Picamilon (nicotinyl-y-aminobutyric acid, or N-nicotinoyl-GABA) is a combination of the inhibitory neurotransmitter GABA with nicotinic acid (Vitamin B3 or niacin). The addition of niacin allows GABA to cross the blood-brain barrier (BBB).
Neurohackers prefer either Picamilon or Phenibut when the goal is to raise GABA levels in the brain because GABA alone cannot cross the BBB. And note that taking GABA and niacin as a stack will not produce the same effect as Picamilon. GABA is bonded with niacin to produce Picamilon and it’s this molecule that does its magic in the brain.
Picamilon was developed in Russia in 1969 by the All-Union Research Institute. And it has been used since 1986 as a pharmaceutical in Russia to treat attention, memory, and learning problems, and for treatment of loss of brain blood circulation, brain trauma, chronic alcoholism and other disorders.
The company’s promotional material states, “The important property of Picamilon is the ability to quickly restore mental and physical fitness for work, which was lost through overstress”.
Once Picamilon crosses the blood-brain barrier it hydrolyzes into GABA and niacin. GABA activates GABA receptors producing an anxiolytic response. And niacin acts as a vasodilator relaxing constricted blood vessels and improving blood flow in the brain.
Picamilon helps:
- Balance mood. Picamilon has an inhibitory effect on overly stimulated neurons because it raises GABA levels in your brain. Low GABA levels lead to anxiety, depression and insomnia. GABA helps restore that balance. Promoting a more positive mood which improves focus and relaxation.[i]
- Cerebral Circulation. Picamilon is unique among GABA boosters because it can boost cerebral circulation as well.[ii] It increases cerebrovascular activity better than Piracetam and Vinpocetine. The nicotinic acid (niacin) in Picamilon boosts blood flow, enhances cell metabolism and oxygen supply in the brain. Resulting in an improvement in short-term and long-term memory.
- Neurotransmitters. Picamilon has been shown to normalize serotonin and dopamine content, and dopamine uptake in the brain. Dopamine aids in memory formation, attention, focus, and cognition.
Table of Contents
Overview
Picamilon (nicotinyl-y-aminobutyric acid, or N-nicotinoyl-GABA) is a derivative of the inhibitory neurotransmitter GABA and nicotinic acid (niacin or Vitamin B3).
Russian scientists conducted a lot of research into GABA and cognitive health in the 1960’s and 70’s. The nootropics community has benefited from this research. It was the Belgians who started the development of the racetam-family of nootropics. And not too long afterwards, Russian scientists continued the research on GABA-derived compounds and gave us Phenibut and Picamilon.
GABA’s role is to keep glutamate, the primary excitatory transmitter, from overwhelming your brain. Too much glutamate can cause a seizure, and too little GABA can put you in a coma. A healthy brain maintains a critical balance of GABA and glutamate.
GABA acts like a “brake” on neuron circuits during stress. Low GABA levels can result in anxiety, insomnia, poor mood and restlessness.
Clinical studies show that boosting GABA with a supplement like Picamilon relieves anxiety, stress, and boosts the production of alpha brain waves.[iii] If GABA is optimized in your brain you’ll feel focused, relaxed and stress-free.
But the big challenge for cognitive health is trying to boost GABA levels in the brain. GABA cannot cross the blood-brain barrier on its own. It needs help to carry it across this barrier.
Including Vitamin B3 (niacin) in the Picamilon formula helps GABA to cross the blood-brain barrier. And the reason why some neurohackers prefer Picamilon when the goal is to raise GABA levels in the brain.
Picamilon is unique among GABA boosters because it can boost cerebral circulation as well.[iv] It increases cerebrovascular activity better than Piracetam and Vinpocetine. It’s even better at boosting blood flow than prescription vasodilating agents like cinnarizine, papaverine, and xanthinol niacinate.
So when using Picamilon to boost GABA, you enhance cerebral circulation, and lower blood pressure. GABA even stimulates the pituitary gland to secrete Human Growth Hormone. And helps produce endorphins that make you feel good after a workout or sex.
As a nootropic, when you use Picamilon to normalize GABA levels you’ll improve blood flow to and within your brain. And you’ll experience a reduction in anxiety, insomnia, nervousness, restlessness and stress.
