Buspiron (Buspar) je anksiolitički psihoaktivni lek iz azapironske hemijske klase. On se prvenstveno koristi za tretiranje generalizovanog anksioznog poremećaja.

Buspiron
(IUPAC) ime
8-[4-(4-pirimidin-2-ilpiperazin-1-il)butil]-8-azaspiro[4.5]dekan-7,9-dion
Klinički podaci
Robne marke Buspar
AHFS/Drugs.com Monografija
MedlinePlus a688005
Identifikatori
CAS broj 36505-84-7
ATC kod N05BE01
PubChem[1][2] 2477
DrugBank DB00490
ChemSpider[3] 2383
UNII TK65WKS8HL YesY
KEGG[4] D07593 YesY
ChEBI CHEBI:3223 YesY
ChEMBL[5] CHEMBL49 YesY
Hemijski podaci
Formula C21H31N5O2 
Mol. masa 385,50314 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost 5%
Vezivanje za proteine plazme 95%
Metabolizam Hepatic
Poluvreme eliminacije 2-3 sata
Izlučivanje Urin (29-63%), izmet (18-38%)
Farmakoinformacioni podaci
Trudnoća B(US)
Pravni status Prescription only
Način primene Oralno

Medicinska upotrebaUredi

  • Generalizovani anksiozni poremećaj blagog do umerenog intenziteta.[6]

HemijaUredi

Sinteza buspirona počinje sa N-alkilacijom 1-(2-pirimidil)piperazina sa 4-hlorobutironitrilom čemu sledi hidrogenacija nitrila preko Ranejev nikal katalizatora. Primarni aminski produkt prethodnog koraka sa spirocikličnim kiselim anhidridom daje buspiron.[10]

 

ReferenceUredi

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). "Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining". J Cheminform 2 (1): 3. PMID 20331846. doi:10.1186/1758-2946-2-3.  edit
  4. Joanne Wixon, Douglas Kell (2000). "Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG". Yeast 17 (1): 48–55. doi:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. 
  5. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  6. "Buspirone monograph". Drugs.com. http://www.drugs.com/pro/buspirone.html. Pristupljeno 27. 8. 2011.. 
  7. National Institute Of Health. "Questions and Answers about the NIMH Sequenced Treatment Alternatives to Relieve Depression (STAR*D) Study — All Medication Levels". http://www.nimh.nih.gov/trials/practical/stard/allmedicationlevels.shtml. Pristupljeno 12. 8. 2012.. 
  8. Trivedi MH, Fava M, Wisniewski SR, Thase ME, Quitkin F, Warden D, Ritz L, Nierenberg AA, Lebowitz BD, Biggs MM, Luther JF, Shores-Wilson K, Rush AJ (March 2006). "Medication augmentation after the failure of SSRIs for depression". N. Engl. J. Med. 354 (12): 1243–52. PMID 16554526. doi:10.1056/NEJMoa052964. 
  9. Appelberg BG, Syvälahti EK, Koskinen TE, Mehtonen OP, Muhonen TT, Naukkarinen HH (June 2001). "Patients with severe depression may benefit from buspirone augmentation of selective serotonin reuptake inhibitors and in a Class of Drugs called Benzodiazepines and effects similar if not idenical to Alprazelam,Lorazepam etc : results from a placebo-controlled, randomized, double-blind, placebo wash-in study". J Clin Psychiatry 62 (6): 448–52. PMID 11465522. 
  10. Wu YH, Rayburn JW, Allen LE, Ferguson HC, Kissel JW (May 1972). "Psychosedative agents. 2. 8-(4-Substituted 1-piperazinylalkyl)-8-azaspiro(4.5)decane-7,9-diones". J. Med. Chem. 15 (5): 477–9. PMID 5035267. doi:10.1021/jm00275a009.  ;
    Rayburn JW, Wu YH, "Heterocyclische Azaspirodecandione und Verfahren zu ihrer Herstellung", DE patent 2057845, published 9. 6. 1971.
     ;
    Rayburn JW, Wu YH, "N-(heteroarcyclic)piperazinylalkyl-azaspiroalkanediones", US patent 3717634, published 20. 2. 1973. ;
    Rayburn JW, Wu YH, "N8 (4-pyridyl-piperazino)-alkyl9-azaspiroalkanediones", US patent 3907801, published 23. 9. 1975. ;
    Rayburn JW, Wu YH, "Tranquilizer process employing N-(heteroarcyclic)piperazinylalkylazaspiroalkanediones", US patent 3976776, published 24. 8. 1976. 

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