Disclaimer: This post is not a recommendation or endorsement for the use of picamilon. The FDA has not approved this compound for any specific medical or other use, and the available research on it is still in a very early stage. We have written this post for informational purposes only, and our goal is solely to inform people about what science currently says about picamilon’s potential effects, mechanisms, and side-effects.

What is Picamilon?

Picamilon (nicotinoyl-gamma-aminobutyric acid) is a synthetic combination of GABA and niacin (vitamin B3) that has been used by some in the past for the treatment of anxiety disorders, among other potential applications [R].

GABA is one of the major inhibitory neurotransmitters in the brain. Although its range of mechanisms and functions are complex, it has been generally associated with relaxing and anti-anxiety effects when its levels are increased [R, R].

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

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].

Picamilon 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 not enough is known about its effects or its safety, and subsequently ordered five different supplement companies to remove it from their products. However, there are still some companies based in the United States that sell it illegally. Additionally, a review of the available consumer versions of picamilon reported that the dosages can vary wildly from product to product – ranging from as little as 2.7 mg all the way up to over 700mg – and users cannot always be sure exactly what these supplements contain, which raises many major questions related to consumer safety [R].

Mechanism of Action

When taken as an oral supplement by itself, GABA is generally not able to cross the blood-brain barrier (only a small amount does). However, picamilon (i.e. a compound formulation in which GABA is bound to niacin)

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