About: Eprosartan     Goto   Sponge   NotDistinct   Permalink

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http://linked.open...gbank/description
  • Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. It 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. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Ruilope L, Jager B, Prichard B: Eprosartan versus enalapril in elderly patients with hypertension: a double-blind, randomized trial. Blood Press. 2001;10(4):223-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11800061 # Hedner T: The clinical profile of the angiotensin II receptor blocker eprosartan. J Hypertens Suppl. 2002 Jun;20(5):S33-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12184062 # Puig JG, Lopez MA, Bueso TS, Bernardino JI, Jimenez RT: Clinical profile of eprosartan. Cardiovasc Drugs Ther. 2002 Dec;16(6):543-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12766389 # Ruilope L, Jager B: Eprosartan for the treatment of hypertension. Expert Opin Pharmacother. 2003 Jan;4(1):107-14. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12517247 # de la Sierra A, Ram CV: Introduction: The pharmacological profile of eprosartan--implications for cerebrovascular and cardiovascular risk reduction. Curr Med Res Opin. 2007 Nov;23 Suppl 5:S1-3. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18093407 # Blankestijn PJ, Rupp H: Clinical profile of eprosartan: a different angiotensin II receptor blocker. Cardiovasc Hematol Agents Med Chem. 2008 Oct;6(4):253-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18855637 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • The terminal elimination half-life of eprosartan following oral administration is typically 5 to 9 hours. (en)
http://linked.open...ugbank/indication
  • For the management of hypertension alone or in combination with other classes of antihypertensive agents. Also used as a first-line agent in the treatment of diabetic nephropathy, as well as a second-line agent in the treatment of congestive heart failure (only in those intolerant of ACE inhibitors). (en)
http://linked.open...bank/manufacturer
sameAs
Title
  • Eprosartan (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Eprosartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT<sub>1</sub> receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland). There is also an AT<sub>2</sub> receptor found in many tissues but it is not known to be associated with cardiovascular homeostasis. Eprosartan does not exhibit any partial agonist activity at the AT<sub>1</sub> receptor. Its affinity for the AT<sub>1</sub> receptor is 1,000 times greater than for the AT<sub>2</sub> receptor. In vitro binding studies indicate that eprosartan is a reversible, competitive inhibitor of the AT<sub>1</sub> receptor. Eprosartan has also been shown to bind to AT<sub>1</sub> receptors both presynaptically and synaptically. Its action on presynaptic AT<sub>1</sub> receptors results in the inhibition of sympathetically stimulated noradrenaline release. Unlike ACE inhibitors, eprosartan and other ARBs do not interfere with response to bradykinins and substance P, which allows for the absence of adverse effects that are present in ACE inhibitors (eg. dry cough). (en)
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http://linked.open.../drugbank/synonym
  • Eprosartan (en)
  • Eprosartanum (en)
  • (e)-Alpha{[2-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazole-5-yl]methylene}-2-thiopheneproprionic acid (en)
  • Éprosartan (en)
  • (e)-2-Butyl-1-(P-carboxybenzyl)-alpha-2-thenylimidazole-5-acrylic acid (en)
  • (e)-3-[2-N-Butyl-1-{(4-carboxyphenyl)methyl}-1H-imidazol-5-yl]-2-(2-thienyl)methyl-2-propenoic acid (en)
http://linked.open...drugbank/toxicity
  • There was no mortality in rats and mice receiving oral doses of up to 3000 mg eprosartan/kg and in dogs receiving oral doses of up to 1000 mg eprosartan/kg. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • Take without regard to meals. (en)
http://linked.open.../drugbank/mixture
http://linked.open...nk/proteinBinding
  • Plasma protein binding of eprosartan is high (approximately 98%) and constant over the concentration range achieved with therapeutic doses. (en)
http://linked.open...ogy/drugbank/salt
  • (en)
http://linked.open...ynthesisReference
  • Richard T. Matsuoka, Peng Liu, "Process for preparing eprosartan using regioselective protection of 2,4-disubstituted-imidazole intermediates." U.S. Patent US6294675, issued June, 1992. (en)
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http://linked.open...ugbank/absorption
  • Absolute bioavailability following a single 300 mg oral dose of eprosartan is approximately 13%. Administering eprosartan with food delays absorption. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 133040-01-4 (en)
http://linked.open...gbank/containedIn
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