Evidence-based·Last reviewed May 31, 2026·How we grade evidence

Picamilon

PhytochemicalGABA derivativeBest in the morningBest taken with food

Picamilon is a Soviet-era prescription drug (a niacin-GABA conjugate) developed for cerebrovascular and anxiety disorders. The FDA ruled in 2015 that it is NOT a legal dietary ingredient in the United States — major retailers removed it from sale. Modern, rigorous human RCTs are essentially absent; the original Russian clinical literature is small, open-label, and decades old. Treat any picamilon-containing 'supplement' you find as a regulatory red flag rather than a credible product.

Research compound — not an approved drug or dietary supplement

This compound is sold for research and is not FDA-approved for human use or as a dietary supplement. Human evidence is limited; purity and dosing of consumer products are unverified. The data below is an evidence review for education only — talk to a clinician before considering it.

Quick decision guide

May help most

Nobody, as a US dietary supplement — the FDA has explicitly said it doesn't qualify. In Russia and a few other markets it is a prescription medicine for cerebrovascular insufficiency, dosed under medical supervision.

Common dosing range

Russian prescribing references list 60–200 mg/day for cerebrovascular conditions and 40–80 mg/day for anxiety. Not a US supplement dose recommendation — it is not a legal supplement here.

When to expect effects

Not reliably established in modern controlled trials.

Watch out for

FDA classifies picamilon as an unapproved drug, not a dietary ingredient. Products containing it are considered adulterated. Quality and dose of consumer products are unverified.

Evidence snapshot

Cerebrovascular / cognitive (Russian prescribing)Low

Anxiety (older open-label Russian data)Low

Modern RCT replicationLow

US regulatory statusNot a legal supplement

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.

Is it worth it for you?

Use this as a quick fit check, not a diagnosis.

Worth considering if…

You're a researcher or clinician evaluating the Russian pharmacology literature with appropriate context

Probably skip if…

You're shopping for an over-the-counter US 'nootropic' — the FDA has ruled picamilon is not a legal dietary ingredient

You're hoping for rigorous modern RCT support — the human data is sparse, small, and largely Russian-language open-label work

You'd be combining it with prescription GABAergic drugs (benzodiazepines, gabapentinoids, alcohol) — additive sedation/respiratory-depression risk hasn't been studied

You're pregnant, breastfeeding, on antihypertensives, or have liver impairment — no safety data and FDA flag stands

You see picamilon listed in a multi-ingredient 'cognitive enhancer' — the product itself is a regulatory and quality red flag

Evidence at a glance

Goal	Effect	Best fit	Time
Cerebrovascular insufficiency (Russian prescription use) Mixed Evidence	Russian dossier reports modest improvements in cerebrovascular reactivity and cognitive scores; no Western RCT replication; effect size unquantified in modern terms	None as a US OTC product. In Russian prescribing it is used in post-stroke recovery and chronic cerebrovascular disease under physician supervision	Russian prescribing typically uses 1–2 month courses
Anxiety (Russian prescription use) Mixed Evidence	Anecdotal/open-label improvement in anxiety scales in Russian use; not replicated in modern RCT	None as a US OTC product	Russian use typically 2–4 weeks before judging
Cognitive enhancement / 'nootropic' use Weak Evidence	No reliable human cognitive-performance benefit in controlled trials	None	Not established

Cerebrovascular insufficiency (Russian prescription use)

Mixed Evidence

Effect: Russian dossier reports modest improvements in cerebrovascular reactivity and cognitive scores; no Western RCT replication; effect size unquantified in modern terms
Best fit: None as a US OTC product. In Russian prescribing it is used in post-stroke recovery and chronic cerebrovascular disease under physician supervision
Time: Russian prescribing typically uses 1–2 month courses

Anxiety (Russian prescription use)

Mixed Evidence

Effect: Anecdotal/open-label improvement in anxiety scales in Russian use; not replicated in modern RCT
Best fit: None as a US OTC product
Time: Russian use typically 2–4 weeks before judging

Cognitive enhancement / 'nootropic' use

Weak Evidence

Effect: No reliable human cognitive-performance benefit in controlled trials
Best fit: None
Time: Not established

Evidence for 3 uses

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

Cerebrovascular insufficiency (Russian prescription use)

Disease adjunct

Mixed Evidence

Picamilon was developed at the USSR All-Union Vitamin Research Institute in the late 1960s and approved as a prescription cerebrovascular agent. The proposed mechanism is that the niacin moiety crosses the blood-brain barrier carrying GABA, which is then released in the CNS while niacin produces local vasodilation. Russian-language clinical literature reports improvements in cerebral blood flow and cognitive parameters in stroke recovery, vascular dementia, and chronic cerebral ischaemia — but trials are small, mostly open-label or with weak controls, and have not been independently replicated in Western RCTs.

