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Kvetijapin Садржај Farmakologija Sinteza Reference Literatura Spoljašnje veze Мени за навигацијуMonografijaa698019111974-69-7WHO500250DB012244827BGL0JSY5SID08456CHEBI:8707CHEMBL716Details for SeroquelPatent Document, U.S. Patent and Trademark OfficeBlockbuster Drugs That Will Go Generic SoonSeroquel patent expiration„Quepin Full Prescribing Information in Drug Reference Encyclopedia”„SEROQUEL (quetiapine fumarate) tablet, extended release”„Seroquel (quietapine fumarate) tablets”оригинала„Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds”1113224310.1016/S0024-3205(00)00911-5Neuropsychopharmacology: the fifth ... - Google BooksSeroquel Official FDA information, side effects and usesU.S. Patent 4.879.288Neuropsychopharmacology: the fifth ... - Google Books„Quetiapine”NAMI pregledууууу

Атипични антипсихотициДопамински антагонистиСеротонински антагонистиХипнотициСедативиПиперазиниДибензотиазепиниЕтриАлкохоли


atipični antipsihotikšizofrenijebipolarnog poremećajadepresiju20112012Quetiapine syn.pngAzaperonBenperidolBromperidolDroperidolFluanizonHaloperidolLenperonMoperonPipamperonSpiperonTimiperonTrifluperidolKlopimozidFluspirilenPenfluridolPimozidAcepromazinAcetofenazinButaperazinKarfenazinHloracizinHlorproetazinHlorpromazinCijamemazinDiksirazinFluacizinFlufenazinLevomepromazin/MetotrimeprazinMezoridazinPerazinPericijazinPerfenazinPiperacetazinPipotiazinProhlorperazinPromazinPrometazinPropiomazinSulforidazinTietilperazinTiopropazatTioproperazinTioridazinTrifluoperazinTriflupromazinHlorprotiksenKlopentiksolFlupentiksolTiotiksenZuklopentiksolButaklamolFluotracenLoksapinTrimipraminCinuperonMelperonSetoperonIloperidonOkaperidonPaliperidonRisperidonLurasidonePerospironRevospironTiospironZiprasidonAmperozidAripiprazolBifeprunoksBrekspiprazolElopiprazolUmespironAmoksapinAsenapinKarpipraminKlocapraminKlorotepinKlotiapinKlozapinFluperlapinGevotrolinMetitepinMosapraminNDMCOlanzapinPihindonKvetijapinTenilapinZotepinWHO-EMPovučeniKlinička ispitivanjaFaza IIINije dospeo do faze IIIMPSOPSImeprdsrdodbpasspecspvoprocN5A5B5C6A6B6D










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Kvetijapin




Из Википедије, слободне енциклопедије

(преусмерено са Kvetiapin)





Иди на навигацију
Иди на претрагу


Kvetijapin
Quetiapine.svgQuetiapine-from-xtal-3D-balls.png
IUPAC ime
2-(2-(4-dibenzo[b,f][1,4]tiazepin- 11-il- 1-piperazinil)etoksi)etanol
Klinički podaciProdajno ime
Serokvel
Drugs.com
Monografija
MedlinePlus
a698019
Kategorija trudnoće


  • US: C (Mogući rizik)

Način primene
Oralnot
Pravni statusPravni status



  • US: ℞-only



Farmakokinetički podaciBioraspoloživost
9%
Metabolizam
Hepatički
Poluvreme eliminacije
6 sata
Izlučivanje
Renalno

IdentifikatoriCAS broj

111974-69-7 ДаY
ATC kod

N05AH04 (WHO)
PubChem
CID 5002

IUPHAR/BPS
50
DrugBank

DB01224 ДаY
ChemSpider

4827 ДаY
UNII

BGL0JSY5SI ДаY
KEGG

D08456 ДаY
ChEBI

CHEBI:8707 ДаY
ChEMBL

CHEMBL716 ДаY
Hemijski podaciFormula

C21H25N3O2S

Molarna masa
383,5099 g/mol



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.[1] Američki patent,[2] je trebalo da istekne 2011, ali je njegov vek produžen radi pedijatrijske ekskluzivnosti do marta 2012.[3][4][5]




Садржај





  • 1 Farmakologija


  • 2 Sinteza


  • 3 Reference


  • 4 Literatura


  • 5 Spoljašnje veze




Farmakologija

































Poređenje afiniteta (Ki, nM)[6]
Receptor
Kvetijapin
Norkvetijapin
D142899.8
D2626489
5-HT1A1040191
5-HT2A382.9
α1B14.646.4
α26171290
H14.411.15
M1108638.3
NET>1000034.8

Kvetijapin poseduje sledeća farmakološka dejstva:[7][8][9][10]



  • D1 (IC50 = 1268nM), D2 (IC50 = 329nM), D3, i D4 receptor antagonist


  • 5-HT1A (IC50 = 717nM), 5-HT2A (IC50 = 148nM), 5-HT2C, and 5-HT7 receptor antagonist


  • α1-adrenergički (IC50 = 94nM) i α2-adrenergički receptor (IC50 = 271nM) antagonist


  • H1 receptor (IC50 = 30nM) antagonist


  • mACh receptor (IC50 = >5000nM) antagonist


Sinteza


Jedan od mogućih sintetičkih puteva je:[11]


Quetiapine syn.png



Reference




  1. ^ Details for Seroquel


  2. ^ Patent Document, U.S. Patent and Trademark Office


  3. ^ Blockbuster Drugs That Will Go Generic Soon


  4. ^ Seroquel patent expiration


  5. ^ „Quepin Full Prescribing Information in Drug Reference Encyclopedia”. Приступљено 3. 4. 2010. 


  6. ^ AstraZeneca Pharmaceuticals LP (2011). „SEROQUEL (quetiapine fumarate) tablet, extended release”. DailyMed. National Library of Medicine. Section 12.2: Pharmacodynamics. Приступљено 26. 4. 2011. 


  7. ^ AstraZeneca. „Seroquel (quietapine fumarate) tablets” (PDF). 276521. Архивирано из оригинала (PDF) на датум 14. 04. 2008. Приступљено 23. 03. 2012. 


  8. ^ Richelson E, Souder T (2000). „Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds”. Life Sciences. 68 (1): 29—39. PMID 11132243. doi:10.1016/S0024-3205(00)00911-5. 


  9. ^ Davis, Kenneth L; Neuropsychopharmacology, American College of (2002). Neuropsychopharmacology: the fifth ... - Google Books. ISBN 9780781728379. 


  10. ^ Seroquel Official FDA information, side effects and uses


  11. ^ Warawa, E. J.; Migler, B. M.; 1988, U.S. Patent 4.879.288.



Literatura



  • Davis, Kenneth L; Neuropsychopharmacology, American College of (2002). Neuropsychopharmacology: the fifth ... - Google Books. ISBN 9780781728379. 


Spoljašnje veze




  • „Quetiapine”. MedlinePlus. The American Society of Health-System Pharmacists, Inc. 1. 9. 2008. 

  • NAMI pregled









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