Procaine is a slow onset local ester anaesthetic used for local anesthesia, peripheral nerve block and spinal nerve block. Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in neuronal membranes of peripheral nerves. It also binds or antagonized NMDA receptors, nicotinic acetylcholine receptors, and serotonin receptor-ion channel complex. Procaine is injected into the tissue and spreads to the nerves through infiltration. In the local post-synaptic neurons, it binds or antagonizes NMDA receptors. This prevents calcium from entering the postsynaptic neuron. This causes hyperpolarization and prevents depolarization, which has an anaesthetic effect on the local tissue

Procaine NMDA Antagonist Pathway References