Picamilon

updated

Picamilon is registered in Russia as a nootropic tablet, and its leaflet wording on reduced anxiety and normalized sleep closely matches the supplier's claims. The human data are small open or uncontrolled studies in cerebral ischemia, and PubMed searches on 10 October 2026 found no controlled human trial of anxiety, stress or sleep. FDA says supplements containing picamilon are misbranded because it is not a dietary ingredient.

Nicotinic acid and GABA conjugate (N-nicotinoyl-GABA)

  • A Russian leaflet describes Picamilon tablets as a nootropic with tranquilizing and psychostimulating action, in wording that closely matches the supplier's claims.
  • On 30 November 2015 FDA issued warning letters to five companies whose supplements claimed to contain picamilon, saying the products are misbranded because picamilon is not a dietary ingredient.
  • An openFDA Drugs@FDA search on 10 October 2026 returned No matches found for picamilon, and DailyMed returned no labels.
  • Of 31 picamilon supplements bought from US retailers, 30 contained picamilon, from 2.7 to 721.5 mg per recommended daily serving.
  • In a 50-patient open cohort in cerebral ischemia, MoCA scores rose over three visits, but there was no control group.
  • PubMed searches on 10 October 2026 returned 11 and 5 records, and none was a controlled trial of anxiety, stress or sleep.

What is picamilon, and what is its regulatory status?

Picamilon is nicotinoyl-GABA, registered in Russia as a nootropic tablet. No FDA-approved picamilon drug turned up, and FDA says supplements containing it are misbranded because it is not a dietary ingredient.

A Russian patient leaflet for Picamilon 20 mg and 50 mg tablets (sodium nicotinoyl-gamma-aminobutyrate, registration number printed as R N000851/01) describes a nootropic that widens cerebral vessels and has tranquilizing and psychostimulating action. Its listed uses include cerebrovascular insufficiency, asthenia, depression in the elderly, states with anxiety, fear or irritability, migraine prevention, glaucoma, urinary disorders, and improving tolerance of physical and mental loads, including restoring work capacity in athletes. It states that with courses the drug normalizes sleep and reduces anxiety. These are label descriptions, not trial results. The leaflet was read as a copy hosted on a drug-information site, its version date is not shown, and a Russian registration is not an FDA or EMA review.

On 30 November 2015 FDA issued warning letters to five companies whose dietary supplements claimed to contain picamilon. FDA's constituent update says these products are misbranded because picamilon does not meet the statutory definition of a dietary ingredient. The update is current as of 30 November 2015, and later FDA actions were not examined.

On 10 October 2026, an openFDA Drugs@FDA search on the generic name picamilon returned No matches found, and a DailyMed label search for picamilon returned no labels.

Picamilon as the free acid (N-nicotinoyl-GABA, 4-(pyridine-3-carbonylamino)butanoic acid) is PubChem CID 60608 (C10H12N2O3, 208.21 g/mol, CAS 34562-97-5). The sodium salt, which the Russian leaflet names as the active substance, is CID 23663986 (C10H11N2NaO3, 230.20 g/mol, CAS 62936-56-5). A supplement labeled picamilon may be either form, and the same milligrams of each hold about 11% different amounts of picamilon, going by molecular weight (230.20 versus 208.21).

Picamilon leaflet: nootropic, anxiolytic and anti-asthenic wording; label PK statements

Official label

Russian-language patient leaflet for Picamilon 20 mg and 50 mg tablets (sodium nicotinoyl-gamma-aminobutyrate), registration number printed as R N000851/01. Copy hosted on medi.ru; version date not shown.

The leaflet describes a nootropic that widens cerebral vessels and has tranquilizing and psychostimulating action. Its listed uses include cerebrovascular insufficiency, asthenia, depression in the elderly, states with anxiety, fear or irritability, migraine prevention, glaucoma, urinary disorders, and improving tolerance of physical and mental loads, including restoring work capacity in athletes. It states that with courses the drug normalizes sleep and reduces anxiety. It states oral bioavailability of 50 to 88% and a half-life of 0.51 hours, with no source given. Listed side effects are irritability, excitement, anxiety, dizziness, headache, nausea and allergic reactions. It is contraindicated in hypersensitivity, chronic renal failure, pregnancy, lactation and under age 3.

Participants / model
Adults, and children over 3 for some uses
Treatment
Picamilon 20 mg and 50 mg oral tablets
Follow-up
Version date not shown
Study design
Russian-language patient leaflet, copy hosted on a drug-information site
Funding
not stated in the source

These are label descriptions, not trial results, and they match the supplier wording closely. A Russian registration is not an FDA or EMA review. The copy was read on a commercial drug-information site, not on the Russian state register.

Read the original source
FDA constituent update: warning letters to five companies, 30 November 2015

Regulatory record

U.S. Food and Drug Administration. Recent FDA action on dietary supplements labeled as containing picamilon, constituent update current as of 30 November 2015.

On 30 November 2015 FDA issued warning letters to five companies whose dietary supplements claimed to contain picamilon. FDA's constituent update says these products are misbranded because picamilon does not meet the statutory definition of a dietary ingredient.

Participants / model
Not a clinical population
Treatment
Dietary supplement products labeled as containing picamilon
Follow-up
Update current as of 30 November 2015
Study design
Official FDA record
Funding
not stated in the source

Later FDA actions were not examined.

Read the original source
Searches, 10 October 2026: no FDA application or label

Regulatory record

U.S. Food and Drug Administration. openFDA Drugs@FDA search on the generic name picamilon, with a DailyMed label search for picamilon, run on 10 October 2026.

The openFDA Drugs@FDA search returned No matches found, and the DailyMed search returned no labels. No FDA-approved picamilon drug turned up.

Participants / model
Records reviewed, not a population
Treatment
Not applicable
Follow-up
Searches run on 10 October 2026
Study design
Dated regulator database search
Funding
not stated in the source

The result covers FDA application and label records only. No US label is cited here.

