Angiotensin receptor blockers: how important is selectivity?
During the last decade, angiotensin-receptor blockers have established themselves as effective antihypertensive agents with impressive safety profile and placebo-like tolerability. Additionally, these compounds provide benefits beyond the reduction in blood pressure, in conditions such as heart failure and in patients with type 2 diabetes and renal insufficiency. It is tempting to group all angiotensin-receptor blockers together as a class, but a closer look reveals differences, for example, in chemical structure, metabolism, dissociation rates, and receptor affinities. Recent findings on the respective roles of the angiotensin receptors AT(1) and AT(2) have raised the possibility that the degree of selectivity for AT(1) over AT(2) might affect the performance of the drug. This review attempts to put the concept of selectivity in context and to assess the potential benefits in different organs, with focus on the kidney, endothelium and the heart.
Siragy
Helmy M
HM
Department of Internal Medicine, Box 800482, University of Virginia Health System, Charlottesville, VA 22908, USA, hms7a@virginia.edu
D057911:Angiotensin Receptor Antagonists; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D000959:Antihypertensive Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D004730:Endothelium, Vascular / Q000187:drug effects*; D006321:Heart / Q000187:drug effects*; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology; D007668:Kidney / Q000187:drug effects*; D011945:Receptors, Angiotensin / Q000378:metabolism
D057911:Angiotensin Receptor Antagonists; D000806:Angiotensin-Converting Enzyme Inhibitors; D000959:Antihypertensive Agents; D011945:Receptors, Angiotensin