The safety of Chinese materia medica is a solid foundation for guiding the clinical application of it. Radix Aconiti Lateralis Praeparata, the head of Chinese materia medica, has a variety of pharmacological function, but Radix Aconiti Lateralis Praeparata also showed significant neurotoxicity on humans. Ester type alkaloid is the main toxic substance of Radix Aconiti Lateralis Praeparata. The central nervous system and peripheral nervous system are the target organs of aconite neurotoxicity. The underlying mechanism of Radix Aconiti Lateralis Praeparata neurotoxicity is mainly involving in ion channel, neurotransmitter, energy metabolism, and signal transduction. In order to enhance the safety of clinical application of Radix Aconiti Lateralis Praeparata and reduce the neurotoxicity, this study was based on clinical researches and animal experiments. The neurotoxicity of Radix Aconiti Lateralis Praeparata was summarized from the three aspects of neurotoxic material base, neurotoxic target organs and the specific mechanism.