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|Summary sheet: Picamilon|
|Common names||Picamilon, Pycamilon, Pikamilon, Пикамилон, N-nicotinoyl-GABA|
|Substitutive name||N-nicotinoyl-γ-aminobutyric acid|
|Systematic name||4-(pyridine-3-carbonylamino)butanoic acid|
|Psychoactive class||Depressant \ Nootropic|
|Chemical class||GABA analogue|
|Routes of Administration|
N-nicotinoyl-GABA, also known as Picamilon (Russian: Пикамилон), is a synthetic compound made of GABA and niacin (vitamin B3) used in the treatment of anxiety disorders or as part of a nootropic stack.
GABA is a neurotransmitter with relaxing and anti-anxiety effects. Niacin is a vitamin involved in DNA repair, fat and cholesterol synthesis, and widening of blood vessels. When taken as an oral supplement by itself GABA is not able to cross the blood-brain barrier (only a small amount does). However, picamilon (GABA bound to niacin) is able to cross the blood-brain barrier.
Picamilon was developed in the Soviet Union in 1969 and further studied in both Russia and Japan as a prodrug of GABA.
- 1 History and culture
- 2 Chemistry
- 3 Pharmacology
- 4 Subjective effects
- 5 Toxicity and harm potential
- 6 Legal status
- 7 See also
- 8 External links
- 9 References
History and culture
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.
In October, 2015 the Oregon Attorney General filed a lawsuit against US supplement mega-retailer GNC for selling products containing picamilon, claiming that GNC was knowingly violating the law. GNC countered that it had received no direct notice from the FDA on the ban and only learned of the FDA’s ruling on picamilon after the suit was filed. GNC stopped selling products containing picamilon, but the publicity created by the lawsuit sent GNC’s stock prices plunging and stockholders filed a class action suit against the company.
A month after the Oregon lawsuit was filed, Montana Senator Claire McCaskill of the Senate Special Committee on Aging wrote directly to major retailers, asking them to voluntarily remove products containing picamilon. She said she did so because of the FDA’s failure to respond to her repeated requests to take action, and because the agency remained silent on whether products containing picamilon should be recalled or removed from sale.
Picamilon’s ability to cross the blood-brain barrier (BBB) is mostly due to the ability of niacin to widen blood vessels. Once picamilon enters the brain, the molecule is broken down by water into GABA and niacin.
Once in the brain, GABA activates GABA (both GABAA and GABAB) receptors potentially producing an relaxing and anti-anxiety effect, while niacin increases blood flow to the brain by dilating blood vessels. This additional blood flow to the brain is thought to provide the neuroprotective and nootropic benefits of picamilon. New blood coming into the brain brings fresh oxygen, enhances the delivery and absorption of glucose and other nutrients, which may increase alertness and overall brain energy.
Studies have shown 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.
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. These effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.
- Anxiety suppression - GABA is the brain’s primary inhibitory neurotransmitter, and greater levels of this molecule are associated with decreased levels of anxiety. This effect is weaker than that of gabapentinoids and benzodiazepines.
- Motivation enhancement
- Focus enhancement or Focus suppression - Lower doses of picamilon can enhance focus and concentration. This effect typically reverses as the dose is increased.
- Analysis enhancement
- Memory enhancement
- Thought acceleration
- Dream potentiation
- Cognitive euphoria
- Thought deceleration - Picamilon can only cause thought deceleration at a high dosage.
There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:
Toxicity and harm potential
This toxicity and harm potential section is a stub.
As such, it may contain incomplete or even dangerously wrong information. You can help by expanding or correcting it.
Picamilon has a low toxicity relative to dose. Intake of extremaly high dose of picamilon every day may lead to hepatotoxicity. Flushing of the face is the most common side effect. Flushing can result in burning, tingling, itching, and redness of the face, arms, and chest, as well as headaches. Picamilon potentially lethal when mixed with depressants like alcohol, benzodiazepines or opioids.
It is strongly recommended that one use harm reduction practices when using this substance.
Tolerance and addiction potential
The dependence potential for picamilon is unknown. There is currently no evidence to suggest that picamilon has addictive potential, but due to one of its mechanisms of actions (enhancing GABA signalling) it is still theoretically possible for picamilon to be somewhat addictive.
Tolerance will develop to the sedative-hypnotic effects within a couple of days of continuous use. After cessation, the tolerance returns to baseline in 7 - 14 days.
Picamilon produces cross-tolerance with all GABAgenic depressants, meaning that after its consumption, depressants will have a reduced effect.
- Depressants (1,4-Butanediol, 2M2B, alcohol, antihistamine, benzodiazepines, barbiturates, gabapentinoids, GHB/GBL, methaqualone, opioids) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
This legality section is a stub.
As such, it may contain incomplete or wrong information. You can help by expanding it.
- Russia: In Russia, picamilon is sold as a prescription drug.
- United States: Selling picamilon or any product containing it as a dietary supplement is a violation of the FDA’s ruling, which makes it very difficult to find for purchase. At the same time, it is not a scheduled or controlled substance in the US and it is not illegal to posess or use.
- Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
- Pikamilon pharmacokinetics in animals. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/1884802
- Senator McCaskill Frustrated by FDA Inaction, Calls on Retailers to Pull Picamilon Supplements | http://www.nutritionaloutlook.com/regulatory/senator-mccaskill-frustrated-fda-inaction-calls-retailers-pull-picamilon-supplements
- Behavioral effects of GABA agonists in relation to anxiety and benzodiazepine action. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/2884549
- The new cerebrovascular preparation pikamilon. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/2707413
- Correction by nicotinamide and nicotinoyl-GABA of dopamine metabolism in rat brain in experimental Parkinson's disease. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/12199067
- Efficacy of vision correcting system "focus" for prevention and treatment of dry form of age macular degeneration. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/22741296
- Pathogenetic treatment of central chorioretinal dystrophies with pikamilon. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/11510167?dopt=AbstractPlus
- Hepatotoxicity upon using niacin to pass a drug test: A case report. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/29941333
- Koski, A., Ojanperä, I., & Vuori, E. (2002). Alcohol and benzodiazepines in fatal poisonings. Alcoholism: Clinical and Experimental Research, 26(7), 956-959.