Carvedilol inhibits reactive oxygen species generation by leukocytes and oxidative damage to amino acids.

Background: The purpose of this study was to test whether carvedilol has an antioxidant effect in humans in vivo.

Methods And Results: We administered 3.125 mg of carvedilol twice daily to normal subjects for 1 week. ROS generation by polymorphonuclear leukocytes and mononuclear cells fell from 314+/-183.43 and 303+/-116 mV to 185+/-157 and 189+/-63 mV (P<0.025), respectively. m-Tyrosine fell from 4.24+/-0.99 to 4.03+/-0.97 ng/mL (P=0.01), and o-tyrosine fell from 4.59+/-1.10 to 4.24+/-0.99 ng/mL (P=0.004) in the absence of a change in phenylalanine concentrations.

Conclusions: We conclude that carvedilol significantly inhibits ROS generation by leukocytes and oxidative conversion of phenylalanine to m- and o-tyrosine.