4-Local Anesthetics

Local Anesthetics
 Used at multiple sites throughout

the body:
 Epidural
 Spinal
 Peripheral nerve blocks
 IV (Bier Block)
 Skin sites locally
Amides and Esters
 Chloroprocaine (Nesacaine)
 Cocaine (crack)
 Procaine
 Tetracaine (Pontocaine)
 Lidocaine (Xylocaine)
 Bupivacaine (Marcaine)
 Etidocaine (Duranest)
 Mepivacaine (Carbocaine)
 Prilocaine (Citanest)
 Ropivacaine
Mechanism of Action
 Local anesthetics work in general by
binding to sodium channel receptors
inside the cell and thereby inhibiting
action potentials in a given axon. They
work the best when the axon is firing.
 The Cell membrane consists of ion
pumps, most notably the Na/K pump
that create a negative 70mV resting
potential by pumping 2 K+
intracellular for every 3 Na+ it pumps
extracellular.
Clinical Uses
 Esters
 Benzocaine- Topical, duration of 30
minutes to 1 hour
 Chloroprocaine- Epidural,
infiltration and peripheral nerve
block, max dose 12mg/kg, duration
30minutes to 1 hour
 Cocaine- Topical, 3mg/kg max., 30
minutes to one hour
 Tetracaine- Spinal, topical, 3mg/kg
max., 1.5-6 hours duration
Clinical Uses
 Bupivacaine- Epidural, spinal,
infiltration, peripheral nerve block,
3mg/kg max., 1.5-8 hours duration
 Lidocaine- Epidural, spinal,
intravenous regional, topical, 4.5mg/kg
or 7mg/kg with epi, 0.75-2 hours
duration
 Mepivacaine- Epidural, infiltration,
peripheral nerve block, 4.5mg/kg or
7mg/kg with epi, 1-2 hours
 Prilocaine- Peripheral nerve block
(dental), 8mg/kg, 30 minutes to 1 hour
duration
 Ropivacaine- Epidural, spinal,
3mg/kg, 1.5-8 hours duration
Systemic Toxicity
 Blockage of voltaged-gated Na
channel affects action potential
propagation throughout the
body…therefore the potential is
present for systemic toxicity.
 Mixtures of LA have additive
affects
 i.e. a 50% toxic dose of lidocaine
and a 50% toxic dose of bupivicaine
have 100% the toxic affect of either
drug
Systemic Toxicity
 Neurological
 Symptoms include cicumoral
numbness, tongue paresthesia,
dizziness, tinnitus, blurred vision,
restlessness, agitation, nervousness,
paranoia, slurred speech,
drowsiness, unconsciousness.
 Muscle twitching heralds the onset
of tonic-clonic seizures with
respiratory arrest to follow.
Local anesthetic toxicity
 Seizure treatment:
 Thiopental 1-2mg/kg abruptly
terminates seizure activity
 Benzos and hyperventilation…
decrease CBF and therefore drug
exposure. These raise the
threshold of local anesthetic-
induced seizures
 Chloroprocaine injected
intrathecally can cause prolonged
neurotoxicity. This is likely due
to a preservative no longer used
with this agent. (Sodium
bisulfate)
 Repeated doses of 5% lidocaine
and .5% tetracaine may be responsible
for cauda equina syndrome following
infusion through small bore catheters
in spinal anesthetics.
 Pooling of drug around the cauda
equina resulted in permanent
neurological damage
 Animal studies suggest that neuro
damage is:
Lido=tetracaine>bupivacaine>ropivaca
ine. Also perservative free
chloroprocaine may be neurotoxic
 Transient Neurological Symptoms
 This is associated with dysethesia,
burning pain and aching in lower ext,
buttocks.
 Follows spinal anesthesia with variety
of agents (lido), attributed to radicular
irritation and resolves in 1 week
usually
 Risk factors include
 Lidocaine intrathecally
 Lithotomy position
 Obesity
 Outpatient status
Local anesthestic
toxicity
 Respiratory center may be
depressed (medullary)…
postretrobulbar apnea syndrome
 Lidocaine depresses hypoxic
respiratory drive (PaO2)
 Direct paralysis of phrenic or
intercostal nerves
LA cardio toxicity
 All LA’s depress spontaneous
Phase IV depolarization and
reduce the duration of the
refractory period
 Myocardial contractility and
conduction velocity are depressed
at higher concentrations
 All LA’s except cocaine cause
smooth muscle relaxation and
therefore vasodilation (art) whick
can lead to brady, heart block and
hypotension…cardiac arrest.
LA cardio toxicity
 Major cardiovascular toxicity
usually results from 3 times the
blood concentration of LA that
causes seizures.
 Therefore cardiac collapse is
usually the presenting sign under
GA.
 R isomer of bupivacaine avidly
blocks cardiac sodium channels
and dissociates very slowly.
Making resuscitation prolonged
and difficult.
LA cardio toxicity
 Levo-bupivacaine (S isomer) is
no longer avaliable in the US but
had a cardiovascular profile
similar to ropivacaine.
 Ropivacaine has a larger
therapeutic index and it is 70%
less likely to cause severe cardiac
dsyrhythmias than bupivacaine
 Also ropviacaine has greater CNS
tolerance
 The improved safety profile is
due to a lower lipid solubility
LA toxicity treatment
 Supportive care: intubation,
vasopressors, appropriate
defibrillation, fluids, stop injection of
LA, anything else….
 Intralipid…Bolus 1cc/kg of 20%
intralipid, 0.25cc/kg/min of 20%
intralipid for 10 minutes
 Bolus can be repeated every 5 minutes
up to a maximum of 8cc/kg of 20%
intralipid
 Cardiac support should be continued as
ACLS dictates
 Epi and vasopresin should likely both
be used in the resusitation efforts

(animal model data from A & A)
True Allergic Reactions

to LA’s
 Very uncommon
 Esters more likely because of p-
aminobenzoic acid (allergen)
 Methylparaben preservative
present in amides is also a known
allergen
Local Anesthetic
Musculoskeletal
 Cause myonecrosis when injected
directly into the muscle
 When steroid or epi added the
myonecrosis is worsened
 Regeneration usually takes 3-4
weeks
 Ropivacaine produces less sereve
muscle injury than bupivacaine
Drug Interactions
 Chloroprocaine epidurally may interfere with
the analgesic effects of intrathecal morphine
 Opioids and 2 agonists potentiate LA’s
 Propranolol and cimetidine decrease hepatic
blood flow and decrease lidocaine clearance
 Pseudocholinesterase inhibitors decrease
Ester LA metabolism
 Dibucaine (amide LA) inhibits
pseudocholinesterase used to detect abn
enzyme
 Sux and ester LA need pseudochol. for
metabolism therefore adminstering both may
potentiate their activity
 LA potentiate nondepolarizing muscle
relaxant blockade
Other agents with LA
properties
 Meperidine
 TCAs (amitriptyline)
 Volatile anesthetics
 Ketamine
 Tetrodotoxin (blocks Na channels
from the outside of the cell
membrane) Animal studies
suggest that when used in low
doses with vasoconstrictors it will
significantly prolong duration of
action of LA.

4-Local Anesthetics

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Local Anesthetics

 Used at multiple sites throughout

True Allergic Reactions

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