Toxicology, rooted in ancient civilizations and evolving through pivotal historical figures like Paracelsus and Alice Hamilton, has become a multidisciplinary field encompassing various branches such as pharmacology, medical, forensic, and environmental toxicology. This exploration embarks on a journey through time and science, unravelling the intricate interplay between chemicals, pollutants, and their profound impacts on human, animal, and environmental well-being. Spanning from ancient practices like the use of hemlock in Greek capital punishment to modern-day concerns surrounding industrial chemicals and pesticides, the review delves into the mechanisms by which toxins disrupt biochemical pathways and induce organ dysfunctions. From heavy metals and pesticides persistent effects on the nervous and reproductive systems to the carcinogenic properties of polychlorinated biphenyls (PCBs), hydrocarbons, polycyclic aromatic hydrocarbons (PAHs), and volatile organic compounds (VOCs). The review highlights the diverse range of toxicants and their widespread impact on human health. Additionally, the review underscores the importance of proactive measures to mitigate exposure to harmful substances, advocating for the development of antidotes, bioremediation techniques, and stricter environmental regulations. By addressing the urgent need for comprehensive strategies to combat toxicological hazards, this review aims to contribute to ongoing efforts to safeguard public health and environmental sustainability in the face of evolving chemical threats.