Newer Antihypertensive Agents: Angiotensin-Receptor Antagonists and Vasopeptidase Inhibitors

The pharmacology of agents that interfere with renin-angiotensin system activity

“…1 This is applicable to the issues of absolute bioavailability, rate of absorption, volume of distribution (V d …”

“…[1][2][3][4] To date, there does not appear to be any meaningful efficacy difference, attributable to prodrug considerations, between candesartan cilexetil and olmesartan medoximil and those ARBs, which are not prodrugs.…”

“…The pharmacology of ARBs has generated much discussion, however, in the main the pharmacologic differences between the several compounds in this class are of little practical significance (table 1). 1 This is applicable to the issues of absolute bioavailability, rate of absorption, volume of distribution (V d ), lipid solubility, plasma half-life (t 1/2 ), mode of metabolism (CYP 450 or not), and route of elimination (liver and liver/kidney). Several of the…”

“…ARBs are administered as prodrugs (candesartan cilexetil, and olmesartan medoximil) or a less active parent compound (losartan). [1][2][3][4] To date, there does not appear to be any meaningful efficacy difference, attributable to prodrug considerations, between candesartan cilexetil and olmesartan medoximil and those ARBs, which are not prodrugs. Amongst the ARBs, candesartan, olmesartan and the active metabolite of losartan (E-3174), undergo modest renal clearance; however, this feature is of no particular advantage (or disadvantage) when these drugs are given to patients with moderate-to-severe chronic kidney disease (CKD).…”