Gvanfacin

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Gvanfacin
(IUPAC) ime
N-(diaminometiliden)-2-(2,6-dihlorofenil)acetamid
Klinički podaci
Robne marke Tenex, Intuniv
AHFS/Drugs.com Monografija
MedlinePlus a601059
Identifikatori
CAS broj 29110-47-2
ATC kod C02AC02
PubChem[1][2] 3519
DrugBank DB01018
ChemSpider[3] 3399
UNII 30OMY4G3MK YesY
KEGG[4] D08031 YesY
ChEMBL[5] CHEMBL862 YesY
Hemijski podaci
Formula C9H9Cl2N3O 
Mol. masa 246,093 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost 99,9%
Metabolizam CYP3A4
Poluvreme eliminacije 14,8–18,3 h
Izlučivanje renal
Farmakoinformacioni podaci
Trudnoća ?
Pravni status Prescription only
Način primene oralno, intravenozno

Guanfacin (Teneks, Intuniv) je simpatolitik. On je selektivni agonist α2A receptora. Ti receptori su koncentrisani u prefrontalnom korteksu, te guanfacin potencijalno može da poboljša sposobnost pažnje putem modulisanja postsinaptičkih α2A receptora.[6] Guanfacin snižava sistolni i dijastolni krvni pritisak putem aktivacije α-2a norepinefrinskih autoreceptora centralnog nervnog sistema, što dovodi do redukcije perifernog simpatetičkog odliva i stoga do redukcije perifernog simpatetičkog tona.[7] Njegove nuspojave su zavisne od doze. Pri dozama do 2 mg efekat suvih usta se praktično ne javlja.[8]

Reference[uredi - уреди | uredi kôd]

  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. http://www.sciencedirect.com/science/article/pii/S1359644610007737.  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. http://www.jcheminf.com/content/2/1/3.  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. http://onlinelibrary.wiley.com/doi/10.1002/%28SICI%291097-0061%28200004%2917:1%3C48::AID-YEA2%3E3.0.CO;2-H/full. 
  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. Kolar, Dusan; Keller, Amanda; Golfinopoulos, Maria; Cumyn, Lucy; Syer, Cassidy & Hechtman, Lily (2008), „Treatment of adults with attention-deficit/hyperactivity disorder”, Neuropsychiatric Disease and Treatment 4 (2): 389–403, PMC 2518387, PMID 18728745 .
  7. Van Zwieten, P.; Thoolen, M. & Timmermans, P. (1983), „The pharmacology of centrally acting antihypertensive drugs”, British Journal of Clinical Pharmacology 15 (Suppl 4): 455S–462S, PMC 1427667 .
  8. Jerie, P. (1980), „Clinical experience with guanfacine in long-term treatment of hypertension: Part II: adverse reactions to guanfacine”, British Journal of Clinical Pharmacology 10 (Suppl 1): 157S–164S, PMC 1430125, PMID 6994770 .

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