Picamilon

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Picamilon
Clinical data
Trade namesНПК ЭХО
Other namesnicotinoyl-GABA
Routes of
administration		Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability50%–88%
Elimination half-life30 minutes
ExcretionRenal
Identifiers
  • 4-(Pyridine-3-carbonylamino)butanoic acid
JSmol)
  • O=C(NCCCC(=O)O)c1cccnc1
  • 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) checkY
  • Key:NAJVRARAUNYNDX-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Picamilon (also known as N-nicotinoyl-GABA, pycamilon, and pikamilon) is a drug formed by a synthetic combination of

γ-aminobutyric acid (GABA). It was developed in the Soviet Union in 1969[2] and further studied in both Russia[3] and Japan as a prodrug of GABA.[4]

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 an adulterating agent in

dietary supplements,[5] with five American companies required to remove their picamilon products from the market in November, 2015.[6] However, as recently as 2020, picamilon has been found in pharmaceutical dosages in over-the-counter supplements in the US.[7]

Mechanism of action and potential therapeutic applications

One study in animals showed that picamilon permeated the

vasodilator.[11][12]

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.[13] 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.[13]

Picamilon
Picamilon 20 mg from Russia

Regulation

In the United States, the

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 that had been marketed in the United States before 1994. Despite the FDA ruling, picamilon remains an ingredient in supplements marketed as nootropics in the US.[7]

References

  1. FDA
    . November 29, 2017. Retrieved June 9, 2023.
  2. S2CID 36930437
    .
  3. PMID 2707413
    .
  4. PMID 6529802
    .
  5. PMID 26426301
    .
  6. ^ a b "FDA sends five warning letters over supplements containing picamilon". NutraIngredients-USA.com, William Reed Business Media. 2 December 2015. Retrieved 3 December 2015.
  7. ^
    PMID 34484905
    .
  8. PMID 1884802
    .
  9. ^ "Technical Description of Picamilon". Archived from the original on 2018-11-09. Retrieved 2015-10-22.
  10. PMID 2884549
    .
  11. PMID 17705685
    .
  12. PMID 15673472
    .
  13. ^
    PMID 20359966
    .
  14. ^ Welch C. "Declaration of Dr. Cara Welch" (PDF). Department of Health and Human Services. Retrieved 21 October 2015.

External links

Retrieved from "https://en.wikipedia.org/w/index.php?title=Picamilon&oldid=1188096242"