Picamilon (also known as nicotinoyl-GABA) is a synthetic substance—that is, it is created in a laboratory. It is found in some dietary supplement products advertised as a pre-workouts to improve alertness and provide extra focus, determination, and endurance. However, picamilon does not fit any of the categories of dietary ingredients under the Federal Food, Drug, and Cosmetic Act. In addition, the Food and Drug Administration (FDA) states, “any products marketed as dietary supplements that declare picamilon as a dietary ingredient are misbranded.”

Picamilon does not meet the definition of a dietary supplement ingredient.

It is prohibited for use by Military Service Members.

Picamilon is a prescription drug in Russia, where it is used to treat a variety of neurological conditions. It’s a synthetic substance made through the combination of niacin (a B vitamin) and gamma-amino butyric acid (GABA, a neurotransmitter that sends chemical messages through the brain and nervous system). Picamilon was developed to  enhance GABA activity in the brain. When taken orally, picamilon is able to cross the “blood-brain barrier,” which GABA alone cannot.

In the U.S., picamilon has never been approved as a drug to treat any condition, and in 2015 FDA announced that picamilon is not a dietary ingredient. Therefore, products containing this substance are misbranded and otherwise should be considered unapproved drugs. For more information, please see FDA’s information page on Picamilon in Dietary Supplements.

What does the science say?

Most of the research investigating the effects of picamilon as a drug are in Russian. There is insufficient evidence to show if picamilon is safe or effective for any claim you might find for a dietary supplement product. The latest research analyzing dietary supplement products that list picamilon as an ingredient shows that labels are not always accurate; some contain amounts of picamilon exceeding what is claimed on the label, and some even exceed the quantity used as a prescription drug in Russia.

How can I watch out for this prohibited ingredient?

Since picamilon is not a dietary ingredient, it is not lawful for a dietary supplement product to contain picamilon. However, such products are available in the marketplace. Military Service Members should watch out for such products because they are prohibited for use. Other names for picamilon to watch out for on labels are the following:

  • pikatropin
  • pikamilon
  • nicotinyl-gamma-aminobutyric acid
  • nicotinyl-GABA
  • 4-(pyridine-3-carbonylamino) butanoic acid

Bottom line

Picamilon is not a lawful dietary supplement ingredient. It is prohibited for Military Service Members to use dietary supplement products containing picamilon.

 

Published 14 September 2021

References

Avula, B., Chittiboyina, A. G., Sagi, S., Wang, Y. H., Wang, M., Khan, I. A., & Cohen, P. A. (2015). Identification and quantification of vinpocetine and picamilon in dietary supplements sold in the United States. Drug Testing and Analysis, 8(3-4), 334–343. doi:10.1002/dta.1853

Cohen, P. A., Avula, B., Wang, Y. H., Zakharevich, I., & Khan, I. (2021). Five unapproved drugs found in cognitive enhancement supplements. Neurology: Clinical Practice, 11(3), e303–e307. doi:10.1212/cpj.0000000000000960

Cui, W., Chen, X., Zhan, Y., Zhang, Z., Zhang, Y., & Zhong, D. (2010). Determination of picamilon concentration in human plasma by liquid chromatography–tandem mass spectrometry. Journal of Chromatography B, 878(15-16), 1181–1184. doi:10.1016/j.jchromb.2010.03.013

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Matsuyama, K., Yamashita, C., Noda, A., Goto, S., Noda, H., Ichimaru, Y., & Gomita, Y. (1984). Evaluation of isonicotinoyl-.GAMMA.-aminobutyric acid (GABA) and nicotinoyl-GABA as pro-drugs of GABA. Chemical and Pharmaceutical Bulletin, 32(10), 4089–4095. doi:10.1248/cpb.32.4089

Oketch-Rabah, H. A., Madden, E. F., Roe, A. L., & Betz, J. M. (2021). United States Pharmacopeia (USP) safety review of gamma-aminobutyric acid (GABA). Nutrients, 13(8), article 2742. doi:10.3390/nu13082742