Home Ingredients Picamilon (N-Nicotinoyl-GABA)
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Picamilon (N-Nicotinoyl-GABA)

Synthetic — niacin-GABA conjugate
Evidence Level
Preliminary
3 Clinical Trials
5 Documented Benefits
1/5 Evidence Score

Synthetic combination of niacin (vitamin B3) and GABA developed in the USSR (1969). It acts as a GABA prodrug: the niacin moiety enables blood-brain-barrier penetration, and it is cleaved in the CNS to release GABA plus niacin. Approved in Russia for anxiety, depression, and cerebrovascular disease. FDA warning letters in 2015 declared it not legal as a dietary supplement in the US (a synthetic drug, not natural). Rigorous Western RCTs are limited; most clinical literature is Russian and Japanese.

Studied Dose 50 mg 3×/day (150 mg/day). Cerebrovascular: 100-300 mg/day. Anxiety: 100-200 mg/day.
Active Compound Picamilon (N-nicotinoyl-γ-aminobutyric acid; nicotinoyl-GABA, pikamilon) — niacin (nicotinic acid) covalently bonded to GABA via an amide linkage.

Benefits

Anxiety with mild stimulating profile (Russian indication)

Russian approval for anxiety states. Unique mechanism: GABA prodrug providing anxiolysis without typical sedation due to niacin moiety's vasodilatory/stimulating effects. Mechanism: in CNS, cleaved to release GABA (anxiolytic) + niacin (vasodilator/possibly mild stimulant). Distinct from benzodiazepines (sedating) and from selank (peptide). Less rigorous evidence base than other Russian anxiolytics.

Supported by Trial 1, Trial 2

Cerebrovascular disease and cerebral circulation

Russian indication for cerebrovascular insufficiency and chronic cerebral ischemia. Mechanism: niacin component provides vasodilation enhancing cerebral blood flow. Used in older Russian clinical practice for elderly cognitive complaints related to cerebrovascular insufficiency. Limited rigorous clinical evidence outside Russian/CIS literature.

Supported by Trial 1

Mild depression / asthenic depression

Approved Russian indication for asthenic depression and chronic fatigue with depressive component. Combined GABA + niacin mechanism may provide both anxiolysis and mild activation. Limited rigorous Western RCT evidence.

Supported by Trial 1

GABA prodrug delivery (mechanism advantage)

Distinguishing pharmacological feature: Picamilon is GABA prodrug. Pure GABA cannot cross BBB efficiently. Niacin component provides lipophilicity for BBB penetration; once in CNS, amide bond cleaved by amidases to release GABA + nicotinic acid. Mechanism design rationale similar to phenibut (phenyl-GABA) but with niacin's additional vasodilatory and metabolic effects.

Supported by Trial 1, Trial 2

Migraine prophylaxis (limited Russian evidence)

Used in Russia for migraine prophylaxis based on theoretical cerebrovascular benefits. Limited rigorous evidence; not first-line treatment in any modern guidelines outside Russian clinical practice.

Supported by Trial 1, Trial 2

Mechanism of action

1

GABA prodrug — CNS amidase cleavage

Picamilon is N-nicotinoyl-GABA — synthetic conjugate cleaved in CNS by amidase enzymes to release: (1) GABA — inhibitory neurotransmitter providing anxiolytic effects via GABA-A receptor activation; (2) nicotinic acid (niacin) — vasodilator with vitamin B3 activity. Dual delivery mechanism distinguishes from pure GABA-mimetic compounds.

2

Niacin vasodilation enhancing cerebral blood flow

Niacin component provides vasodilation — enhances cerebral blood flow and microcirculation. Mechanism for cerebrovascular insufficiency indications. Less prominent than direct GABA effects but contributes to overall pharmacology.

3

GABA-A receptor activation (post-cleavage)

Released GABA acts at GABA-A receptors providing anxiolysis. Less potent than direct GABA-A modulators (benzodiazepines) but more selective due to local CNS GABA release vs peripheral effects.

4

Modest BBB penetration via lipophilic conjugate

Amide-bonded niacin-GABA conjugate is more lipophilic than free GABA — crosses BBB. Once in CNS, cleaved to active components. Mechanism design similar to other prodrug strategies.

Clinical trials

1
Russian Cerebrovascular Disease Studies

Russian-language clinical studies in cerebrovascular insufficiency and cognitive disorders (multiple Russian publications, 1980s-1990s).

Russian patients with cerebrovascular insufficiency, chronic cerebral ischemia, asthenic disorders, anxiety states with autonomic features.

Russian clinical evidence supports use for cerebrovascular and anxiety conditions. Limited Western methodological scrutiny due to Russian-language predominance. Mechanism via GABA + niacin dual delivery. Approved Russian regulatory use since 1969 launch.

2
Picamilon GABAergic Cerebrovascular Effects

Russian preclinical/clinical pharmacology study (Silkina IV, Gan'shina TC, Seredin SB, Mirzoian RS 2005, Eksp Klin Farmakol 68(1):20-24).

Comparative pharmacology study of GABAergic mechanisms — afobazole (fabomotizole) and picamilon — in cerebrovascular and neuroprotective effects.

