Amisulprid

Amisulprid
(IUPAC) ime
	(RS)-4-amino-N-[(1-etilpirolidin-2-il)metil]-; 5-etilsulfonil-2-metoksi-benzamid
Klinički podaci
AHFS/Drugs.com	Internacionalno ime leka
Identifikatori
CAS broj	71675-85-9
ATC kod	N05AL05
PubChem	2159
DrugBank	DB06288
ChemSpider	2074
UNII	8110R61I4U
KEGG	D07310
ChEMBL	CHEMBL243712
Hemijski podaci
Formula	C17H27N3O4S
Mol. masa	369,48 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C17H27N3O4S/c1-4-20-8-6-7-12(20)11-19-17(21)13-9-16(25(22,23)5-2)14(18)10-15(13)24-3/h9-10,12H,4-8,11,18H2,1-3H3,(H,19,21) ; Key: NTJOBXMMWNYJFB-UHFFFAOYSA-N
Farmakokinetički podaci
Bioraspoloživost	48%
Metabolizam	?
Poluvreme eliminacije	12 h
Izlučivanje	Renalno
Farmakoinformacioni podaci
Trudnoća	B3(AU)
Pravni status	℞ Prescription only
Način primene	Oralno, intramuskularno

Amisulprid (Amazeo, Torent, Solian, Sulpitak, Amitreks, Soltus) je atipični antipsihotik koji se koristi za lečenje psihoze u šizofreniji i epizoda manije u bipolarnom poremećaju. On se takođe koristi u malim dozama za lečenje depresije. Ovaj lek je razvila kompanija Sanofi-Aventis tokom 1990-tih.^[8]^[9]

Farmakologija

Amisulprid prvenstveno deluje kao antagonist D₂ i D₃ receptora. On ima visok afinitet za te receptore sa konstantom disocijacije od 2.8 nM i 3.2 nM, respektivno. Mada standardne doze u opsegu 400 do 1200 mg na dan, koje se koriste za lečenje psihoze, inhibiraju dopaminergičku neurotransmisiju, niske doze u opsegu 50 do 200 mg preferentno blokiraju inhibitorne presinaptičke autoreceptore. To rezultuje u olakšavanju dopamina aktivnosti, iz tog razloga, niske doze amisulprida se takođe koriste za lečenje kliničke depresije.

Reference

↑ ^1,0 ^1,1 „Amisulpride” (French). BIAM online. 2000. Arhivirano iz originala na datum 2012-04-15. Pristupljeno 2014-04-05.
↑ 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
↑ ^7,0 ^7,1 ^7,2 Rosenzweig, P.; Canal, M.; Patat, A.; Bergougnan, L.; Zieleniuk, I.; Bianchetti, G. (2002). „A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers.”. Human Psychopharmacology 17 (1): 1–13. DOI:10.1002/hup.320. PMID 12404702.
↑ Hardman JG, Limbird LE, Gilman AG. (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10 izd.). New York: McGraw-Hill. DOI:10.1036/0071422803. ISBN 0-07-135469-7.
↑ Pdr Staff (2009). PDR: Physicians Desk Reference 2010 (Physicians' Desk Reference (Pdr)). Rozelle, N.S.W: Thomson Reuters. ISBN 1-56363-748-0.

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	Portal Hemija
	Portal Medicina

Kategorije

[cas_biam-1] 1,0 ^1,1 „Amisulpride” (French). BIAM online. 2000. Arhivirano iz originala na datum 2012-04-15. Pristupljeno 2014-04-05.

[2] 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

[3] 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.

[4] 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

[5] 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.

[6] 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

[Rosenzweig-7] 7,0 ^7,1 ^7,2 Rosenzweig, P.; Canal, M.; Patat, A.; Bergougnan, L.; Zieleniuk, I.; Bianchetti, G. (2002). „A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers.”. Human Psychopharmacology 17 (1): 1–13. DOI:10.1002/hup.320. PMID 12404702.

[Goodman_Gilman-8] Hardman JG, Limbird LE, Gilman AG. (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10 izd.). New York: McGraw-Hill. DOI:10.1036/0071422803. ISBN 0-07-135469-7.

[PDR-9] Pdr Staff (2009). PDR: Physicians Desk Reference 2010 (Physicians' Desk Reference (Pdr)). Rozelle, N.S.W: Thomson Reuters. ISBN 1-56363-748-0.

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Amisulprid

Izvor: Wikipedija

Farmakologija

Reference

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