Picamilon

7.2

Anxiolytic

6.6 /10

Memory

6.0 /10

Learning

9.0 /10

Picamilon

Anxiety Support
Cognitive
Post Workout
Relaxation
Sleep Quality
Weight Loss
Nootropics
Mood Support

Description

Summary

Picamilon (nicotinyl-y-aminobutyric acid) was first synthesized in the Soviet Union during the Cold War, and has been widely used by prescription in Russia since the 1970’s for a variety of complaints.[1,2] A combination of the nutrients Niacin and GABA(Gamma-aminobutyric_acid), Picamilon is able to cross the blood-brain barrier, esentially carrying the neurotransmitter GABA into the central nervous system for use. Certain substances are poorly absorbed by themselves, and Picamilon essentially facilitates the absorption of GABA for use by the human body. After crossing the blood-brain barrier, Picamilon hydrolyzes (chemically splits) into two substances. The first substance is Niacin, a B-vitamin that the body uses for digestion of carbohydrates, and healthy functioning of skin, nervous system and eyes. The other metabolite formed from the breakdown of Picamilon is GABA(Gamma-aminobutyric_acid). GABA is an important amino acid that serves to transmit inhibitory impulses to the CNS. GABA levels may be influential on mood, memory, and pain.[5] One commonly used family of supplements that mimic the actions on the body similar to inhibitory amino acids, such as GABA, are benzodiazepines.

Picamilon is a combination of the neurotransmitter GABA and niacin, which is better known as vitamin B3. GABA naturally reduces anxiety by promoting relaxation while niacin assists with DNA repair and cholesterol synthesis. Additionally, niacin helps facilitate the opening of constricted blood vessels.

Developed decades ago in the Soviet Union, picamilon has been prescribed in Eastern Europe for treatment of anxiety disorders since the 1980s. [1] The US FDA, however, has not approved picamilon as neither a prescription treatment nor a dietary supplement. [2] Recent research suggests that picamilon has nootropic properties in addition to its anti-anxiety benefits.

Benefits and Effects of Picamilon

Based on clinical research, potential uses for picamilon supplements include:

Reducing Anxiety and Depression

Picamilon lowers anxiety by providing the brain with extra GABA. GABA works by slowing communication between neurons, which restricts glutamate activity. Glutamate, the brain’s primary excitatory neurotransmitter, is largely responsible for feelings of anxiety and muscular tension, so slowing down the rate at which neurons fire can help alleviate such symptoms. [3] Because anxiety and depression are closely linked, picamilon is also believed to be an effective antidepressant. [4]

Improving Vision

Studies suggest that picamilon can be used to treat retinal disorders. Three months of picamilon treatment improved the vision of patients who suffer from macular degeneration. [5] Likewise, picamilon supplementation has helped patients with central chorioretinal dystrophy better distinguish certain shapes and colors in addition to improving peripheral vision and reducing the severity of glaucoma. [6]

Enhancing Memory

Rats given picamilon demonstrated improvements in short and long term memory. Additionally, picamilon prevented memory loss following electroshock treatments. [7]

Protecting the Brain

Picamilon may help prevent excitotoxicity, or the death of neurons, due to overuse. In a study of rats with brain trauma, picamilon increased mitochondrial functioning in brain cells. [8] Picamilon also protects brain and immune cells from membrane damage and oxidative stress resulting from sleep deprivation. [9]

Promoting Blood Flow to the Brain

According to a study that compared the effects of different nootropic drugs, picamilon was more effective than piracetam and vinpocetine at increasing blood flow to the brain. [10] For this reason, picamilon is prescribed in Russia as a treatment for migraine headaches.

Treating Parkinson’s Disease

Picamilon stabilized serotonin and dopamine levels in rats with Parkinson’s disease. Since Parkinson’s symptoms are caused by deficiencies in these neurotransmitters, picamilon could help control the illness. [11]

Preventing Inflammation of Nerves

In a study of diabetic rats, picamilon successfully reduced neuropathy, or nerve inflammation. [12]

Benefits of Picamilon

Picamilon can be used as nutritional support by individuals who wish to improve mood and energy levels. It is not a muscle relaxant or a tranquilizer.[5] There has been recent evidence to link low levels of GABA with depression in people who have a normal level of Seratonin, which is one of the neurotransmitters typically linked to depression.[7] Picamilon has also been shown to increase concentration and focus for many individuals[8]

Suggested Use of Picamilon

As a nutritional supplement, recommended adult dose is initially 50-100mg daily, increasing if needed to a maximum dose of 200mg in the morning and 100mg in the mid-afternoon.[8] Kava and Valerian may potentiate, or increase, the effects of Picamilon. A 2010 study showed that inhaling the scent of jasmine may positively effect users of this dietary supplement.[6]

Bioavailability, Mixing and Solubility of Picamilon

This product is a white crystalline powder that is odorless, that takes up moisture readily, and is soluble in water or juice.[1]

How Picamilon Works

Oral GABA supplements alone are inefficient at crossing the blood-brain barrier. Binding GABA to niacin eliminates this problem since niacin dilates blood vessels. Therefore, picamilon works by activating GABA receptors and increasing blood flow to the brain. [13] This process facilitates more efficient delivery of oxygen and nutrients throughout the body, thus enhancing focus, alertness and motivation. GABA is primarily responsible for picamilon’s sedative properties.

