Picamilon

non-nutrient/non-botanical

What is it

Picamilon (also spelled pikamilon or picamillion) is a synthetic compound formed by combining niacin (vitamin B3) and gamma-aminobutyric acid (GABA). Developed in the Soviet Union in the 1960s, it is a prescription medication in Russia for cerebrovascular conditions and anxiety; in the US, the FDA does not classify it as a legal dietary supplement ingredient.

How it works

Picamilon is designed to deliver GABA to the brain. Because GABA itself does not cross the blood-brain barrier well, attaching it to niacin allows the molecule to enter the central nervous system. Once across, picamilon is hydrolyzed to release free GABA, which activates GABA receptors and produces anxiolytic and sedative effects. The niacin portion contributes vasodilation, potentially increasing cerebral blood flow. In Russian clinical studies, picamilon has been used for anxiety, depression, migraine, asthenic states, and post-stroke recovery, with reports of improved cerebral circulation and reduced anxiety. Western clinical evidence by modern standards is limited.

Evidence for 3 uses

AI-assisted evidence assessment — talk to your doctor before relying on any single supplement.

Anxiety / mood (Russian clinical use)

Grade C

Moderate evidence

Russian clinical studies have reported anxiolytic effects and improvements in mood and asthenic symptoms, especially when combined with conventional therapies. Quality of trials by modern Western standards is limited.

Cerebral blood flow / cognitive effects

Grade C

Moderate evidence

The niacin component is reported to increase cerebral blood flow, and Russian studies have used picamilon for cerebrovascular conditions and post-stroke rehabilitation. Western clinical evidence is sparse.

Migraine prevention

Grade D

Mixed evidence

Some Russian studies have used picamilon for migraine prevention. Evidence is limited and outdated, and Western clinical trials are absent.

2 commercial forms

Picamilon (sodium salt)

Crosses blood-brain barrier; hydrolyzed to GABA + niacin in CNS

The standard form used in Russian clinical settings.

Picamilon HCl

Same general pharmacokinetics

Less common; used in some supplement formulations.

Dosage

In Russian clinical use, doses range from 20 to 50 mg up to three times daily, with higher doses (up to 150-300 mg per day) used for cerebrovascular conditions. There is no established dose for over-the-counter use, and the FDA does not recognize picamilon as a legal supplement ingredient in the United States.

When and how to take it

If used in jurisdictions where legal, taking earlier in the day may reduce sleep disruption. Effects typically develop within 1-3 hours. Avoid combining with alcohol or sedatives. Take with water; with food if stomach upset occurs.

Safety

Generally well tolerated in clinical use at recommended doses. Possible side effects include headache, dizziness, mild nausea, sleep disturbance, skin rash, and (rarely) niacin-related flushing. Long-term safety data outside of Russia are limited. Unlike phenibut, dependence and severe withdrawal are not as well documented but are possible with chronic high-dose use.

Who should be cautious

Avoid in pregnancy and breastfeeding. People with liver disease, kidney disease, bleeding disorders, or those taking blood pressure or sedative medications should avoid picamilon. In the US, the FDA has issued warnings against marketing picamilon as a dietary supplement; consumers should be aware it is not legally permitted in supplements there.

Interactions

Picamilon may interact with antihypertensive medications, anticoagulants (due to vasodilatory effects), CNS depressants (sedatives, alcohol), and other GABA-active substances. The niacin component may interact with cholesterol-lowering drugs. Avoid combining with other compounds affecting the central nervous system.

Frequently asked questions

Is picamilon legal in the US?⌄

No. The FDA has stated that picamilon does not qualify as a dietary supplement ingredient and has issued warnings to companies marketing it. Selling it as a supplement in the US is not permitted.

How is picamilon different from phenibut?⌄

Both are Russian-developed GABA derivatives. Phenibut acts primarily on GABA-B receptors with strong sedative and dependence potential; picamilon delivers GABA more directly and includes vasodilatory niacin, with a milder profile.

Will picamilon make me drowsy?⌄

It can have mild sedative effects, especially at higher doses, but is generally less sedating than phenibut or benzodiazepines.

Is picamilon addictive?⌄

Dependence is not as well documented as with phenibut, but long-term high-dose use of any GABAergic compound carries some risk. Use cautiously, if at all.

What are the alternatives for anxiety?⌄

Evidence-based options include cognitive-behavioral therapy, prescribed medications (SSRIs, SNRIs, buspirone), exercise, sleep hygiene, and stress management. Discuss with a clinician.

References

  • Picamilon (Wikidata) — Wikidata link
  • Picamilon (PubChem CID 60608) — PubChem link

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Disclaimer: These statements have not been evaluated by the FDA. This page is educational, not a substitute for personalized medical advice. Evidence grades are AI-assisted assessments — talk to your doctor before starting any new supplement, especially if you're pregnant, breastfeeding, on medications, or managing a chronic condition.