Read the original source
PubChem: picamilon free acid and sodium salt identity

Chemical identity record

National Library of Medicine. PubChem compound records CID 60608 (picamilon) and CID 23663986 (picamilon sodium).

Picamilon as the free acid (N-nicotinoyl-GABA, 4-(pyridine-3-carbonylamino)butanoic acid): PubChem CID 60608, C10H12N2O3, 208.21 g/mol, CAS 34562-97-5. The sodium salt, which the Russian leaflet names as the active substance: CID 23663986, C10H11N2NaO3, 230.20 g/mol, CAS 62936-56-5.

Participants / model
Chemical identity, not a clinical population
Treatment
Defined free acid and sodium salt
Follow-up
Not applicable
Study design
NLM chemical record
Funding
not stated in the source

A supplement labeled picamilon may be either form, and the same milligrams of each hold about 11% different amounts of picamilon, going by molecular weight (230.20 versus 208.21). Identity record only; it says nothing about efficacy or safety.

Read the original source

What do the studies in cerebral ischemia show?

The studies are small, open or uncontrolled, and Russian-language. In a single-arm cohort of 50 patients with stage II chronic cerebral ischemia, MoCA scores rose over three visits, but with no control group none of it can be attributed to picamilon.

In an open cohort of 50 patients with stage II chronic cerebral ischemia given picamilon intravenously for 10 days then as tablets for 60 days, MoCA scores rose over the three visits (20.9, 24.6, 25.9), sleep normalized in 55% by visit 2 and 81% by visit 3, and Doppler flow velocity rose. There was no placebo or control group, so none of this can be attributed to the drug.

An open randomized comparison in 44 patients aged 46 to 67 with stage I chronic cerebral ischemia compared two picamilon regimens, oral tablets for 60 days (n = 23) and intramuscular injection for 10 days then tablets (n = 21). The regimens were compared with each other and not with placebo. By the end the cognitive effect was comparable between regimens (p = 0.508). The abstract reports good tolerability in 98% of patients and adverse events at under 8.6%, without stating the denominator.

An open multicenter randomized study of 278 patients over 45 with chronic cerebral ischemia and cognitive impairment compared a combination product (Picamilon Ginkgo, 139 patients) with ginkgo biloba extract alone (139) for 90 days. The combination gave greater cognitive gains (MMSE p = 0.007, MoCA p = 0.0003) and no significant difference on the Hamilton depression scale. The product contains ginkgo, so the result cannot be credited to picamilon alone.

Open cohort: 50 patients, single arm, MoCA and sleep scores rose, no control group

Clinical trial

Danilov AB et al. Zh Nevrol Psikhiatr Im S S Korsakova. 2024;124(8):71-80. PMID 39269299.

MoCA scores rose over the three visits (20.9, 24.6, 25.9), sleep normalized in 55% by visit 2 and 81% by visit 3, and Doppler flow velocity rose.

Participants / model
50 patients with stage II chronic cerebral ischemia
Treatment
Picamilon 200 mg intravenously for 10 days then 50 mg tablets three times a day for 60 days
Follow-up
10 days intravenously then 60 days orally
Study design
Open-label single-arm cohort, Russian-language
Funding
not stated in the source

There was no placebo or control group, so none of this can be attributed to the drug. Endpoints were MoCA, a sleep scale, Doppler cerebral blood flow and endothelial markers.

Read the original source
Regimen comparison: 44 patients, two picamilon regimens, no placebo

Clinical trial

Danilov AB et al. Zh Nevrol Psikhiatr Im S S Korsakova. 2024;124(7):119-130. PMID 39113452.

By the end the cognitive effect was comparable between regimens (p = 0.508). The abstract reports good tolerability in 98% of patients and adverse events at under 8.6%, without stating the denominator.

Participants / model
44 patients aged 46 to 67 with stage I chronic cerebral ischemia
Treatment
Picamilon 50 mg three times a day for 60 days (n = 23), or 100 mg intramuscularly for 10 days then tablets (n = 21)
Follow-up
60 days
Study design
Open randomized comparison of two regimens, small, Russian-language, no placebo
Funding
not stated in the source

The two regimens were compared with each other and not with placebo. Endpoints were MoCA, autonomic, neurological and sleep scales, Doppler and adverse events.

Read the original source
Combination product: 278 patients, 90 days, versus ginkgo alone

Clinical trial

Zakharov VV et al. Zh Nevrol Psikhiatr Im S S Korsakova. 2022;122(9):95-103. PMID 36168693.

The combination gave greater cognitive gains (MMSE p = 0.007, MoCA p = 0.0003) and no significant difference on the Hamilton depression scale.

Participants / model
278 patients over 45 with chronic cerebral ischemia and cognitive impairment
Treatment
Oral Picamilon Ginkgo (139 patients) versus ginkgo biloba extract alone (139)
Follow-up
90 days
Study design
Open multicenter randomized study of a combination product, Russian-language
Funding
not stated in the source

The product contains ginkgo, so the result cannot be credited to picamilon alone. Endpoints were MoCA, MMSE, the Hamilton depression scale and EQ-5D.

Read the original source

Has picamilon been tested in athletes?

One Russian-language study gave picamilon to swimmers with a dysadaptation syndrome as a recovery aid and measured brain blood filling after a warm-up load. The abstract gives no group sizes, no placebo group, and no performance, anxiety or sleep outcome.

In swimmers with a dysadaptation syndrome given aminalon, phenibut or picamilon for 4 weeks as a recovery aid, the abstract reports changes in brain blood filling and venous outflow 20 minutes after a warm-up load. One group (hypokinetic, on picamilon) did not show the change. The abstract gives no group sizes, no placebo group, and no performance, anxiety or sleep outcome.

The Russian leaflet lists restoring work capacity in athletes among the uses of picamilon, but that is a label statement, not a trial result.

Swimmers: brain blood filling after warm-up, no performance outcome

Human study

Likhodeev VA et al. Eksp Klin Farmakol. 2009;72(4):15-9. PMID 19803364.

