Terpenoids, a structurally diverse class of natural compounds derived from isoprene units, exhibit profound pharmacological potential in healthcare management. This chapter explores their classification, mechanisms of action, and therapeutic applications, emphasizing their role in modern and traditional medicine. Terpenoids demonstrate antimicrobial, anti-inflammatory, anticancer, neuroprotective, and metabolic regulatory properties, as evidenced by their ability to modulate cellular pathways (e.g., receptor interactions, enzyme inhibition, and antioxidant activity). Despite challenges like low bioavailability and standardization and advancements in drug delivery systems (e.g., nanoencapsulation), growing research on clinical validation highlights their potential. By bridging traditional knowledge and contemporary research, terpenoids offer promising avenues for developing safer, multitarget therapies for chronic and infectious diseases.