Angiotensin Receptor Blockers: Pharmacology, Efficacy, and Safety

The renin-angiotensin-aldosterone system (RAAS) plays an important role in protecting vertebrates against cardiovascular collapse due to hypotension and volume loss in the event of traumatic injury that involves blood loss. In certain humans, however, inappropriate or exaggerated activity of the RAAS contributes to the development of hypertension and the initiation of a molecular cascade in tissues with consequent injury to critical organs such as the brain, kidneys, heart, and blood vessels.As understanding of the pathologic role of the RAAS in hypertensive vascular disease has unfolded during the past century, so has the interest in developing drugs that could interdict specific components of the RAAS. The first of the RAAS-blocking drugs to become commercially available were the aldosterone antagonists in the 1970s, followed by the angiotensin-converting enzyme (ACE) inhibitors in the 1980s and the angiotensin II receptor blockers (ARBs) in the 1990s. Unlike ACE inhibitors that inhibit the conversion of angiotensin I to II, ARBs bind to the angiotensin II AT1 receptor, thereby inhibiting the cellular actions of angiotension II mediated by the receptor in which the tissue is located. During the past 20 years, studies in the laboratory and clinic have documented that ARBs, either alone or in combination with drugs of other classes, reduce blood pressure (BP) in hypertensive animals and humans; reduce rates of myocardial infarction (MI), stroke, and progression of renal impairment; and positively impact other markers of cardiovascular (CV) events such as left ventricular hypertrophy (LVH) and urinary protein excretion independent of their effect on BP. Although improvement in mortality and morbidity has been demonstrated after treatment of patients with congestive heart failure (HF) and following MI, this review paper will focus primarily on evidence supporting the use of ARBs in the management of hypertensive patients with and without comorbidities.

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Blackwell Futura Media Services designates this journal-based CME activity for a maximum of 1 AMA PRA Category 1 Credit™. Physicians should only claim credit commensurate with the extent of their participation in the activity.

Blackwell Futura Media Services is accredited by the Accreditation Council for Continuing Medical Education to provide continuing medical education for physicians.
Educational Objectives

• Discuss the current clinical research in hypertension that adds to the body of scientific evidence in the treatment of patients with hypertension.

• Apply their awareness and knowledge of current clinical research and scientific evidence that will contribute to the overall care of patients with hypertension and other cardiovascular disease factors.

• Discuss the efficacy, safety, and tolerability of the different pharmacologic treatment modalities that modulate the renin-angiotensin-aldosterone system to reduce blood pressure and mitigate the negative consequences of poor blood pressure control.

• Identify high-risk patient characteristics and determine optimal therapy to achieve target blood pressure.Jump to…Top of pageAccreditation and Designation StatementEducational ObjectivesActivity DisclosuresInstructions on Receiving Credit

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