Medicinal plants are the local heritage with global importance playing a vital role in world health care system of developing countries. Calotropis procera (Asclepiadaceae), a giant milk weed, is known for its pharmacological importance for centuries. The coarse shrub is a very promising source of anticancerous, ascaricidal, schizonticidal, anti-microbial, anthelmintic, insecticidal, anti-inflammatory, anti-diarrhoeal, larvicidal with many other beneficial properties. Plant is described as a golden gift for human kind containing calotropin, calotropagenin, calotoxin, calactin, uscharin, amyrin, amyrin esters, uscharidin, coroglaucigenin, frugoside, corotoxigenin, calotropagenin and voruscharine used in many therapeutic applications. Different compounds like norditerpenic esters, organic carbonates, the cysteine protease procerain, alkaloids, flavonoids, sterols and numerous cardenolides made this plant of scientific attraction for centuries. Plant is not only a great source of natural hydrocarbons but also contains several metabolites used as folk medicine for the treatment of leprosy, elephantiasis, fever, menorrhagia, malaria and snake bite. The review discusses the potential of Calotropis procera in health care management.