Carvedilol is a non-selective β-blocker with α1-blocking properties which is widely prescribed for treating hypertension, heart failure, and left ventricular dysfunction following myocardial infarction. It has a unique pharmacological profile and acts by several mechanisms of action, making it particularly effective in cardiovascular disorders therapy. Carvedilol exhibits antioxidant properties by scavenging reactive oxygen species (ROS) and reducing oxidative stress. Moreover, it has anti-inflammatory effects by reducing the levels of pro-inflammatory cytokines. Furthermore, it exhibits antiapoptotic properties, which play a crucial role in its therapeutic effects. By mitigating ROS, carvedilol helps to preserve mitochondrial function and prevent the release of pro-apoptotic factors which would otherwise initiate the cell death cascade. Additionally, carvedilol modulates signaling pathways that influence apoptosis. Overall, the combination of adrenergic-blocking, antioxidant, antiapoptotic, and anti-inflammatory properties makes carvedilol a multifaceted drug with significant therapeutic benefits. In our lab, we investigated new pharmacological actions of carvedilol in different experimental models. Therefore, this review aims to illustrate our new findings in addition to other labs' findings in a comprehensive way to be helpful to readers interested in this field. These studies involved in vitro and in vivo experiments using cellular and animal models, which have paved the way for clinical investigation of carvedilol in the management of distinct types of diseases.