The toxic effects of Aconitum alkaloids are known to affect mainly the central nervous system, heart and muscle tissues. Their toxicological mechanisms may involve interaction with voltage-dependent Na+ channels, modulation of neurotransmitter release and related receptors, promotion of lipid peroxidation and induction of cell apoptosis in heart, liver or other organs. Of them, the mechanism of interaction with voltage-dependent Na+ channels is quite well known, but the other factors are still unclear, and need to be further studied. This review focuses on the toxicological mechanisms of Aconitum alkaloids.