Differential efficacy of immediate-release metoprolol tartrate and carvedilol in the treatment of congestive heart failure remains a subject of ongoing debate. The degree of beta1-blockade can be assessed by percentage reduction of exercise heart rate. Twelve healthy subjects underwent symptom-limited cardiopulmonary exercise testing repeated weekly and 2 hours after randomized, double-blind administration of 50 mg metoprolol tartrate vs 25 mg carvedilol. Baseline heart rate, heart rate at 40% and 70% peak O2 consumption, and maximal exercise were significantly blunted more by metoprolol tartrate than by carvedilol (P<.05 for all). Peak O2 consumption was significantly reduced by metoprolol tartrate (P<.03) but not by carvedilol (P=.054). The change in O2 consumption was significantly correlated with the degree of beta1-blockade (r =0.45; P<.05). In healthy subjects, a higher degree of beta1-blockade is achieved with 50 mg metoprolol tartrate compared with 25 mg carvedilol.