LOCAL ANESTHETICS

Local anesthetic (LA) is a medication that causes absence of pain sensation.

In the context of surgery, a local anesthetic creates an absence of pain in a specific location of the
body without a loss of consciousness, as opposed to a general anesthetic.
History
The anesthetic properties of coca leaves (Erythroxylon coca Lam) became known to Europeans
from the natives of Peru, who chewed the leaves for a general feeling of well-being.
The active principle of the coca leaf, however, was not discovered until 1860 by Niemann, who
obtained a crystalline alkaloid from the leaves, to which he gave the name cocaine, and who noted
the anesthetic effect on the tongue.
MOA
All LAs are membrane-stabilizing drugs; they reversibly decrease the rate of depolarization and
repolarization of excitable membranes (like nociceptors).
LA drugs act mainly by inhibiting sodium influx through sodium-specific ion channels in the
neuronal cell membrane (voltage-gated sodium channels).
When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is
inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium
channel.
Local anesthetic drugs bind more readily to sodium channels in an activated state, thus onset of
neuronal blockade is faster in rapidly firing neurons.

Classification of Local anesthetics

1. Ester based:
• Natural
- Cocaine
 • Synthetic
• Benzoic acid derivatives: Cyclomethicaine, Piperocaine
• p- benzoic acid derivatives: Benzocaine, Procaine, Butacaine, Tetracaine,
Benoxinate
1. Amide based: Lignocaine, Mepivacaine, Prilocaine, Etidocaine, Dibucaine
2. Amino ether based: Pramoxine
3. Amino ketone based: Dyclonine
4. Alcohol based: Benzyl alcohol, Eugenol
5. Miscellaneous: Phenacaine
SAR of Local Anesthetics
Synthesis
1. Benzocaine

2. Procaine

3. Dibucaine