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ORGANIZATION OF CLASS

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These drugs are applied locally and block nerve conduction. Nerve fibers are not affected equally. Loss of sympathetic function occurs first, followed by loss of pinprick sensation and temperature, and, finally, motor function. The effect of local anesthetics is reversible: their use is followed by complete recovery of nerve function with no evidence of structural damage.

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All the local anesthetics consist of a hydrophilic amino group linked through a connecting group of variable length to a lipophilic aromatic portion (benzene ring, Figure 24–1). In the intermediate chain, there is either an ester linkage or an amide linkage.

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FIGURE 24–1

Main structures of the ester and amide local anesthetics.

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The commonly used local anesthetics can be classified as esters or amides based on the linkage in this intermediate chain. It is not as important to know which drugs are esters and which are amides, as it is to know that there is a difference. The amide local anesthetics are chemically stable in vivo, whereas the esters are rapidly hydrolyzed by plasma cholinesterase. One interesting but trivial fact is that metabolism of the ester local anesthetics leads to formation of para-aminobenzoic acid (PABA), which is thought to be allergenic.

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ESTERS AMIDES

COCAINE

PROCAINE

benzocaine

chloroprocaine

tetracaine

 

 

 

LIDOCAINE

bupivacaine

etidocaine

mepivacaine

prilocaine

ropivacaine

articaine

levobupivacaine

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The “-caine” ending on each of these drug names tells you that they are local anesthetics.

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Adverse effects of the local anesthetics result from systemic absorption of toxic amounts of the drugs.

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Death can occur from respiratory failure secondary to medullary depression or from hypotension and cardiovascular collapse.

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MECHANISM OF ACTION

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Local anesthetics block the sodium channel in the nerve membrane.

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Application of a local anesthetic inhibits the inward movement of Na+ ions. This results in elevation of the threshold for electrical excitation, reduction in the rate of rise of the action potential, and slowing of the propagation of the impulse. At high enough concentrations, the local anesthetics completely block conduction of impulses down the nerve.

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For those of you interested in this area, there is a fascinating story relating pH to ionization of the local anesthetics to drug action. For details, see your textbook.

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SPECIAL FEATURES ABOUT INDIVIDUAL AGENTS

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LIDOCAINE is a local anesthetic used intravenously in the treatment of cardiac arrhythmias.

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COCAINE is better known as a drug of abuse, but it is also an effective local anesthetic.

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