Gvanfacin

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	3519
DrugBank	DB01018
ChemSpider	3399
UNII	30OMY4G3MK
KEGG	D08031
ChEMBL	CHEMBL862
Hemijski podaci
Formula	C9H9Cl2N3O
Mol. masa	246,093 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C9H9Cl2N3O/c10-6-2-1-3-7(11)5(6)4-8(15)14-9(12)13/h1-3H,4H2,(H4,12,13,14,15) ; Key: INJOMKTZOLKMBF-UHFFFAOYSA-N
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 α_2A receptora. Ti receptori su koncentrisani u prefrontalnom korteksu, te guanfacin potencijalno može da poboljša sposobnost pažnje putem modulisanja postsinaptičkih α_2A 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

↑ 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
↑ 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 .
↑ 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 .
↑ 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 .

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Intuniv Arhivirano 2012-08-06 na Wayback Machine-u

[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

[Kolar-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 .

[Jerie-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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