Anxiety is something that everyone is familiar with. We all experience moments of worry and stress.
A little anxiety, from time to time, is perfectly normal. But when daily anxiety prevents us from living life the way we want to, that’s when it becomes a problem.
Anxiety disorders affect 18.1% of the adult population every year.1 And of those people with anxiety disorders, 22.8% of them are classified as having severe anxiety.
While there are a number of different prescription drugs available to treat anxiety, more and more people are looking for non-prescription ways to combat anxiety. Prescription drugs often have serious side effects, can be highly addictive, and lose their effectiveness over time.
One of the non-prescription drugs that people are using to fight anxiety is called picamilon. It’s an interesting drug with a long history and a great safety record. Using picamilon for anxiety and other benefits is common among people that use nootropics.
What Is Picamilon?
Picamilon (aka N-nicotinoyl-GABA, picamilone, pikamilon, & pycamilon) is modified version of gamma-aminobutyric acid (GABA). It was first developed in Russia in the late 1960’s.2
GABA is a neurotransmitter. Neurotransmitters are the chemical messengers that allow our nervous systems to send messages from one neuron to another.3 GABA is the chief inhibitory neurotransmitter in humans. It is known to play an important role in anxiety, stress, relaxation, sleep, and many other functions. Drugs that modulate GABA receptors generally have calming, anti-anxiety, and anti-convulsant effects.4
GABA is sold as a dietary supplement. While some users report that it supports feelings of relaxation, there is no scientific evidence to back up that claim. That’s because GABA, when taken by itself, does not readily cross the blood-brain barrier.5
In the 1960’s and 70’s, Russian scientists experimented with GABA molecules.6 They modified GABA in a number of different ways, trying to increase its ability to cross the blood-brain barrier (BBB). And they were successful, creating a number of different drugs that were able to cross the BBB. One of these drugs (as you may have guessed) was picamilon. Another one that you may have heard of is phenibut.
Russian scientists created picamilon by chemically attaching niacin (vitamin B3) and GABA. They found that, unlike GABA by itself, picamilon was able to cross the blood-brain barrier.7
Once in the brain, picamilon is hydrolyzed into GABA and niacin. The niacin acts as a vasodilator, increasing blood flow in the brain.8 And the GABA binds to GABA receptors, reducing anxiety and having a general calming effect.9
Picamilon was sold as a dietary supplement in the United States. However, the Food and Drug Administration (FDA) ruled in 2015 that picamilon does not fit into any of the categories outlined in the Dietary Supplement Health and Education Act of 1994.10 This puts it in a legal grey-area, where it is perfectly legal to purchase and possess, but it is not legal to sell as a dietary supplement. Because of this, most nootropic sellers have stopped carrying picamilon.
In Russia, where picamilon has undergone the most research, it is only available with a prescription. It is used to treat a number of conditions, including anxiety, depression, headaches, and insomnia.
Benefits of Picamilon
Picamilon has been shown to have a number of benefits. Many of these benefits are supported by scientific research. Others have only been reported anecdotally, and require further research.
Using picamilon for anxiety is the most common reason that people use this interesting supplement. By increasing GABA in the brain, picamilon is able to decrease anxiety and create a sense of relaxed focus.9
Picamilon is also reported to have some nootropic benefits. Some users have reported an improvement in memory, learning, and focus. While more research needs to be done in this area, preliminary data is encouraging. One study done on rats, for example, showed that picamilon helped them to learn to navigate a maze 80% faster.11
Another benefit of picamilon is that it acts as a vasodilator.12 Vasodilators are drugs that widen blood vessels and improve circulation. Due at least partially to this effect, picamilon may be helpful for the treatment of migraine headaches.13 It may also be useful as a treatment for benign prostatic hyperplasia (enlarged prostate)14, diabetic neuropathy15, and Parkinson’s Disease.16
Here is a list of some picamilon benefits that users report:
- Decreased Anxiety
- Improved Mood
- Increased Memory
- Improved Learning
- Overall Cognitive Enhancement
- Treats Migraine Headaches
- Creates a Feeling of “Relaxed Focus”
- Improved Sleep
Picamilon Side Effects
When taken at the recommended dosage, picamilon has been shown to be very safe and with few side effects.
Side effects are rare but may include sedation, tiredness, headache, hypotension (low blood pressure), dizziness, and nausea. If you experience any of these side effects, they should go away on their own shortly after you stop taking picamilon.
Use with caution if you are taking other medications that cause drowsiness. Taking picamilon with certain drugs for anxiety and insomnia may lead to over-sedation.
