Chinese medicinal has both toxicity and efficacy, especially in extremely toxic drugs with potent efficacy. The toxicity and efficacy of Chinese medicinal are both contradictory and unified. The toxic and effective material basis often affect and transform to each other. Radix Aconiti Lateralis Praeparata, a famous Chinese medicinal, not only has significant efficacy, but also extremely toxic. Thus, it has been a hotspot for research. Although more than 90 compounds have been isolated from Radix Aconiti Lateralis Praeparata, the basic reason for its efficacy and toxicity still remains to be revealed. The complexity of the problem is that the toxicity and efficacy of Radix Aconiti Lateralis Praeparata can transform to each other under different conditions. For example, it has significant cardiotonic effect, while it can also cause cardiotoxicity. Similarly, it can release pain, but has neurotoxicity. Moreover, the same component may exert completely different biological effect due to the different dosage, model, processing method, compatibility of Chinese medicinals, and drug metabolism. Based on our research results and literatures of Radix Aconiti Lateralis Praeparata, this paper will discuss on the material basis of Radix Aconiti Lateralis Praeparata by “integrated analytical method of toxicity and efficacy”.