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]
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  Y
|
| KEGG[4]
|
D08031 Y
|
| ChEMBL[5]
|
CHEMBL862 Y
|
| 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) Y
Key: INJOMKTZOLKMBF-UHFFFAOYSA-N Y |
|
| 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
|
- ↑ 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 .
