Carvedilol is a third-generation, neurohormonal antagonist with multiple activities. It blocks both beta(1)- and beta(2)-adrenergic receptors, enhances vasodilation via alpha(1)-adrenergic blockade, and, at high concentrations, has ion channel-blocking activities. Carvedilol lacks sympathomimetic activity. In addition to these well-known properties, carvedilol has a number of ancillary activities, including antioxidant, anti-inflammatory, and antiapoptotic properties. Together, they contribute to the clinical efficacy of carvedilol in a broad spectrum of patient types and may also confer a range of cardioprotective benefits.