Picamilon

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Picamilon
Picamilon2d.png
Picamilon3d.png
Systematic (IUPAC) name
4-(Pyridine-3-carbonylamino)butanoic acid
Clinical data
Trade names НПК ЭХО
Legal status OTC US Rx only Russia
Routes Oral
Pharmacokinetic data
Bioavailability 50%–88%
Half-life 30 minutes
Excretion Renal
Identifiers
CAS number 34562-97-5 N
ATC code N02CX
PubChem CID 60608
ChemSpider 54634 YesY
Synonyms nicotinoyl-GABA
Chemical data
Formula C10H12N2O3 
Mol. mass 208.214 g/mol
 N (what is this?)  (verify)

Picamilon (also known as nicotinoyl-GABA, pycamilon, and pikamilon) is a dietary supplement formed by combining niacin with GABA. It was developed in the Soviet Union in 1969 by the All-Union Vitamins Scientific Research Institute[1][2][full citation needed] and further studied in both Russia[3] and Japan as a prodrug of GABA.[4]

Picamilon is sold in the United States as a dietary supplement, while in Russia it is sold as a prescription drug. The rights to the drug belong to the Russian pharmaceutical company NPK ECHO ("НПК ЭХО").

Mechanism of action and potential therapeutic applications[edit]

Picamilon is able to cross the blood–brain barrier[5] and then is hydrolyzed into GABA and niacin.[citation needed] The released GABA in theory would activate GABA receptors potentially producing an anxiolytic response.[6] The second released component, niacin acts as a strong vasodilator,[7] which might be useful for the treatment of migraine headaches.[8][9]

Medical use in Russia[edit]

Picamilon
Picamilon 20 mg from Russia

In Russia, Picamilon is used for treatment of these illness.[10]

  1. Violations of cerebral blood flow (ischemic acute, subacute and rehabilitation period of ischemic stroke, chronic insufficiency of cerebral blood flow);
  2. Vasoneurosis;
  3. Asthenia;
  4. Depression;
  5. Senile psychosis;
  6. Alcohol (period of abstinence), acute alcohol intoxication;
  7. Migraine
  8. Craniocerebral trauma
  9. Neuroinfections;
  10. Primary open-angle glaucoma (for stabilization of visual function).

References[edit]

  1. ^ Kopelevich VM, Gunar VI (April 1999). "Some approaches to the directed search for new drugs based on nicotinic acid". Pharmaceutical Chemistry Journal 33 (4): 177–187. doi:10.1007/BF02509934. 
  2. ^ Kopelevich VM, Shmuylovichem LM, Trubnikov VI.  Missing or empty |title= (help)
  3. ^ Mirzoian RS, Gan'shina TS (1989). "[The new cerebrovascular preparation pikamilon]". Farmakologiia i toksikologiia (in Russian) 52 (1): 23–6. PMID 2707413. 
  4. ^ Matsuyama K, Yamashita C, Noda A, Goto S, Noda H, Ichimaru Y, Gomita Y (October 1984). "Evaluation of isonicotinoyl-gamma-aminobutyric acid (GABA) and nicotinoyl-GABA as pro-drugs of GABA". Chem. Pharm. Bull. 32 (10): 4089–95. PMID 6529802. 
  5. ^ Dorofeev BF, Kholodov LE (1991). "[Pikamilon pharmacokinetics in animals]". Farmakologiia i toksikologiia (in Russian) 54 (2): 66–9. PMID 1884802. 
  6. ^ Shephard RA (June 1987). "Behavioral effects of GABA agonists in relation to anxiety and benzodiazepine action". Life Sci. 40 (25): 2429–36. doi:10.1016/0024-3205(87)90758-2. PMID 2884549. 
  7. ^ Gille A, Bodor ET, Ahmed K, Offermanns S (2008). "Nicotinic acid: pharmacological effects and mechanisms of action". Annu. Rev. Pharmacol. Toxicol. 48: 79–106. doi:10.1146/annurev.pharmtox.48.113006.094746. PMID 17705685. 
  8. ^ Pukhal'skaia TG, Maĭsov NI, Mirzoian RS (1989). "[The effect of antimigraine preparations on serotonin transport in the brain synaptosomes of rats]". Farmakol Toksikol (in Russian) 52 (6): 39–43. PMID 2625145. 
  9. ^ Prousky J, Seely D (2005). "The treatment of migraines and tension-type headaches with intravenous and oral niacin (nicotinic acid): systematic review of the literature". Nutr J 4: 3. doi:10.1186/1475-2891-4-3. PMC 548511. PMID 15673472. 
  10. ^ "Пикамилон". Энциклопедия лекарств. Регистр лекарственных средств России. 

External links[edit]