Roksatidin

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Roksatidin acetat
(IUPAC) ime
2-okso-2-(3-[3-(piperidin-1-ilmetil)fenoksi]propilamino)etil acetat
Klinički podaci
Identifikatori
CAS broj 78628-28-1
ATC kod A02BA06
PubChem[1][2] 5105
DrugBank DB08806
ChemSpider[3] 4926
UNII IV9VHT3YUM YesY
KEGG[4] D08495 YesY
ChEMBL[5] CHEMBL46102 YesY
Hemijski podaci
Formula C19H28N2O4 
Mol. masa 348,437 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost 80–90%
Vezivanje za proteine plazme 5–7%
Metabolizam Hepatička deacetilacija
Minje učešće CYP2D6 i CYP2A6
Poluvreme eliminacije 5–7 sata
Izlučivanje Renalno
Farmakoinformacioni podaci
Trudnoća ?
Pravni status
Način primene Oralno

Roksatidin acetat je specifični i kompetitivni antagonist H2 receptora. Antisekretorno dejstvo roksatidin acetata je posredovano njegovim glavnim metabolitom, roksatidinom.

Farmakodinamičke studije su pokazale da je 150 mg roksatidin acetata optimalno u suzbijanju sekrecije želudačne kiseline.[6]

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. Murdoch D, McTavish D (1991). „Roxatidine acetate. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic potential in peptic ulcer disease and related disorders”. Drugs 42 (2): 240-260. PMID 1717223. http://ukpmc.ac.uk/abstract/MED/1717223. 

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