Share to: share facebook share twitter share wa share telegram print page

Eprosartan

Eprosartan
(IUPAC) ime
4-({2-Butil-5-[2-karboksi-2-(tiofen-2-ilmetil)et-1-en-1-il]-1H-imidazol-1-il}metil)benzojeva kiselina
Klinički podaci
Robne marke Teveten
AHFS/Drugs.com Monografija
MedlinePlus a601237
Identifikatori
CAS broj 133040-01-4
ATC kod C09CA02
PubChem[1][2] 5281037
DrugBank DB00876
ChemSpider[3] 4444504
UNII 2KH13Z0S0Y DaY
KEGG[4] D04040 DaY
ChEBI CHEBI:4814 DaY
ChEMBL[5] CHEMBL813 DaY
Hemijski podaci
Formula C23H24N2O4S 
Mol. masa Eprosartan mesilat: 520,625 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost 15% (Eprosartan mesilat)
Metabolizam ne metabolizuje se
Poluvreme eliminacije 5 do 9 Sati
Izlučivanje Renalno 10%, bilijarno 90%
Farmakoinformacioni podaci
Trudnoća ?
Pravni status
Način primene Oralno

Eprosartan je antagonist angiotenzin II receptora koji se koristi za tretiranje visokog krvnog pritiska. Preduzeće Abbott Laboratories prodaje ovaj lek pod imenom Teveten u SAD i većini drugih zemalja. Preduzeće INTAS Pharmaceuticals ga prodaje pod imenom Eprozar u Indiji. U jednoj od formulacija se eprosartan zajedno sa hidrohlorotiazidom prodaje kao Teveten HCT (SAD) i TevetenPlus.

Poput drugih antagonista angiotenzin II receptora, eprosartan je generalno bolje tolerisan od enalaprila (ACE inhibitora), posebno među osobama u godinama.[6]

Osobine

Osobina Vrednost
Broj akceptora vodonika 5
Broj donora vodonika 2
Broj rotacionih veza 10
Particioni koeficijent[7] (ALogP) 4,8
Rastvorljivost[8] (logS, log(mol/L)) -7,4
Polarna površina[9] (PSA, Å2) 120,7

Reference

  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. Ruilope L, Jäger B, Prichard B (2001). „Eprosartan versus enalapril in elderly patients with hypertension: a double-blind, randomized trial”. Blood Press. 10 (4): 223–9. DOI:10.1080/08037050152669747. PMID 11800061. 
  7. Ghose, A.K., Viswanadhan V.N., and Wendoloski, J.J. (1998). „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragment Methods: An Analysis of AlogP and CLogP Methods”. J. Phys. Chem. A 102: 3762-3772. DOI:10.1021/jp980230o. 
  8. Tetko IV, Tanchuk VY, Kasheva TN, Villa AE. (2001). „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Chem Inf. Comput. Sci. 41: 1488-1493. DOI:10.1021/ci000392t. PMID 11749573.  edit
  9. Ertl P., Rohde B., Selzer P. (2000). „Fast calculation of molecular polar surface area as a sum of fragment based contributions and its application to the prediction of drug transport properties”. J. Med. Chem. 43: 3714-3717. DOI:10.1021/jm000942e. PMID 11020286.  edit

Spoljašnje veze

Kembali kehalaman sebelumnya