Kvetijapin
Kvetijapin (Serokvel, Ketipinor) je atipični antipsihotik koji je odorobren za lečenje šizofrenije, bipolarnog poremećaja i kao dodatni tretman za depresiju.
![]() | |||
![]() | |||
(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 ![]() | ||
KEGG[4] | D08456 ![]() | ||
ChEBI | CHEBI:8707 ![]() | ||
ChEMBL[5] | CHEMBL716 ![]() | ||
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 |
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
urediReceptor | 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]
- 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
urediJedan od mogućih sintetičkih puteva je:[16]
Reference
uredi- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ Details for Seroquel
- ↑ „Patent Document, U.S. Patent and Trademark Office”. Arhivirano iz originala na datum 2017-01-06. Pristupljeno 2014-04-05.
- ↑ Blockbuster Drugs That Will Go Generic Soon
- ↑ Seroquel patent expiration
- ↑ „Quepin Full Prescribing Information in Drug Reference Encyclopedia”. Pristupljeno 3. 4. 2010.
- ↑ AstraZeneca Pharmaceuticals LP (March 2011). „SEROQUEL (quetiapine fumarate) tablet, extended release”. DailyMed. National Library of Medicine. Section 12.2: Pharmacodynamics. Pristupljeno 26. 4. 2011.
- ↑ AstraZeneca (PDF). Seroquel (quietapine fumarate) tablets. 276521. Arhivirano iz originala na datum 2008-04-14. Pristupljeno 2014-04-05.
- ↑ 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.
- ↑ Davis, Kenneth L; Neuropsychopharmacology, American College of (2002). Neuropsychopharmacology: the fifth ... - Google Books. ISBN 9780781728379.
- ↑ Seroquel Official FDA information, side effects and uses
- ↑ Warawa, E. J.; Migler, B. M.; 1988, U.S. Patent 4.879.288.
Literatura
uredi- Davis, Kenneth L; Neuropsychopharmacology, American College of (2002). Neuropsychopharmacology: the fifth ... - Google Books. ISBN 9780781728379.
Spoljašnje veze
uredi- „Quetiapine”. MedlinePlus. The American Society of Health-System Pharmacists, Inc.. 1. 9. 2008..
- NAMI pregled Arhivirano 2003-09-25 na Wayback Machine-u