Nefazodon

Nefazodon
(IUPAC) ime
	1-(3-[4-(3-hlorofenil)piperazin-1-il]propil)-3-etil-4-(2-fenoksietil)-1H-1,2,4-triazol-5(4H)-on
Klinički podaci
AHFS/Drugs.com	Monografija
MedlinePlus	a695005
Identifikatori
CAS broj	83366-66-9
ATC kod	N06AX06
PubChem	4449
DrugBank	DB01149
ChemSpider	4294
UNII	59H4FCV1TF
KEGG	D08257
ChEBI	CHEBI:7494
ChEMBL	CHEMBL623
Hemijski podaci
Formula	C25H32ClN5O2
Mol. masa	470,01 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C25H32ClN5O2/c1-2-24-27-31(25(32)30(24)18-19-33-23-10-4-3-5-11-23)13-7-12-28-14-16-29(17-15-28)22-9-6-8-21(26)20-22/h3-6,8-11,20H,2,7,12-19H2,1H3 ; Key: VRBKIVRKKCLPHA-UHFFFAOYSA-N
Farmakokinetički podaci
Bioraspoloživost	20% (promenljiva)
Vezivanje za proteine plazme	>99%
Metabolizam	Hepatički (aktivni metaboliti, uključujući mCPP)
Poluvreme eliminacije	2–4 sato
Izlučivanje	Urin (55%), fekalije (20–30%)
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	℞ Prescription only
Način primene	Oralnot

Nefazodon (Serzon, Nefadar) je antidepresiv. Njegova prodaja je prekinuta 2003. u nekim zemljama zbog retke pojave hepatotoksičnosti (oštećenja jetra), koje može da dovede do potrebe za transplantom jetre, pa i smrti. Učestalos ozbiljnog oštećenja jetre je oko 1 na svakih 250.000 do 300.000 pacijenata godišnje.^[7] Prodaja je prekinuta 2004. u SAD-u i Kanadi. Nekoliko generičkih formulacija nefazodona je još uvek dostupno.^[8]^[9]

Hemija[uredi | uredi kod]

Nefazadon je piperazinsko jedinjenje koje sadrži 1,2,4-triazol-3-onski prsten.

Reference[uredi | uredi kod]

↑ 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
↑ 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. edit
↑ 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. edit
↑ Lexi-Comp (September 2008). „Nefazodone”. The Merck Manual Professional. Retrieved on November 29, 2008.
↑ Rxlist.com: "Nefazodone Prescribing Information" Arhivirano 2008-08-25 na Wayback Machine-u, accessed 8 January 2007.]
↑ FDA Orange Book, accessed 15 January 2006.
↑ About.com: "Serzone Pulled from U.S. Market", accessed 15 January 2006.^{[mrtav link]}

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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

[Lexi-Comp-6] Lexi-Comp (September 2008). „Nefazodone”. The Merck Manual Professional. Retrieved on November 29, 2008.

[pi-7] Rxlist.com: "Nefazodone Prescribing Information" Arhivirano 2008-08-25 na Wayback Machine-u, accessed 8 January 2007.]

[fdaob-8] FDA Orange Book, accessed 15 January 2006.

[about-9] About.com: "Serzone Pulled from U.S. Market", accessed 15 January 2006.^{[mrtav link]}

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Nefazodon

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