Picamilon exhibits the properties of a tranquilizer with a stimulating component. But unlike tranquilizer drugs, Picamilon does not induce muscle relaxation, drowsiness or lethargy.
How does Picamilon work in the Brain?
Picamilon helps brain health and function in several ways. But two in particular stand out.
- Picamilon boosts cognition. Picamilon is a derivative of GABA and niacin. And easily crosses the blood-brain barrier. GABA on its own cannot cross this barrier unless paired with a dedicated carrier.[v] When niacin is bonded to GABA the molecule easily enters the brain.
Once in the brain, Picamilon separates back into niacin and GABA. GABA works by preventing neural signaling associated with anxiety from reaching other neurons. It does this by attaching to the receptors that would otherwise excite those neurons. Over-stimulating neurons in certain areas of your brain is what causes anxiety-related symptoms.
Studies have shown this unique combination of niacin and GABA affect the regulation of neurotransmitters in the brain. Picamilon was shown in one study on Parkinson’s disease to normalize serotonin and dopamine content, and dopamine uptake in the brain.[vi]
- Picamilon improves cerebral blood flow. Picamilon is more effective than Piracetam and Vinpocetine in improving blood flow to cerebral vessels in the brain. It easily crosses the blood-brain barrier to protect neurons against the effects of diminished oxygen flow. Improving cognitive function.
Picamilon separates into niacin and GABA once it crosses the blood-brain barrier. Niacin acts as a vasodilator relaxing blood vessels and allowing the freer flow of blood in the brain.
Picamilon is often prescribed in Russia for treatment of migraine headaches. A study published in Nutrition Journal reviewed clinical trials from 1990 – 2004 looking at studies using niacin to treat migraines, and other tension-type headaches.
The conclusion from this review showed niacin’s effectiveness for its vasodilatory properties in increasing cerebral blood flow. And its ability to improve mitochondrial energy metabolism.[vii] The result is fewer migraines and less headaches when using a nootropic containing niacin.
How things go bad
Low levels of GABA and poor cerebral circulation are associated with a variety of health problems.
↑ Anxiety[viii], panic attacks, stress and insomnia
↑ Muscle spasms, hypertension, convulsion, Tourette’s Syndrome and epilepsy
↓ Neurotransmitters decline
↓ ATP energy levels decline starving mitochondria in brain cells
When your neurotransmitters, including GABA, are in balance, you feel motivated, productive and energetic. And you feel calm and relaxed during downtime.
When GABA levels are low you feel filled with dread, you’re constantly worried, you have racing thoughts, and you’re frequently late and disorganized.[ix]
Many people in this GABA-slump resort to high carbohydrate foods, and drugs or alcohol to relax.
Picamilon benefits
Picamilon is an analogue of GABA and nicotinic acid (Vitamin B3 or niacin). The addition of niacin allows GABA to cross the blood-brain barrier (BBB).
We need adequate GABA levels in our brain because it’s an inhibitory neurotransmitter. When we raise GABA levels by supplementing with Picamilon, we help keep glutamate in check.
Glutamate is your body’s most abundant excitatory neurotransmitter. Which is responsible for attention span, brain energy, learning ability, memory, and staying awake.
So GABA is calming and glutamate is stimulating. And they must be in balance with each other for optimal cognitive health.
An imbalance of these two neurotransmitters can cause fibromyalgia, chronic fatigue syndrome, poor memory and cognition, anxiety and depression.
But when these two neurotransmitters work together efficiently, you feel relaxed with no stress or feelings of anxiety. And you get a more restful night’s sleep.
The addition of nicotinic acid in the Picamilon formula helps improve cognition even more. One study with 96 healthy volunteers was done to determine the effects on memory with nicotinic acid. The study found that nicotinic acid (niacin) enhanced cell metabolism and oxygen supply in the brain. Resulting in an improvement in short-term and long-term memory.[x]
Adding Picamilon to your nootropic stack can help bring GABA and glutamate back into balance.
How does Picamilon feel?
When you balance GABA levels in your brain, you feel relaxed and calm. But many neurohackers who try using GABA as a supplement don’t feel the effects. Because the GABA molecule is too large to cross the blood-brain barrier.[xi]
Note: If you do feel the calming effects of supplementing with GABA within a ½ hour of taking it, it may mean you have a “leaky” blood-brain barrier. Not a good thing.[xii]
Because if GABA can get through, all kinds of nasty stuff can get through too. Including toxins, undigested food particles and anything else in your blood stream that shouldn’t be in your brain.
