Autophagy refers to the process in which the cellular lysosome degrades the cell's own damaged organelles and related macromolecule substances. It plays important roles in the homeostasis of organs, cell survival, and stable development. Previous studies indicate that the process of cardiopathology is closely associated with autophagy and some of Chinese medicines (active compounds and formulae) are found to have beneficial effects on injured cardiomyocytes via the modulation of autophagy. This review highlights the efficacy of the action of Chinese medicine on the regulation of myocardial autophagy and summarizes the related molecular and signal mechanisms. Our study discovers that some active compounds and formulae of Chinese medicines react on the specific targets of autophagy in related signal pathways to exert protective effects in the processes of ischemia and reperfusion, as well as, in other cardiopathological models. Parts of these compounds even have the characteristics of multiple targets in autophagic signal pathways and dual-directional regulated actions on autophagy, suggesting that Chinese medicines, which possess the ability to modulate autophagy, might improve effective cardio protection in the treatment of cardiovascular disease.