Since picamilon stimulates the mind while relaxing the body, many users find it helpful for studying or performing other cognitively demanding tasks. Based on picamilon reviews online, some users even take picamilon for ADHD management. Because it improves blood flow and oxygen consumption, taking picamilon pre-workout could help you get the most of your exercise. On the other hand, some people take picamilon for sleep. The optimal picamilon dosage for sleep is less than 100 mg; higher doses are likely to cause sleep disturbances.

Picamilon vs Phenibut

Picamilon works similarly to another nootropic called phenibut, which is permitted for sale as a supplement in the US. Therefore, phenibut is a popular alternative in places where picamilon is banned. However, based on anecdotal evidence, phenibut may have higher potential for abuse due to its high potency and rough withdrawal symptoms. Picamilon is considered to be safe for daily consumption whereas phenibut is not.

Dosage

While picamilon is often sold as a stand-alone supplement, it can also be found in dozens of nootropic blends. As a cognitive enhancer, picamilon user reviews indicate an optimal daily amount of 100-200 mg split between two or three doses. In picamilon studies, daily amounts of 50-400 mg have proven effective for various conditions; consult cited research for more information about using the drug for specific purposes.

Picamilon is typically sold in powdered form, which you may see marketed as picamilon sodium salt. Picamilon capsules are also available. You can even find picamilon sublingual lozenges that dissolve under your tongue, but picamilon tastes pretty bland by itself. Fortunately, picamilon powder is water soluble, so it mixes well with most beverages including juices and smoothies.

You should start feeling the effects of picamilon within an hour. Wait at least 4-6 hours between doses to give picamilon time to work. Taking picamilon on an empty stomach can help prevent nausea. Some users like to cycle picamilon to avoid gaining a dependency, but picamilon toxicity studies suggest that moderate daily usage doesn’t appear to have any long term adverse effects. That said, picamilon is very potent, so you should start with the smallest suggested amount. Once you find the minimum effective dosage, don’t increase your intake.

Side Effects

People around the world have been taking picamilon as anxiety treatment for several decades, so its safety is well documented. In some individuals, picamilon may cause mild side effects like dizziness and nausea. [14] Niacin supplements can sometimes cause flushing of the skin, which is harmless. Allergic reactions and skin rashes have been reported in rare instances. In high doses, picamilon can cause drastic drops in blood pressure, which can be dangerous for users with hypotension. [15]

Avoid taking picamilon with other drugs that affect the GABA receptors like alcohol, barbiturates and benzodiazepines. Mixing picamilon and alcohol is particularly dangerous because it can exacerbate the negative effects of both substances. You should also avoid aspirin and uricosuric agents when taking niacin supplements. Picamilon bulk powder sometimes contains additives, so check your picamilon ingredients to make sure you’re not allergic to any of them.

Despite picamilon’s low toxicity, the US FDA sent letters to five retailers in 2015 indicating that the drug doesn’t meet the legal definition of a dietary supplement, so it may not be marketed as such. However, there is no law prohibiting individual possession or consumption of picamilon in the US, so it’s relatively easy to buy picamilon online no matter where you live.

Stacks

Combing picamilon with racetams should accentuate picamilon’s nootropic properties. Picamilon, aniracetam and a choline supplement like Alpha GPC is a popular stack for lifting mood. Picamilon pairs particularly well with drugs like modafinil, adderall and caffeine since it can negate the anxiety and agitation that often results from using stimulants. Taking picamilon and theanine together may also boost picamilon’s cognitive benefits.

Combining picamilon with other relaxants can enhance its calming effects. For example, picamilon and tianeptine are a good combination for anxiety relief. On the other hand, taking picamilon with kava purportedly produces an energizing effect.

 

Sources

Sources

 

[1] Norton W. Milgram, Heather Callahan and Christina Siwak, 1999. Adrafinil: A Novel Vigilance Promoting Agent.

 

[2] Christina T. Swiak, Heather Callahan and Norton W. Milgram, 2000. Adrafinil: Effects on Behaviour and Cognition in Aged Canines.

 

[3] https://en.wikipedia.org/wiki/Adrafinil

 

[4] http://enacademic.com/dic.nsf/enwiki/616907

 

[5] http://www.chemeurope.com/en/encyclopedia/Adrafinil.html

 

[6] Mosstafa Kazemi, Sami Sajjadifar, Abdelkarim Aydi, Mohammad Mirzaei Heydari, 2018. Biological and Pharmaceutical Organosulfur Molecules.

