Tetrabenazin (Nitoman, Ksenazin) je lek za simptomatički tretman hiperkinetikog poremećaja kretanja. FDA je augusta 2008. odobrila njegovu upotrebu za tretman horeje vezane za Hantingtonovu bolest.[6] Ovo jedinjenje je poznato od 1950-tih. Inicijativu za FDA odobrenje je predvodio Josef Janković.[7][8]

Tetrabenazin
(IUPAC) ime
(SS,RR)-3-Izobutil-9,10-dimetoksi-1,3,4,6,7,11b-heksahidro-pirido[2,1-a]izohinolin-2-on
Klinički podaci
Robne marke Ksenazin
AHFS/Drugs.com Potrošačka informacije o leku
Identifikatori
CAS broj 58-46-8
ATC kod N07XX06
PubChem[1][2] 6018
DrugBank DB04844
ChemSpider[3] 5796
UNII Z9O08YRN8O DaY
KEGG[4] D08575 DaY
ChEMBL[5] CHEMBL117785 DaY
Hemijski podaci
Formula C19H27NO3 
Mol. masa 317,427 g/mol
SMILES eMolekuli & PubHem
Sinonimi Ro-1-9569
Farmakokinetički podaci
Bioraspoloživost Niska
Vezivanje za proteine plazme 82–85%
Metabolizam Hepatički (CYP2D6-posredovano)
Izlučivanje Renalno i fekalno
Farmakoinformacioni podaci
Trudnoća ?
Pravni status ℞-only (US)
Način primene Oralno (tablete, 25 mg)

Farmakologija uredi

Tetrabenazin deluje prvenstveno kao VMAT-inhibitor,[9] te promoviše ranu metaboličku degradaciju monoamina, posebno neurotransmitera dopamina.

Reference uredi

  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
  6. „1st US drug for Huntington's disease wins approval”. Arhivirano iz originala na datum 2020-02-13. Pristupljeno 2014-04-05. 
  7. Doctor spent decades getting tetrabenazine to market
  8. Specialty TrendsRx Availability Alert:Xenazine® (tetrabenazine)
  9. Zheng G, Dwoskin LP, Crooks PA (2006). „Vesicular monoamine transporter 2: role as a novel target for drug development”. AAPS J 8 (4): E682–92. DOI:10.1208/aapsj080478. PMC 2751365. PMID 17233532. 

Spoljašnje veze uredi