PreclinicalResearch compound

Picamilon

Nicotinic acid + GABA conjugate, Russian prescription anxiolytic.

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WHAT IS PICAMILON?

Detailed overview

Picamilon (Pikatropin) is a Soviet development (1969, All-Union Vitamin Research Institute) in which nicotinic acid (vitamin B3) is linked to GABA by an amide bond. The nicotinic acid moiety **causes cerebral vasodilation**, supporting brain blood flow; after crossing the BBB the conjugate hydrolyzes → **GABA + nicotinic acid** are released. Moderate activation of GABA-A and GABA-B provides anxiolytic and mild sedative effects with a substantially lower dependence risk than Phenibut (shorter half-life ~0.5 h, fast clearance). Clinically used in Russia for migraine, vascular cognitive impairment, and asthenic syndrome. **The FDA removed it from US supplement market in 2015** on the grounds that it does not meet the dietary supplement definition (it is a synthetic drug).

Mechanism

GABA prodrug + vasodilation

Half-life

~0.5 h (rapid hydrolysis)

Legal status

Russia Rx / USA: removed (2015)

Safety

Side effects, stop signs, contraindications

Side effects · 6

  • Niacin flush: skin redness, warmth, itching (from the nicotinic acid moiety)
  • Lowered blood pressure, dizziness from cerebral vasodilation
  • Mild sedation, drowsiness, lethargy (GABAergic effect)
  • Headache, feeling of head pressure
  • Nausea, gastric upset, irritability
  • At excessive doses the GABAergic effect can cause rebound anxiety

Contraindications · 6

  • Pregnancy and breastfeeding: no safety data, avoid
  • Low blood pressure (hypotension): vasodilation may worsen it
  • Severe renal or hepatic disease (clearance/metabolism affected)
  • Concurrent use with other GABAergic or sedative agents, alcohol (additive sedation)
  • Antihypertensive medication: enhanced hypotensive effect
  • Active peptic ulcer or gout: nicotinic acid may aggravate

Related Nootropics

Same therapeutic category

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MolekulaX Editorial Team·Source-verified · PubMed · FDA · EMA
Updated: June 19, 2026

The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.