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Procaine is a local anesthetic of the amino ester group, primarily used to produce local or regional anesthesia, especially in dental procedures and minor surgeries. It was first synthesized in 1905 by Alfred Einhorn and introduced under the trade name Novocain. Its mechanism of action involves blocking voltage-gated sodium channels on neuronal cell membranes, thereby inhibiting nerve impulse conduction and producing loss of sensation. In addition to its primary action as a sodium channel blocker, procaine has been shown to antagonize NMDA receptors, nicotinic acetylcholine receptors, serotonin receptor-ion channel complexes (notably 5-hydroxytryptamine receptor 3A), inhibit monoamine oxidase activity, block calcium-activated potassium channels, and inhibit DNA methyltransferases among other targets. It is metabolized by plasma esterases into para-amino benzoic acid (PABA) and excreted via the kidneys[1][5][7].
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