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Local Anesthetics

Unlike other drugs which act in the region of the synapse, local anesthetics are agents that reversibly block the generation and conduction of nerve impulses along a nerve fiber. They depress impulses from sensory nerves of the skin, surfaces of mucosa, and muscles to the central nervous system. These agents are widely used in surgery, dentistry, and ophthalmology to block transmission of impulses in peripheral nerve endings.

Introduction

Most local anesthetics can be represented by the following general formula. In both the official chemical name and the proprietary name, a local anesthetic drug can be recognized by the "-caine" ending. The ester linkage can also be an amide linkage. The most recent research indicates that the local anesthetic binds to a phospholipid in the nerve membrane and inhibits the ability of the phospholipid to bind Ca+2 ions.

675procaine.gif

Practically all of the free-base forms of the drugs are liquids. For this reason most of these drugs are used as salts (chloride, sulfate, etc.) which are water soluble, odorless, and crystalline solids. As esters these drugs are easily hydrolyzed with consequent loss of activity. The amide form of the drug is more stable and resistant to hydrolysis.

Benzocaine and Lidocaine

Two local anesthtics are shown below.

 675benzocaine.gif

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