Since ancient times, activated carbon (AC) has been known for its medicinal uses. Egyptians and Hippocrates used AC to treat epilepsy, vertigo, wounds, and anthrax. Due to its large surface area in the range of about 950–2000 m² g⁻¹ and high porosity, AC is an excellent adsorbent, especially for adsorbing toxins of high molecular masses. The medical uses of AC can be external-type or internal-type depending on the course of treatment administered to the patient. It is commonly used as a universal antidote for the poisoned human body, and in wound dressing materials and gas masks. Usually, AC is non-specific in its absorption capacity and thus can be used to remove almost all undesirable, unwanted, and even important metabolites from the body. Various routes for administering ‘medical grade’ AC have been widely studied, especially in the post-Chernobyl nuclear disaster cleanup. However, AC has limitations since it cannot be excreted easily from the human body. Also, AC may reduce the absorption of other oral drugs if administered in a combined dosage form. The present chapter discusses the use of AC in intoxication treatment, wound healing agents, and drug delivery systems with a detailed discussion on its cytotoxicity, limitations, and current scenario in medicine.