The abstract reports changes in brain blood filling and venous outflow 20 minutes after a warm-up load. One group (hypokinetic, on picamilon) did not show the change.

Participants / model
Swimmers with a dysadaptation syndrome; group sizes not stated
Treatment
Oral picamilon 0.10 g for 4 weeks, with other groups given aminalon 0.25 g or phenibut 0.25 g, as a recovery aid
Follow-up
4 weeks
Study design
Clinical study, Russian-language; design not stated
Funding
not stated in the source

The abstract gives no group sizes, no placebo group, and no performance, anxiety or sleep outcome. Endpoints were cerebral hemodynamics before and after warm-up.

Read the original source
Picamilon leaflet: nootropic, anxiolytic and anti-asthenic wording; label PK statements

Official label

Russian-language patient leaflet for Picamilon 20 mg and 50 mg tablets (sodium nicotinoyl-gamma-aminobutyrate), registration number printed as R N000851/01. Copy hosted on medi.ru; version date not shown.

The leaflet describes a nootropic that widens cerebral vessels and has tranquilizing and psychostimulating action. Its listed uses include cerebrovascular insufficiency, asthenia, depression in the elderly, states with anxiety, fear or irritability, migraine prevention, glaucoma, urinary disorders, and improving tolerance of physical and mental loads, including restoring work capacity in athletes. It states that with courses the drug normalizes sleep and reduces anxiety. It states oral bioavailability of 50 to 88% and a half-life of 0.51 hours, with no source given. Listed side effects are irritability, excitement, anxiety, dizziness, headache, nausea and allergic reactions. It is contraindicated in hypersensitivity, chronic renal failure, pregnancy, lactation and under age 3.

Participants / model
Adults, and children over 3 for some uses
Treatment
Picamilon 20 mg and 50 mg oral tablets
Follow-up
Version date not shown
Study design
Russian-language patient leaflet, copy hosted on a drug-information site
Funding
not stated in the source

These are label descriptions, not trial results, and they match the supplier wording closely. A Russian registration is not an FDA or EMA review. The copy was read on a commercial drug-information site, not on the Russian state register.

Read the original source

Does picamilon calm anxiety without sedation, improve sleep or build stress resilience?

No controlled human trial found tests those claims. A PubMed search on 10 October 2026 returned 11 records on anxiety, stress, sleep, asthenia or neurosis, none a controlled trial in people with those complaints or in healthy people, and a second search returned 5 records, none placebo-controlled.

Sellers say picamilon reduces anxiety with clarity rather than sedation, improves cerebral blood flow, builds stress resilience and improves sleep. That wording closely repeats the Russian leaflet's descriptions, which are label statements, not trial results.

A PubMed search on 10 October 2026 for picamilon and its alternative names with anxiety, anxious, stress, sleep, insomnia, asthenia, fatigue or neurosis returned 11 records. The human ones were the two open studies above, where sleep was a secondary scale in cerebral ischemia, and a Russian review of asthenia. The rest were animal or mechanism studies from 1984 to 2006, mostly in rats. None was a controlled trial of anxiety, stress or sleep in people with those complaints or in healthy people.

A second search for picamilon with randomized, placebo, double-blind or controlled returned 5 records. By title and abstract none was a placebo-controlled trial. They were an uncontrolled glaucoma series (1994), an uncontrolled prostate series (1999) whose author calls for placebo-controlled studies, the ginkgo combination study, a 94-patient glaucoma comparison of mexidol plus picamilon against picamilon alone in which picamilon was the comparator, and the open regimen comparison above.

The blood-flow claim rests on a rise in Doppler flow velocity in the single-arm cohort above, which had no control group.

PubMed searches, 10 October 2026: 11 records and 5 records, no placebo-controlled trial

PubMed search record

PubMed search run on 10 October 2026: (picamilon OR pikamilon OR nicotinoyl-GABA OR "nicotinoyl gamma-aminobutyric") AND (anxiety OR anxious OR stress OR sleep OR insomnia OR asthenia OR fatigue OR neurosis). 11 records returned. A second search for picamilon with randomized, placebo, double-blind or controlled returned 5 records.

The first search returned 11 records. The human ones were the two open studies above, where sleep was a secondary scale in cerebral ischemia, and a Russian review of asthenia. The rest were animal or mechanism studies from 1984 to 2006, mostly in rats. None was a controlled trial of anxiety, stress or sleep in people with those complaints or in healthy people. The second search returned 5 records, and by title and abstract none was a placebo-controlled trial: an uncontrolled glaucoma series (1994), an uncontrolled prostate series (1999) whose author calls for placebo-controlled studies, the ginkgo combination study, a 94-patient glaucoma comparison of mexidol plus picamilon against picamilon alone in which picamilon was the comparator (PMID 23808185), and the open regimen comparison. The anxiety, clarity, sleep and stress-resilience claims have no controlled human trial among these records.

Participants / model
Records returned, not a population
Treatment
Not applicable
Follow-up
Searches run on 10 October 2026
Study design
Literature search
Funding
not stated in the source

A search result shows what PubMed returned on that date. It is not proof that no unindexed study exists.

Read the original source
Picamilon leaflet: nootropic, anxiolytic and anti-asthenic wording; label PK statements

Official label

Russian-language patient leaflet for Picamilon 20 mg and 50 mg tablets (sodium nicotinoyl-gamma-aminobutyrate), registration number printed as R N000851/01. Copy hosted on medi.ru; version date not shown.

The leaflet describes a nootropic that widens cerebral vessels and has tranquilizing and psychostimulating action. Its listed uses include cerebrovascular insufficiency, asthenia, depression in the elderly, states with anxiety, fear or irritability, migraine prevention, glaucoma, urinary disorders, and improving tolerance of physical and mental loads, including restoring work capacity in athletes. It states that with courses the drug normalizes sleep and reduces anxiety. It states oral bioavailability of 50 to 88% and a half-life of 0.51 hours, with no source given. Listed side effects are irritability, excitement, anxiety, dizziness, headache, nausea and allergic reactions. It is contraindicated in hypersensitivity, chronic renal failure, pregnancy, lactation and under age 3.

