Eprosartan is an
angiotensin II receptor antagonist
Angiotensin II receptor blockers (ARBs), formally angiotensin II receptor type 1 (AT1) antagonists, also known as angiotensin receptor blockers, angiotensin II receptor antagonists, or AT1 receptor antagonists, are a group of pharmaceuticals tha ...
used for the treatment of
high blood pressure. It is marketed in the
United States
The United States of America (U.S.A. or USA), commonly known as the United States (U.S. or US) or America, is a country primarily located in North America. It consists of 50 states, a federal district, five major unincorporated territori ...
as ''Teveten'' by
Abbvie
AbbVie is an American publicly traded biopharmaceutical company founded in 2013. It originated as a spin-off of Abbott Laboratories.
History
On October 19, 2011, Abbott Laboratories announced its plan to separate into two publicly traded compani ...
, the
spin-off of the pharmaceutical discovery division of
Abbott Laboratories; it is marketed as ''Eprozar'' by
Intas Pharmaceuticals in
India
India, officially the Republic of India (Hindi: ), is a country in South Asia. It is the seventh-largest country by area, the second-most populous country, and the most populous democracy in the world. Bounded by the Indian Ocean on the so ...
, 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
Hydrochlorothiazide is a diuretic medication often used to treat high blood pressure and swelling due to fluid build-up. Other uses include treating diabetes insipidus and renal tubular acidosis and to decrease the risk of kidney stones in ...
, whereupon it is marketed in the US as ''Teveten HCT'' and elsewhere as ''Teveten Plus''.
The drug acts on the
renin–angiotensin system
The renin–angiotensin system (RAS), or renin–angiotensin–aldosterone system (RAAS), is a hormone system that regulates blood pressure, fluid and electrolyte balance, and systemic vascular resistance.
When renal blood flow is reduced, ...
to decrease
total peripheral resistance
Vascular resistance is the resistance that must be overcome to push blood through the circulatory system and create flow. The resistance offered by the systemic circulation is known as the systemic vascular resistance (SVR) or may sometimes be cal ...
in two ways. First, it blocks the binding of
angiotensin II to AT
1 receptors in vascular
smooth muscle, causing vascular dilatation. Second, it inhibits
sympathetic norepinephrine
Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as both a hormone and neurotransmitter. The name "noradrenaline" (from Latin '' ad' ...
production, further reducing blood pressure.
As with other angiotensin II receptor antagonists, eprosartan is generally better tolerated than
enalapril
Enalapril, sold under the brand name Vasotec among others, is an ACE inhibitor medication used to treat high blood pressure, diabetic kidney disease, and heart failure. For heart failure, it is generally used with a diuretic, such as furose ...
(an
ACE inhibitor), especially among the elderly.
Structure activity Relationship
One feature that compares in Eprosartan versus other molecules is that Eprosartan is dosed relatively high at 400 to 800 mg/day. Eprosartan has an alpha-beta unsaturated hydrocarbon group which makes the compound difficult to absorb and contributes to its instability, thus there is a need for higher doses. The lipophilic aspects of the molecule also contribute to its low bioavailibility.
See also
*
Discovery and development of angiotensin receptor blockers
References
External links
*
*
{{Portal bar , Medicine
Angiotensin II receptor antagonists
Imidazoles
Thiophenes
AbbVie brands
Benzoic acids