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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
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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
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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 |
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 |
Molecular mass |
Eprosartan mesylate: 520.625 g/mol |
SMILES
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O=C(O)\C(=C\c1cnc(n1Cc2ccc(C(=O)O)cc2)CCCC)Cc3sccc3
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InChI
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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
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Key:OROAFUQRIXKEMV-LDADJPATSA-N Y
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Y (what is this?) (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.[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]
See also
- Discovery and development of angiotensin receptor blockers
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.
External links
Antihypertensives: agents acting on the renin–angiotensin system (C09)
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ACE inhibitors
("-pril") |
- Sulfhydryl-containing: Captopril
- Zofenopril
- Dicarboxylate-containing: Enalapril#
- Ramipril
- Quinapril (+HCT)
- Perindopril
- Lisinopril (+HCT)
- Benazepril
- Phosphonate-containing: Fosinopril (+HCT)
- Other/ungrouped: Alacepril
- Cilazapril
- Delapril
- Imidapril
- Moexipril
- Rentiapril
- Spirapril
- Temocapril
- Trandolapril
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AIIRAs/
("-sartan") |
- Azilsartan
- Candesartan
- Eprosartan
- Fimasartan
- Irbesartan
- Losartan (+HCT)
- Olmesartan (+amlodipine)
- Tasosartan§
- Telmisartan (+HCT)
- Valsartan (+HCT, +amlodipine, +sacubitril)
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Renin inhibitors/
("-kiren") |
- Aliskiren (+amlodipine, +amlodipine and HCT)
- Remikiren§
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
Index of the circulatory system
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Description |
- Anatomy
- Arteries
- head and neck
- arms
- chest
- abdomen
- legs
- Veins
- head and neck
- arms
- chest
- abdomen and pelvis
- legs
- Development
- Cells
- Physiology
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Disease |
- Congenital
- Neoplasms and cancer
- Lymphatic vessels
- Injury
- Vasculitis
- Other
- Symptoms and signs
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|
Treatment |
- Procedures
- Drugs
- beta blockers
- channel blockers
- diuretics
- nonsympatholytic vasodilatory antihypertensives
- peripheral vasodilators
- renin–angiotensin system
- sympatholytic antihypertensives
- vasoprotectives
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UpToDate Contents
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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
Related Links
- Professional guide for Eprosartan Mesylate. Includes: pharmacology, pharmacokinetics, contraindications, interactions, adverse reactions and more. ... Drugs.com provides accurate and independent information on more than 24,000 ...
- WARNING: FETAL TOXICITY See full prescribing information for complete boxed warning. • When pregnancy is detected, discontinue Eprosartan mesylate tablets as soon as possible. • Drugs that act directly on the renin-angiotensin ...
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★リンクテーブル★
[★]
- 英
- eprosartan、eprosartan mesylate
- 関
- メシル酸エプロサルタン
[★]
- 英
- eprosartan mesylate
- 関
- エプロサルタン
[★]
- 関
- mesilate、methanesulfonate
[★]
エプロサルタン
- 関
- eprosartan mesylate