Picamilon

Unapproved Nootropicprescriptionoral · inferred

Synthetic conjugate of nicotinic acid and GABA used as a prescription drug in some countries but not FDA approved and not a lawful US dietary ingredient. A small healthy-volunteer study established rapid, dose-proportional oral plasma exposure, but controlled evidence for cognitive enhancement is not established and supplement labeling has been shown to be highly unreliable.

Projected serum levels — 50 mg, once daily

Picamilon
Picamilon modeled serum levels, 50 mg once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 1 days. 0 6.3 12.5 18.8 25 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 1

Maintenance schedule: 50 mg once daily (oral).

Modeled steady state after ~1 days: peak ≈ 22.0 mg, trough ≈ 0.000 mg body load. Population-based estimate over 15 days for a 50 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Unapproved Nootropic
Route modeled
Oral
Model confidence
inferred
Half-life
41 min
Common dose
50 mg
Suggested maximum
200 mg/day
Reference dose range
12.5–200 mg (single dose)
Suggested cadence
once daily
Validated against
50 mg oral — Cmax 1.3 mg/L at 0.73 h

Research behind this entry

  1. Determination of picamilon concentration in human plasma by liquid chromatography-tandem mass spectrometry Cui W, Chen X, Zhan Y, Zhang Z, Zhang Y, Zhong D · Journal of Chromatography B, 2010 DOI

    Validated LC-MS/MS assay was applied to healthy-volunteer oral dosing and confirmed linear plasma exposure over single 50-200 mg doses. The linked pharmacokinetic report found rapid peaks near 0.7 hours and elimination…

  2. Identification and quantification of vinpocetine and picamilon in dietary supplements sold in the United States Avula B, Chittiboyina AG, Sagi S, Wang YH, Wang M, Khan IA, Cohen PA · Drug Testing and Analysis, 2016 DOI

    Laboratory testing found picamilon in 30 of 31 labeled supplements, with recommended daily servings ranging from 2.7 to 721.5 mg. The extreme label-content variability shows why a user-entered dose cannot guarantee…

  3. Picamilon, a GABA analogue and marketed nootropic, is inactive against 50 biological targets Santillo MF, Sprando RL · Basic and Clinical Pharmacology and Toxicology, 2023 DOI

    In-silico and in-vitro screening found weak or no activity at 50 selected safety-related receptors, channels, enzymes, and transporters at 10 micromolar. This negative panel does not establish clinical efficacy or rule…

3 published studies referenced in the app, each with a plain-language summary.