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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/11/27 05:51:33」(JST)

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Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. It is marketed in the United States as Teveten by Abbvie, the spin-off of the pharmaceutical discovery division of Abbott Laboratories; it is marketed as Eprozar by INTAS Pharmaceuticals in India, and by Abbott Laboratories elsewhere. The compound came into the Abbott Laboratories cardiovascular pipeline with its acquisition of Kos Pharmaceuticals in 2006, which had licensed it, along with "a range of hypertensive treatments", from the Biovail Corporation.^[1]

Eprosartan is sometimes paired with hydrochlorothiazide, whereupon it is marketed in the US as Teveten HCT and elsewhere as Teveten Plus.

The drug acts on the renin-angiotensin system to decrease total peripheral resistance in two ways. 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.^[2]

References

^ Anon., 2006, Abbott Laboratories: Kos Pharmaceuticals a wise buy, Datamonitor ResearchStore (online), November 8, 2006, see [1], accessed 29 January 2015.
^ 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.

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English Journal

Identification and determination of selected angiotensin II receptor antagonist group drugs by HPLC method.

Czerwińska K, Mazurek AP.SourceBasic and Applied Pharmacy Department, National Medicines Institute, 30/34 Chełmska St., 00-725 Warszawa, Poland. kczerwinska@il.waw.pl
Acta poloniae pharmaceutica.Acta Pol Pharm.2011 Nov-Dec;68(6):831-7.
Losartan potassium, valsartan, telmisartan, irbesartan, eprosartan mesylate and candesartan cilexitil, the angiotensin II receptor antagonists, were analyzed in bulk substances and in tablets: Lorista tablets 50 mg, Diovan tablets 160 mg, Micardis tablets 20 mg, Aprovel tablets 300 mg, Teveten table
PMID 22125946

Eprosartan mesylate, an angiotensin II receptor antagonist.

Qian JJ, Hu XR, Gu J, Wu SX.AbstractThe title compound, eprosartan mesylate {systematic name: 2-butyl-1-(4-carb-oxy-benz-yl)-5-[(E)-2-carb-oxy-3-(thio-phen-2-yl)prop-1-en-yl]-1H-imidazol-3-ium methane-sulfonate}, C(23)H(25)N(2)O(4)S(+)·CH(3)O(3)S(-), one of the angiotensin II-receptor antagonists, is effective in regulating hypertension, induced or exacerbated by angiotensin II, and in the treatment of congestive heart failure, renal failure and glaucoma. In the eprosartan residue, which appears in this crystal in the cationic imidazolium form, the benzene ring plane is almost orthogonal to that of the imidazole ring, making a dihedral angle of 87.89 (2)°. The thio-phene ring forms dihedral angles of 66.54 (2) and 67.12 (2)° with the benzene and imidazole rings, respectively. The imidazolium NH group and the H atom of the aromatic carboxyl group participate in hydrogen bonds with the the O atoms of the anion, thus forming centrosymmetric aggregates made up of two cations and two anions each. The second carboxyl group further links the above-mentioned aggregates through a conventional centrosymmetric hydrogen-bonding motif into infinite chains along [011].
Acta crystallographica. Section E, Structure reports online.Acta Crystallogr Sect E Struct Rep Online.2011 Apr 1;67(Pt 4):o770-1. Epub 2011 Mar 2.
The title compound, eprosartan mesylate {systematic name: 2-butyl-1-(4-carb-oxy-benz-yl)-5-[(E)-2-carb-oxy-3-(thio-phen-2-yl)prop-1-en-yl]-1H-imidazol-3-ium methane-sulfonate}, C(23)H(25)N(2)O(4)S(+)·CH(3)O(3)S(-), one of the angiotensin II-receptor antagonists, is effective in regulating hypertens
PMID 21754064

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リンク元	「エプロサルタン」「メシル酸エプロサルタン」
関連記事	「mesylate」「eprosartan」

「エプロサルタン」

Eprosartan
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
Routes of; administration	Oral
Pharmacokinetic data
Bioavailability	15% (Eprosartan mesylate)
Metabolism	not metabolized
Biological half-life	5 to 9 hours
Excretion	Renal 10%, biliary 90%
Identifiers
CAS Number	133040-01-4
ATC code	C09CA02
PubChem	CID: 5281037
IUPHAR/BPS	588
DrugBank	DB00876
ChemSpider	4444504
UNII	2KH13Z0S0Y
KEGG	D04040
ChEBI	CHEBI:4814
ChEMBL	CHEMBL813
Chemical data
Formula	C23H24N2O4S
Molecular mass	Eprosartan mesylate: 520.625 g/mol
	SMILES O=C(O)\C(=C\c1cnc(n1Cc2ccc(C(=O)O)cc2)CCCC)Cc3sccc3 ;
	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 ;
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