eprosartan

エプロサルタン

関

eprosartan mesylate

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/08/03 19:44:01」(JST)

wiki en

[Wiki en表示]

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 Y
ATC code	C09CA02 (WHO)
PubChem	CID 5281037
IUPHAR/BPS	588
DrugBank	DB00876 Y
ChemSpider	4444504 Y
UNII	2KH13Z0S0Y Y
KEGG	D04040 Y
ChEBI	CHEBI:4814 Y
ChEMBL	CHEMBL813 Y
Chemical data
Formula	C23H24N2O4S
Molar 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+ Y Key:OROAFUQRIXKEMV-LDADJPATSA-N Y
(verify)

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.

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.

See also

• Discovery and development of angiotensin receptor blockers

References

External links

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

• 1. 心臓におけるアンギオテンシンⅡの作用 actions of angiotensin ii on the heart

English Journal

• Formulation and statistical optimization of self-microemulsifying drug delivery system of eprosartan mesylate for improvement of oral bioavailability.

• Dangre P1,2, Gilhotra R3, Dhole S4.
• Drug delivery and translational research.Drug Deliv Transl Res.2016 Oct;6(5):610-21. doi: 10.1007/s13346-016-0318-7.
• The present investigation is aimed to design a statistically optimized self-microemulsifying drug delivery system (SMEDDS) of eprosartan mesylate (EM). Preliminary screening was carried out to find a suitable combination of various excipients for the formulation. A 3(2) full factorial design was emp
• PMID 27465619

• Angiotensin II, hypertension, and angiotensin II receptor antagonism: Roles in the behavioural and brain pathology of a mouse model of Alzheimer's disease.

• Wiesmann M1, Roelofs M2, van der Lugt R2, Heerschap A3, Kiliaan AJ2, Claassen JA4.
• Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism.J Cereb Blood Flow Metab.2016 Sep 5. pii: 0271678X16667364. [Epub ahead of print]
• Elevated angiotensin II causes hypertension and contributes to Alzheimer's disease by affecting cerebral blood flow. Angiotensin II receptor blockers may provide candidates to reduce (vascular) risk factors for Alzheimer's disease. We studied effects of two months of angiotensin II-induced hypertens
• PMID 27596834

• Acute eprosartan-induced intrarenal vasodilation in hypertensive humans is not influenced by dietary sodium intake or angiotensin II co-infusion.

• van Twist DJ1, Houben AJ, de Leeuw PW, Kroon AA.
• Journal of hypertension.J Hypertens.2016 Aug;34(8):1607-14. doi: 10.1097/HJH.0000000000000974.
• BACKGROUND: Angiotensin II (Ang II) is thought to play an important role in the development of hypertension. Nevertheless, knowledge on the angiotensin II type-1-receptors (AT1Rs) in the hypertensive kidney and the influence of sodium intake and renin-angiotensin system activity on intrarenal AT1R b
• PMID 27214088

Japanese Journal

• Determination of eprosartan in human plasma and urine by LC/MS/MS

• Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 853(1), 47-53, 2007-06-15
• NAID 10025803552

• PE-573 Combinational Use of Rosuvastatin with Eprosartan or Ramipril Enhances Inhibition of Monocyte Chemoattractant Protein, Interleukin-6, and Cyclooxygenase-2 in Endothelial Cells(Endothelium-4 (H) PE99,Poster Session (English),The 70th Anniversary Annual Scientific Meeting of the Japanese Circulation Society)

• Circulation journal : official journal of the Japanese Circulation Society 70(Supplement_I), 476, 2006-03-01
• NAID 110005942675

• Morbidity and mortality after stroke, eprosartan compared with nitrendipine for secondary prevention : principal results of a prospective randomized controlled study (MOSES)

• Stroke 36, 1218-1226, 2005
• NAID 30022682084

Related Pictures

---

★リンクテーブル★

リンク元	「エプロサルタン」
拡張検索	「eprosartan mesylate」

「エプロサルタン」

　　[★]

英

eprosartan、eprosartan mesylate

関

メシル酸エプロサルタン

「eprosartan mesylate」

　　[★]

• メシル酸エプロサルタン

関

eprosartan