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Local Anesthetics
Local Anesthetics
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