Bismuth compounds are considered relatively non-toxic due to their low solubility in aqueous solutions, making them safe for use in treating gastrointestinal disorders such as peptic ulcers, functional dyspepsia, and chronic gastritis. They are also explored for antimicrobial and anticancer applications. Despite their therapeutic benefits, excessive use or abuse can lead to toxicity, which is often reversible upon discontinuation. This review summarizes the pharmacotoxicological properties of bismuth compounds, focusing on in vitro, in vivo, and clinical studies to assess their toxicity. Bismuth compounds are used in various therapeutic areas, including antimicrobial, anticancer, and antileishmanial activities. They have also shown antiviral potential, such as inhibiting proteases from Zika and West Nile viruses. In cancer therapy, bismuth compounds have demonstrated antitumor effects, with some derivatives showing higher cytotoxicity than traditional chemotherapeutic agents. However, bismuth toxicity can result from high doses or prolonged exposure, leading to neurological, renal, and other systemic effects. Clinical cases highlight the risks of bismuth overuse, including encephalopathy, nephropathy, and gastrointestinal damage. Local application of bismuth iodoform paraffin paste (BIPP) has also been associated with toxicity, particularly in cases of prolonged exposure. Despite these risks, bismuth compounds remain widely used due to their safety profile and therapeutic benefits. Further research is needed to fully understand their toxicity mechanisms and long-term safety, particularly in clinical settings. Overall, bismuth-based products are considered relatively safe but require careful monitoring to prevent adverse effects.Bismuth compounds are considered relatively non-toxic due to their low solubility in aqueous solutions, making them safe for use in treating gastrointestinal disorders such as peptic ulcers, functional dyspepsia, and chronic gastritis. They are also explored for antimicrobial and anticancer applications. Despite their therapeutic benefits, excessive use or abuse can lead to toxicity, which is often reversible upon discontinuation. This review summarizes the pharmacotoxicological properties of bismuth compounds, focusing on in vitro, in vivo, and clinical studies to assess their toxicity. Bismuth compounds are used in various therapeutic areas, including antimicrobial, anticancer, and antileishmanial activities. They have also shown antiviral potential, such as inhibiting proteases from Zika and West Nile viruses. In cancer therapy, bismuth compounds have demonstrated antitumor effects, with some derivatives showing higher cytotoxicity than traditional chemotherapeutic agents. However, bismuth toxicity can result from high doses or prolonged exposure, leading to neurological, renal, and other systemic effects. Clinical cases highlight the risks of bismuth overuse, including encephalopathy, nephropathy, and gastrointestinal damage. Local application of bismuth iodoform paraffin paste (BIPP) has also been associated with toxicity, particularly in cases of prolonged exposure. Despite these risks, bismuth compounds remain widely used due to their safety profile and therapeutic benefits. Further research is needed to fully understand their toxicity mechanisms and long-term safety, particularly in clinical settings. Overall, bismuth-based products are considered relatively safe but require careful monitoring to prevent adverse effects.