicotine and coffee.” They also reported that their mild depression disappeared, vivid dreams, being sick less often, and increased motivation.

Another user will social anxiety said that after taking one 150 mg pill, they feel “extremely sociable and calm.” They also reported that “random people will strike up conversations with me in elevators when I normally would appear closed off.”

“Is there any crash after taking these? I don’t really notice one. Usually, a cup of coffee will calm my nerves for a while then crash 5 hours later. I don’t seem to notice any additional crash when taking picamilon alongside the coffee.”

One user reported picamilon making them “sleepy and kind of lifeless” from a 200 mg dose. They noted “after about 30 minutes I’ve got the feeling like when you down two or three beers you sit down on the sofa to watch tv and a few minutes later eyelids get heavy and you just want to sleep, literally this kind of feeling. I can’t imagine how it suppose to give you cognitive boost let alone energy.” They stated they would not purchase it again.

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8 COMMENTS

  • Charlie

    I tried Picamilon in earnest several years ago at dosages up to 500 mg but it had no perceptible effect. (I really wanted it to work so I kept raising my doses.) However, on a educated guess, I suggested to my wife to try it for her severe Restless Legs Syndrome, and she reports that it’s effective roughly 75% of the time. I dissolve 250 mg Picamilon in 1 ml of distilled water in a small syringe and she holds it SL for about 30 seconds before swallowing.
    Note that I’ve also tried Phenibut, another GABA supplement with some similarities to Picamilon, but it also had no perceptible effect, at doses up to 4 grams.
    I subscribed to Self-Decode today so maybe I’ll discover some clues to my odd GABA chemistry lurking in the SNPs.

  • Jimmy Surface

    IAS, international anti ageing systems, is a reputable company. I have purchased many products from them since the late 1990’s with not one complaint! They are located in England but ship to the US.

  • Clément

    Is there any risk of developing tolerance to it?
    Would it cause downregulation of GABA production and/or receptors and cause withdrawal?

    Thanks

    1. Will Hunter

      Hi Clément,

      It does not appear to cause tolerance with short-term use (under 30 days). While there isn’t any research on long-term tolerance, there is a risk of tolerance due to constant activation of the GABA receptors. This study in rats showed that picamilon did not cause downregulation of GABA receptors: http://europepmc.org/abstract/med/20821973 . The niacin in picamilon wouldn’t cause tolerance as it is a water-soluble B vitamin and your body will excrete what it does not use.

  • LEE TURNER

    As much as I want to try picamilon, where can I buy it? Can’t find it anywhere on-line. And if you do find a seller, how do you know that its not talcum powder? I use phenibut, and its a lifesaver for someone suffering from insomnia. I would like to cycle with picamilon… so where can I buy picamilon?
    Thanks!

    1. Will Hunter

      Hi Lee,

      We can’t recommend a source as we have not verified any of the current suppliers’ products. A preliminary search reveals a couple international sellers: https://thoughtfoods.com and http://rupharma.com/picamilon/. Please note that we are not affiliated with these companies in any way and can’t vouch for their quality or efficacy.

  • Lisa Kay

    Is this correct? “Too much GABA can contribute to feelings of anxiety, muscular tension, and even increased the risk of seizures” – I thought it was the opposite. did you mean to say too much Glutamate…?

    1. Will Hunter

      Hi Lisa,

      Thank you for pointing out this error. I have corrected it to say glutamate.

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