Over the past decade, several studies have established a direct link between functional foods, nutraceuticals, and a reduced risk of oxidative-stress-related diseases. Nutraceuticals, which encompass a variety of bioactive molecules, exhibit both nutritional and therapeutic properties. The cactus pear (Opuntia spp.) is a plant genus with many species recognized as functional foods, largely attributed to their high content of nutraceuticals, including polyphenols, fatty acids, vitamins, amino acids, pigments, and phytosterols. These compounds of different structures and functions possess different biological activities, contributing to the health-promoting properties of cactus pear. This makes cactus pears a valuable plant for the food, cosmetic, and pharmaceutical industries. While extensive research has focused on the nutritional profile of cactus pear fruits, the cladodes have received comparatively limited attention. Notably, the nutritional composition of cladodes can exhibit considerable variability, influenced by species and growing conditions. Furthermore, although various bioactive compounds have been identified in cladodes, studies elucidating their mechanisms of action, health benefits, and potential therapeutic applications remain insufficient. Addressing these gaps is crucial for enhancing the understanding and utilization of cactus pear cladodes. This paper provides a comprehensive overview of the structure–function relationships of the main nutraceuticals found in cactus pear cladodes. It synthesizes data from recent and relevant literature to elucidate the content of these compounds in relation to species and geographical origin, while also detailing the main biological activities and health-promoting benefits associated with cactus pear cladodes.