As a famous geo-authentic medicine distributed in Sichuan Province, Radix Aconiti Lateralis Praeparata is also a traditionally toxic medicine with curative effect in clinic. Heart is the key target for both toxicity and efficacy of Radix Aconiti Lateralis Praeparata. However, the correlation between toxicity and efficacy on heart remains unknown. Under the guidance of the research idea “multidimensional evaluation and integrated analysis between ‘toxicity and efficacy’ for Chinese materia medica” proposed by professor Peng Cheng, the article tightly focused on the six factors as “variety, quality, processing, property, efficacy, application” of Chinese materia medica. The research status of ‘toxicity-efficacy’ material basis, mechanism, and effect-enhancing and toxicity-reducing principle for Radix Aconiti Lateralis Praeparata on heart were summarized based on our years of researches and other relative researches at home and abroad. Cardiac toxicity-efficacy mechanism was integrated analyzed then. It was shown that diester-type alkaloids (DA) was material base for heart toxicity in Radix Aconiti Lateralis Praeparata, while total alkaloids (AD), water-soluble alkaloids (WA), polysaccharide and some other compounds in Radix Aconiti Lateralis Praeparata were responsible for effects of cardiotonic and protecting myocardial cells. There were the same targets in myocardial cells for toxicity and efficacy of Radix Aconiti Lateralis Praeparata, such as cell morphology and function, membrane stability, cellular environmental homeostasis, ion transport-related ATPase and channels, and energy metabolism. However, there was some respective mechanism for each other. Multi-means could be taken to control cardiac toxicity and enhance effects on heart for Radix Aconiti Lateralis Praeparata, including legal processing, reasonable compatibility, differentiation for use, extending time of decoction, dosage control.