The history of cocaine is charted with specific reference to its usefulness as a medicine and local anesthetic. It is common knowledge that coca leaves were used as a panacea and local anesthetic throughout the history of the Incan Empire of Peru. In Europe, however, its medical usefulness was not fully recognized until Carl Koller used it to anesthetize the cornea of the eye. Over the next 20 years, cocaine became a popular medicine and tonic in Europe and America, where it was credited with curing a wide variety of diseases and illnesses. However, reports soon started to appear claiming that cocaine was a drug with a high social abuse potential and in America it seemed to underpin growing crime figures. As a result, cocaine was misclassified as a narcotic and its use was restricted to specific surgical procedures and medicinal preparations. Today, cocaine and its derivatives are still popular local anesthetics in operations of the ear, nose and throat and it is also used in a preparation given to alleviate the pain (physical and mental) of terminal diseases. Although cocaine has a high public profile as a drug of addictive potential, this drug has also had a long and distinguished history as a medicine and local anesthetic. The legitimate uses of cocaine exacerbate the problems of controlling this substance of abuse and should provide a stimulus for generating local anesthetics that lack addictive potential.