The chemistry that underlies the development of local and regional anesthesia is explored. Starting from the first medicinal use of cocaine as a topical anesthetic in 1884, the gradual advancement of knowledge and practice until today is presented. In so far as possible, the original synthesis of each agent is included. Emphasis is placed upon the importance of acidity constants and lipophilic versus hydrophilic character in interpreting what affect a particular compound has upon biological processes. Two examples of current hospital practices are included.
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Brunsvold, Robert; Ostercamp, Daryl L. J. Chem. Educ.2006 83 1816.
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