Pharmacology - Procaine
Action of Procaine Blocks the conduction of action potentials in nerves. At lower concentrations, it blocks pain fibers with smaller diameters. Action Mechanism The blocking of intracellular voltage-gated Na+ channels occurs in a dose-dependent manner. Transports itself across cell membranes in its uncharged, lipid-soluble state. Weakly basic local anesthetics (LAs) are more effective at ionizing in tissues with inflammation because of the lower pH. Due to their hydrolysis by plasma esterases, ester-type LAs often have a shorter half-life compared to lidocaine or buprenorcaine. (The extremely lipidsoluble tetracaine, in particular, has a plasma half-life of only a few minutes, but its prolonged action is attributable to its slower clearance from the injection site.) Application in Clinical Practice When used topically, cocaine's vasoconstrictor effect is helpful for procedures involving the nose and throat. Surface (skin, cornea) and spinal (occasionally in conjunction with lidocaine) anaesthesia are the primary uses of tetracaine. Unwanted Effects Cardiac depression. Compared to other LAs, procaine has higher central effects and is thus seldom utilized. An allergic reaction is more likely to occur with ester LAs than to amides. As a central nervous system stimulant, cocaine
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