What Is Picamilon?

Picamilon is a unique and controversial drug. Initially developed in the Soviet Union for the treatment of neurological disorders, it was sold legally in the US until 2015, when the USFDA banned it as a dietary ingredient and ruled that all products containing it be removed.‍[1]

The FDA ruling and its repercussions sparked a major controversy that has triggered accusations against the FDA,‍[2] spawned a pair of lawsuits,‍[3]‍[4] and sunk the legality of picamilon into a confusing gray area.

Picamilon, which is still sold by prescription in Russia, is created by synthesizing niacin (vitamin B3) and the inhibitory neurotransmitter GABA. Picamilon crosses the blood-brain barrier and then separates into its separate components; the GABA is believed to reduce anxiety by stimulating the brain’s GABA receptors, while the niacin acts as a vasodilator, improving blood flow and circulation in the brain.

In October, 2015 the Oregon Attorney General filed a lawsuit against US supplement mega-retailer GNC for selling products containing picamilon, claiming that GNC was knowingly violating the law. GNC countered that it had received no direct notice from the FDA on the ban and only learned of the FDA’s ruling on picamilon after the suit was filed. GNC stopped selling products containing picamilon, but the publicity created by the lawsuit sent GNC’s stock prices plunging and stockholders filed a class action suit against the company.

A month after the Oregon lawsuit was filed, Montana Senator Claire McCaskill of the Senate Special Committee on Aging wrote directly to major retailers, asking them to voluntarily remove products containing picamilon. She said she did so because of the FDA’s failure to respond to her repeated requests to take action, and because the agency remained silent on whether products containing picamilon should be recalled or removed from sale.‍[5]

In December, 2016 the Department of Justice announced that GNC Holdings Inc. agreed to pay $2.25 million and take steps to ensure the legality of its products, but upheld GNC’s claim that it did not sell banned substances knowingly.‍[6] The shareholders’ lawsuit was dismissed in 2017.‍[7]

In the meantime, the legality of picamilon is questionable and confusing. Selling picamilon or any product containing it as a dietary supplement is a violation of the FDA’s ruling, which makes it very difficult to find for purchase. At the same time, it is not a scheduled or controlled substance in the US and it is not illegal to posess or use.

Benefits and Effects of Picamilon

Picamilon has not been extensively tested, and much of the research that has been done is documented in Russian. But the studies and trials that exist suggest that it offers a variety of cognitive and mood-enhancing benefits.

Learning and Memory Enhancement

Picamilon has been shown to make learning faster and easier and to improve both long-term and short-term memory.

In animal studies a single dose elevated subjects to 80% level of learning and subjects achieved maximal level of learning within 3–5 trials. In these tests picamilon far outperformed piracetam, which had no significant effect on either short or long term memory.‍[8]‍[9]

Better Concentration, Alertness, and Mental Stamina

Picamilon has been shown to have significant positive effects on a wide array of cognitive functions, including increasing the ability to focus thought and enhancing overall mental energy or stamina.‍[10] This effect is believed to be due at least in part to picamilon’s ability to stimulate better flow and circulation of blood in the brain.

Anti-Anxiety and Mood Stabilization

Picamilon is most well known for its anti-anxiety and stress reducing effects, which are thought to be due in large part to the GABA it delivers to the brain.

GABA is the body’s most important inhibitory neurotransmitter and increasing levels of GABA is known to have calming, relaxing effects.

In animal studies, injections of picamilon normalized behavorial effects of anxiety and depression and effectively increased the number of active GABA-A receptors.‍[11]

Many users report that picamilon has a welcome anxiolytic effect, but some note that it is subtle rather than powerful. ‍[12]

How It Works

Picamilon is a combination of two common but essential nutrients, niacin and GABA or gamma-aminobutyric acid. Supplemental GABA cannot cross the blood-brain barrier on its own, but the niacin component of picamilon crosses the blood-brain barrier easily, taking the bonded GABA component with it.

The actual mechanism of action through which picamilon works is both rapid and direct. It is a water-soluble compound that is absorbed readily and reaches maximum bioavailability within an hour of ingestion.

After crossing the blood-brain barrier picamilon is hydrolyzed, or chemically split back into separate components.

The niacin component acts as a vasodilator, increasing blood flow within the brain and improving the absorption of oxygen and other nutrients.

At the same time, the GABA component increases brain levels of this important inhibitory neurotransmitter, which acts as a calmative and anxiolytic by reducing neuronal excitability.‍[13]

Research suggests that picamilon’s cognitive enhancement effects can be attributed in large part to increased brain blood circulation and oxygen absorption.‍[14] Improved blood flow in the brain also enhances the delivery and absorption of glucose and other nutrients, which may increase alertness and overall brain energy.

Picamilon is also believed to have an antioxidant effect,‍[15] helping break down and remove toxins in the brain.

Dosage

The product information sheet provided with Russian-manufactured picamilon provides the following dosage recommendations:‍[16]

  • For anxiety: 40–80 mg daily for 4 to 6 weeks.
  • For depression: 40–200 mg daily for up to three months.
  • For treatment of cerebrovascular diseases: 60-150 mg daily, taken over an initial treatment course of 1–2 months and followed up with a second course 5 to 6 months later.
  • For athletes: 60–80 mg daily for two weeks of the training period.

Stacking

Picamilon is effective in many modes: it can be taken alone on a daily basis, cycled with other supplements, or combined with other nootropics.

In a stack with racetam-class nootropics such as piracetam or pramiracetam, picamilon’s cognitive enhancement properties will be potentiated. However, depending on which racetam supplement you combine with picamilon, you could also experience heightened energy or relaxation effects, or even both. In combination with ampakine racetam supplements such as aniracetam and oxiracetam, both of which have stimulant properties, picamilon’s energy-boosting and mood-modulating effects will be enhanced.

Some users say combining picamilon with other supplements such as kava can increase its energy producing properties while using it in combination with relaxant supplements like valerian will make its calming properties stronger.

Side Effects

Picamilon is typically considered to be safe and well-tolerated, but reported side effects include nausea, headache, dizziness, irritability, agitation, anxiety, and allergic reactions such as rash and itching.‍[17]

Where to Buy

Picamilon is no longer available for sale in the United States due to recent regulatory changes with the FDA.

For an alternative substance that has a similar effect as picamilon, have a look at phenibut.

Closing Thoughts

For many years picamilon enjoyed increasing popularity as a useful anxiolytic with nootropic potential, but the picture has changed.

It has never been approved as a drug in the US or Canada and the FDA’s 2015 ruling that it doesn’t qualify as a dietary ingredient means it can’t be sold as a supplement, so picamilon is effectively no longer readily available in North America.

If you’re looking for a nootropic with similar effects, our best advice is to consider an alternative like phenibut.

References   [ + ]

Planning to start a new supplementation regimen? See our medical disclaimer.

This page was last updated on April 8, 2019.