LOCAL ANAESTHESIA (2)

Ass.Professor.Dr. Abdulmageed Al-Yhary

Terminology
Analgesia :
Is loss of pain sensation un accompanied by
loss of other forms of sensibility.

Anaesthesia :
Is loss of all forms of sensation including
pain, touch, by impairment of motor
function.
Methods which induced LOCAL ANAESTHESIA

1. Mechanical trauma (compression of

tissues)
2. Low temperature
3. Anoxia
4. Chemical irritants
5. Neurolytic agents such as alcohol &
phenol
6. Chemical agents such as local anesthetic
Properties deemed most desirable for a
LOCAL ANAESTHESIA
1. It should not be irritating to the tissue to
which it is applied.
2. It should not cause any permanent alteration
of nerve structure.
3. It’s systemic toxicity should be low.
4. It must be effective regardless of whether it is
injected into the tissue or is applied locally to
mucous membrane.
5. The time most onset of anesthesia should be
as short as possible.
In addition to these qualities, Bennett 2 lists
other desirable properties of an ideal
LOCAL ANESTHETIC
7. It should have potency sufficient to give
complete anesthesia without the use of
harmful concentrated solutions.
8. It should be relatively free from producing
allergic reactions.
9. It should be stable in solution and should
readily undergo biotransformation in the body.
10. It should sterile or capable of being sterilized
heat without deterioration.
Properties of LOCAL ANAESTHETIC solutions

◦ Potency and reliability

◦ Reversibility of action
◦ Safety
◦ Lack of irritation
◦ Rapidity of onset
◦ Duration of effect
◦ Sterility
◦ Adequate ‘Shelf Life’
◦ Penetration of mucous membrane
Classification of Local Anaesthesia
A. Esters :
1- Esters of benzoic acid
Butacaine Cocaine
Ethyl aminobrnzoate (Benzocaine)
Hexylcaine Piperocaine
Tetracaine

2- Esters of para-aminobenzoic acid

Chloroprocaine
Procaine
Propoxycaine
Classification of Local Anaesthesia
B. Amides :
Articaine Bupivacaine Dibucaine
Etidocaine lidocaine Mepivacaine
Prilocaine Ropivacaine

C. Quinoline :
Centbucridine
All local anesthetics posses a degree of
vasoactivity most producing dilation of the
vascular bed into which they are deposited,
although the degree of vasodilation may
vary, and some may produce
vasoconstriction. (concentration dependent)
Ester local anesthetics are also potent
voasodilating drugs.
Procaine, the most potent vasodilator
among local anesthetics.
Time to Achieve Peak Blood Level
Route Time, min

Intravenous 1

Topical 5 (approximately)

Intramuscular 5-10

Subcutaneous 30-90
ORAL ROUTE
With the exception of cocaine, local
anesthetics are absorbed poorly, if at
all, from the gastrointestinal tract
after oral administration.
TOPICAL ROUTE
Local anesthetics are absorbed at differing rates
after application to mucous membrane: In the
tracheal mucosa, absorption is almost as rapid
as with intravenous (IV) administration (indeed,
intratracheal drug administration {epinephrine,
lidocaine, atropine, naloxone and flumazenil} is
used in certain emergency situations); in the
pharyngeal mucosa, absorption is slower; and in
the esophageal or bladder mucosa, uptake is
even slower than occurs through the pharynx.
INJECTION
The rate of uptake (absorption) of
local anesthetics after parenteral
administration (subcutaneous,
intramuscular, or IV) is related to
both the vascularity of the injection
site and the vasoactivity of the drug.
Pattern of Distribution of Local
Anesthetics after absorption

Site of
Fat Slow
injection
equilibrium
B Muscle space
L
O
Brain Rapid
O
Myocardium equilibrium
D
Lungs space
Liver

ELIMINATION