Oxethazaine and Related Congeners: A Series of Highly Potent Local Anesthetics.

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Abstract
Oxethazaine, N,N-bis-(N-methyl-N-phenyl-t-butylacetamido)-[beta]-hydroxyethylamine HC1, and several N-substituted bis-acetamide congeners constitute a new series of powerful local anesthetics, exceeding by far the potency of either cocaine, procaine, lidocaine or dibucaine. Applied topically to the cornea or infiltration of the canthus they are effective in concentrations ranging from 0.001 to 0.0001%. They are also equally effective intraspinally. Since oxethazaine combines effective topical anesthetic activity with a large margin of safety when administered intragastrically, it has proven to be useful clinically for control of pain due to gastritis, duodenal ulcer, hiatus hernia and peptic esophagitis. Its effectiveness at the acidity of the gastric environment is due to the fact that oxethazaine, a weak base, is relatively non-ionized at pH 1. Moreover, the solubility of its salts in organic solvents (CHCl3 CCl4) at gastric pH indicates that it easily penetrates the lipids of nerve sheaths to effect adequate anesthesia of long duration.