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Losartan, valsartan, candesartan, irbesartan, telmisartan and olmesartan all contain a biphenyl-methyl group. Losartan is partly metabolized to its 5-carboxylic acid metabolite EXP 3174, which is a more potent AT 1 receptor antagonist than its parent compound [17] and has been a model for the continuing development of several other ARBs. [1]
Losartan is excreted in the urine, and in the feces via bile, as unchanged drug and metabolites. [44] About 4% of an oral dose is excreted unchanged in urine, and about 6% is excreted in urine as the active metabolite. [44] The terminal elimination half-lives of losartan and EXP3174 are about 1.5 to 2.5 hours and 3 to 9 hours, respectively. [44]
Losartan, the first ARB. Angiotensin II receptor blockers (ARBs), formally angiotensin II receptor type 1 (AT 1) antagonists, [1] also known as angiotensin receptor blockers, [2] [3] angiotensin II receptor antagonists, or AT 1 receptor antagonists, are a group of pharmaceuticals that bind to and inhibit the angiotensin II receptor type 1 (AT 1) and thereby block the arteriolar contraction and ...
Telmisartan works by blocking the effects of angiotensin II while amlodipine works by decreasing calcium ion entry into smooth muscle and heart muscle. [2] The combination was approved for medical use in the United States in 2009. [2] The combination is on the World Health Organization's List of Essential Medicines.
Telmisartan, sold under the brand name Micardis among others, is a medication used to treat high blood pressure and heart failure. [ 3 ] [ 6 ] It is a reasonable initial treatment for high blood pressure. [ 6 ]
losartan; olmesartan; telmisartan; valsartan; fimasartan; In 2004, an article in the BMJ examined the evidence for and against the suggestion that ARBs may increase the risk of myocardial infarction (heart attack). [22] The matter was debated in 2006 in the medical journal of the American Heart Association. There is no consensus on whether ARBs ...
Amlodipine/olmesartan, sold under the brand name Azor, among others is a fixed-dose combination medication used to treat high blood pressure. [5] It contains amlodipine, as the besilate, a dihydropyridine calcium channel blocker, and olmesartan medoxomil, an angiotensin II receptor blocker.
There are four S pockets, and three S′ pockets (table 1). The pockets alternate on either side of the backbone in the ligand. This alternation affects the orientation of the pockets, making the S3 and S1 pockets arrange together and the S2 pocket close to both S4 and S1′ pockets. [43]
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