Cocaine was the first local anesthetic agent to be isolated by Albert Niemann in 1860. However, it was Carl Köller of Vienna, who pioneered its use in topical anesthesia by introducing it in his ophthalmology practice in 1884. Later on, Halstead innovated its use in infiltrative anesthesia and nerve blocks. Procaine was the first synthetic local anesthetic to be synthesized in 1905 by Alfred Einhorn, a German chemist. Lidocaine, the most popular local anesthetic was synthesized in 1943 by Nils Löfgren, a Swedish chemist. Bupivacaine and prilocaine were introduced later in 1957 and 1959 respectively. As the first local anesthetic cocaine, was a natural alkaloid, all local anesthetic agents were designated with names ending with caine. Local anesthesia is analgesia restricted to particular area or field of interest without causing any impairment of consciousness and cognizance. Most of the procedures done by dermatosurgeons are performed on outpatient or day care basis and hence, local anesthesia has been the preferred mode of achieving anesthesia. Though considered safe, the agents used in local anesthesia may rarely cause various systemic side effects with significant morbidity and mortality. The techniques of local anesthesia have expanded to include tumescent anesthesia, which has allowed dermatosurgeons to perform such surgeries as liposuction under local anesthesia. Hence it is important for dermatologists and dermatosurgeons to be aware of these molecules and the different local anesthetic techniques. Local anesthesia is an invaluable tool in dermatosurgery and esthetic procedures. When used appropriately, it greatly enhances patient comfort. However, proper use of technique and awareness of possible side effects is very important.