Toad toxin, a bioactive compound revered in traditional Chinese medicine, has been employed therapeutically for centuries. Recent studies have increasingly confirmed its pharmacological benefits, including cardioprotection, anesthetic effects, anti-inflammatory properties, enhancement of sexual function, and antineoplastic activities. This toxin is applied in the treatment of diverse medical conditions such as chronic bronchitis, pharyngitis, and colon cancer. Nonetheless, the consumption of toad-related substances-such as flesh, eggs, gallbladders-or the medicinal use of toad toxin frequently leads to poisoning incidents, some of which are fatal. This paper comprehensively reviews the principal features of toad toxin poisoning, encompassing clinical symptoms, therapeutic approaches, and other relevant factors to aid in the diagnosis and management, as well as the forensic evaluation of lethal cases. We advocate for further research into the cardiotoxic and neurotoxic effects of toad toxin to deepen our understanding of its poisoning mechanisms and pharmacological profile. Future efforts should focus on regulatory standardization of treatment practices and public education to mitigate the risks associated with toad toxin exposure.