Effect size

Russian dossier reports modest improvements in cerebrovascular reactivity and cognitive scores; no Western RCT replication; effect size unquantified in modern terms

Time to effect

Russian prescribing typically uses 1–2 month courses

Best fit

None as a US OTC product. In Russian prescribing it is used in post-stroke recovery and chronic cerebrovascular disease under physician supervision

Less likely

Healthy adults seeking 'cognitive enhancement' — there is no rigorous modern evidence supporting that use, and it isn't a legal US supplement

Bottom line: Mechanistically interesting, regulatorily off-limits in the US, clinically under-tested by modern standards.

SourceCohen et al., 2015 (JAMA Intern Med) — PubMed — JAMA Internal Medicine Cohen et al., 2016 (Drug Test Anal) — PubMed — Drug Testing and Analysis

Anxiety (Russian prescription use)

Disease adjunct

Mixed Evidence

Older Russian trials and clinical experience claim an anxiolytic effect at 40–80 mg/day, attributed to centrally released GABA. Modern Western anxiety treatment relies on SSRIs/SNRIs (first-line), short-term benzodiazepines, or non-medication approaches — all with dramatically stronger evidence. No published placebo-controlled RCT meeting modern standards supports picamilon for generalised anxiety disorder.

Effect size

Anecdotal/open-label improvement in anxiety scales in Russian use; not replicated in modern RCT

Time to effect

Russian use typically 2–4 weeks before judging

Best fit

None as a US OTC product

Less likely

Adults with diagnosable anxiety disorder seeking first-line evidence-based care

Bottom line: Better to discuss SSRIs, CBT, or short-term benzodiazepines with a clinician than self-treat with a banned ingredient.

SourceCohen et al., 2015 (JAMA Intern Med) — PubMed — JAMA Internal Medicine

Cognitive enhancement / 'nootropic' use

Mechanism only

Weak Evidence

Marketed in US 'nootropic stacks' before the 2015 FDA action; no controlled trial in healthy adults supports a meaningful cognitive enhancement effect. The mechanism (centrally released GABA + niacin vasodilation) would predict sedation as much as 'clarity', and user reports are inconsistent. This category is the main reason picamilon ended up in adulterated US supplements.

Effect size

No reliable human cognitive-performance benefit in controlled trials

Time to effect

Not established

Best fit

None

Less likely

Anyone hoping for a cognitive boost — the regulatory and evidence base both argue against it

Bottom line: Skip. Caffeine + L-theanine has better evidence and no regulatory cloud.

SourceCohen et al., 2016 (Drug Test Anal) — PubMed — Drug Testing and Analysis

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.

How to take it

1. Typical dose

There is no US supplement dosing recommendation because picamilon is not a legal US dietary ingredient. For reference only, Russian prescribing references list 60–200 mg/day for cerebrovascular conditions and 40–80 mg/day for anxiety, under physician supervision.

2. Higher studied dose

Russian clinical literature describes courses of 200–300 mg/day for short periods in cerebrovascular indications. Doses above this have not been systematically studied.

3. Timing

Russian prescribing typically divides the daily dose into 2–3 administrations with meals.

4. With food

With food in Russian prescribing context.

5. Split dosing

Russian protocols typically split into 2–3 daily doses.

6. How long to try

Russian protocols use 1–2 month courses with breaks; chronic uninterrupted use is not recommended.

What to track

Stop and consult a clinician if you experience drowsiness, dizziness, or low blood pressure

Watch for niacin-related flushing or itching

Be honest with any clinician about taking it — it can mask or complicate diagnosis

Bottom line: There is no recommended consumer dose. The FDA action means there is no quality-controlled supply chain in the US.

2 commercial forms

Compare the main delivery options and what they’re best suited for.

Picamilon sodium salt (Russian prescription)

Prescription drug (RU)

Available in Russia and several CIS countries as a prescription medicine (Pikamilon, sodium salt). Manufactured under medicinal-product GMP; dosed under physician supervision. Not a legal supplement form in the US.

Standard oral bioavailability for a small water-soluble molecule.

Picamilon HCl (research-chemical / OTC pre-2015)

Adulterated supplement

Sold in US 'nootropic' stacks before the 2015 FDA action. Quality and dose unverified; Cohen 2016 measured wildly inconsistent contents across 31 sampled products (a few mg to nearly 1 g per serving).

Comparable to the sodium salt; unregulated quality is the real concern.

Safety

Know the common side effects, key cautions, and who should avoid it.

