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Aim of the Study: This review aims to investigate the pharmacologically induced discoloration of teeth and bones, focusing on how various medications affect the coloration of tooth enamel and dentin. The study seeks to provide insight into the mechanisms behind intrinsic and extrinsic discoloration and their clinical implications. Materials and Methods: A comprehensive literature search was conducted using databases such as PubMed, Google Scholar, and Web of Science. Keywords related to tooth discoloration and medications were used to identify relevant studies, including clinical trials and case reports published between 1990 and 2023. Studies that focused on medication-related discoloration of enamel and bone were analyzed to explore the biochemical interactions between drugs and dental tissues. Results and Discussion: The review identified several classes of medications, including tetracyclines, fluoride, antineoplastic agents, antimalarials, and iron supplements, as primary contributors to both intrinsic and extrinsic tooth discoloration. Tetracycline binds to calcium during tooth formation, leading to permanent discoloration. Fluoride can cause enamel hypomineralization, resulting in fluorosis. Antimalarials and iron supplements cause extrinsic stains due to complex formation with enamel minerals. Treatment options range from professional cleaning and bleaching to more invasive procedures like veneers and crowns, depending on the type and severity of the discoloration. Conclusion: Medication-induced tooth discoloration presents significant clinical challenges due to its varied mechanisms, including intrinsic staining from systemic incorporation of drugs and extrinsic staining from surface agents. Early identification of high-risk medications, preventive measures, and appropriate treatment are essential to minimize aesthetic and psychological impacts. While extrinsic stains are easier to manage, intrinsic discoloration often requires restorative approaches, such as veneers or crowns, for effective resolution.