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Tetracaine is synthesized from 4-butylaminobenzoic acid. The synthesis involves forming the ethyl ester through an acid-catalyzed esterification reaction, followed by base-catalyzed transesterification by boiling the ethyl ester with excess 2-dimethylaminoethanol.

Tetracaine functions by reversibly binding to voltage-gated sodium ion channels in neuronal cell membranes. This action inhibits sodium influx, preventing the initiation and conduction of nerve impulses, stabilizing neuronal membranes, and leading to a temporary loss of sensation.

Tetracaine is mainly used as a potent local anesthetic of the ester group. It is commonly applied topically in ophthalmology to numb the eyes, nose, or throat, used on the skin to reduce pain before intravenous procedures, and has applications in spinal anesthesia.

Tetracaine HCl is highly soluble in water, whereas Tetracaine base is generally insoluble in cold water. However, some Tetracaine base can dissolve in hot water.

Tetracaine is highly potent. Its local anesthesia strength follows the order: Tetracaine > Lidocaine > Benzocaine > Procaine. Additionally, the anesthetic effect of the base form is stronger than the HCl form.

In biomedical research, Tetracaine acts as an allosteric blocker of calcium release channels (ryanodine receptors) that control calcium release from intracellular stores. Low concentrations cause initial inhibition of spontaneous calcium release, while high concentrations block the release completely.