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Picamilon

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Picamilon
File:Picamilon2d.png
File:Picamilon3d.png
Systematic (IUPAC) name
4-(Pyridine-3-carbonylamino)butanoic acid
Clinical data
Trade names НПК ЭХО
Oral
Pharmacokinetic data
Bioavailability 50%–88%
Half-life 30 minutes
Excretion Renal
Identifiers
34562-97-5 7pxN
N02CX
PubChem CID 60608
ChemSpider 54634 7pxY
UNII 0S5N9SEK4N 7pxY
Synonyms nicotinoyl-GABA
Chemical data
Formula C10H12N2O3
208.214 g/mol
 14pxN (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

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

File:Picamilon.jpg
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 (weakness);
  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

  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. doi:10.1248/cpb.32.4089. 
  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. PMID 2884549. doi:10.1016/0024-3205(87)90758-2. 
  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. PMID 17705685. doi:10.1146/annurev.pharmtox.48.113006.094746. 
  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. PMC 548511. PMID 15673472. doi:10.1186/1475-2891-4-3. 
  10. ^ "Пикамилон". Энциклопедия лекарств. Регистр лекарственных средств России. 

External links