Kvetijapin

Izvor: Wikipedia
Kvetijapin
(IUPAC) ime
2-(2-(4-dibenzo[b,f][1,4]tiazepin- 11-il- 1-piperazinil)etoksi)etanol
Klinički podaci
Robne marke Serokvel
AHFS/Drugs.com Monografija
MedlinePlus a698019
Identifikatori
CAS broj 111974-69-7
ATC kod N05AH04
PubChem[1][2] 5002
DrugBank DB01224
ChemSpider[3] 4827
UNII BGL0JSY5SI YesY
KEGG[4] D08456 YesY
ChEBI CHEBI:8707 YesY
ChEMBL[5] CHEMBL716 YesY
Hemijski podaci
Formula C21H25N3O2S 
Mol. masa 383,5099 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost 9%
Metabolizam Hepatički
Poluvreme eliminacije 6 sata
Izlučivanje Renalno
Farmakoinformacioni podaci
Trudnoća C(US)
Pravni status -only (SAD)
Način primene Oralnot

Kvetijapin (Serokvel, Ketipinor) je atipični antipsihotik koji je odorobren za lečenje šizofrenije, bipolarnog poremećaja i kao dodatni tretman za depresiju.

Godišnja prodaja ovog leka je vredna oko USD $5,7 milijardi globalno, do čega je $2.9 milijardi u SAD-u.[6] Američki patent,[7] je trebalo da istekne 2011, ali je njegov vek produžen radi pedijatrijske ekskluzivnosti do marta 2012.[8][9][10]

Farmakologija[uredi - уреди]

Poređenje afiniteta (Ki, nM)[11]
Receptor Kvetijapin Norkvetijapin
D1 428 99.8
D2 626 489
5-HT1A 1040 191
5-HT2A 38 2.9
α1B 14.6 46.4
α2 617 1290
H1 4.41 1.15
M1 1086 38.3
NET >10000 34.8

Kvetijapin poseduje sledeća farmakološka dejstva:[12][13][14][15]

Sinteza[uredi - уреди]

Jedan od mogućih sintetičkih puteva je:[16]

Quetiapine syn.png

Reference[uredi - уреди]

  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. doi:10.1016/j.drudis.2010.10.003. PMID 20970519.  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. doi:10.1186/1758-2946-2-3. PMID 20331846.  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. doi:10.1093/nar/gkr777. PMID 21948594.  edit
  6. Details for Seroquel
  7. Patent Document, U.S. Patent and Trademark Office
  8. Blockbuster Drugs That Will Go Generic Soon
  9. Seroquel patent expiration
  10. "Quepin Full Prescribing Information in Drug Reference Encyclopedia". http://www.theodora.com/drugs/quepin_tablets_specifar.html. pristupljeno 3. 4. 2010.. 
  11. AstraZeneca Pharmaceuticals LP (March 2011). "SEROQUEL (quetiapine fumarate) tablet, extended release". DailyMed. National Library of Medicine. Section 12.2: Pharmacodynamics. http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=41375#section-15.2. pristupljeno 26. 4. 2011.. 
  12. AstraZeneca. Seroquel (quietapine fumarate) tablets (PDF). 276521. 
  13. Richelson E, Souder T (November 2000). "Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds". Life Sciences 68 (1): 29–39. doi:10.1016/S0024-3205(00)00911-5. PMID 11132243. 
  14. Davis, Kenneth L; Neuropsychopharmacology, American College of (2002). Neuropsychopharmacology: the fifth ... - Google Books. ISBN 9780781728379. http://books.google.com/?id=BKwkonZwZD0C&pg=PA778#v=onepage&q=. 
  15. Seroquel Official FDA information, side effects and uses
  16. Warawa, E. J.; Migler, B. M.; 1988, U.S. Patent 4,879,288.

Literatura[uredi - уреди]

Spoljašnje veze[uredi - уреди]


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