Eprosartan: Difference between revisions
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'''Eprosartan''' is an [[angiotensin II receptor antagonist]] used for the treatment of [[hypertension|high blood pressure]]. It is marketed as '''Teveten''' by [[Abbvie]] |
'''Eprosartan''' is an [[angiotensin II receptor antagonist]] used for the treatment of [[hypertension|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]].<<Anon., 2006, Abbott Laboratories: Kos Pharmaceuticals a wise buy, Datamonitor ResearchStore (online), November 8, 2006, see [http://www.datamonitor.com/store/News/abbott_laboratories_kos_pharmaceuticals_a_wise_buy?productid=0BE8B1AB-14F9-4B92-99D2-80E8DC7ECA16], accessed 29 January 2015.</ref> |
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Eprosartan is sometimes paired with [[hydrochlorothiazide]], whereupon it is marketed in the US as '''Teveten''' '''HCT''' and elsewhere as '''Teveten''' '''Plus'''.''' |
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⚫ | The drug acts on the [[renin-angiotensin system]] |
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⚫ | 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 AT<sub>1</sub> receptors in vascular [[smooth muscle]], causing vascular dilatation. Second, it inhibits [[sympathetic nervous system|sympathetic]] [[norepinephrine]] production, further reducing blood pressure. |
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As with other angiotensin II receptor antagonists, eprosartan is generally better tolerated than [[enalapril]] (an [[ACE inhibitor]]), especially among the elderly.<ref>{{cite journal |author=Ruilope L, Jäger B, Prichard B |title=Eprosartan versus enalapril in elderly patients with hypertension: a double-blind, randomized trial |journal=Blood Press. |volume=10 |issue=4 |pages=223–9 |year=2001 |pmid=11800061 |doi=10.1080/08037050152669747}}</ref> |
As with other angiotensin II receptor antagonists, eprosartan is generally better tolerated than [[enalapril]] (an [[ACE inhibitor]]), especially among the elderly.<ref>{{cite journal |author=Ruilope L, Jäger B, Prichard B |title=Eprosartan versus enalapril in elderly patients with hypertension: a double-blind, randomized trial |journal=Blood Press. |volume=10 |issue=4 |pages=223–9 |year=2001 |pmid=11800061 |doi=10.1080/08037050152669747}}</ref> |
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==Synthesis== |
==Synthesis== |
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The following is a medicinal chemistry (early discovery stage) synthesis of eprosartan from [[Merck & Co.|Merck]] research into [[QSAR]] of this class of drug, which represents an approach to the construction of its carbon skeleton (though which is not necessarily related to the actual manufacturing synthesis of the on-market drug). Note, the reagents indicated alongside the arrows are a summary list, and are not complete for what is required in each transformation: |
The following is a medicinal chemistry (early discovery stage) synthesis of eprosartan from [[Merck & Co.|Merck]] research into [[QSAR]] of this class of drug, which represents an approach to the construction of its carbon skeleton (though which is not necessarily related to the actual manufacturing synthesis of the on-market drug). Note, the reagents indicated alongside the arrows are a summary list, and are not complete for what is required in each transformation: |
Revision as of 14:41, 29 January 2015
Clinical data | |
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Trade names | Teveten |
AHFS/Drugs.com | Monograph |
MedlinePlus | a601237 |
Routes of administration | Oral |
ATC code | |
Pharmacokinetic data | |
Bioavailability | 15% (Eprosartan mesylate) |
Metabolism | not metabolized |
Elimination half-life | 5 to 9 hours |
Excretion | Renal 10%, biliary 90% |
Identifiers | |
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CAS Number | |
PubChem CID | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
Chemical and physical data | |
Formula | C23H24N2O4S |
Molar mass | Eprosartan mesylate: 520.625 g/mol g·mol−1 |
3D model (JSmol) | |
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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.<<Anon., 2006, Abbott Laboratories: Kos Pharmaceuticals a wise buy, Datamonitor ResearchStore (online), November 8, 2006, see [1], accessed 29 January 2015.</ref>
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.[1]
Synthesis
The following is a medicinal chemistry (early discovery stage) synthesis of eprosartan from Merck research into QSAR of this class of drug, which represents an approach to the construction of its carbon skeleton (though which is not necessarily related to the actual manufacturing synthesis of the on-market drug). Note, the reagents indicated alongside the arrows are a summary list, and are not complete for what is required in each transformation:
See also
References
- ^ 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.
{{cite journal}}
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|doi=10.1021/jm00047a009
instead.