Participants / model
Adults, and children over 3 for some uses
Treatment
Picamilon 20 mg and 50 mg oral tablets
Follow-up
Version date not shown
Study design
Russian-language patient leaflet, copy hosted on a drug-information site
Funding
not stated in the source

These are label descriptions, not trial results, and they match the supplier wording closely. A Russian registration is not an FDA or EMA review. The copy was read on a commercial drug-information site, not on the Russian state register.

Read the original source

What do supplements labeled as picamilon contain?

Amounts vary widely and labels are unreliable. Of 31 picamilon supplements bought from US retailers, 30 contained picamilon, from 2.7 to 721.5 mg per recommended daily serving, and in 10 cognitive enhancement supplements bought online, 9 of 12 declared quantities were inaccurate.

Of 31 picamilon dietary supplements bought from a variety of US retailers, 30 contained picamilon, from 2.7 to 721.5 mg per recommended daily serving. The authors state picamilon has never been approved by the FDA and note it is prescribed in many countries for cerebrovascular disorders. Consumers could not get accurate dose information from labels.

In 10 cognitive enhancement supplements bought online and tested, 5 unapproved drugs were found, including phenibut, vinpocetine and picamilon, at up to 90.1 mg of picamilon per recommended serving. Several detected drugs were not on the label, and 9 of 12 declared quantities were inaccurate.

31 picamilon supplements: 30 contained it, 2.7 to 721.5 mg per serving

Analytical product survey

Avula B et al. Drug Test Anal. 2016;8(3-4):334-43. PMID 26426301.

Of 31 picamilon dietary supplements bought from a variety of US retailers, 30 contained picamilon, from 2.7 to 721.5 mg per recommended daily serving. The authors state picamilon has never been approved by the FDA and note it is prescribed in many countries for cerebrovascular disorders. Consumers could not get accurate dose information from labels.

Participants / model
31 commercial supplement products
Treatment
Dietary supplements, mixed forms
Follow-up
Not applicable
Study design
Analytical product survey
Funding
not stated in the source

A product analysis, not a study in people.

Read the original source
10 cognitive enhancement supplements: 5 unapproved drugs, 9 of 12 declared amounts inaccurate

Analytical product survey

Cohen PA et al. Neurol Clin Pract. 2021;11(3):e303-e307. PMID 34484905.

In 10 cognitive enhancement supplements bought online and tested, 5 unapproved drugs were found, including phenibut, vinpocetine and picamilon, at up to 90.1 mg of picamilon per recommended serving. Several detected drugs were not on the label, and 9 of 12 declared quantities were inaccurate.

Participants / model
10 commercial supplement products
Treatment
Dietary supplements, mixed forms
Follow-up
Not applicable
Study design
Analytical product survey
Funding
not stated in the source

A product analysis, not a study in people. The 12 declared quantities cover all the drugs the products declared, not picamilon alone.

Read the original source

How does picamilon work, and what is known about how the body handles it?

The Russian leaflet describes a nootropic that widens cerebral vessels, but that is a label description. In vitro, picamilon showed weak or no binding at 50 safety-related targets, and the leaflet's half-life of 0.51 hours has no source.

The Russian leaflet describes a nootropic that widens cerebral vessels and has tranquilizing and psychostimulating action. These are label descriptions, not trial results. In a screen of picamilon against 50 safety-related targets (receptors, ion channels, enzymes, transporters), the compound showed weak or no binding in silico and in vitro at 10 micromolar, so it does not share the binding profile of GABA analogues with a similar structure. The authors work at the FDA's food-safety center, and the paper is research, not FDA policy. It is cell-free and in-silico work, not evidence of any effect in people.

The leaflet states oral bioavailability of 50 to 88% and a half-life of 0.51 hours, with no source given. No human pharmacokinetic study with numbers turned up in the sources reviewed, so these figures stay at label level.

Picamilon leaflet: nootropic, anxiolytic and anti-asthenic wording; label PK statements

Official label

Russian-language patient leaflet for Picamilon 20 mg and 50 mg tablets (sodium nicotinoyl-gamma-aminobutyrate), registration number printed as R N000851/01. Copy hosted on medi.ru; version date not shown.

The leaflet describes a nootropic that widens cerebral vessels and has tranquilizing and psychostimulating action. Its listed uses include cerebrovascular insufficiency, asthenia, depression in the elderly, states with anxiety, fear or irritability, migraine prevention, glaucoma, urinary disorders, and improving tolerance of physical and mental loads, including restoring work capacity in athletes. It states that with courses the drug normalizes sleep and reduces anxiety. It states oral bioavailability of 50 to 88% and a half-life of 0.51 hours, with no source given. Listed side effects are irritability, excitement, anxiety, dizziness, headache, nausea and allergic reactions. It is contraindicated in hypersensitivity, chronic renal failure, pregnancy, lactation and under age 3.

Participants / model
Adults, and children over 3 for some uses
Treatment
Picamilon 20 mg and 50 mg oral tablets
Follow-up
Version date not shown
Study design
Russian-language patient leaflet, copy hosted on a drug-information site
Funding
not stated in the source

These are label descriptions, not trial results, and they match the supplier wording closely. A Russian registration is not an FDA or EMA review. The copy was read on a commercial drug-information site, not on the Russian state register.

Read the original source
In silico and in vitro screen: weak or no binding at 50 targets

Cell study

Santillo MF et al. Basic Clin Pharmacol Toxicol. 2023;132(4):355-358. PMID 36668678.

A screen of picamilon against 50 safety-related targets (receptors, ion channels, enzymes, transporters) found weak or no binding in silico and in vitro at 10 micromolar, so picamilon does not share the binding profile of GABA analogues with a similar structure. The authors state there are few in silico, in vitro and in vivo safety data for picamilon.

