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Pharmacology of LA
Pharmacology of LA
Dr P sreenivas reddy
Composition of Local Anesthesia
pharmacokinitics
• Uptake:- all anesthetics r potent
vasodilators except cocaine.
• Oral:-
local anesthetic agents r poorly absorbed
from GIT except cocaine.
pseudocholinesterase
PABA
• Amides r primarily biotransformed
in liver.
• Articaine metabolizes both in liver and
in plasma.
Excretion
Systemic action of local
anesthetics
O N
OOO
Lipophylic Hydrophylic
portion portion
. BASED ON CHEMICAL STRUCTURE :
Esters Amides
Benziocacid esters lignocaine
cocaine prilocaine
Para-amino benzoic esters mepivacaine
procaine / tetracaine bupivacaine
benzocaine / chloroprocaine
. BASED ON ORIGIN :
a. Natural : Cocaine
b. Synthetic: PABA derivatives – procaine /
tetracaine
Acetanilide derivatives – lignocaine
Quinolone derivatives – cinchocaine
Acrinide derivatives – bucricaine
Kinetics of LA onset and duration of action
Barriers of diffusion
Induction of LA
• Diffusion
• Blocking process
• Induction time
Recovery from LA block
Factors affecting local anesthetic
action
?