Homeostasis in the cardiovascular system is maintained by physiological functions of the
Renin Angiotensin Aldosterone System (RAAS). In pathophysiological conditions, over activation of
RAAS leads to an increase in the concentration of Angiotensin II (AngII) and over activation of Angiotensin
Type 1 Receptor (AT1R), resulting in vasoconstriction, sodium retention and change in
myocyte growth. It causes cardiac remodeling in the heart which results in left ventricular hypertrophy,
dilation and dysfunction, eventually leading to Heart Failure (HF). Inhibition of RAAS using angiotensin
converting enzyme inhibitors (ACEi) or angiotensin receptor blockers (ARBs) has shown to
significantly reduce morbidity and mortality due to HF. ACEi have been shown to have higher drug
withdrawal rates due to discomfort when compared to ARBs; therefore, ARBs are the preferred choice
of physicians for the treatment of HF in combination with other anti-hypertensive agents. Currently,
eight ARBs have been approved by FDA and are clinically used. Even though they bind to the same
site of AT1R displacing AngII binding but clinical outcomes are significantly different. In this review,
we described the clinical significance of each ARB in the treatment of HF and their clinical outcome.
Keywords: AT1R, AngII, angiotensin receptor blockers, heart failure, cardiovascular diseases, hypertension, GPCRs.
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