 

[7] https://pubchem.ncbi.nlm.nih.gov/compound/adrafinil#section=Pharmacology-and-Biochemistry

 

[8] https://www.lookchem.com/Adrafinil/

 

[9] R. Nageswara Rao, Dhananjay D. Shinde, M.V.N. Kumar Talluri, Sachin B. Agawane, 2008. LC-ESI-MS determination and pharmacokinetics of adrafinil in rats.

 

[10] Norton W. Milgram, Christina T. Swiak, Philippe Gruet, Patricia Atkinson, Frederique Woehrle and Heather Callahan, 2000. Oral Administration of Adrafinil Improves Discrimination Learning in Aged Beagle Dogs.

 

[11] Dongsoo Kim, 2012. Practical Use and Risk of Modafinil, A Novel Waking drug.

 

[12] MV Solbrig, GF Koob and WI Lipkin, 1999. Orofacial dyskinesias and dystonia in rats infected with Borna disease virus; a model for tardive dyskinetic syndromes.

 

[13] Ronald M. Kobayashi, 1976. Orofacial Dyskinesia. Clinical Features, Mechanisms and Drug Therapy.

 

[14] Stephane Thobois, Jing Xie, Helena Mollion, Isabelle Benatru and Emmanuel Broussolle, 2004. Adrafinil-Induced Orofacial Dyskinesia.

 

[15] Michael G. Tramontana, Ronald L. Cowan, David Zald, Jonathan W. Prokop, and Oscar Guillamondegui, 2014. Traumatic brain injury-related attention deficits: Treatment outcomes with lisdexamfetamine dimesylate (Vyvanse).

 

[16] David W. Goodman, 2010. Lisdexamfetamine Dimesylate (Vyvanse), A Prodrug Stimulant for Attention-Deficit/Hyperactivity Disorder.

 

[17] https://en.wikipedia.org/wiki/Prodrug

 

[18] Helene Bastuji and Michel Jouvet, 1988. Successful Treatment of Idiopathic Hypersomnia and Narcolepsy with Modafinil.

 

[19] Antonio Osorio-Lozada, Thomas Prisinzano and Horacio F. Olivo, 2004. Synthesis and determination of the absolute stereochemistry of the enantiomers of adrafinil and modafinil.

 

[20] https://www.drugsand.me/en/modafinil/

 

[21] Dubey S, Ahi S, Beotra A, Reddy IM, Kaur T, Jain S, 2008. A novel study of mass spectrometric fragmentation of adrafinil, modafinil and their metabolite modafilinic acid under ESI-LC-MS/MS and EI-GC-MS.

 

[22] https://psychonautwiki.org/wiki/Adrafinil

 

[23] Geraldine Dowling, Pierce V. Kavanagh, Brian Talbot, John O’Brien, Gary Hessman, Gavin McLaughlin, Brendan Twamley, and Simon D. Brandt, 2016. Outsmarted by nootropics? An investigation into the thermal degradation of modafinil, modafinic acid, adrafinil, CRL-40,940 and CRL-40,941 in the GC injector: formation of 1,1,2,2-tetraphenylethane and its tetra fluoro analog. Drug Testing and Analysis.

 

[24] K. Deventer, K. Roels, F.T Delbeke, P. Van Eenoo, 2011. Prevelance of legal and illegal stimulating agents in sports.

 

[25] Solveiga Grinberga, Liga Zvejniece, Edgars Liepinsh, Maija Dambrova and Osvalds Pugovics, 2008. Quantitative analysis of phenibut in rat brain tissue extracts by liquid chromatography-tandem mass spectrometry.

 

[26] Seth Sankary, Peter Canino, Jennifer Jackson, 2016. Phenibut Overdose. American Journal of Emergency Medicine.

 

[27] V.V. Bagmetova, A.N. Krivitskaya, and I.N. Tyurenkov, 2015. Effects of Phenibut and Citrocard on Non-Competitive and Competitive Behaviour during Provoked Aggression in Animals. Bulletin of Experimental Biology and Medicine.

 

[28] Izyaslav lapin, 2001. Phenibut (beta-Phenyl-GABA): A Tranquilizer and Nootropic Drug.

 

[29] Carl L Hansen, Scott H. Burton, Christophe Giraud-Carrier, Josh H. West, Michael D. Barnes, and Bret Hansen, 2013. Tweaking and Tweeting: Exploring Twitter for Nonmedical Use of a Psychostimulant Drug (Adderall) Among College Students.

 

[30] Rohini R. Vanga, Bikram Bal, and Kevin W. Olden, 2013. Adderall Induced Acute Liver Injury: A Rare Case and Review of the Literature.

Also known as:Pikamilon, Pycamilon, Nicotinoyl-GABA
Type:Anxiolytic
Good for: , , , , , , ,
Stacks well with: Adrafinil
Typical dose:100 - 200mg
Half Life :3 - 6 Hours
Picamilon

Picamilon

Anxiety Support
Cognitive
Post Workout
Relaxation
Sleep Quality
Weight Loss
Nootropics
Mood Support