Participants / model
In silico and in vitro screen; no people or animals
Treatment
Picamilon at 10 micromolar
Follow-up
Not applicable
Study design
Original in vitro study
Funding
not stated in the source

The authors work at the FDA's food-safety center, and the paper is research, not FDA policy. It is cell-free and in-silico work, not evidence of any effect in people.

Read the original source

What risks and warnings are reported?

The Russian leaflet lists irritability, excitement, anxiety, dizziness, headache, nausea and allergic reactions, and contraindicates use in chronic renal failure and pregnancy. Few safety data exist, no human study here had a placebo group, and supplement content varies widely.

The Russian leaflet lists irritability, excitement, anxiety, dizziness, headache, nausea and allergic reactions as side effects. It is contraindicated in hypersensitivity, chronic renal failure, pregnancy, lactation and under age 3.

The open regimen comparison reports good tolerability in 98% of 44 patients and adverse events at under 8.6%, without stating the denominator. None of the human studies on this page had a placebo group, so none gives a placebo-referenced adverse-event rate.

The authors of the in silico and in vitro screen state that few in silico, in vitro and in vivo safety data exist for picamilon. FDA says supplements containing it are misbranded, and the supplement analyses found contents from 2.7 to 721.5 mg per recommended daily serving, with labels that gave consumers inaccurate dose information.

Picamilon leaflet: nootropic, anxiolytic and anti-asthenic wording; label PK statements

Official label

Russian-language patient leaflet for Picamilon 20 mg and 50 mg tablets (sodium nicotinoyl-gamma-aminobutyrate), registration number printed as R N000851/01. Copy hosted on medi.ru; version date not shown.

The leaflet describes a nootropic that widens cerebral vessels and has tranquilizing and psychostimulating action. Its listed uses include cerebrovascular insufficiency, asthenia, depression in the elderly, states with anxiety, fear or irritability, migraine prevention, glaucoma, urinary disorders, and improving tolerance of physical and mental loads, including restoring work capacity in athletes. It states that with courses the drug normalizes sleep and reduces anxiety. It states oral bioavailability of 50 to 88% and a half-life of 0.51 hours, with no source given. Listed side effects are irritability, excitement, anxiety, dizziness, headache, nausea and allergic reactions. It is contraindicated in hypersensitivity, chronic renal failure, pregnancy, lactation and under age 3.

Participants / model
Adults, and children over 3 for some uses
Treatment
Picamilon 20 mg and 50 mg oral tablets
Follow-up
Version date not shown
Study design
Russian-language patient leaflet, copy hosted on a drug-information site
Funding
not stated in the source

These are label descriptions, not trial results, and they match the supplier wording closely. A Russian registration is not an FDA or EMA review. The copy was read on a commercial drug-information site, not on the Russian state register.

Read the original source
Regimen comparison: 44 patients, two picamilon regimens, no placebo

Clinical trial

Danilov AB et al. Zh Nevrol Psikhiatr Im S S Korsakova. 2024;124(7):119-130. PMID 39113452.

By the end the cognitive effect was comparable between regimens (p = 0.508). The abstract reports good tolerability in 98% of patients and adverse events at under 8.6%, without stating the denominator.

Participants / model
44 patients aged 46 to 67 with stage I chronic cerebral ischemia
Treatment
Picamilon 50 mg three times a day for 60 days (n = 23), or 100 mg intramuscularly for 10 days then tablets (n = 21)
Follow-up
60 days
Study design
Open randomized comparison of two regimens, small, Russian-language, no placebo
Funding
not stated in the source

The two regimens were compared with each other and not with placebo. Endpoints were MoCA, autonomic, neurological and sleep scales, Doppler and adverse events.

Read the original source
In silico and in vitro screen: weak or no binding at 50 targets

Cell study

Santillo MF et al. Basic Clin Pharmacol Toxicol. 2023;132(4):355-358. PMID 36668678.

A screen of picamilon against 50 safety-related targets (receptors, ion channels, enzymes, transporters) found weak or no binding in silico and in vitro at 10 micromolar, so picamilon does not share the binding profile of GABA analogues with a similar structure. The authors state there are few in silico, in vitro and in vivo safety data for picamilon.

Participants / model
In silico and in vitro screen; no people or animals
Treatment
Picamilon at 10 micromolar
Follow-up
Not applicable
Study design
Original in vitro study
Funding
not stated in the source

The authors work at the FDA's food-safety center, and the paper is research, not FDA policy. It is cell-free and in-silico work, not evidence of any effect in people.

Read the original source
FDA constituent update: warning letters to five companies, 30 November 2015

Regulatory record

U.S. Food and Drug Administration. Recent FDA action on dietary supplements labeled as containing picamilon, constituent update current as of 30 November 2015.

On 30 November 2015 FDA issued warning letters to five companies whose dietary supplements claimed to contain picamilon. FDA's constituent update says these products are misbranded because picamilon does not meet the statutory definition of a dietary ingredient.

Participants / model
Not a clinical population
Treatment
Dietary supplement products labeled as containing picamilon
Follow-up
Update current as of 30 November 2015
Study design
Official FDA record
Funding
not stated in the source

Later FDA actions were not examined.

Read the original source
31 picamilon supplements: 30 contained it, 2.7 to 721.5 mg per serving

Analytical product survey

Avula B et al. Drug Test Anal. 2016;8(3-4):334-43. PMID 26426301.

Of 31 picamilon dietary supplements bought from a variety of US retailers, 30 contained picamilon, from 2.7 to 721.5 mg per recommended daily serving. The authors state picamilon has never been approved by the FDA and note it is prescribed in many countries for cerebrovascular disorders. Consumers could not get accurate dose information from labels.

Participants / model
31 commercial supplement products
Treatment
Dietary supplements, mixed forms
Follow-up
Not applicable
Study design
Analytical product survey
Funding
not stated in the source

A product analysis, not a study in people.

Read the original source

Why does picamilon sit in D tier?

