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 Y | ||
KEGG[4] | D04040 Y | ||
ChEBI | CHEBI:4814 Y | ||
ChEMBL[5] | CHEMBL813 Y | ||
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
- ↑ 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
- ↑ 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.
- ↑ 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.
- ↑ 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
- ↑ 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
Portal Medicina | |
Portal Hemija |
- Teveten website Arhivirano 2008-02-09 na Wayback Machine-u
- p
- r
- u
("-pril")
Dikarboksilat: Enalapril# • Ramipril • Kvinapril • Perindopril • Lisinopril • Benazepril
Ostali/negrupisani: Alacepril • Cilazapril • Delapril • Imidapril • Moeksipril • Rentiapril • Spirapril • Temokapril • Trandolapril("-sartan")
("-kiren")
|