LOCAL ANESTHETICS

FACULTY OF MEDICAL
MALAHAYATI UNIVERSITY

LOCAL ANESTHETICS
Introduction
Is the condition that results when sensory
transmission from a local area of the body to the
CNS is blocked
Agents that the block the sodium channels of
excitable membranes
The duration of local action is therefore limited
unless blood flow to the area is reduced. It can be
accomplished by administration of a
vasoconstrictor (usually an agonist
sympathomimetic)
Local anesthetics prevent or relieve pain by
interrupting nerve conduction. They bind to a
spesific reseptor site within the pore of the Na+
channels in nerves and block ion movement
through this pore

LOCAL ANESTHETICS

ESTHERS

- LONG DURATION (TETRACAINE)

- MEDIUM DURATION (COCAINE)
- SHORT DURATION (PROCAINE)
- SURFACE ACTIVE
(BENZOCAINE,COCAINE)

AMIDES

- LONG DURATION
(BUPIVACAINE,ROPIVACAINE)
- MEDIUM DURATION
(LIDOCAINE)

 Cocaine has intrinsic

sympathomimetic action because

inhibits norepinephrine reuptake into
nerve terminals, so cocaine doesnt
need any vasoconstrictor
Metabolism of ester local anesthetics
is carried out by plasma
cholinesterases and may be rapid.
The amides are hydrolyze in the liver
and have half lives from 1,8 hours to
6 hours

EFFECTS
Differential sensitivity of various types
of nerve fibers to local anesthetics is
associated with several factors:
- fiber diameter,
- myelination,
- physiologic firing rate, and
- anatomic location

CLINICAL USE
Most commonly used for minor

surgical procedures
Are also used in spinal anesthesia
and to produce autonomic blockade
in ischemic conditions

TOXICITY
CNS Effects: nystagmus, tonic-clonic

convulsions, coma with respiratory and

cardiovascular deppression
Cardiovascular Effects: arrhythmias and
hypotension except cocaine that may cause
hypertension with cerebral hemorrhage,
cardiac arrhythmias and myocardial infarction
In high concentrations, local anesthetics may
cause a local neurotoxic action that includes
histologic damage and permanent
impairment of function

TREATMENT OF TOXICITY
Convulsions are often treated with

intravenous diazepam or a short

acting barbiturate such as thiopental,
hyperventilation with oxygen is
helpful

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