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AUC and Cmax values of valsartan are observed to be approximately linearly dose-dependent over therapeutic dosing range. Owing to its relatively short elimination half life attribution, valsartan concentration in plasma does not accumulate in response to repeated dosing. [7]
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, 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, 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 ...
Absorption half-life 1 h, elimination half-life 12 h. Biological half-life (elimination half-life, pharmacological half-life) is the time taken for concentration of a biological substance (such as a medication) to decrease from its maximum concentration (C max) to half of C max in the blood plasma.
Valsartan has an oral bioavailability of approximately 25% and reaches peak blood concentrations around 2–4 hours after ingestion. [2] [13] The estimated elimination half-life is determined to be approximately 6 hours, volume distribution of 17 litres, and a protein binding of 95% is seen.
ATC code C09 Agents acting on the renin–angiotensin system is a therapeutic subgroup of the Anatomical Therapeutic Chemical Classification System, a system of alphanumeric codes developed by the World Health Organization (WHO) for the classification of drugs and other medical products.
There is an important relationship between clearance, elimination half-life and distribution volume. The elimination rate constant of a drug K e l {\displaystyle K_{el}} is equivalent to total clearance divided by the distribution volume