D reflects a Russian-registered drug whose leaflet wording the supplier repeats, with no controlled human trial of anxiety, clarity, sleep or stress resilience. The human data are small open or uncontrolled studies, and FDA says supplements containing picamilon are misbranded.

The human data are small open or uncontrolled Russian-language studies in cerebral ischemia, a combination product study, and one swimmer study without performance outcomes. The only mechanistic screen found weak or no binding at 50 targets, and the leaflet's half-life of 0.51 hours has no source.

For the supplier's claims, the wording comes from the Russian leaflet but is not supported by controlled human evidence among the records reviewed, and no FDA drug approval exists. The claims outrun the data.

Picamilon leaflet: nootropic, anxiolytic and anti-asthenic wording; label PK statements

Official label

Russian-language patient leaflet for Picamilon 20 mg and 50 mg tablets (sodium nicotinoyl-gamma-aminobutyrate), registration number printed as R N000851/01. Copy hosted on medi.ru; version date not shown.

The leaflet describes a nootropic that widens cerebral vessels and has tranquilizing and psychostimulating action. Its listed uses include cerebrovascular insufficiency, asthenia, depression in the elderly, states with anxiety, fear or irritability, migraine prevention, glaucoma, urinary disorders, and improving tolerance of physical and mental loads, including restoring work capacity in athletes. It states that with courses the drug normalizes sleep and reduces anxiety. It states oral bioavailability of 50 to 88% and a half-life of 0.51 hours, with no source given. Listed side effects are irritability, excitement, anxiety, dizziness, headache, nausea and allergic reactions. It is contraindicated in hypersensitivity, chronic renal failure, pregnancy, lactation and under age 3.

Participants / model
Adults, and children over 3 for some uses
Treatment
Picamilon 20 mg and 50 mg oral tablets
Follow-up
Version date not shown
Study design
Russian-language patient leaflet, copy hosted on a drug-information site
Funding
not stated in the source

These are label descriptions, not trial results, and they match the supplier wording closely. A Russian registration is not an FDA or EMA review. The copy was read on a commercial drug-information site, not on the Russian state register.

Read the original source
FDA constituent update: warning letters to five companies, 30 November 2015

Regulatory record

U.S. Food and Drug Administration. Recent FDA action on dietary supplements labeled as containing picamilon, constituent update current as of 30 November 2015.

On 30 November 2015 FDA issued warning letters to five companies whose dietary supplements claimed to contain picamilon. FDA's constituent update says these products are misbranded because picamilon does not meet the statutory definition of a dietary ingredient.

Participants / model
Not a clinical population
Treatment
Dietary supplement products labeled as containing picamilon
Follow-up
Update current as of 30 November 2015
Study design
Official FDA record
Funding
not stated in the source

Later FDA actions were not examined.

Read the original source
Open cohort: 50 patients, single arm, MoCA and sleep scores rose, no control group

Clinical trial

Danilov AB et al. Zh Nevrol Psikhiatr Im S S Korsakova. 2024;124(8):71-80. PMID 39269299.

MoCA scores rose over the three visits (20.9, 24.6, 25.9), sleep normalized in 55% by visit 2 and 81% by visit 3, and Doppler flow velocity rose.

Participants / model
50 patients with stage II chronic cerebral ischemia
Treatment
Picamilon 200 mg intravenously for 10 days then 50 mg tablets three times a day for 60 days
Follow-up
10 days intravenously then 60 days orally
Study design
Open-label single-arm cohort, Russian-language
Funding
not stated in the source

There was no placebo or control group, so none of this can be attributed to the drug. Endpoints were MoCA, a sleep scale, Doppler cerebral blood flow and endothelial markers.

Read the original source
Regimen comparison: 44 patients, two picamilon regimens, no placebo

Clinical trial

Danilov AB et al. Zh Nevrol Psikhiatr Im S S Korsakova. 2024;124(7):119-130. PMID 39113452.

By the end the cognitive effect was comparable between regimens (p = 0.508). The abstract reports good tolerability in 98% of patients and adverse events at under 8.6%, without stating the denominator.

Participants / model
44 patients aged 46 to 67 with stage I chronic cerebral ischemia
Treatment
Picamilon 50 mg three times a day for 60 days (n = 23), or 100 mg intramuscularly for 10 days then tablets (n = 21)
Follow-up
60 days
Study design
Open randomized comparison of two regimens, small, Russian-language, no placebo
Funding
not stated in the source

The two regimens were compared with each other and not with placebo. Endpoints were MoCA, autonomic, neurological and sleep scales, Doppler and adverse events.

Read the original source
Combination product: 278 patients, 90 days, versus ginkgo alone

Clinical trial

Zakharov VV et al. Zh Nevrol Psikhiatr Im S S Korsakova. 2022;122(9):95-103. PMID 36168693.

The combination gave greater cognitive gains (MMSE p = 0.007, MoCA p = 0.0003) and no significant difference on the Hamilton depression scale.

Participants / model
278 patients over 45 with chronic cerebral ischemia and cognitive impairment
Treatment
Oral Picamilon Ginkgo (139 patients) versus ginkgo biloba extract alone (139)
Follow-up
90 days
Study design
Open multicenter randomized study of a combination product, Russian-language
Funding
not stated in the source

The product contains ginkgo, so the result cannot be credited to picamilon alone. Endpoints were MoCA, MMSE, the Hamilton depression scale and EQ-5D.

Read the original source
Swimmers: brain blood filling after warm-up, no performance outcome

Human study

Likhodeev VA et al. Eksp Klin Farmakol. 2009;72(4):15-9. PMID 19803364.

The abstract reports changes in brain blood filling and venous outflow 20 minutes after a warm-up load. One group (hypokinetic, on picamilon) did not show the change.

Participants / model
Swimmers with a dysadaptation syndrome; group sizes not stated
Treatment
Oral picamilon 0.10 g for 4 weeks, with other groups given aminalon 0.25 g or phenibut 0.25 g, as a recovery aid
Follow-up
4 weeks
Study design
Clinical study, Russian-language; design not stated
Funding
not stated in the source

The abstract gives no group sizes, no placebo group, and no performance, anxiety or sleep outcome. Endpoints were cerebral hemodynamics before and after warm-up.

