The development of local anaesthetic has fundamentally altered practices in surgery, and is an interesting journey to follow. It began in 1555 with Augustin de Zarate, a Spanish explorer who discovered the anaesthetic properties of the coca plant and subsequently the active compound cocaine was localised in 1860 by Albert Niemann. It was around 1880 when cocaine was first used in an operating theatre where it was used intranasally to anesthetise the nasal mucosa. Subsequently, cocaine was synthesised to procaine in 1905 to provide a safer and less toxic substance. Lidocaine was introduced in the 1940s and has since revolutionised medicine, with modern versions having various onsets and duration. This historical progression underscores the importance of local anesthesia in modern medicine, reflecting a continual evolution driven by scientific inquiry and clinical need.