Learn how to fix a “leaky” blood-brain barrier here >How to Heal a Leaky Blood-Brain Barrier .
But here were talking about increasing our GABA levels using Picamilon. Neurohackers report that adding Picamilon to their stack relieves anxiety “better than Xanax”. There is less stress and they feel more relaxed.
Picamilon also offers a stimulant effect providing mental clarity, dreams can be vivid, and it’s not sedating like Phenibut.
Social functions could get some help with Picamilon. You could feel less inhibited, speak freely and feel more confident. Picamilon generates a calm focus without making you drowsy.
Some neurohackers maintain that the ‘magic’ with Picamilon is in the nicotinic acid. And I’d have to agree with this observation. It’s what provides the stimulant-effect and gives you an energized type of calmness.
The cognitive benefits of niacin are considerably understated in the nootropics community. Just check out the research and studies in my NADH article for more on the magic of niacin.
Picamilon Clinical Research
Nearly all the research with Picamilon has taken place in Russia. It’s published in Russian journals in Russian. Most of these trials are not indexed in international or US medical databases.
We won’t get into the politics of this type of behavior here on Nootropics Expert. We’re here to educate and collate information for you on nootropics to help cognitive health.
The sources we have been able to find shows Picamilon extensively studied in animals and humans. And has been shown to act like a tranquilizer without the sedative effects of muscle relaxation, drowsiness or lethargy.
The studies show Picamilon decreases anxiety, fear, irritability and symptoms of emotional stress. It inhibits aggression, and restores physical working capacity after stressful work.
Picamilon has been proven to prevent forgetfulness, enhance memory, recall and improve mood. It decreases headaches, dizziness and tinnitus. It increases mental and motor activity in patients with anxiety and depression.
Picamilon has been shown to prevent or suppress diabetic neuropathy[xiii], and alleviate the effects of alcohol withdrawal. It helps glaucoma, retinal and optic nerve damage[xiv]. And helps those with neurologically-based urinary problems.
Here we talk about how Picamilon, nicotinic acid and GABA can affect your cognition and overall health. This research supports the idea of using Picamilon to raise GABA and niacin levels. And the cognitive benefits can have a profound effect on your quality of life.
Picamilon increases dopamine uptake
Reports by neurohackers repeatedly show that Picamilon provides a ‘calm focus’ without making you drowsy. And this study, done in the Ukraine gives us a clue on how this works.
This study was done with Parkinson’s patients. It’s well know that serotonin and dopamine content and dopamine uptake by neurons in Parkinson’s Disease is decreased.
This research found that Picamilon normalized dopamine uptake in Parkinsonism. And that Picamilon is “involved in the regulation of brain neurotransmission under experimental parkinsonism and can be useful in treatment of Parkinson’s disease”.[xv]
Picamilon boosts brain cell mitochondria function
We know from our research on Nootropics Expert that NADH boosts ATP energy production within brain cell mitochondria. And this “energizing” effect that’s often spoken of when using Picamilon comes at least in part from its niacin component.
This study done on one-month old rats looked at trauma of the brain. The researchers studied oxidative damage done on brain mitochondria 1, 4, 7 days and 4 weeks after the trauma.
The young rats were given several different nootropics to see the effect on the rat’s mitochondria. And they concluded that Picamilon had a protective effect on the function of brain mitochondria during the trauma.[xvi]
Picamilon increases blood supply, oxygen saturation and blood circulation in the brain.[xvii] This boost in blood flow[xviii] brings the nutrients and oxygen needed to fuel ATP that power brain cell mitochondria.
Picamilon Recommended Dosage
The recommended daily starting dosage of Picamilon for anxiety is 50 mg 2 or 3 times per day. If you’re looking for a stimulatory effect you can safely increase your dose to 100 mg 2 or 3 times daily.
Picamilon Side Effects
Picamilon is considered safe when taken in normal recommended doses.
Picamilon has not been shown in clinical trials to produce any allergic or toxic effects. The only side effects noted were headache, dizziness and nausea. And nearly always when taken above recommended doses.
At higher doses Picamilon can lower blood pressure. So if you are already on blood lowering medication, or have an issue with low blood pressure, you should not use Picamilon.