Read the original source
PubMed searches, 10 October 2026: 11 records and 5 records, no placebo-controlled trial

PubMed search record

PubMed search run on 10 October 2026: (picamilon OR pikamilon OR nicotinoyl-GABA OR "nicotinoyl gamma-aminobutyric") AND (anxiety OR anxious OR stress OR sleep OR insomnia OR asthenia OR fatigue OR neurosis). 11 records returned. A second search for picamilon with randomized, placebo, double-blind or controlled returned 5 records.

The first search returned 11 records. The human ones were the two open studies above, where sleep was a secondary scale in cerebral ischemia, and a Russian review of asthenia. The rest were animal or mechanism studies from 1984 to 2006, mostly in rats. None was a controlled trial of anxiety, stress or sleep in people with those complaints or in healthy people. The second search returned 5 records, and by title and abstract none was a placebo-controlled trial: an uncontrolled glaucoma series (1994), an uncontrolled prostate series (1999) whose author calls for placebo-controlled studies, the ginkgo combination study, a 94-patient glaucoma comparison of mexidol plus picamilon against picamilon alone in which picamilon was the comparator (PMID 23808185), and the open regimen comparison. The anxiety, clarity, sleep and stress-resilience claims have no controlled human trial among these records.

Participants / model
Records returned, not a population
Treatment
Not applicable
Follow-up
Searches run on 10 October 2026
Study design
Literature search
Funding
not stated in the source

A search result shows what PubMed returned on that date. It is not proof that no unindexed study exists.

Read the original source
In silico and in vitro screen: weak or no binding at 50 targets

Cell study

Santillo MF et al. Basic Clin Pharmacol Toxicol. 2023;132(4):355-358. PMID 36668678.

A screen of picamilon against 50 safety-related targets (receptors, ion channels, enzymes, transporters) found weak or no binding in silico and in vitro at 10 micromolar, so picamilon does not share the binding profile of GABA analogues with a similar structure. The authors state there are few in silico, in vitro and in vivo safety data for picamilon.

Participants / model
In silico and in vitro screen; no people or animals
Treatment
Picamilon at 10 micromolar
Follow-up
Not applicable
Study design
Original in vitro study
Funding
not stated in the source

The authors work at the FDA's food-safety center, and the paper is research, not FDA policy. It is cell-free and in-silico work, not evidence of any effect in people.

Read the original source

Studies and sources

Picamilon leaflet: nootropic, anxiolytic and anti-asthenic wording; label PK statements

Official label

Russian-language patient leaflet for Picamilon 20 mg and 50 mg tablets (sodium nicotinoyl-gamma-aminobutyrate), registration number printed as R N000851/01. Copy hosted on medi.ru; version date not shown.

The leaflet describes a nootropic that widens cerebral vessels and has tranquilizing and psychostimulating action. Its listed uses include cerebrovascular insufficiency, asthenia, depression in the elderly, states with anxiety, fear or irritability, migraine prevention, glaucoma, urinary disorders, and improving tolerance of physical and mental loads, including restoring work capacity in athletes. It states that with courses the drug normalizes sleep and reduces anxiety. It states oral bioavailability of 50 to 88% and a half-life of 0.51 hours, with no source given. Listed side effects are irritability, excitement, anxiety, dizziness, headache, nausea and allergic reactions. It is contraindicated in hypersensitivity, chronic renal failure, pregnancy, lactation and under age 3.

Participants / model
Adults, and children over 3 for some uses
Treatment
Picamilon 20 mg and 50 mg oral tablets
Follow-up
Version date not shown
Study design
Russian-language patient leaflet, copy hosted on a drug-information site
Funding
not stated in the source

These are label descriptions, not trial results, and they match the supplier wording closely. A Russian registration is not an FDA or EMA review. The copy was read on a commercial drug-information site, not on the Russian state register.

Read the original source
FDA constituent update: warning letters to five companies, 30 November 2015

Regulatory record

U.S. Food and Drug Administration. Recent FDA action on dietary supplements labeled as containing picamilon, constituent update current as of 30 November 2015.

On 30 November 2015 FDA issued warning letters to five companies whose dietary supplements claimed to contain picamilon. FDA's constituent update says these products are misbranded because picamilon does not meet the statutory definition of a dietary ingredient.

Participants / model
Not a clinical population
Treatment
Dietary supplement products labeled as containing picamilon
Follow-up
Update current as of 30 November 2015
Study design
Official FDA record
Funding
not stated in the source

Later FDA actions were not examined.

Read the original source
31 picamilon supplements: 30 contained it, 2.7 to 721.5 mg per serving

Analytical product survey

Avula B et al. Drug Test Anal. 2016;8(3-4):334-43. PMID 26426301.

Of 31 picamilon dietary supplements bought from a variety of US retailers, 30 contained picamilon, from 2.7 to 721.5 mg per recommended daily serving. The authors state picamilon has never been approved by the FDA and note it is prescribed in many countries for cerebrovascular disorders. Consumers could not get accurate dose information from labels.

Participants / model
31 commercial supplement products
Treatment
Dietary supplements, mixed forms
Follow-up
Not applicable
Study design
Analytical product survey
Funding
not stated in the source

A product analysis, not a study in people.

Read the original source
10 cognitive enhancement supplements: 5 unapproved drugs, 9 of 12 declared amounts inaccurate

Analytical product survey

Cohen PA et al. Neurol Clin Pract. 2021;11(3):e303-e307. PMID 34484905.

In 10 cognitive enhancement supplements bought online and tested, 5 unapproved drugs were found, including phenibut, vinpocetine and picamilon, at up to 90.1 mg of picamilon per recommended serving. Several detected drugs were not on the label, and 9 of 12 declared quantities were inaccurate.

