10.22376/ijpbs.2019.10.1.p1-12 Volume 1 Issue 2 2010 (April - June) Physiologically, cardiovascular functions are regulated by a variety of central and peripheral mechanisms that control vascular tone, blood pressure and cardiac functions. Under certain pathological conditions, physiological control is disturbed leading to serious cardiovascular disorders such as hypertension, cardiac arrhythmias and heart failure. These detrimental effects possibly occur due to chronic over-activation of the sympathetic systems and cardiovascular α and β adrenergic receptors. Sustained adrenergic activation and norepinephrine release raise cardiac output and heart rate, which then increase myocardial oxygen demand, ischemia, and oxidative stress. At the same time, peripheral vasoconstriction elevates blood pressure and increases both cardiac preload and afterload, causing additional stress on the ventricles and may end up by heart failure. There are now three available generations of β-adrenergic antagonists. Although very effective in management of cardiovascular disorders, the first generation drugs were suffering from some considerable side effects especially in asthmatic and diabetic patients. These adverse effects were significantly reduced upon the introduction of the second generation of β-blockers but such agents still have some adverse interactions. Fortunately during the last decade a third generation drugs have been developed and proved very particular efficiency in treatment of cardiovascular disorders associated with other serious co-morbidities. This short review will focus on "carvedilol" as a novel 3rd generation β-blocker that revolutionized therapy with β-adrenergic antagonists in hypertension and heart failure. Carvedilol's mechanism of action, pharmacokinetics, dosage and administration as well as its side effects and tolerability are also discussed. Tarek T. Abdel-Razek,MD,Ph.d,,Hassen Bennasir,Ph.d,Shanmugam Sridhar,M.Tech -