Picamilon demonstrated GABAergic cerebrovascular and neuroprotective effects. Mechanistic confirmation of GABA-mediated CNS effects via prodrug delivery. Foundational comparative evidence for picamilon's place in Russian neuropharmacology.

3
FDA Warning (Regulatory Significance)

FDA Warning Letters issued to multiple supplement companies marketing picamilon.

Supplement companies marketing picamilon as dietary supplement in US.

FDA determined picamilon not a legal dietary ingredient — declared synthetic drug rather than natural compound (vitamin, herb, or other DSHEA-eligible substance). Many companies removed picamilon products following warning letters. Important regulatory history — distinguishes picamilon from other Russian peptides as not eligible for US dietary supplement marketing despite continued sales by some vendors. Demonstrates regulatory uncertainty for Russian-developed compounds in US market.

Side effects and drug interactions

Common Potential side effects

Generally well-tolerated; safety profile better than phenibut.
Mild headache (rare).
Dizziness from niacin component vasodilation.
Skin flushing (less than free niacin due to controlled release).
GI upset (occasional).
Pregnancy/lactation: avoid.
Long-term safety: Russian clinical experience supports general safety.
FDA does not consider it legal dietary supplement in US.

Important Drug interactions

Antihypertensives: theoretical additive vasodilation effects.
Statins (simvastatin, atorvastatin): theoretical additive effects on lipid metabolism via niacin component.
Benzodiazepines: theoretical additive GABA effects.
Niacin supplements: additive niacin effects (skin flushing, lipid effects).
Most medications: limited interaction data.

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Frequently asked questions about Picamilon (N-Nicotinoyl-GABA)

What is picamilon?

Picamilon is a compound combining niacin and GABA, developed in the former Soviet Union, designed so GABA can cross into the brain (which GABA alone does poorly). It is used for calm, focus, and circulation, but the US FDA has ruled it is not a legal dietary ingredient.

What is picamilon used for?

It is marketed for relaxation, mood, and mental clarity, on the idea that it delivers GABA to the brain and dilates blood vessels via niacin. Human research is limited and mostly older Russian studies.

What is picamilon's legal status?

The US FDA has stated picamilon does not qualify as a dietary ingredient, so it should not be sold in US supplements. Its availability and legality vary, which is an important consideration.

Is picamilon safe?

Human safety data is limited. Reported effects are generally mild, but because of its uncertain regulatory status and limited research, caution is warranted; consult a healthcare professional before considering it.

What is the recommended dosage of Picamilon?

The clinically studied dose is 50 mg 3×/day (150 mg/day). Cerebrovascular: 100-300 mg/day. Anxiety: 100-200 mg/day. Always follow the product label and check with a healthcare provider for personal advice.

Is Picamilon safe, and does it have side effects?

For most healthy adults, Picamilon is well tolerated at studied doses. Reported effects can include: Generally well-tolerated; safety profile better than phenibut. Mild headache (rare). It may also interact with some medications. Picamilon is not right for everyone, so check with a healthcare provider first if you are pregnant or breastfeeding, have a medical condition, or take prescription medication.

Does Picamilon interact with any medications?

Possible interactions include: Antihypertensives: theoretical additive vasodilation effects. Statins (simvastatin, atorvastatin): theoretical additive effects on lipid metabolism via niacin component. If you take prescription medication, check with a pharmacist or doctor before using it.

How strong is the scientific evidence for Picamilon?

NutraSmarts rates the evidence for Picamilon as Preliminary (1 out of 5). It is backed by 3 clinical trials and 3 cited references summarized on this page. A higher rating reflects more, larger, and better-designed human studies.

References(3 citations)

Evidence ratings on NutraSmarts are based on the totality of human clinical research, with emphasis on randomized controlled trials, meta-analyses, and systematic reviews. The references below directly support claims made throughout this page.

  1. Danilov AB, Shindryaeva NN, Borodulina IV, Lunegov TD, Kristeleva DA Clinical efficacy and safety of Picamilon in patients with progressive chronic cerebral ischemia Zhurnal Nevrologii i Psikhiatrii imeni S.S. Korsakova. 2024;124(8):71-80. doi:10.17116/jnevro202412408171.PubMedUsed to support: Russian clinical study of picamilon in patients with progressive chronic cerebral ischemia reporting efficacy and safety data; supports the cerebrovascular disease indication for which picamilon is approved in Russia
  2. Silkina IV, Gan'shina TC, Seredin SB, Mirzoian RS Gabaergic mechanism of cerebrovascular and neuroprotective effects of afobazole and picamilon Eksperimental'naia i Klinicheskaia Farmakologiia. 2005;68(1):20-4..PubMedUsed to support: Animal pharmacology study characterizing picamilon's GABAergic mechanism underlying its cerebrovascular and neuroprotective effects; supports the GABA prodrug delivery mechanism and cerebrovascular benefit claims
  3. Avula B, Chittiboyina AG, Sagi S, Wang YH, Wang M, Khan IA, Cohen PA Identification and quantification of vinpocetine and picamilon in dietary supplements sold in the United States Drug Testing and Analysis. 2016;8(3-4):334-43. doi:10.1002/dta.1853.PubMedUsed to support: Analytical study confirming the presence and quantification of picamilon in US dietary supplements and noting its regulatory status; relevant context for picamilon's unapproved dietary supplement situation in the US