Gvanfacin
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(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 ![]() | ||
KEGG[4] | D08031 ![]() | ||
ChEMBL[5] | CHEMBL862 ![]() | ||
Hemijski podaci | |||
Formula | C9H9Cl2N3O | ||
Mol. masa | 246,093 g/mol | ||
SMILES | eMolekuli & PubHem | ||
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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]
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- Intuniv Arhivirano 2012-08-06 na Wayback Machine-u