Eprosartan

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Eprosartan
Eprosartan.svg
Systematic (IUPAC) name
4-({2-Butyl-5-[2-carboxy-2-(thiophen-2-ylmethyl)eth-1-en-1-yl]-1H-imidazol-1-yl}methyl)benzoic acid
Clinical data
Trade names Teveten
AHFS/Drugs.com monograph
MedlinePlus a601237
Legal status
?
Routes Oral
Pharmacokinetic data
Bioavailability 15% (Eprosartan mesylate)
Metabolism not metabolized
Half-life 5 to 9 hours
Excretion Renal 10%, biliary 90%
Identifiers
CAS number 133040-01-4 YesY
ATC code C09CA02
PubChem CID 5281037
DrugBank DB00876
ChemSpider 4444504 YesY
UNII 2KH13Z0S0Y YesY
KEGG D04040 YesY
ChEBI CHEBI:4814 YesY
ChEMBL CHEMBL813 YesY
Chemical data
Formula C23H24N2O4S 
Mol. mass Eprosartan mesylate: 520.625 g/mol
 YesY (what is this?)  (verify)

Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. It is marketed as Teveten by Abbvie in the United States.It is marketed as Eprozar by INTAS Pharmaceuticals in India and by Abbott Laboratories elsewhere. It is sometimes paired with hydrochlorothiazide, marketed in the US as Teveten HCT and elsewhere as Teveten Plus.

The drug acts on the renin-angiotensin system in two ways to decrease total peripheral resistance. First, it blocks the binding of angiotensin II to AT1 receptors in vascular smooth muscle, causing vascular dilatation. Second, it inhibits sympathetic norepinephrine production, further reducing blood pressure.

As with other angiotensin II receptor antagonists, eprosartan is generally better tolerated than enalapril (an ACE inhibitor), especially among the elderly.[1]

Synthesis[edit]

Eprosartan synthesis:[2]

See also[edit]

References[edit]

  1. ^ 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. 
  2. ^ Higley, C. A.; Wilde, R. G.; Maduskuie, T. P.; Johnson, A. L.; Pennev, P.; Billheimer, J. T.; Robinson, C. S.; Gillies, P. J.; Wexler, R. R. (1994). "Acyl CoA:Cholesterol Acyltransferase (ACAT) Inhibitors: Synthesis and Structure-Activity Relationship Studies of a New Series of Trisubstituted Imidazoles". Journal of Medicinal Chemistry 37 (21): 3511. doi:10.1021/jm00047a009.  edit

External links[edit]