Buspiron

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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

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

Medicinska upotreba[uredi - уреди | uredi izvor]

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

Hemija[uredi - уреди | uredi izvor]

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]

Buspirone synthesis.png

Reference[uredi - уреди | uredi izvor]

  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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