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 AMIDES

- LONG DURATION (TETRACAINE) - LONG DURATION

- MEDIUM DURATION (COCAINE) (BUPIVACAINE,ROPIVACAINE)
- SHORT DURATION (PROCAINE) - MEDIUM DURATION
- SURFACE ACTIVE (LIDOCAINE)
(BENZOCAINE,COCAINE)
• Cocaine has intrinsic sympathomimetic
action because inhibits norepinephrine
reuptake into nerve terminals, so cocaine
doesn’t 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
THANK YOU