Where to buy Picamilon
Picamilon as a nootropic supplement is available in powder, tablet and capsule form. I recommend Cosmic Nootropic – Picamilon tablets.
If you choose the buy bulk Picamilon powder from a vendor, make sure you ask for a genuine Certificate of Analysis to verify its authenticity.
Nootropics Expert Recommendation
Picamilon 50 – 100 mg 2 or 3 times per day.
I recommend using Picamilon as a nootropic supplement if you’re feeling anxiety or stress. And to calm or keep in check the stimulatory effects of some nootropics.
Your body does make GABA on its own from glutamate in your brain. Most healthy people have an adequate supply of GABA. But if you’re dealing with anxiety or stress and need some extra help in calming things down, Picamilon can help.
Picamilon is particularly helpful if you’re dealing with anxiety. Some neurohackers report that Picamilon is as effective in dealing with anxiety as many prescription anti-anxiety meds.
Picamilon exhibits the properties of a tranquilizer with a stimulating component. But unlike tranquilizer drugs, Picamilon does not induce muscle relaxation, drowsiness or lethargy.
In addition to its calming effects, Picamilon may help improve your memory, recall and concentration.
There is no reported added benefit to doses higher than those recommended. In fact, the reverse appears to be true. Lower recommended doses have more of a calming and cognitive effect for most people.
I recommend Cosmic Nootropic – Picamilon tablets.
[i] Lapin I. “Phenibut (beta-phenyl-GABA): a tranquilizer and nootropic drug.” CNS Drug Revues. 2001 Winter;7(4):471-81. (source)
[ii] Mirzoyan R.S., Gan’shina T.S., Kosoi M.Y., Aleksandrin V.V., Aleksandrov P.N. “Effect of picamilon on the cerebral cortical blood supply and microcirculation in the pial arteriolar system” Bulletin of Experimental Biology and Medicine May 1989, Volume 107, Issue 5, pp 668-670 (source)
[iii] Nemeroff C.B. “The role of GABA in the pathophysiology and treatment of anxiety disorders.” Psychopharmacology Bulletin. 2003;37(4):133-46. (source)
[iv] Mirzoyan R.S., Gan’shina T.S., Kosoi M.Y., Aleksandrin V.V., Aleksandrov P.N. “Effect of picamilon on the cerebral cortical blood supply and microcirculation in the pial arteriolar system” Bulletin of Experimental Biology and Medicine May 1989, Volume 107, Issue 5, pp 668-670 (source)
[v] Kuriyama K., Sze P.Y. “Blood-brain barrier to H3-γ-aminobutyric acid in normal and amino oxyacetic acid-treated animals”Neuropharmacology Volume 10, Issue 1, January 1971, Pages 103–108 (source)
[vi] Kuchmerovs’ka T.M., Donchenko H.V., Fomenko H.I., Chichkovs’ka H.V., Pakirbaieva L.V., Klymenko A.N. “[Correction by nicotinamide and nicotinoyl-GABA of dopamine metabolism in rat brain in experimental Parkinson’s disease].” in Ukrainian Ukr Biokhim Zh (1999). 2001 Nov-Dec;73(6):108-12. (source)
[vii] Prousky R., Seely D. “The treatment of migraines and tension-type headaches with intravenous and oral niacin (nicotinic acid): systematic review of the literature” Nutrition Journal 2005 (source)
[viii] Enna S.J. “Role of gamma-aminobutyric acid in anxiety.”Psychopathology. 1984;17 Suppl 1:15-24. (source)
[ix] Struzyńska L., Sulkowski G. “Relationships between glutamine, glutamate, and GABA in nerve endings under Pb-toxicity conditions.”Journal of Inorganic Biochemistry. 2004 Jun;98(6):951-8. (source)
[x] Loriaux S.M., Deijen J.B., Orlebeke J.F., De Swart J.H. “The effects of nicotinic acid and xanthinol nicotinate on human memory in different categories of age. A double blind study.” Psychopharmacology (Berl). 1985;87(4):390-5. (source)
[xi] Kuriyama K., Sze P.Y. “Blood-brain barrier to H3-γ-aminobutyric acid in normal and amino oxyacetic acid-treated animals”Neuropharmacology Volume 10, Issue 1, January 1971, Pages 103–108 (source)
[xii] Montagne A., et. Al. “Blood-brain barrier breakdown in the aging human hippocampus.” Neuron 2015 Jan 21;85(2):296-302 (source)
