Picamilon for Anxiety.

Picamilon is a synthetic compound made of GABA and vitamin B3 (niacin). It crosses the blood-brain barrier more easily than GABA alone, and has been claimed to potentially improve cognitive function and reduce anxiety. But what does the science actually say, and how much do we really know about this compound? Read on to learn more about picamilon, how it might work, and what we know about its efficacy and safety.

What Do We Know About 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.

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.

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.

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.

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) is believed to be able to cross the blood-brain barrier, which reportedly allows this particular formulation to affect the brain more readily and directly.

Picamilon’s reported ability to more readily cross the blood-brain barrier (BBB) is believed to be mostly due to the ability of niacin to widen blood vessels. Once picamilon enters the brain, the combined molecule is then broken down into its simpler components, GABA and niacin.

Once in the brain, GABA activates GABA receptors (both GABAA and GABAB types), while niacin may increase blood flow throughout the brain (by dilating blood vessels). By bringing fresh oxygen and other essential nutrients that nourish brain cells, this additional blood flow to the brain is believed to account for at least some of the purported neuroprotective and “nootropic” (“cognitive-enhancing”) benefits of picamilon – although more research will be needed to fully confirm this, as very little hard evidence regarding its effectiveness in human users is currently available.

How Picamilon Affects Anxiety & Depression?

GABA is the brain’s primary inhibitory neurotransmitter, and greater levels of this molecule have been generally associated with decreased levels of anxiety. 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.

When released, GABA reduces the firing rate of neurons by blocking the activity of glutamate, the brain’s primary excitatory neurotransmitter. Too much glutamate can contribute to feelings of anxiety, muscular tension, and even increased the risk of seizures. One of the (many) functions of GABA is to counteract these effects, which may account for its reported “anti-anxiety” or “calming” effects.

People with relatively lower levels of GABA have been reported to have a relatively higher likelihood of developing anxiety disorders, which has led some researchers to suggest that increasing GABA could offer a potentially effective approach for treating anxiety.

However, actual hard data on this use in humans is so far lacking, and what little evidence there is comes only from animal studies.

For example, according to one animal study, picamilon was reported to reduce anxiety- and depression-related behaviors in rats – supposedly by activating GABA receptors.

In other animal studies, picamilon was reported to suppress aggressive responses to startling stimuli and slowed down the animals’ orientation to such stimuli. This may suggest a diminished anxiety response, although this evidence is very indirect, and would need to be confirmed by a lot more studies

Picamilon for Beginners

Picamilon is a derivative of GABA with the addition of a Niacin or Vitamin B3 molecule. It was invented as a way to increase GABA levels in the brain since simply giving a GABA supplement to someone will not actually result in the active ingredient reaching your brain.

The presence of Niacin means that more of Picamilon gets to your cerebrum where it can hydrolyze into GABA and interact with anxiety-causing pathways.

This nootropic is not a cure for anxiety, but it can inhibit its onset and lessen symptoms. The Picamilon experience is typically described as a relaxed, feel-good state of mind without the drowsiness that is caused by many anxiety medications.

It has been used for several different medical conditions such as migraines, asthenia, depression, dementia, ADHD and other forms of cognitive impairment. In some countries, Picamilon is prescribed to treat anxiousness, phobias, mood disorders, and social anxiety.

However, in the USA and Canada it is not regulated as a prescription drug and is legal to buy in supplement form. You can purchase it over the counter in either pill or powder format with the bulk Picamilon powder costing as little as $0.20 per dosage.

It is frequently combined in a “nootropic stack” with other anxiety-eliminators like Aniracetam, Noopept, Sulbutiamine, Adrafinil, and Choline.

Does Picamilon Really Work for Anxiety?

Picamilon by itself is an inactive compound until it reaches your brain where it is converted into the neurotransmitter GABA and the vitamin Niacin. Both of these substances can offer benefits for temporary relief from anxiety.

GABA is the major inhibitory neurotransmitter in the Central Nervous System, use to counterbalance the effects of excitatory transmitters like glutamate and noradrenaline.

GABA is frequently released as part of a negative feedback loop when certain neurons detect an excessive rate of stimulation (one of the signs of anxiety).

Picamilon has a fairly straightforward anxiolytic mechanism of action, by activating GABA receptors so that your neurons are less likely to become over-excited. The result is a feeling of calm and what many say is a “positive buzz”.

What makes Picamilon different from Phenibut and many other anti-anxiety drugs is that it does not lead to the characteristic feelings of sedation, lethargy or muscle incoordination. Picamilon supplements can actually have a positive effect on mental energy levels, leading to greater vigilance and acuity.

Users who take this nootropic say that it gives them better focus, improves memory performance and can make it easier to study, read or write for extended periods of time. This is attributable to the presence of Niacin in the Picamilon formula.

Niacin is a cerebrovasodilator which increases blood, oxygen and glucose circulation to the brain. In addition to having benefits for brain health, Niacin is a moderate cognitive enhancer that can contribute to higher fluid intelligence as well as productivity.