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 Hypertension (HTN or HT), also known as high blood pressure (HBP), is a long-term medical condition in which the blood pressure in the arteries is persistently elevated. High blood pressure usually does not cause symptoms. Long-term high b ...

. 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 U.S. state, states, a Washington, D.C., federal district, five ma ...

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 Abbott Laboratories is an American multinational medical devices and health care company with headquarters in Abbott Park, Illinois, United States. The company was founded by Chicago physician Wallace Calvin Abbott in 1888 to formulate known dr ...

; 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 ...

, and by

elsewhere. The compound came into the

cardiovascular pipeline with its acquisition of

Kos Pharmaceuticals Kos or Cos (; el, Κως ) is a Greek island, part of the Dodecanese island chain in the southeastern Aegean Sea. Kos is the third largest island of the Dodecanese by area, after Rhodes and Karpathos; it has a population of 36,986 (2021 cens ...

in 2006, which had licensed it, along with "a range of hypertensive treatments", from the

Biovail Corporation Biovail Corporation was a Canadian pharmaceutical company, operating internationally in all aspects of pharmaceutical products. Its major production facility was located in Steinbach, Manitoba. It merged with Valeant Pharmaceuticals Internationa ...

. 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 th ...

, 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, j ...

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 Angiotensin is a peptide hormone that causes vasoconstriction and an increase in blood pressure. It is part of the renin–angiotensin system, which regulates blood pressure. Angiotensin also stimulates the release of aldosterone from the adr ...

to AT₁ receptors in vascular

smooth muscle Smooth muscle is an involuntary non- striated muscle, so-called because it has no sarcomeres and therefore no striations (''bands'' or ''stripes''). It is divided into two subgroups, single-unit and multiunit smooth muscle. Within single-unit ...

, 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 furosem ...

(an

ACE inhibitor Angiotensin-converting-enzyme inhibitors (ACE inhibitors) are a class of medication used primarily for the treatment of high blood pressure and heart failure. They work by causing relaxation of blood vessels as well as a decrease in blood volum ...

), 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.

References

External links

* * {{Portal bar , Medicine Angiotensin II receptor antagonists Imidazoles Thiophenes AbbVie brands Benzoic acids

Structure activity Relationship

See also

References

External links