[xiii] Kuchmerovskaia T.M., Parkhomets P.K., Donchenko G.V., Obrosova I.G., Klimenko A.P., Kuchmerovskiĭ N.A., Pakirbaeva L.V., Efimov A.S. in Russian “[Correction of diabetic neuropathies using aldose reductase inhibitors and pikamilon].” Vopr Med Khim. 1998 Nov-Dec;44(6):559-64. (source)
[xiv] Basinskiĭ S.N., Krasnogorskaia V.N., Lenis Iu.A. in Russian “[Pathogenetic treatment of central chorioretinal dystrophies with pikamilon].” Vestn Oftalmol. 2001 Mar-Apr;117(2):42-4. (source)
[xv] Kuchmerovs’ka T.M., Donchenko H.V., Fomenko H.I., Chichkovs’ka H.V., Pakirbaieva L.V., Klymenko A.N. in Ukrainian “[Correction by nicotinamide and nicotinoyl-GABA of dopamine metabolism in rat brain in experimental Parkinson’s disease].” Ukr Biokhim Zh (1999). 2001 Nov-Dec;73(6):108-12. (source)
[xvi] Novikov V.E., Kovaleva L.A. in Russian “[The effect of nootropic agents on brain mitochondrial function in the dynamics of craniocerebral trauma from the age aspect].” Eksp Klin Farmakol. 1998 Mar-Apr;61(2):65-8. (source)
[xvii] Sapegin I.D., Beketov A.I. in Russian “[The effect of pikamilon and fenibut on the blood supply of the brain at rest and under gravitational exposures].” Eksp Klin Farmakol. 1993 Jan-Feb;56(1):28-31. (source)
[xviii] Mirzoian R.S., Gan’shina T.S. in Russian “[The new cerebrovascular preparation pikamilon].” Farmakol Toksikol. 1989 Jan-Feb;52(1):23-6. (source)
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Hello David,
I wanted to ask you if, from your point of view, it is necessary to pay attention to tolerance development with Picamilon. And if so, what kind of cycling you suggest.
In my experience, a decrease in effect is not unusual with drugs that act in the GABA range.
Thank you very much!
Max
Max, I’m not a big fan of cycling. But if you have experienced tolerance with similar ingredients the only way to figure out a cycling program is by experimenting. It could be every second day. Or it could be 5 days on and 2 days off and variations on that theme.
Hello David, I get pretty serious withdrawal symptoms from phenibut. Should I expect a similar withdrawal or any withdrawal symptoms at all when discontinuing picamilon?
Shaymus, some experience withdrawal when stopping Picamilon. But many do not. It all depends on your system and how it responds to the use of the this supplement.
Can you update the where to buy section? The source is no longer available. It seems that science.bio deleted the product… I can’t seem to find a good vendor for this supplement anywhere… 🙁
Wayne, thanks for the reminder and I’ll update that info because science.bio went out of business a while back likely because of pressure from the FDA. None of my trusted suppliers carry Picamilon any more. So the only thing you can now do is a search for “where to buy Picamilon” and see who turns up. Then I highly recommend doing a search for reviews on that vendor before placing an order. Another place you can check is reddit.
I’ve purchased from here a few months ago.
Nutritional Health Supplements – Australia – Picamilon
t/y David for all you do.
Thanks Don. Note anyone seeing this comment, this company is in Australia and may not ship to your country. They suggest you begin filling out the shopping cart and you’ll see a drop down menu. If your country is on the list that means they can ship to you.
“Intellimeds [net]” has a good selection of the common but also exotic nootropics.
They ship worldwide. So maybe worth a visit
Thanks for the tip Zach.
I’m not sure if it’s been pointed out, but right under
How does Picamilon work in the Brain?
you typed Phenibut. No biggie, I realize it’s typo; those P words! Thanks!
Thank you Judy.
Hi David..hope you are ok! I found that the combo Picamilon and l-arginine makes the trick for me when I try to relax at night.
Is there something that I should be aware with this stack ? Thanks in advance.
George, as long as it works for you and does not cause any problems keep on using it if it helps.
Hello again David. Can picamilon be taken sublingually?
Henry, some use it sublingually. Try it and see if it works for you.