Picamilon

Picamilon

Systematic (IUPAC) name
4-(Pyridine-3-carbonylamino)butanoic acid
Clinical data
Trade names	НПК ЭХО
Legal status	US: Not FDA approved; unscheduled RU: OTC
Routes of administration	Oral
Pharmacokinetic data
Bioavailability	50%–88%
Biological half-life	30 minutes
Excretion	Renal
Identifiers
CAS Number	34562-97-5 N
ATC code	N02CX (WHO)
PubChem	CID: 60608
ChemSpider	54634 Y
UNII	0S5N9SEK4N Y
Synonyms	nicotinoyl-GABA
Chemical data
Formula	C10H12N2O3
Molecular mass	208.214 g/mol
SMILES O=C(NCCCC(=O)O)c1cccnc1
InChI InChI=1S/C10H12N2O3/c13-9(14)4-2-6-12-10(15)8-3-1-5-11-7-8/h1,3,5,7H,2,4,6H2,(H,12,15)(H,13,14) Y Key:NAJVRARAUNYNDX-UHFFFAOYSA-N Y
NY (what is this?)  (verify)

Picamilon (also known as N-nicotinoyl-GABA, pycamilon, and pikamilon) is a drug formed by a synthetic combination of niacin and GABA. It was developed in the Soviet Union in 1969 and further studied in both Russia and Japan as a prodrug of GABA.

In Russia, picamilon is sold as a prescription drug. The rights to the drug belong to the Russian pharmaceutical company NPK ECHO ("НПК ЭХО"). It is not approved for sale in the United States and has been deemed as an adulterating agent in dietary supplements, with five American companies required to remove their picamilon products from the market in November, 2015.

Mechanism of action and potential therapeutic applications

One study in animals showed that picamilon penetrated the blood–brain barrier and then is hydrolyzed into GABA and niacin. The released GABA in theory would activate GABA receptors potentially producing an anxiolytic response. The second released component, niacin, is a vasodilator.

Detection in biological fluids

Plasma picamilon concentrations are generally in the 500–3000 μg/L range during the first few hours after single oral doses of 50–200 mg with a half-life of 1–2 hours. The drug undergoes hydrolysis to GABA and nicotinic acid. Urinary excretion of parent drug and the two metabolites accounts for up to 79% of a single dose.

Picamilon 20 mg from Russia

Regulation

In the United States, the Food and Drug Administration ruled in 2015 that picamilon does not fit any of the dietary ingredient categories in the Dietary Supplement Health and Education Act of 1994, namely that it is not a vitamin; a dietary mineral; an herb or other botanical; an amino acid; a dietary substance for use by humans to supplement the diet by increasing the total dietary intake; or a concentrate, metabolite, constituent, extract, or combination of any ingredient described above. This led to the removal of picamilon as a pure substance or from various supplements manufactured in the US.

External links

• nicotinoyl-GABA at the US National Library of Medicine Medical Subject Headings (MeSH)