Date: 02 Nov 2010

Novelty without toxicity: a quest for a safer local anesthetic

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The search for an “ideal” local anesthetic for perioperative anesthesia and analgesia has continued for more than a century. The ideal local anesthetic is an agent with a rapid onset and desirable duration of action that is capable of producing reversible and selective blockade of sensory nerve conduction without risks of local (neurotoxic and myotoxic) or systemic (neurological and cardiovascular) toxicity. Since Koller’s introduction of cocaine as a surgical anesthetic in 1884, several hundred compounds have been tested and found to produce local anesthetic effects. The chemical structures of these agents are diverse and include amino esters (procaine analogues), aminoamides (lidocaine analogues), alcohols (benzyl alcohol), and phenol. However, only a handful of these agents are of clinical value, and the search for the “ideal” local anesthetic continues.

For decades, systemic local anesthetic toxicity has received much attention due to the relatively large quantity of local anestheti ...