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Doksepin

Izvor: Wikipedija

smeša cis- i trans-izomera
(IUPAC) ime
(E,Z)-3-(dibenzo[b,e]oksepin-11(6H)-iliden)-N,N-dimetilpropan-1-amin
Klinički podaci
Robne marke Sinequan, Zonalon
AHFS/Drugs.com Monografija
MedlinePlus a682390
Identifikatori
CAS broj 1668-19-5
ATC kod N06AA12
PubChem[1][2] 3158
DrugBank DB01142
ChemSpider[3] 3046
UNII 5ASJ6HUZ7D DaY
KEGG[4] D07875 DaY
ChEBI CHEBI:4710 DaY
ChEMBL[5] CHEMBL101740 DaY
Hemijski podaci
Formula C19H21NO 
Mol. masa 279,376 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost Apsolutna: 25%
sa glavnim metabolitom desmetildoksepinom: 31%
Metabolizam Hepatički
Poluvreme eliminacije Doksepin 17 sati, glavni metabolit desmetildoksepin 51 sata
Izlučivanje Renalno
Farmakoinformacioni podaci
Trudnoća C(AU)
Pravni status Prescription only
Način primene Oralno, intramuskularno, IV

Doksepin je psihotropni agens sa svojstvima tricikličnog antidepresanta i anksiolitika. On je u prodaju pod nizom imena, kao što su Aponal, Adapin, Doksal, Deptran, Sinquan i Sinequan (Pfizer). U obliku doksepin hidrohlorida, on je aktivni sastojak u kremama (Zonalon i Ksepin) za tretmant dermatološkog svraba. Doksepin se takođe koristi za tratmant održavanja sna (Silenor).

Medicinska upotreba

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Doksepin se koristi za tretiranje depresije, anksioznih poremećaja, i kao secudarni tretman za hronične idiopatske urtikarije.[6]

Niska doza doksepina (3 do 6 mg) je odobrena od strane FDA za upotrebu u tretmanu insomnije.[7][8]

Farmakologija

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Doksepin inhibira preuzimaje serotonina i norepinefrina. Njegov uticaj na preuzimaje dopamina je zanemarljiv. Doksepin je takođe antagonist više receptora:

Reference

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  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. „Doxepin”. The American Society of Health-System Pharmacists. Pristupljeno 3. 4. 2011. 
  7. „Phase 3 Data Show New Insomnia Drug, Silenor(R), Effective Without Side Effects”. Medical News Today. 12. 04. 2006.. Pristupljeno 01. 02. 2008. 
  8. Hajak G, Rodenbeck A, Voderholzer U i dr.. (2001). „Doxepin in the treatment of primary insomnia: a placebo-controlled, double-blind, polysomnographic study”. J Clin Psychiatry 62 (6): 453–63. DOI:10.4088/JCP.v62n0609. PMID 11465523. 

Spoljašnje veze

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Portal Medicina
Portal Hemija
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Doksepin
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