Participants / model
10 commercial supplement products
Treatment
Dietary supplements, mixed forms
Follow-up
Not applicable
Study design
Analytical product survey
Funding
not stated in the source

A product analysis, not a study in people. The 12 declared quantities cover all the drugs the products declared, not picamilon alone.

Read the original source
In silico and in vitro screen: weak or no binding at 50 targets

Cell study

Santillo MF et al. Basic Clin Pharmacol Toxicol. 2023;132(4):355-358. PMID 36668678.

A screen of picamilon against 50 safety-related targets (receptors, ion channels, enzymes, transporters) found weak or no binding in silico and in vitro at 10 micromolar, so picamilon does not share the binding profile of GABA analogues with a similar structure. The authors state there are few in silico, in vitro and in vivo safety data for picamilon.

Participants / model
In silico and in vitro screen; no people or animals
Treatment
Picamilon at 10 micromolar
Follow-up
Not applicable
Study design
Original in vitro study
Funding
not stated in the source

The authors work at the FDA's food-safety center, and the paper is research, not FDA policy. It is cell-free and in-silico work, not evidence of any effect in people.

Read the original source
Open cohort: 50 patients, single arm, MoCA and sleep scores rose, no control group

Clinical trial

Danilov AB et al. Zh Nevrol Psikhiatr Im S S Korsakova. 2024;124(8):71-80. PMID 39269299.

MoCA scores rose over the three visits (20.9, 24.6, 25.9), sleep normalized in 55% by visit 2 and 81% by visit 3, and Doppler flow velocity rose.

Participants / model
50 patients with stage II chronic cerebral ischemia
Treatment
Picamilon 200 mg intravenously for 10 days then 50 mg tablets three times a day for 60 days
Follow-up
10 days intravenously then 60 days orally
Study design
Open-label single-arm cohort, Russian-language
Funding
not stated in the source

There was no placebo or control group, so none of this can be attributed to the drug. Endpoints were MoCA, a sleep scale, Doppler cerebral blood flow and endothelial markers.

Read the original source
Regimen comparison: 44 patients, two picamilon regimens, no placebo

Clinical trial

Danilov AB et al. Zh Nevrol Psikhiatr Im S S Korsakova. 2024;124(7):119-130. PMID 39113452.

By the end the cognitive effect was comparable between regimens (p = 0.508). The abstract reports good tolerability in 98% of patients and adverse events at under 8.6%, without stating the denominator.

Participants / model
44 patients aged 46 to 67 with stage I chronic cerebral ischemia
Treatment
Picamilon 50 mg three times a day for 60 days (n = 23), or 100 mg intramuscularly for 10 days then tablets (n = 21)
Follow-up
60 days
Study design
Open randomized comparison of two regimens, small, Russian-language, no placebo
Funding
not stated in the source

The two regimens were compared with each other and not with placebo. Endpoints were MoCA, autonomic, neurological and sleep scales, Doppler and adverse events.

Read the original source
Combination product: 278 patients, 90 days, versus ginkgo alone

Clinical trial

Zakharov VV et al. Zh Nevrol Psikhiatr Im S S Korsakova. 2022;122(9):95-103. PMID 36168693.

The combination gave greater cognitive gains (MMSE p = 0.007, MoCA p = 0.0003) and no significant difference on the Hamilton depression scale.

Participants / model
278 patients over 45 with chronic cerebral ischemia and cognitive impairment
Treatment
Oral Picamilon Ginkgo (139 patients) versus ginkgo biloba extract alone (139)
Follow-up
90 days
Study design
Open multicenter randomized study of a combination product, Russian-language
Funding
not stated in the source

The product contains ginkgo, so the result cannot be credited to picamilon alone. Endpoints were MoCA, MMSE, the Hamilton depression scale and EQ-5D.

Read the original source
Swimmers: brain blood filling after warm-up, no performance outcome

Human study

Likhodeev VA et al. Eksp Klin Farmakol. 2009;72(4):15-9. PMID 19803364.

The abstract reports changes in brain blood filling and venous outflow 20 minutes after a warm-up load. One group (hypokinetic, on picamilon) did not show the change.

Participants / model
Swimmers with a dysadaptation syndrome; group sizes not stated
Treatment
Oral picamilon 0.10 g for 4 weeks, with other groups given aminalon 0.25 g or phenibut 0.25 g, as a recovery aid
Follow-up
4 weeks
Study design
Clinical study, Russian-language; design not stated
Funding
not stated in the source

The abstract gives no group sizes, no placebo group, and no performance, anxiety or sleep outcome. Endpoints were cerebral hemodynamics before and after warm-up.

Read the original source
PubChem: picamilon free acid and sodium salt identity

Chemical identity record

National Library of Medicine. PubChem compound records CID 60608 (picamilon) and CID 23663986 (picamilon sodium).

Picamilon as the free acid (N-nicotinoyl-GABA, 4-(pyridine-3-carbonylamino)butanoic acid): PubChem CID 60608, C10H12N2O3, 208.21 g/mol, CAS 34562-97-5. The sodium salt, which the Russian leaflet names as the active substance: CID 23663986, C10H11N2NaO3, 230.20 g/mol, CAS 62936-56-5.

Participants / model
Chemical identity, not a clinical population
Treatment
Defined free acid and sodium salt
Follow-up
Not applicable
Study design
NLM chemical record
Funding
not stated in the source

A supplement labeled picamilon may be either form, and the same milligrams of each hold about 11% different amounts of picamilon, going by molecular weight (230.20 versus 208.21). Identity record only; it says nothing about efficacy or safety.

Read the original source

Why is Picamilon in D tier?

D fits a drug registered in Russia whose leaflet wording the supplier repeats, with no controlled human trial of the claimed anxiety, clarity, sleep or stress outcomes. The human data are small open or uncontrolled studies in cerebral ischemia, a combination product study and one swimmer study without performance outcomes. FDA's position that supplements containing picamilon are misbranded, and supplement contents that vary widely, add to the case for a low grade.