Pharmacology of local Anesthetics

Dr P sreenivas reddy
Composition of Local Anesthesia
pharmacokinitics
• Uptake:- all anesthetics r potent
vasodilators except cocaine.

• PROCAINE a potent vasodilator is

also used therapeutically( in
accidental IA injection of
thiopental)
 Route of
administration

• Oral:-
local anesthetic agents r poorly absorbed
from GIT except cocaine.

Tocai ni deHcl is an analogue of lidocaine

that is well absorbed from GIT.
Topical route

Solarcaine = lidocaine + benzocaine

EMLA:- oil in water emulsion that contains lidocaine&
prilocaine

5% cream contains 25mg/g lidocaine &

25mg/g prilocaine.
Injection
• Used mainly for
ventricular
dysrhythmias.
Distribution
 Metabolism
(biotransformation)

• Esters hydrolyzed in plasma by

pseudocholinesterase

Intermediate metabolite of procaine

PABA
• Amides r primarily biotransformed
in liver.
• Articaine metabolizes both in liver and
in plasma.
Excretion
Systemic action of local
anesthetics

• They reversibly block the action

potentials of excitable membranes
• CNS, CVS r more susceptible
CNS
MECHANISM
• Increasing the threshold of
hyperexcitable cortical neurons
PRECONVULSIVE SIGNS
&SYMPTOMS
Clinical manifestations
MINIMAL TO MODERATE OVERDOSE
LEVELS
Moderate to high overdose levels
Normal cerebral cortex
Preconvulsive stage
Convulsive stage
Final Convulsive phase
Etc…….
• Analgesia procaine
• Mood elevation
• Rejuvenation

Restore youthful vigor

On CVS
Action on other systems
Active forms of local anesthetics
amphipathic

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
?