Local anesthetics

Drug produce reversible conduction

block of neural impulses transmission
of autonomic, sensory and motor
neural impulses
 History
• The natives of Peru have chewed the
leaves of the indigenous plant
“Erythroxylon coca” the source of cocaine,
to induce a feeling of well-being
• Koller used cocaine for the eye in 1884
• Halsted used cocaine as nerve block
• First synthetic local-- procaine in 1905
• Lidocaine synthesized in 1943
 Local anesthetic

Esters Amides
Cocaine Lidocaine
Procaine Bupivacaine
Tetracaine Prilocaine
Mechanism of action is by reversibly
blocking sodium channels to prevent
depolarization

Structure
• Linear molecules that have a lipophilic and
hydrophilic end (ionizable)
– low pH-- more in ionized state and unable to
cross membrane
– adding sodium bicarb-- more in non-ionized
state
• Two groups: esters and amides
– esters metabolized by plasma cholinesterase
– amides metabolized by cytochrome p-450
Clinical uses
• Local anesthetics
2. Nerve block (brachial plexus block, wrist
block, ankle block----etc.)
3. Local infiltration
4. Ointment, spray, lotion, lozenges, EMLA
5. Regional block (spinal, epidural, caudal)
6. Intravenous regional block (Bier’s block)
• Lidocaine uses:
2. Prevent or treat cardiac ventricular
dysrhythmias
3. Attenuate presser responses associated
with intubation of the trachea
4. Prevent or treat increases in intracranial
pressure as are often associated with
intubation of the trachea
5. Minimize coughing during intubation or
extubation of the trachea
 Addition of epinephrine to local
anesthetic solutions
Epinephrine 1:200000 or 5μg/ml
Advantage:
3. Limits systemic absorption
4. Prolongs the duration of local anesthetics by
keeping them in contact with nerve fibers
5. Decreasing the possibility of systemic toxicity
cause the rate of metabolism will match the
rate of absorption
6. As test in epidural regional anesthesia
Addition of epinephrine to local anesthetics
is not recommended in:
2. Unstable angina pectoris
3. Cardiac dysrhythmias
4. Uncontrolled hypertension
5. Uteroplacental insufficiency
6. Peripheral nerve block anesthesia in
areas that may lack collateral blood flow
(digits, penis)
7. Intravenous regional anesthesia
Side effects
2. Local Anesthetic Toxicity
• Central nervous system
– initially-- lightheadedness, circumoral
numbness, dizziness, tinnitus, visual
change
– later-- drowsiness, disorientation, slurred
speech, loss of consciousness,
convulsions
– finally-- respiratory depression
• Cardiovascular
– myocardial depression and vasodilation--
hypotension and circulatory collapse
specially with bupivacaine

2. Allergic reactions-- rare (less than 1%)

– preservatives or metabolites of esters
– rash, bronchospasm
 Prevention and Treatment of Toxicity

• Primarily from intravascular injection or

excessive dose – anticipation or from absorption
from tissue injection sites
– aspirate often with slow injection
– ask about CNS toxicity
– have monitoring available
– prepare with resuscitative equipment, CNS-
depressant drugs, cardiovascular drugs
– ABC’s
• All cases
Assure adequate ventilation
Administer supplemental oxygen
• Seizures
Diazepam
• Hypotension
Trendelenburg position (head down legs up)
IV fluid bolus (isotonic saline or Ringer lactate)
Vasopressor (dopamine)
• Dysrthymia
accordingly
Thank you