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	5281037
DrugBank	DB00876
ChemSpider	4444504
UNII	2KH13Z0S0Y
KEGG	D04040
ChEBI	CHEBI:4814
ChEMBL	CHEMBL813
Hemijski podaci
Formula	C23H24N2O4S
Mol. masa	Eprosartan mesilat: 520,625 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C23H24N2O4S/c1-2-3-6-21-24-14-19(12-18(23(28)29)13-20-5-4-11-30-20)25(21)15-16-7-9-17(10-8-16)22(26)27/h4-5,7-12,14H,2-3,6,13,15H2,1H3,(H,26,27)(H,28,29)/b18-12+ ; Key: OROAFUQRIXKEMV-LDADJPATSA-N
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[uredi | uredi kod]

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[uredi | uredi kod]

↑ 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[uredi | uredi kod]

	Portal Medicina
	Portal Hemija

Teveten website Arhivirano 2008-02-09 na Wayback Machine-u

[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

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Eprosartan

Osobine[uredi | uredi kod]

Reference[uredi | uredi kod]

Spoljašnje veze[uredi | uredi kod]

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