Secondary metabolites comprise a major class of compounds, among which alkaloids are one of the most important due to their diverse structures and wide spectrum of biological activities. While these nitrogen-containing compounds are mainly extracted from plants, they have been known to be useful in the synthesis of a large variety of analogues with applications as pharmaceuticals, for example analgesics, antineoplastic agents, and antimicrobial drugs. A complete and detailed knowledge of alkaloids’ structures and classifications is crucial for efforts in drug discovery and development because quite often the structural features are also associated with their biological activities. Alkaloids are a large and complex group of natural compounds that are characterized by a nitrogenous base. Much has been said about their importance when derived from different plant species on the wide spectrum of pharmacological effects. This literature review paper will attempt to synthesize recent findings pertaining to alkaloids’ clinical importance in modern-day therapeutics and medicine, critically analyzing their traditional and potential contemporary medicinal uses, further indicating the existing lacunae of knowledge and scopes for future study.