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Practical Considerations of the Pharmacology of Angiotensin Receptor Blockers
Author(s) -
McConnaughey Mona M.,
McConnaughey J. Scott,
Ingenito Alphonse J.
Publication year - 1999
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/00912709922008155
Subject(s) - pharmacology , chymase , medicine , angiotensin ii , receptor , angiotensin receptor , angiotensin receptor blockers , angiotensin converting enzyme , in vivo , mechanism of action , ace inhibitor , renin–angiotensin system , in vitro , chemistry , blood pressure , biology , immunology , biochemistry , microbiology and biotechnology , mast cell
A review of the drug class of angiotensin receptor blockers (ARBs) as well as the ARBs currently available by prescription in the United States is presented. The importance of angiotensin II production by non‐angiotensin‐converting enzyme (non‐ACE) pathways, particularly human chymase, is discussed. Emphasis is placed on the mechanism of action of ARBs and the different binding kinetics of these agents. Although all ARBs, as a group, block the AT 1 receptor, they may differ in the pharmacological characteristics of their binding and be classified as either surmountable or insurmountable antagonists. Mechanisms of surmountable and insurmountable antagonism as well as possible benefits of these blocking characteristics are discussed in relation to the various ARBs. The cardiovascular effects of activation of the two main subtypes of angiotensin receptors (AT 1 and AT 2 ) are presented. In addition to their treatment of hypertension, ACE inhibitors are recognized as being effective in the management of heart failure, left ventricular hypertrophy, recurrent myocardial infarctions, and renal disease. ARBs are currently indicated only for the treatment of hypertension; however, in vitro and in vivo pharmacological studies as well as preliminary clinical data suggest that ARBs, like ACE inhibitors, may also provide effective protection against end‐organ damage in these conditions .