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5 Cards in this Set

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Local anesthetics include?
Esters: cocaine, provcaine, tetracaine, benzocaine.//

Amides: lidocaine, bupivacaine
Chemistry?
Lipophilic group: aromatic group

hydrophilic group: 2 or tertiary amine

mainly weak basis that are predomin. charged at body's pH.

Receptor is intracellular, so non-charged drug must pass through then become charged to activate the receptor.
What is critical length?
blocking happens quicker if nerve is shorter, faster, and the one in the outer part of the bundle:::

So, C > Adelta > Agamma > A beta > A alpha.

Sensation lost in order: pain then temp then touch then pressure then motor.
Role of epi and clonidine
these act at alpha 2, decreasing firing and inhibiting release of substance P, so less pain.
Metabolism of local anesthetics
ester type except for Cocaine by psuedocholinesterase. Cocain by liver. PABA metabolites of these inhibit sulfonamide action. Can also cause hypersensitivity rxn///

Amide by CYP450 i.e. lidocaine