Common side effects

drowsiness / sedationheadacheniacin-flush (warm flushing of the face/neck)low blood pressure / lightheadednessGI upset

Serious risks

Regulatory: FDA considers picamilon-containing products adulterated. There is no FDA-overseen quality control on consumer products; dose and purity are unverified.
SourceFDA — Picamilon is not a dietary ingredient (2015) — U.S. Food and Drug Administration Cohen et al., 2016 (Drug Test Anal) — PubMed — Drug Testing and Analysis
Additive CNS depression when combined with alcohol, benzodiazepines, opioids, gabapentinoids, or sedating antihistamines — this interaction is biologically expected but not studied.
SourceCohen et al., 2015 (JAMA Intern Med) — PubMed — JAMA Internal Medicine
Possible additive hypotension with antihypertensives — vasodilatory effect of the niacin moiety could potentiate blood-pressure lowering.
SourceCohen et al., 2015 (JAMA Intern Med) — PubMed — JAMA Internal Medicine

Who should avoid it

Anyone in the US looking for a regulated, quality-controlled supplement — picamilon doesn't qualify as a dietary ingredient (FDA, 2015).
SourceFDA — Picamilon is not a dietary ingredient (2015) — U.S. Food and Drug Administration
Pregnant or breastfeeding women — no safety data and FDA flag stands.
SourceFDA — Picamilon is not a dietary ingredient (2015) — U.S. Food and Drug Administration
Children and adolescents — no controlled pediatric data; never appropriate as an OTC product.
SourceFDA — Picamilon is not a dietary ingredient (2015) — U.S. Food and Drug Administration
People on antihypertensive medications, benzodiazepines, opioids, or sedating drugs of any kind without explicit physician supervision.
SourceCohen et al., 2015 (JAMA Intern Med) — PubMed — JAMA Internal Medicine
People with hepatic impairment — niacin and GABA-conjugate metabolism in liver disease is not characterised.
SourceCohen et al., 2015 (JAMA Intern Med) — PubMed — JAMA Internal Medicine

Pregnancy & breastfeeding

Avoid in pregnancy and breastfeeding. There are no controlled human studies, and picamilon is not a legal US dietary ingredient. The Russian product label specifies caution in pregnancy.

SourceFDA — Picamilon is not a dietary ingredient (2015) — U.S. Food and Drug Administration

Bottom line: The FDA's 2015 ruling is the dominant safety message. If you see picamilon on a US supplement label, treat the product itself as a regulatory and quality red flag.

Interactions

alcohol and CNS depressants (benzodiazepines, opioids, sedating antihistamines)Major

Biologically expected additive sedation and respiratory depression from the centrally released GABA. Not studied in humans; assume the same caution as with other GABAergic agents.

SourceCohen et al., 2015 (JAMA Intern Med) — PubMed — JAMA Internal Medicine

antihypertensive medicationsModerate

Niacin moiety produces vasodilation; can potentiate blood-pressure lowering and cause symptomatic hypotension at higher doses.

SourceCohen et al., 2015 (JAMA Intern Med) — PubMed — JAMA Internal Medicine

anticoagulants / antiplatelet agentsMinor

Niacin can have a mild antiplatelet effect; theoretical additive bleeding risk with warfarin or aspirin.

statins (in flushing-prone individuals)Minor

The niacin moiety can cause flushing, which may overlap with niacin-induced flushing reactions; not a pharmacokinetic interaction.

Choosing a product

What to look for on the label — and what to be skeptical of.

Look for…

Honestly, the most useful 'label feature' is the absence of picamilon — its presence on a US supplement label is a regulatory red flag

If you see picamilon in any 'cognitive enhancer' / 'mood blend' / 'nootropic stack' product, that's a signal the brand is selling unapproved ingredients

Reputable third-party-tested supplement brands do not carry picamilon — they tracked the 2015 FDA action and removed it

Be skeptical of…

'Boosts brain blood flow' — extrapolated from Russian prescribing and not replicated in modern RCTs

'Anxiety relief without sedation' — Russian use describes both anxiolysis AND sedation, and the magnitude has not been quantified by modern standards

'Pharmaceutical-grade Russian nootropic' — picamilon is a Russian prescription drug, not a legal US supplement; the label phrasing itself signals the regulatory gap

Combination 'GABA stacks' that hide picamilon in a proprietary blend at unstated dose

Any product claiming picamilon is 'FDA-compliant as a dietary ingredient' — the FDA explicitly ruled the opposite in 2015

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 by claim

Cerebrovascular insufficiency (Russian prescription use)

Cohen et al., 2015 (JAMA Intern Med) — PubMed — JAMA Internal Medicine (2015) link

Cohen et al., 2016 (Drug Test Anal) — PubMed — Drug Testing and Analysis (2016) link

Safety

FDA — Picamilon is not a dietary ingredient (2015) — U.S. Food and Drug Administration (2015) link

Other references

Picamilon on Wikidata — Wikidata link

Picamilon (PubChem CID 60608) — PubChem link

Track Picamilon with Pilora

Set up dose reminders, check interactions, and join the community in the Pilora iPhone app.

Coming to App Store

Evidence-based·Last reviewed May 31, 2026·Evidence current as of May 31, 2026·How we grade evidence

Disclaimer: This compound is not approved by the FDA for human use and is not a dietary supplement. This page is an educational review of available research — much of it preclinical or early-stage — not a recommendation to use it. Consumer product quality is unregulated. Consult a qualified clinician.