And, as always, we recommend you consult a licensed healthcare provider before starting or stopping any new drug, supplement, herb, diet, or exercise routine. Just be aware that most American physicians have never heard of picamilon. You may need to educate your doctor about the benefits and risks of this interesting drug.
Most users don’t notice any effects at the low end of that range. The dosages that we’ve seen used the most is either 200 or 300 mg, taken 2-3 times a day.
Picamilon can be taken with or without food. However, it probably works better and faster when taken on an empty stomach.
As you can see, picamilon is an interesting drug that has been around for almost 50 years. It has a number of benefits, include anxiety reduction, increased learning and memory, and overall cognitive improvement.
Unfortunately, it can be hard to find. The FDA ruled in 2015 that it can no longer be sold as a dietary supplement in the United States. This doesn’t mean that people in the US can’t still legally order it from other countries, though. It wasn’t banned because it’s dangerous, but because sellers were making health claims about it without the proper scientific evidence to back them up.10
Picamilon is still widely used as a prescription medication in Russia and is available as a dietary supplement in other parts of the world. And although it may be hard to find in the United States now, using picamilon for anxiety is still common in other parts of the world.
1Kessler, R., Chiu, W., Demler, O., & Walters, E. (2005). Prevalence, severity, and comorbidity of twelve-month DSM-IV disorders in the National Comorbidity Survey Replication (NCS-R). Archives of General Psychiatry, 62(6):617-27.
2Kopelevich, V., & Gunar, V. (1999). Some approaches to the directed search for new drugs based on nicotinic acid. Pharmaceutical Chemistry Journal, 33(4):177-187.
3Lodish, H., Berk, A., & Zipursky, S. (2000). Neurotransmitters, synapses, and impulse transmission (Ed.). Molecular cell biology. (Section 21.4). New York: W.H. Freeman.
4Foster, A., & Kemp. J. (2006). Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol, 6(1):7-17.
5Kuriyama, K., & Sze, P. (1971). Blood-brain barrier to H3-y-aminobutyric acid in normal and amino oxyacetic acid-treated animals. Neuropharmacology, 10(1):103-8.
6Mirzoian, R., & Gan-shina, T. (1989). The new cerebrovascular preparation pikamilon. Farmakologiia I Toksikologiia, 52(1):23-6.
7Dorofeev, B., & Kholodov, L. (1991). Pikamilon pharmacokinetics in animals. Farmakologiia I Toksikologiia, 54(2):66-9.
8Gille, A., Bodor, E., Ahmed, K., & Offermanns, S. (2008). Nicotinic acid: pharmacological effects and mechanisms of action. Annual Review of Pharmacology and Toxicology, 48:79-106.
9Shephard, R. (1987). Behavioral effects of GABA agonists in relation to anxiety and benzodiazepine action. Life Sciences, 40(25):2429-36.
10Daniells, S. (2015). FDA sends five warning letters over supplements containing picamilon. Retrieved on March 13, 2016 from http://www.nutraingredients-usa.com/Regulation/FDA-sends-five-warning-letters-over-supplements-containing-picamilon
11Voznesenskii, A., Kovalev, G., & Sazhin, V. (1989). Comparative study of the effect of picamilone and piracetam on learning in rats in a radial maze. Farmakol Toksikol, 52(4):14-7.
12Sapegin, I. & Beketov, A. (1993). The effect of pikamilon and fenibut on the blood supply of the brain at rest and under gravitational exposures. Eksp Klin Farmakol, 56(1):28-31.
13Prousky, J. & Seely, D. (2005). The treatment of migraines and tension-type headaches with intravenous and oral niacin (nicotinic acid): systematic review of the literature. Nutrition Journal, 4:3.
14Tolstova, S. (1999). Pikamilone treatment of benign prostatic hyperplasia. Urologiia, 5:6-7.
15Shymans’kyi, I., Kuchmerov’ska, T., Donchenko, H., Valykyi, M., Klymenko, A., Palyvoda, O., & Kuchmerovs’kyi, M. (2002). Oxidative stress correction by nicotinamide and nicotynol-GABA in diabetic neuropathy. Ukr Biokhim Zh, 74(5):89-95.
16Kuchmerovs’ka, T., Donchenko, H., Fomenko, H., Chichkovs’ka, H., Pakirbaieva, L., & Klymenko, A. (1999). Correction by nicotinamide and nicotinoyl-GABA of dopamine metabolism in rat brain in experimental Parkinson’s disease. Ukr Biokhim Zh, 73(6):108-12.