The Health Benefits of Picamilon

This Russian "brain booster" is functionally banned in the US

Close-up of a young man taking nutritional supplement pills

Letizia Le Fur / Getty Images 

Picamilon, also known as nicotinoyl-gamma-aminobutyric acid, is a synthetic drug that combines niacin (vitamin B3) with gamma-aminobutyric acid (a neurotransmitter with anti-anxiety effects). Picamilon was discovered in Russia in the 1960s and continues to be sold in the country as a prescription drug, where it is believed to treat mood disorders, improve memory, and prevent dementia.

Picamilon is not approved as a prescription drug in the United States. Moreover, in 2015, the U.S. Food and Drug Administration (FDA) ruled that picamilon cannot be sold as a dietary supplement because it does not fit the definition ascribed by the federal regulator. Subsequently, the FDA ordered five companies to remove it from their products.

Despite the functional ban, there are manufacturers in the United States who claim to use picamilon in many of their multi-ingredient supplements.

Also Known As

  • Pikatropin
  • Pikamilon
  • Nicotinyl-GABA

Health Benefits

Picamilon is considered a nootropic drug, an ill-defined group of drugs and supplements used in alternative medicine to enhance brain function.

On the surface, the rationale behind picamilon's use seems sound enough. Among its many functions, niacin is involved in vasodilation (the widening of blood vessels). For its part, gamma-aminobutyric acid (GABA) is able to stimulate brain receptors but is largely unable to cross the blood-brain barrier that divides the brain from the rest of the body. By combining the two, picamilon is believed to transport GABA more effectively to the brain and, in doing so, treat such conditions as:

In addition, picamilon is thought to sharpen memory, enhance athletic performance, and protect against Alzheimer's disease.

Despite the list of purported benefits, the evidence supporting the claims is fundamentally weak.

A 2010 review of study from Duke University concluded that, while picamilon is able to activate brain receptors in the test tube, it is unable to be broken down in the body by an enzyme known as amidase. The process, known as amidase hydrolysis, is needed to break the niacin and GABA molecules apart. Without it, niacin and GABA will remain attached and unable to bind to—much less activate—GABA receptors in the brain.

At present, there is little evidence that picamilon can treat any medical condition.

Possible Side Effects

Given that niacin and GABA are both well-tolerated and essential to human function, it would seem reasonable to assume that picamilon is safe. However, little is known about the long-term safety of picamilon use, particularly at higher doses.

Side effects are relatively mild and may include headache, dizziness, nausea, and flushing due to an associated drop in blood pressure. People being treated for hypertension (high blood pressure) should avoid picamilon as it may trigger acute hypotension (low blood pressure).

Other drug interactions include:

Due to the lack of research, picamilon should not be used during pregnancy or breastfeeding. Its safety in children has also not been established.

Dosage and Preparation

There are no guidelines to the appropriate use of picamilon. Moreover, picamilon is not approved for use as either a prescription drug, an over-the-counter drug, or a dietary supplement in the United States.

What to Look For

If you do a casual search of Google using the keyword "picamilon," you will find dozens of nootropic remedies promising to treat everything from sleep difficulties to stress. Many of these do not contain picamilon but include other forms of GABA derived from lactic acid bacteria. (It can only be assumed that "picamilon" was used for the purpose of search engine optimization to attract customers.)

However, there are a handful of formulations that claim to contain picamilon. Clearly, there is no way to check the authenticity of the claims. Furthermore, manufacturers who use picamilon in their products are subject to legal action by the FDA.

Common Questions

Why was picamilon banned by the FDA?

Roughly translated, the Federal Food, Drug, and Cosmetic Act (FFDCA) defines "dietary supplement" as a vitamin, mineral, herb, amino acid, or extract that is used to increase the dietary intake of a naturally occurring substance in the body. This includes metabolites (compounds that are broken down into their bioactive elements as part of normal metabolism).

Because picamilon is a chemical synthesized in the lab with a unique mechanism of action, the FDA decided that it did not meet the FFDCA definition. Until such time as the manufacturer submits the product to human clinical trials, picamilon is unlikely to ever be approved.

Interestingly, picamilon and a drug called vinpocetine were both under investigation by the FDA at more or less the same time. At the time, both were sold as prescription drugs in Russia but available as dietary supplements in the United States.

Because vinpocetine was derived from lesser periwinkle (Vinca minor) plant, the FDA eventually allowed it to be classified as a dietary supplement. As a drug synthesized in the lab, picamilon was not.

Detractors argued that the FDA ruling was arbitrary given that vinpocetine is not found in the Vinca minor plant (or anywhere else in nature) but is entirely man-made. Supporters of the ruling believe that the FDA should have gone one step further and banned vinpocetine as well.

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Article Sources

  1. Kopelevich VM, Gunar VI. Some approaches to the directed search for new drugs based on nicotinic acidPharma Chem J. 1999 Apri;33(4):177-87. doi:10.1007/BF02509934

  2. U.S. Food and Drug Administration. Picamilon in Dietary Supplements. Silver Spring, Marylands; November 30, 2015.

  3. Mirzoian RS, Gan'shina TS. The new cerebrovascular preparation pikamilon. Farmakol Toksikol. 1989 Jan-Feb;52(1):23-6.

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