Talk:Picamilon

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Fatal overdose may occur when GABAergic substances are combined with other depressants such as opiates, benzodiazepines, barbiturates, gabapentinoids, thienodiazepines or alcohol.

It is strongly discouraged to combine these substances, particularly in common to heavy doses.

Summary sheet: Picamilon

Picamilon
Chemical Nomenclature
Common names	Picamilon, Pycamilon, Pikamilon, Пикамилон, N-nicotinoyl-GABA
Substitutive name	N-nicotinoyl-γ-aminobutyric acid
Systematic name	4-(pyridine-3-carbonylamino)butanoic acid
Class Membership
Psychoactive class	Depressant \ Nootropic
Chemical class	GABA analogue
Routes of Administration
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section. ⇣ Oral Dosage Threshold 20 - 50 mg Light 50 - 90 mg Common 90 - 200 mg Strong 200 - 350 mg Heavy 350 mg + Duration Total 2 - 4 hours Onset 10 - 45 minutes After effects 1 - 12 hours DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

File:Picamilon.jpg

Picamilon 20 mg from Russia

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.

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.

Chemistry

Picamilon is a synthetic combination of GABA and niacin. Picamilon is similar to phenibut, except instead of having a phenyl ring in the β-position attached to get it across the blood brain barrier, picamilon has a niacin bound to an amine group.

Pharmacology

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 GABA_A and GABA_B) 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.

Subjective effects

In comparison to other used GABAergic depressants such as alcohol, benzodiazepines or phenibut, this compound can be described as more subtle and less intense. It is also less euphoric and recreational.

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.

It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.

Physical effects

• • Sedation & Stimulation - Picamilon is mildly stimulating at light to common dosages but can becomes sedating starting with strong doses at around 150 mg.
  • Vasodilation
  • Itchiness
  • Hyperthermia
  • Increased perspiration
  • Nausea
  • Headaches
  • Diarrhea
  • Stomach cramp
  • Decreased blood pressure
  • Dizziness
  • Increased heart rate

Visual effects

• • Acuity enhancement
  • Colour enhancement

Cognitive effects

• • 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 other GABAergic depressants.
  • Motivation enhancement
  • Focus enhancement
  • Memory enhancement
  • Thought acceleration
  • Dream potentiation
  • Irritability
  • Cognitive euphoria
  • Sleepiness
  • Thought deceleration

Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

• Erowid Experience Vaults: Picamilon

Toxicity and harm potential

This toxicity and harm potential section is a stub. As a result, it may contain incomplete or even dangerously wrong information! You can help by expanding upon or correcting it. Note: Always conduct independent research and use harm reduction practices if using this substance.

Picamilon has a low toxicity relative to dose. Intake of extremaly high dose of niacin (a metabolite 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.

Dangerous interactions

This dangerous interactions section is a stub. As such, it may contain incomplete or invalid information. You can help by expanding upon or correcting it.

Warning: Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).

Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.

• Depressants (1,4-Butanediol, 2M2B, alcohol, benzodiazepines, barbiturates, GHB/GBL, methaqualone, opioids) - This combination potentiates the muscle relaxation, amnesia, sedation, and respiratory depression caused by one another. At higher doses, it can lead to a sudden, unexpected loss of consciousness along with a dangerous amount of depressed respiration. There is also an increased risk of suffocating on one's vomit while unconscious. If nausea or vomiting occurs before a loss of consciousness, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Dissociatives - This combination can unpredictably potentiate the amnesia, sedation, motor control loss and delusions that can be caused by each other. It may also result in a sudden loss of consciousness accompanied by a dangerous degree of respiratory depression. If nausea or vomiting occurs before consciousness is lost, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Stimulants - Stimulants mask the sedative effect of depressants, which is the main factor most people use to gauge their level of intoxication. Once the stimulant effects wear off, the effects of the depressant will significantly increase, leading to intensified disinhibition, motor control loss, and dangerous black-out states. This combination can also potentially result in severe dehydration if one's fluid intake is not closely monitored. If choosing to combine these substances, one should strictly limit themselves to a pre-set schedule of dosing only a certain amount per hour until a maximum threshold has been reached.

Legal status

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.

See also

• Responsible use
• Depressant
• GABA
• Nootropic
• Phenibut

External links

• Picamilon (Wikipedia)