Cissampelos pareira Linn, an herbal medicine deeply rooted in traditional healing practices, has garnered renewed interest in contemporary pharmacological research. This detailed review explores the phytochemical richness and pharmacological potentials of Cissampelos pareira Linn, shedding light on its multifaceted therapeutic attributes. The paper synthesizes current scientific insights into the plant's anti-oxidant, anti-inflammatory, anti-venom, anti-fertility, anti-malarial, anti-insecticide, anti-microbial, and anti-cancer properties, providing a bridge between age-old traditional uses and modern evidence-based medicine. The main bioactive compounds present in this species are alkaloids, particularly isoquinoline alkaloids. Emphasizing the phytochemical diversity of Cissampelos pareira Linn the review navigates through its bioactive compounds, unraveling the intricate tapestry of its medicinal efficacy and also as an agent for making country liquor. The present study aims at exploration of phytochemical, ethno medicinal, ecological, pharmacological as well as medicinal practices of Cissampelos pareira Linn for better understanding of medicinal activities and sustainable use of this plant. The importance of bioactive compounds of Cissampelos pareira Linn in the pharmaceutical industry as well as livelihood of natives is highlighted. Cissampelos pareira L. is widely distributed throughout the world and has its utility in treatment of a large number of diseases and ailments.